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NIACINAMIDE
- Retinol serum
- Collagen serum
- Acne Repair serum
1. Study: Topical nicotinamide compared with clindamycin gel in the treatment of inflammatory acne vulgaris
Shalita AR, Smith JG, Parish LC, Sofman MS, Chalker DK. Topical nicotinamide compared with clindamycin gel in the treatment of inflammatory acne vulgaris. Int J Dermatol. 1995;34(6):434-437.
Conclusion: 4% Niacinamide (nicotinamide) is of comparable efficacy to 1% clindamycin in the treatment of acne vulgaris. Because topical clindamycin, like other antimicrobials, is associated with the emergence of resistant microorganisms, nicotinamide gel is a desirable alternative treatment for acne vulgaris.
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2. Article: A Review of the Range of Effects of Niacinamide in Human Skin
Key Points:
Topical niacinamide 4% has been shown to provide potent anti-inflammatory activity in the treatment of acne vulgaris.
Shalita et al. and others postulate that niacinamide may act via its apparent antihistaminic effect, activity as an electron scavenger, or its inhibition of 3’-5’ cyclic-AMP phosphodiesterase activity. Recent data, however, appear to demonstrate an altogether more fundamental role for topical niacinamide in acne treatment.
Biedermann et al. published that Niacinamide produce significant dose dependent reductions in total sebaceous lipogenesis.
This has important implications for acne pathogenesis as it is accepted that acne is a disease involving the pilosebaceous duct and Propionibacterium acnes.
1. Article: Niacinamide-Containing Facial Moisturizer Improves Skin Barrier and Benefits Subjects With Rosacea
Zoe Diana Draelos, MD; Keith Ertel, PhD; Cindy Berge, BS
Conclusion: Results showed that the niacinamide improved stratum corneum barrier function and hydration. The investigator’s evaluations and subjects’ self assessments showed improvement in the signs and symptoms of rosacea over the course of the study. These results suggest that this patient population can benefit from using a facial moisturizer that improves the stratum corneum barrier.
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Bissett DL, Miyamoto K, Sun P, Li J, Berge CA. Topical niacinamide reduces yellowing, wrinkling, red blotchiness, and hyperpigmented spots in aging facial skin. Int J Cosmet Sci. 2004;26(5):231-238
Previous clinical testing of topical niacinamide (vitamin B3) has revealed a broad array of improvements in the appearance of aging facial skin.
The study reported here was done to confirm some of those previous observations and to evaluate additional end points.
Results: Niacinamide was well tolerated by the skin and provided significant improvements versus control in end points evaluated previously: fine lines/wrinkles, hyperpigmentation spots, texture, and red blotchiness. In addition, skin yellowing (sallowness) versus control was significantly improved.
At concentrations above 2% niacinamide reduces redness and normalizes skin inflammation.
Conclusion: Niacinamide induces a decrease in pigmentation, inflammatory infiltrate, and solar elastosis. Niacinamide is a safe and effective therapeutic agent for this condition.
1. Article: A Review of the Range of Effects of Niacinamide in Human Skin
Conclusions:
- Niacinamide reduces human skin hyperpigmentation
- Niacinamide inhibits transfer of melanosomes from melanocytes to keratinocytes.
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2. Article: The effect of niacinamide on reducing cutaneous pigmentation and suppression of melanosome transfer
Conclusions:
The data suggest niacinamide is an effective skin lightening compound that works by inhibiting melanosome transfer from melanocytes to keratinocytes.
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Bissett DL, Miyamoto K, Sun P, Li J, Berge CA. Topical niacinamide reduces yellowing, wrinkling, red blotchiness, and hyperpigmented spots in aging facial skin. Int J Cosmet Sci. 2004;26(5):231-238
Previous clinical testing of topical niacinamide (vitamin B3) has revealed a broad array of improvements in the appearance of aging facial skin.
The study reported here was done to confirm some of those previous observations and to evaluate additional end points.
Results: Niacinamide was well tolerated by the skin and provided significant improvements versus control in end points evaluated previously: fine lines/wrinkles, hyperpigmentation spots, texture, and red blotchiness. In addition, skin yellowing (sallowness) versus control was significantly improved.
At concentrations above 2% niacinamide reduces redness and normalizes skin inflammation.
1. Article: A Review of the Range of Effects of Niacinamide in Human Skin
Key Points:
- Nicotinamide Coenzymes in skin are depleted with age
- Niacinamide can help normalize this imbalance.
- Niacinamide can stimulate new collagen synthesis.
- Niacinamide up-regulates epidermal ceramide synthesis with concurrent epidermal barrier benefits.
- Niacinamide up-regulates biosynthesis of markers of keratinocyte differentiation.
- Niacinamide exerts multiple benefits on the appearance of ageing / photodamaged skin.
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2. Study: Niacinamide: A B vitamin that improves aging facial skin appearance
Bissett DL, Oblong JE, Berge CA. Niacinamide: A B vitamin that improves aging facial skin appearance. Dermatol Surg. 2005;31(7 Pt 2):860-865.
Background: In multiple chronic clinical studies, topical niacinamide (vitamin B3) has been observed to be well tolerated by skin and to provide a broad array of improvements in the appearance of aging facial skin (eg, reduction in the appearance of hyperpigmentated spots and red blotchiness).
Objective: To clinically determine the effect of topical niacinamide on additional skin appearance and property end points (wrinkles, yellowing, and elasticity).
Results: Analyses of the data revealed a variety of significant skin appearance improvement effects for topical niacinamide: reductions in fine lines and wrinkles, hyperpigmented spots, red blotchiness, and skin sallowness (yellowing). In addition, elasticity (as measured via cutometry) was improved. Corresponding mechanistic information is presented.
Conclusion: In addition to previously observed benefits for topical niacinamide, additional effects were identified (improved appearance of skin wrinkles and yellowing and improved elasticity).
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3. Study: Evaluation of anti-wrinkle effects of a novel cosmetic containing niacinamide
Kawada A, Konishi N, Oiso N, Kawara S, Date A. Evaluation of anti-wrinkle effects of a novel cosmetic containing niacinamide. J Dermatol. 2008;35(10):637-642.
Niacinamide is known to have effectiveness on sallowness, wrinkling, red blotchiness and hyperpigmented spots in aging skin.
In this study, we have evaluated the anti-wrinkle effects of a new cosmetic containing niacinamide.
A randomized, placebo-controlled, split face study was performed in 30 females who had wrinkles in the eye areas. The tested cosmetic containing 4% niacinamide was applied on wrinkles of one side for 8 weeks, and a control cosmetic without niacinamide on another site.
This formula showed marked and moderate improvement in 64% of the subjects with a significant difference as compared with the control site (P < 0.001). Wrinkle grades in the tested area significantly reduced more than pre-application (P < 0.001) and the control (P < 0.001). Reduction in Ra value on the tested area was more than pre-application (P < 0.01) and the control site (P < 0.05) with significant differences. Only one subject stopped the study with minimal irritation. These results indicated that the tested lotion was well tolerated and may be an optional preparation for the treatment of wrinkles in the eye areas.
Tanno O, Ota Y, Kitamura N, Katsube T, Inoue S. Nicotinamide increases biosynthesis of ceramides as well as other stratum corneum lipids to improve the epidermal permeability barrier. Br J Dermatol. 2000;143(3):524-531.
Background: Stratum corneum lipids, particularly ceramides, are important components of the epidermal permeability barrier that are decreased in atopic dermatitis and aged skin.
Objectives: We investigated the effects of nicotinamide, one of the B vitamins, on biosynthesis of sphingolipids, including ceramides and other stratum corneum lipids, in cultured normal human keratinocytes, and on the epidermal permeability barrier in vivo.
Results: When the cells were incubated with 1-30 micromol L-1 nicotinamide for 6 days, the rate of ceramide biosynthesis was increased dose-dependently by 4.1-5. 5-fold on the sixth day compared with control. Nicotinamide also increased the synthesis of glucosylceramide (7.4-fold) and sphingomyelin (3.1-fold) in the same concentration range effective for ceramide synthesis. Furthermore, the activity of serine palmitoyltransferase (SPT), the rate-limiting enzyme in sphingolipid synthesis, was increased in nicotinamide-treated cells. Nicotinamide increased the levels of human LCB1 and LCB2 mRNA, both of which encode subunits of SPT. This suggested that the increase in SPT activity was due to an increase in SPT mRNA. Nicotinamide increased not only ceramide synthesis but also free fatty acid (2.3-fold) and cholesterol synthesis (1.5-fold). Topical application of nicotinamide increased ceramide and free fatty acid levels in the stratum corneum, and decreased transepidermal water loss in dry skin.
Conclusions: Nicotinamide improved the permeability barrier by stimulating de novo synthesis of ceramides, with upregulation of SPT and other intercellular lipids.
Conclusion: Longwave UVA, which is poorly filtered by most sunscreens, was highly immune suppressive even at doses equivalent to 20 min of sun exposure. Nicotinamide, which protected against both UVB and UVA, is a promising agent for skin cancer prevention.
SALICYLIC ACID
- Renewal Facial cleanser: 3%
- Pore Control cleanser: 3%
- Acne Repair serum: 3%
- Daily Acne peel: 5%
- Clarify peel: 15% ; 30%
- Illuminize peel
1. Study: Treatment of acne vulgaris with salicylic acid
Zander E, Weisman S. Treatment of acne vulgaris with salicylic acid pads. Clin Ther. 1992;14(2):247-253.
Conclusion: Comparative studies of salicylic acid have shown it to be superior to benzoyl peroxide in reducing the total number of acne lesions. Adverse reactions to salicylic acid are generally limited to mild, local irritation occurring in a minority of patients.
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2. Study: Salicylic acid treats acne vulgaris by suppressing AMPK/SREBP1 pathway in sebocytes
Lu J, Cong T, Wen X, et al. Salicylic acid treats acne vulgaris by suppressing AMPK/SREBP1 pathway in sebocytes. Exp Dermatol. 2019;28(7):786-794.
Discussion: Excess sebum production contributes to the pathogenesis of acne vulgaris, and suppression of sebum production reduces acne incidence and severity.
Treatment with SA decreased sebocyte lipogenesis by downregulating the adenosine monophosphate-activated protein kinase (AMPK)/sterol response element-binding protein-1 (SREBP-1) pathway and reduced inflammation by suppressing the NF-κB pathway in these cells.
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3. Study: Efficacy and safety of superficial chemical peeling in treatment of active acne vulgaris
Al-Talib H, Al-Khateeb A, Hameed A, Murugaiah C. Efficacy and safety of superficial chemical peeling in treatment of active acne vulgaris. An Bras Dermatol. 2017;92(2):212-216.
Conclusion: This study showed that almost all patients tolerated well the chemical peeling procedures despite a mild discomfort, burning, irritation and erythema have been reported; also the incidence of major adverse events was very low and easily manageable. In conclusion, chemical peeling with glycolic acid is a well-tolerated and safe treatment modality in active acne vulgaris while salicylic acid peels is a more convenient for treatment of darker skin patients and it showed significant and earlier improvement than glycolic acid.
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4. Article: Salicylic acid as a peeling agent: a comprehensive review
Arif, Tasleem. (2015). Salicylic acid as a peeling agent: A comprehensive review. Clinical, Cosmetic and Investigational Dermatology. 8. 10.2147/CCID.S84765.
Conclusion: SA is a safe and efficacious peeling agent for a number of dermatological and cosmetic problems, including acne vulgaris, melasma, photodamage, freckles, and lentigines. It can be safely used in dark skin types.
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Results: All the patients showed improvement of acne at the end of the treatment. The mean improvement of inflammatory acne in Group A was 73.3% and in Group B was 65.4%. The mean improvement of noninflammatory acne in Group A was 39.4%, and Group B was 27.9%. In both groups, the improvement in both inflammatory and noninflammatory lesions was found to be statistically significant (P < 0.05).
Conclusion: Salicylic acid peel was found to be more efficacious than mandelic acid peel. However, the side effects were less common with no postinflammatory hyperpigmentation with mandelic acid peel.
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6. Study: Study of glycolic acid and salicylic acid peels as a sole therapy in treatment of acne vulgaris
Results: After 6 sessions, in the glycolic acid group the reduction in average number of comedones was 88.45%, inflammatory papules 88.65%, pustules 89.62% & nodules/cysts 83.33%. Whereas, in the Salicylic acid group, the reduction was 89.00%, 90.36%, was 84.87% & 100% in comedones, papules, pustules & nodules/cysts respectively.
Conclusion: In our observation, both 35% glycolic acid and 30% salicylic acid are significantly effective as monotherapy in patients of acne. They not only clear the acne lesions but also show improvement in post acne scar and hyperpigmentation to some extent.
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7. Study: Effect of 30% salicylic acid peels in mild to moderate acne vulgaris: a hospital-based non-randomised clinical study
Results: By the end of 6 weeks, excellent improvement in acne severity index was noted in 60% of cases and very good improvement in 30%. By the end of 6 weeks, excellent improvement in total lesion count was noted in 60% and very good improvement in 34%.
Conclusion: Our study showed excellent to good improvement in most of patients. Our study showed that 30% salicylic acid peels can be considered as an important adjuvant therapy in mild to moderate acne with faster clinical response.
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8. Article on anti-inflammatory action: Wu KK. Salicylates and their spectrum of activity. Anti-Inflamm Anti-Allergy Agent Med Chem. 2007;6:278.
Discussions: Experimental and clinical data indicate that salicylates exhibit a spectrum of activities that include anti-inflammatory and antimicrobial actions. As a member of the aspirin family, salicylic acid achieves its analgesic and anti-inflammatory properties by truncating the AA cascade. Salicylates are active in controlling inflammation by altering gene expressions. They suppress the expression of proinflammatory genes by inhibiting the DNA-binding activities of transcription activators.
Salicylic acid is known to decrease the frequency and severity of acne eruptions by reducing acne-associated inflammation in addition to imparting an exfoliating action over the pores.
Salicylic acid has a small molecular size, allowing penetration into the underlying skin layers, cleaning the skin by exfoliating or removing dead skin cells and debris that clogs pores. As salicylic acid clears pores, in increases the rate of cell turnover, making it an effective treatment for skin conditions such as acne or rosacea.
Rosacea often displays as skin bumps formed by a buildup of the skin protein keratin around the hair follicle. Salicylic acid is a keratolytic medication that functions by softening keratin, allowing other medications to penetrate skin layers more effectively.
According to a 2007 study by Julia Yu-Yun Lee, MD and Chao-Kai Hsu, MD published on the Dermatology Online Journal, salicylic acid also helps clear skin pores of demodex folliculorum, a skin mite commonly found in skin pores but that causes excessive inflammation in rosacea patients if they penetrate into underlying skin layers.
Study on anti-inflammatory action: Wu KK. Salicylates and their spectrum of activity. Anti-Inflamm Anti-Allergy Agent Med Chem. 2007;6:278.
Discussion: Experimental and clinical data indicate that salicylates exhibit a spectrum of activities that include anti-inflammatory and antimicrobial actions. As a member of the aspirin family, salicylic acid achieves its analgesic and anti-inflammatory properties by truncating the AA cascade. Salicylates are active in controlling inflammation by altering gene expressions. They suppress the expression of proinflammatory genes by inhibiting the DNA-binding activities of transcription activators.
Study: Wu KK. Salicylates and their spectrum of activity. Anti-Inflamm Anti-Allergy Agent Med Chem. 2007;6:278.
Discussions: Experimental and clinical data indicate that salicylates exhibit a spectrum of activities that include anti-inflammatory and antimicrobial actions. As a member of the aspirin family, salicylic acid achieves its analgesic and anti-inflammatory properties by truncating the AA cascade. Salicylates are active in controlling inflammation by altering gene expressions. They suppress the expression of proinflammatory genes by inhibiting the DNA-binding activities of transcription activators.
Salicylic acid is known to decrease the frequency and severity of acne eruptions by reducing acne-associated inflammation in addition to imparting an exfoliating action over the pores.
Ranjan R, Sarkar R, Garg VK, Gupta T. A Comparative Study of Two Modalities, 4% Hydroquinone Versus 30% Salicylic Acid in Periorbital Hyperpigmentation and Assessment of Quality of Life Before and After Treatment. Indian J Dermatol. 2016;61(4):413-417.
Results: Majority of the cases, i.e. 26 (52%) were in the age group of 20–30 years. Females comprised 74% of the study population. On VAS, most of the patients showed mild improvement (10–30%) at 12 weeks of treatment in both the groups. Separately, both the treatments significantly improved the dermatological life quality index of the patients although there was no significant difference found between the two groups.
Conclusion: POH is less responsive to standard treatments due to its multifactorial etiology and deposition of melanin in both dermis and epidermis. However, even the mild to moderate improvement in appearance can cause an improvement in the quality of life of the patients.
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Sarkar R, Ghunawat S, Garg VK. Comparative Study of 35% Glycolic Acid, 20% Salicylic-10% Mandelic Acid, and Phytic Acid Combination Peels in the Treatment of Active Acne and Postacne Pigmentation. J Cutan Aesthet Surg. 2019;12(3):158-163.
Salicylic acid decreases postacne hyperpigmentation by its anti-inflammatory effects. Ahn and Kim found salicylic acid to have a whitening effect on the skin as well. Mandelic acid also has a beneficial effect in improving skin pigmentation.
Results: Significant reduction in inflammatory and noninflammatory lesion count was noted at 12 weeks in all the three study groups. Reduction in acne score at the end of 12 weeks in the three study groups was 70.55%, 74.14%, and 69.7%, respectively. A significant decline was observed in the postacne hyperpigmentation index in all the three study groups at the end of 12 weeks (P = 0.034).
Conclusion: All three chemical peels are effective in the treatment of mild to moderate acne in Asian population. No significant adverse effects were noted.
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3. Article: Salicylic acid peel in pigmented skin
Okoro OE. Salicylic acid peel in pigmented skin. J Dermat Cosmetol. 2018;2(1):70. DOI: 10.15406/jdc.2018.02.00070
Discussion: Various studies had reported the effectiveness of Salicylic acid (20%-30%) peel in the management of acne vulgaris. However, there are reports of transient pigmentary changes at such concentrations in patients with Fitzpatrick types IV-VI.
Salicylic acid at concentrations of 15-20% remains the best option for superficial peel in pigmented skin with acne and/or excessive sebum secretion. At a lower concentration (15%-20%), Salicylic acid peel is equally effective in pigmented skin with acne.
- It reduces the number of both inflammatory and non-inflammatory lesions.
- It has a comedolytic effect because of the exfoliation of the epidermis.
- In addition, it has anti-inflammatory effects, reducing the effects of inflammatory cytokines.
- Salicylic acid is lipophilic; therefore, it can penetrate to the sebaceous glands when applied to the epidermis.
- It reduces secretion of sebum causing dryness of the facial skin. This is beneficial in reducing comedone formation and controlling sebum secretion in patients with excessive secretion of sebum. However, in the few acne patients with normal or low sebum secretion, lower concentration (15%) of Salicylic acid peels will be effective with minimal discomfort.
- One of the common complications of chemical peels in pigmented skin types is the risk of dyschromia especially post-inflammatory hyper pigmentation. There is little or no risk of post-inflammatory hyper pigmentation when using Salicylic acid peels in pigmented skin. This is unlike the use of Trichloroacetic acid peel in pigmented skin where post-inflammatory hyper pigmentation can occur.
- Salicylic acid peel is cheap and affordable. This makes it an ideal peel in resource poor setting and developing African nations. It is readily available and effective for patients who may not afford the more expensive options.
Conclusion: Superficial chemical peels are important in the treatment of acne in skin types IV–VI. Salicylic acid peels at concentrations of 15%-20% is the better option for pigmented skin types with acne and excessive sebum secretion.
1. Article: Salicylic acid protects the skin from UV damage.
Mammone T, Gan D, Goyarts E, Maes D. Salicylic acid protects the skin from UV damage. Journal of Cosmetic Science. 2006 Mar-Apr;57(2):203-204.
Abstract: Aspirin(acetyl salicylate) has long been used as an analgesic. Salicylic acid has been reported to have anti-inflammatory properties. These activities include inhibiting activity of cox-1, cox-2, and NF-kb. In addition, salicylic acid has also been shown in some systems to induce Hsp70.
We have demonstrated that salicylic acid inhibits UVB-induced sunburn cell formation, as well as increase the removal of UVB induced TT dimer formation in living skin equivalents. Given these protective properties of salicylic acid, we propose the use of salicylic acid as a topical therapeutic to protect the skin from sun damage.
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2. Article: Salicylic acid as a peeling agent: a comprehensive review
Arif, Tasleem. (2015). Salicylic acid as a peeling agent: A comprehensive review. Clinical, Cosmetic and Investigational Dermatology. 8. 10.2147/CCID.S84765.
Abstract: Kligman and Kligman used SA as a superficial peeling agent in women with mild to moderate photodamage, and reported improvement in surface roughness and pigmented lesions, along with a reduction in fine lines.
Grimes treated patients from a darker racial ethnic group who had acne vulgaris, melasma, or post-inflammatory hyperpigmentation with 20% and 30% SA peels, and reported good efficacy with minimal side effects.
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3. Article: Salicylic Acid Peels for the Treatment of Photoaging
KLIGMAN, DOUGLAS MD, PhD1; KLIGMAN, ALBERT M. MD, PhD1 Salicylic Acid Peels for the Treatment of Photoaging, Dermatologic Surgery: March 1998 - Volume 24 - Issue 3 - p 325-328doi: 10.1111/j.1524-4725.1998.tb04162.x
Abstract: Salicylic acid, a beta-hydroxy acid, at a higher strength (30% in a hydro-ethanolic vehicle) has distinct advantages for resurfacing moderately photodamaged facial skin. We have peeled patients singly and multiply at 4-week intervals. The benefits are fading of pigment spots, decreased surface roughness, and reduction of fine lines.
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4. Study: Three clinical studies showing the anti-aging benefits of sodium salicylate in human skin
Merinville E, Byrne AJ, Rawlings AV, Muggleton AJ, Laloeuf AC. Three clinical studies showing the anti-aging benefits of sodium salicylate in human skin. J Cosmet Dermatol. 2010;9(3):174-184.
Background: Anti-aging effects of high concentrations of salicylic acid (SA) peels are commonly known. Like all acids, SA can produce somatosensory and visible irritation to the skin and as such may be unsuitable for subjects with sensitive skin.
Aims: To provide evidence that sodium salicylate (SS) obtained from neutralization of 1% SA by sodium hydroxide can deliver significant anti-aging benefits.
Methods: The effects of SS were examined using three approaches: (1) evaluating its effects on stimulating the synthesis of fibrillin and collagen-1 in vivo; (2) examining its efficacy by using Fast Optical in vivo Topometry (FOITS) in a double-blind, placebo-controlled clinical study; (3) determining its effects on both expert and naïve grader assessement of wrinkles in a double-blind, placebo-controlled study.
Results: In the first study SS produced significant increases of the fibrillin and collagen-1 anti-aging biomarkers compared with the untreated skin control. A commercially available retinol cream delivered similar effects to SS. In the second study using FOITS we showed that the SS formulation significantly reduced wrinkle depth (Rz) and skin roughness (Ra) after 4 and 8 weeks of daily application vs. placebo (Rz: -8.2 ± 1.40% and -11.4 ± 1.07%; Ra: -7.8 ± 1.33% and -11.9 ± 0.61%; P < 0.01). In the third study reductions in wrinkle depth were observed by expert assessment at both 4 and 8 weeks for the SS-containing formulation compared to its placebo (P < 0.05). Equally, non-expert graders recorded the SS formulation superior to its placebo.
Conclusion: Although the mechanism of action is not completely understood, we believe the benefits of SS are derived from its intrinsic stratum corneum exfoliation effects. All three studies demonstrate the significant anti-aging effects of SS that are especially suitable for subjects with sensitive skin.
GLYCOLIC ACID
- Renewal facial cleanser: 5%
- Radiant gel: 10%
- Chemical peel spray: 10%
- Rejuvenize peel: 25% ; 35% ; 50%
- Illuminize peel
1. Study: The effect of glycolic acid on the treatment of acne in Asian skin
Wang CM, Huang CL, Hu CT, Chan HL. The effect of glycolic acid on the treatment of acne in Asian skin. Dermatol Surg. 1997;23(1):23-29. doi:10.1111/j.1524-4725.1997.tb00003.x
Results: Significant resolution of comedones, papules, and pustules was found. The skin texture of each candidate was dramatically rejuvenated. Consistent and repetitive treatment with glycolic acid was needed for the apparent improvement of acne scars and cystic lesions. The follicular pores also became comparatively smaller. Furthermore, most of the candidates had much brighter and lighter looking skin. Only small percentage of patients (5.6%) developed side effects.
Conclusion: Glycolic acid has considerable therapeutic value for acne with minimal side effects even in Asian skin. It may be an ideal adjunctive treatment of acne.
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Erbağci Z, Akçali C. Biweekly serial glycolic acid peels vs. long-term daily use of topical low-strength glycolic acid in the treatment of atrophic acne scars. Int J Dermatol. 2000;39(10):789-794. doi:10.1046/j.1365-4362.2000.00076.x
Results: The differences between the results in the different groups were statistically significant at week 24 (P<0.001). Home application of low-strength glycolic acid was better tolerated and had less side-effects than glycolic acid peels; however, repeated short-contact 70% glycolic acid peels provided superior results compared with the maintenance regimen (P<0.05), and apparently good responses were observed only in the peel group (P<0.01).
Conclusions: Glycolic acid peeling is an effective modality for the treatment of atrophic acne scars, but repetitive peels (at least six times) with 70% concentration are necessary to obtain evident improvement. Long-term daily use of low-strength products may also have some useful effects on scars and may be recommended for patients who cannot tolerate the peeling procedure.
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3. Study: Combination of microneedling and glycolic acid peels for the treatment of acne scars in dark skin
Sharad J. Combination of microneedling and glycolic acid peels for the treatment of acne scars in dark skin. J Cosmet Dermatol. 2011;10(4):317-323. doi:10.1111/j.1473-2165.2011.00583.x
Results: Based on the objective scoring and its statistical analysis, there was significant improvement in superficial and moderately deep scars (grade 1-3). There was also improvement in skin texture, reduction in postacne pigmentation in the second group.
Conclusion: Microneedling is a simple, inexpensive office procedure with no downtime. It is safe in Indian skin (skin types III-IV). The combined sequential treatment with GA peel caused a significant improvement in the acne scars without increasing morbidity.
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4. Study: Microneedling by dermapen and glycolic acid peel for the treatment of acne scars: Comparative study
Saadawi AN, Esawy AM, Kandeel AH, El-Sayed W. Microneedling by dermapen and glycolic acid peel for the treatment of acne scars: Comparative study. J Cosmet Dermatol. 2019;18(1):107-114. doi:10.1111/jocd.12827
Background: Many methods have been performed to achieve a satisfying outcome in acne scars but some of them were high cost and also were associated with low results and some complications.
Objectives: To evaluate and compare the efficacy and safety therapy of glycolic acid (GA) peel, microneedling with dermapen and a combination of both procedures in treatment of atrophic acne scars.
Patents and methods: This study was conducted on 30 patients suffering from acne scars. They were randomly assigned into three groups, each group included 10 patients; group I was treated with GA peel, group II treated was with microneedling. Group III received a combination of both procedures. All patients received six sessions with 2-week intervals. The clinical assessment was based on the qualitative global scar grading system before and after treatment, quartile grading scale, and degree of patient satisfaction.
Results: There was a statistically significant decrease in acne scars grade after treatment among the studied groups (P = 0.04) but it was higher in group III. There was improvement in boxcar, ice pick, and rolling scars in all groups, respectively (P = 0.03, P = 0.04, P = 0.04). Patients' satisfaction was higher in group III (P = 0.04).
Conclusion: The combination of dermapen and GA peel is more effective than monotherapy.
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Abels C, Kaszuba A, Michalak I, Werdier D, Knie U, Kaszuba A. A 10% glycolic acid containing oil-in-water emulsion improves mild acne: a randomized double-blind placebo-controlled trial. J Cosmet Dermatol. 2011;10(3):202-209. doi:10.1111/j.1473-2165.2011.00572.x
Background: Acne is characterized by hyperseborrhea, follicular hyperkeratosis, and growth of propionibacteria. Alpha hydroxy acids depending on the pH of the finished product exhibit comedolytic as well as antimicrobial properties.
Objectives: The aim of this study was to investigate an oil-in-water emulsion-containing 10% glycolic acid (pH 4) as monotherapy in mild acne regarding clinical efficacy and tolerability for 90 days.
Patients and methods: Patients (n = 120; 73 f, 47 m) suffering from mild acne (Leeds score 0.25-1) aged ≥12 (mean 21 ± 5.8) were included in this double-blind, placebo-controlled, randomized, monocentric trial. The cream was applied once daily in the evening. No additional products were used. Cleansing was standardized by supplying the same product to all patients.
Results: The number of patients (n = 115) in the per-protocol and intention-to-treat analysis was the same. Acne improved significantly in the verum group up to day 90. Already at day 45, there was a statistical significant (5% level) difference against placebo. The subjective evaluation of the verum by physicians and patients regarding clinical efficacy and tolerability was favorable. Regarding reported adverse effects, there was no statistically significant difference (5% level) between verum and placebo.
Conclusions: The 10% glycolic acid containing oil-in-water emulsion improved mild acne applied as monotherapy in this study significantly, already after 45 days of treatment. Regarding tolerability, there was no objective or subjective difference between the 10% glycolic acid containing oil-in-water emulsion and the corresponding placebo.
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6. Article: pH-Dependent Antibacterial Activity of Glycolic Acid: Implications for Anti-Acne Formulations
Valle-González ER, Jackman JA, Yoon BK, Mokrzecka N, Cho NJ. pH-Dependent Antibacterial Activity of Glycolic Acid: Implications for Anti-Acne Formulations. Sci Rep. 2020;10(1):7491. Published 2020 May 4. doi:10.1038/s41598-020-64545-9
Abstract: Herein, we report that glycolic acid exhibits pH-dependent antibacterial activity against C. acnes. Cutibacterium acnes (formerly known as Propionibacterium acnes), is a Gram-positive bacterium implicated in acne pathogenesis. The degree of antibacterial activity, including minimum bactericidal concentration (MBC), of glycolic acid was evaluated in the pH range of 3 to 4.5, and the greatest potency was observed at pH 3.
1. Study: Safety and efficacy of glycolic acid facial peel in Indian women with melasma
Javaheri SM, Handa S, Kaur I, Kumar B. Safety and efficacy of glycolic acid facial peel in Indian women with melasma. Int J Dermatol. 2001;40(5):354-357.
Results: In a study by Javaheri et al, peeling was performed upon 15 Indian females with melasma, using 50% Glycolic acid once-monthly for 3 months.
An improvement in Melasma Area Severity Index (MASI) score was observed in 91% of patients (P < 0.01). A better response was seen in patients with epidermal melasma, compared to those with mixed melasma (P < 0.05).
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Kumari R, Thappa DM. Comparative study of trichloroacetic acid versus glycolic acid chemical peels in the treatment of melasma. Indian J Dermatol Venereol Leprol. 2010;76(4):447.
Results: In a comparative study of 10%–20% TCA versus 20%–35% GA peels for the treatment of melasma: Similar improvement was seen with both peels. However, the GA peel was seen to be associated with fewer side effects than the TCA peel, and gave the added benefit of facial rejuvenation.
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3. Study: Comparative study of 15% TCA peel versus 35% glycolic acid peel for the treatment of melasma
Puri N. Comparative study of 15% TCA peel versus 35% glycolic acid peel for the treatment of melasma. Indian Dermatol Online J. 2012;3(2):109-113.
Results: In another similar study of 15% TCA peel versus 35% GA peel for the treatment of melasma: No statistically significant difference in efficacy. Both peels significantly reduced MASI scores, and Both were found to be equally effective in the treatment of melasma. It was also seen that adverse effects were more common with TCA than with Glycolic acid peels.
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MVP Journal of Medical Sciences, Vol 2(1), 39–48, January-June 2015
Background: Melasma, one of the common aesthetically displeasing entities, continues to be a difficult problem to treat. Chemical peeling is one new weapon in the therapeutic armamentarium of melasma. Intense Pulsed Light (IPL) is a noncoherent, broad-spectrum light, ranging from 500 to 1200 nm. Intense Pulsed Light (IPL) treatment is a good option for patients with melasma. Aims and Objective: To compare the efficacy of glycolic acid peel and intense pulsed light in the treatment of melasma. Setting: Outpatient department of Dermatology, Venerology Leprology of a tertiary health care centre with an attached medical college.
Material and Methods: 60 patients of melasma were recruited in the study. Patients were randomly allocated into two groups: one group (glycolic acid 50%) and another group (IPL) with 30 patients in each group. All the participants were subjected to undergo pre-peel programme of daily application of sunscreens (day time) and 0.025% retinoic acid at bed time.
Four peels were carried out at 2 weekly intervals. Four sessions of IPL were done at 3 weeks interval. MASI scoring and coloured photographs (without reavealing identity) of each patient were taken before each peel and at the end of the follow-up period i.e. 2 weeks after 4th sitting in GA peel group and 3 weeks after 4th sitting in IPL group. Side effects, if any, were also recorded. Statistical Analysis Used: SYSTAT version-12.
Results: In both the groups there was constant decrease in MASI scores after each sitting as compared to pre-peel scores. However, the comparison of mean MASI scores i.e. both pre-peel and after each peel, between the two groups showed statistically significant difference (p<0.05). Local reactions, such as burning sensation and erythema during the peel were not significant with both the groups.
Conclusions: Glycolic Acid (GA) peel (50%) is more efficacious & safe treatment modality in melasma compared to IPL.
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Background: Melasma is acquired symmetric hypermelanosis characterized by light-to-deep brown pigmentation over cheeks, forehead, upper lip, and nose. Treatment of this condition is difficult and associated with high recurrence rates. Chemical peels have become a popular modality in the treatment of melasma.
Objective: To compare the therapeutic efficacy and tolerability of glycolic acid (35%) versus salicylicmandelic (SM) acid (20% salicylic/10% mandelic acid) versus phytic combination peels in Indian patients with melasma.
Materials and Methods: Ninety patients diagnosed with melasma were randomly assigned into 3 groups of 30 patients each. Group A received glycolic acid (GA-35%) peel, Group B received SM acid, and Group C received phytic combination peels. Each group was primed with 4% hydroquinone and 0.05% tretinoin cream for 4 weeks before treatment. Chemical peeling was done after every 14 days in all groups until 12 weeks. Clinical evaluation using melasma area and severity index (MASI) score and photography was recorded at every visit and follow-up was done until 20 weeks.
Results: There was a decrease in MASI score in all 3 groups but it was statistically significantly lower in Group A than Group C (p = .00), and it was also statistically significantly lower in Group B than Group C (p = .00) but there was no statistically significant difference between Groups A and B (p = .876). Objective response to treatment evaluated by reduction in MASI scoring after 12 weeks was 62.36% reduction in GA group, 60.98% reduction in SM group, and 44.71% in phytic acid group. Conclusion: It is concluded that GA (35%) and SM acid peels are both equally efficacious and a safe treatment modality for melasma in Indian skin, and are more effective.
1. Study: The therapeutic value of glycolic acid peels in dermatology
Grover C, Reddu BS. The therapeutic value of glycolic acid peels in dermatology. Indian J Dermatol Venereol Leprol. 2003;69(2):148-150.
Results: In a pilot study by Burns et al, postinflammatory hyperpigmentation was treated with a series of Glycolic acid peels in skin types IV–VI.
No adverse effects were reported in dark skin, Glycolic acid peel proved to be efficacious.This echoed the study by Grover and Reddu, in which skin types III–V showed overall improvement of skin texture in almost all patients.
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2. Article: Glycolic acid peel therapy – a current review
Sharad J. Glycolic acid peel therapy - a current review.
Clin Cosmet Investig Dermatol. 2013;6:281-288. Published 2013 Nov 11.
Discussion:
- With cases of postinflammatory hyperpigmentation in skin types III and IV, a series of 35% GA peels has produced good results.
Complete resolution of postinflammatory hyperpigmentation is commonly seen after six to eight peel treatments.
- 15% TCA peel versus 35% GA peel for the treatment of melasma, there was no statistically significant difference in efficacy. Both peels significantly reduced MASI scores, and both were found to be equally effective in the treatment of melasma. It was also seen that adverse effects were more common with TCA than with GA peels.
Comparative study of 15% TCA peel versus 35% glycolic acid peel for the treatment of melasma.
Puri NIndian Dermatol Online J. 2012 May; 3(2):109-13.
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3. Study: Glycolic Acid Peels for Postinflammatory Hyperpigmentation in Black Patients
Background: Treatment of postinflammatory hperpigmentation in patients of Fitzpatrick skin types TV, V, and VI is difficult, Glycolic acid peels are useful for pigment dyschromias in Caucasians; however, there are no controlled studies examining their safety and efficacy in dark-complexioned individuals. objective. To determine if serial glycolic acid peels provide additional improvement when compared with a topical regimen of hydroquinone and tretinoin.
Method: Nineteen patients with Fitzpatrick skin type IV, V, or VI were randomized to a control or peel group. The control group applied 2% hydroquinone/10% glycolic acid get twice daily and 0.05% tretinoin cream at night. The peel patients used the same topical regimen and, in addition, received six serial glycolic acid peels (68% maximum concentration). Patients were evaluated with photography, colorimetry, and subjectively.
Results: Sixteen patients completed the study. Both treatment groups demonstrated improvement, but the patients receiving the glycolic acid peels showed a trend toward more rapid and greater improvement. The peel group also experienced increased lightening of the normal skin.
Conclusions: This pilot study demonstrates that serial glycolic acid peels provide an additional benefit, with minimal adverse effects, for the treatment of postinflammatory hyperpigmentation in dark-complexioned individuals.
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MVP Journal of Medical Sciences, Vol 2(1), 39–48, January-June 2015
Background: Melasma, one of the common aesthetically displeasing entities, continues to be a difficult problem to treat. Chemical peeling is one new weapon in the therapeutic armamentarium of melasma. Intense Pulsed Light (IPL) is a noncoherent, broad-spectrum light, ranging from 500 to 1200 nm. Intense Pulsed Light (IPL) treatment is a good option for patients with melasma. Aims and Objective: To compare the efficacy of glycolic acid peel and intense pulsed light in the treatment of melasma. Setting: Outpatient department of Dermatology, Venerology Leprology of a tertiary health care centre with an attached medical college.
Material and Methods: 60 patients of melasma were recruited in the study. Patients were randomly allocated into two groups: one group (glycolic acid 50%) and another group (IPL) with 30 patients in each group. All the participants were subjected to undergo pre-peel programme of daily application of sunscreens (day time) and 0.025% retinoic acid at bed time.
Four peels were carried out at 2 weekly intervals. Four sessions of IPL were done at 3 weeks interval. MASI scoring and coloured photographs (without reavealing identity) of each patient were taken before each peel and at the end of the follow-up period i.e. 2 weeks after 4th sitting in GA peel group and 3 weeks after 4th sitting in IPL group. Side effects, if any, were also recorded. Statistical Analysis Used: SYSTAT version-12.
Results: In both the groups there was constant decrease in MASI scores after each sitting as compared to pre-peel scores. However, the comparison of mean MASI scores i.e. both pre-peel and after each peel, between the two groups showed statistically significant difference (p<0.05). Local reactions, such as burning sensation and erythema during the peel were not significant with both the groups.
Conclusions: Glycolic Acid (GA) peel (50%) is more efficacious & safe treatment modality in melasma compared to IPL.
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5. Article: FDA Pharmacy Compounding Advisory Committee
Jane Liedtka, MD Clinical Reviewer Division of Dermatology and Dental Products, Office of Drug Evaluation III
Discussion:
- Glycolic acid, 0.08% to 70%, has been nominated for inclusion on the list of bulk drug substances for use in compounding under section 503A of the Federal Food, Drug, and Cosmetic Act (FD&C Act) for topical use in the treatment of hyperpigmentation disorders and photodamaged skin.
- Pharmacology – One theory for the mechanism of action of alphahydroxy acids (AHAs) in exfoliation is: AHAs reduce calcium ion concentration in the epidermis and remove calcium ions from the cell adhesions by chelation; this causes disruption in cell adhesions, and results in desquamation
- Glycolic acid can suppress melanin formation by inhibition of tyrosinase activity.
Summary of Clinical Trial Data
Melasma and Other Hyperpigmentation Disorders: - Glycolic acid peels of 20% to 70%
- Improvement with glycolic acid comparable to that with other peels, such as tretinoin, trichloroacetic acid, lactic acid, Jessner solution, or capryloyl salicylic acid.
- Numerous active controlled trials show consistently positive results in the treatment of melasma with glycolic acid, either as a peel or as a topical agent.
- Evidence from a vehicle-controlled trial support effectiveness of glycolic acid for mitigation of manifestations of photodamaged skin.
Newman N, Newman A, Moy LS, Babapour R, Harris AG, Moy RL. Clinical improvement of photoaged skin with 50% glycolic acid. A double-blind vehicle-controlled study. Dermatol Surg. 1996;22(5):455-460.
Background: Although there is increasing interest in the use of glycolic acid in the treatment of photoaged skin, to our knowledge, no controlled study has been done to assess the efficacy or the mode of this agent.
Objective: The purpose of this study was to determine whether 50% glycolic acid can improve photoaged skin and to study the histological basis for this improvement.
Methods: Forty-one volunteers were recruited into this double-blind vehicle-controlled study. Glycolic acid (50%) or vehicle was applied topically for 5 minutes to one side of the face, forearms, and hands, once weekly for 4 weeks. Punch biopsies were taken at pretherapy and at 5 weeks for histologic study.
Results: Significant improvement noted included decrease in rough texture and fine wrinkling, fewer solar keratoses, and a slight lightening of solar lentigines. Histology showed thinning of the stratum corneum, granular layer enhancement, and epidermal thickening. Some specimens showed an increase in collagen thickness in the dermis.
Conclusion: The results of this study demonstrate that the application of 50% glycolic acid peels improves mild photoaging of the skin.
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2. Study: Glycolic acid treatment increases type I collagen mRNA and hyaluronic acid content of human skin
Bernstein EF, Lee J, Brown DB, Yu R, Van Scott E. Glycolic acid treatment increases type I collagen mRNA and hyaluronic acid content of human skin. Dermatol Surg. 2001;27(5):429-433.
Background: Chronic solar irradiation results in both morphologic and functional changes in affected skin. alpha-hydroxy acids, such as glycolic acid, have been shown to improve photodamaged skin.
Objective: To investigate alterations in collagen gene induction and epidermal and dermal hyaluronic acid production as a result of administered glycolic acid.
Methods: In this study we compared collagen gene expression from skin biopsy specimens, and epidermal and dermal hyaluronic acid immunohistochemical staining between glycolic acid-treated and vehicle-treated skin. Forearm skin was treated with 20% glycolic acid lotion or a lotion vehicle control twice a day for 3 months.
Results: Epidermal and dermal hyaluronic acid and collagen gene expression were all increased in glycolic acid-treated skin as compared to vehicle-treated controls.
Conclusion: Our data suggest that epidermal and dermal remodeling of the extracellular matrix results from glycolic acid treatment. Longer treatment intervals may result in collagen deposition as suggested by the measured increase in mRNA.
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Ditre CM, Griffin TD, Murphy GF, et al. Effects of alpha-hydroxy acids on photoaged skin: a pilot clinical, histologic, and ultrastructural study. J Am Acad Dermatol. 1996;34(2 Pt 1):187-195
Background: alpha-Hydroxy acids (AHAs) have been reported to improve aging skin. The mechanisms of action of AHAs on epidermal and dermal compartments need clarification.
Objective: Our purpose was to determine the effects of AHAs on photoaged human skin by clinical and microanalytic means.
Methods: Patients applied a lotion containing 25% glycolic, lactic, or citric acid to one forearm and a placebo lotion to the opposite forearm for an average of 6 months. Thickness of forearm skin was measured throughout the study. Biopsy specimens from both forearms were processed for analysis at the end of the study.
Results: Treatment with AHAs caused an approximate 25% increase in skin thickness. The epidermis was thicker and papillary dermal changes included increased thickness, increased acid mucopolysaccharides, improved quality of elastic fibers, and increased density of collagen. No inflammation was evident.
Conclusion: Treatment with AHAs produced significant reversal of epidermal and dermal markers of photoaging.
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4. Article: Cosmetic and dermatologic use of alpha hydroxy acids
Discussion:
- Glycolic acid increase epidermal thickness dramatically (by 17%). Meaning it can reverse some of the skin thinning that happens with age.
- GA increase epidermal hyaluronic acid content (by 180%) and hyaluronic acid dermal content too (9%). This increases the water binding capacity of your skin. Skin is plumper and the appearance of wrinkles is lessened. Hyaluronic acid also helps to make skin less fragile, and skin is healthier because cells and nutrients can move around in it better.
- GA turn on the genes for making skin collagen (3 times greater than before). Meaning that wrinkles are actively addressed - because reversing wrinkles requires that skin makes collagen in the dermis (the deeper part of your skin) below the epidermis (the top living layer).
- GA even-out irregular skin pigmentation. Meaning it can get rid of age spots and even help lighten hyperpigmentation from melasma.
- GA reverse the signs of classic sun damage in the epidermis that we see under the microscope. Making the structure of your skin look more like a kid’s when we view it under a microscope (in doctor speak there is a reversal of basal cell atypia and return of the normal undulating rete pattern).
- GA exfoliate the dead skin cells. Meaning your skin looks dewy and moist and feels softer.
RETINOL: Hydroxypinacolone retinoate
- Retinol serum: 3%
- Time Freeze eye serum: 0.5%
- Dark circle eye serum: 0.5%
- Tri-Active Retinol peel: 2%
Veraldi S, Barbareschi M, Guanziroli E, et al. Treatment of mild to moderate acne with a fixed combination of hydroxypinacolone retinoate, retinol glycospheres and papain glycospheres. G Ital Dermatol Venereol. 2015;150(2):143-147.
Aim: A fixed combination of 0.1% hydroxypinacolone retinoate (synthetic esther of 9-cis-retinoic acid), 1% retinol in glycospheres and 2% papain in glycospheres in aqueous gel has been recently introduced into the Italian market in order to reduce the incidence and severity of irritant contact dermatitis caused by topical retinoids, without compromising their efficacy. Primary objectives of this sponsor-free, pilot, open, multicenter study were to evaluate the efficacy and tolerability of this gel in patients with comedonal-papular, mild to moderate acne of the face.
Methods: Ninety-eight Caucasian patients (28 males and 70 females), with an age ranging from 15 to 40 years, were treated with the gel once daily for 12 weeks. Acne severity and treatment efficacy were evaluated by means of the Global Acne Grading System (GAGS) and lesions count.
Results: Ninety-four patients were considered evaluable. A 41% mean reduction in the GAGS score was observed; a 40.8% mean reduction of total lesions was recorded; 15.3% of patients experienced mild to moderate local side effects (dryness, peeling, erythema, burning). No patients stopped the treatment because of these side effects.
Conclusion: This study, based on a high number of evaluable patients, demonstrates that this fixed combination is an effective and safe option for the treatment of comedonal-papular, mild to moderate acne of the face. A controlled clinical study is necessary to confirm these data.
1. Study: 1310 Anti-aging effects of retinoid hydroxypinacolone retinoate on skin models
Discussion:
Tretinoin, also known as all-trans retinoic acid (ATRA), is well-known for its anti-aging effects on skin. However, skin irritation, photochemical instability, and concerns about toxicity have hindered the use of ATRA in cosmetic products. Therefore, it is desirable to find new molecules that have increased retinoic acid-like activity without the negative side effects.
Hydroxypinacolone retinoate (HPR) is a cosmetic grade ester of ATRA that has been shown to have innate retinoic acid activity without causing skin irritation. Here, we compared levels of gene transcription by HPR, ATRA, retinol (ROL), retinaldehyde (RAL), and retinyl palmitate (RP) in DNA using a retinoic acid response element (RARE) reporter assay. In addition, we compared the anti-aging properties of HPR to ATRA by testing the effects on collagen levels and skin irritation in organotypic skin models.
Skin models were treated for 5 days with HPR and ATRA, basal media was collected for ELISA analysis, and skins were stained with Massons trichrome (for collagen).
RARE assay results showed that HPR had greater levels of gene transcription than ROL, RAL, and RP at the same concentrations, and was less cytotoxic to cells at a 10 times higher concentration; however, HPR did not achieve gene transcription levels of ATRA.
Skins treated with HPR significantly increased pro-collagen production as compared with untreated control skins, and was comparable to ATRA.
Histological staining of skins for collagen corroborated these results, with the highest dose of HPR out-performing ATRA.
IL-1α ELISA analysis showed that HPR did not induce more (or less) inflammatory response than either ATRA or the vehicle control.
Together these data suggest that HPR is an effective alternative to ATRA and other less potent retinoids in the treatment of aging skin without the detrimental side effects.
Veraldi S, Barbareschi M, Guanziroli E, et al. Treatment of mild to moderate acne with a fixed combination of hydroxypinacolone retinoate, retinol glycospheres and papain glycospheres. G Ital Dermatol Venereol. 2015;150(2):143-147.
Aim: A fixed combination of 0.1% hydroxypinacolone retinoate (synthetic esther of 9-cis-retinoic acid), 1% retinol in glycospheres and 2% papain in glycospheres in aqueous gel has been recently introduced into the Italian market in order to reduce the incidence and severity of irritant contact dermatitis caused by topical retinoids, without compromising their efficacy. Primary objectives of this sponsor-free, pilot, open, multicenter study were to evaluate the efficacy and tolerability of this gel in patients with comedonal-papular, mild to moderate acne of the face.
Methods: Ninety-eight Caucasian patients (28 males and 70 females), with an age ranging from 15 to 40 years, were treated with the gel once daily for 12 weeks. Acne severity and treatment efficacy were evaluated by means of the Global Acne Grading System (GAGS) and lesions count.
Results: Ninety-four patients were considered evaluable. A 41% mean reduction in the GAGS score was observed; a 40.8% mean reduction of total lesions was recorded; 15.3% of patients experienced mild to moderate local side effects (dryness, peeling, erythema, burning). No patients stopped the treatment because of these side effects.
Conclusion: This study, based on a high number of evaluable patients, demonstrates that this fixed combination is an effective and safe option for the treatment of comedonal-papular, mild to moderate acne of the face. A controlled clinical study is necessary to confirm these data.
2. Article: Granactive Retinoid: The Power of Retinol without the Irritation
1. S Mukherjee, A Date and V Patravale, Retinoids in the treatment of skin aging: An overview of clinical efficacy and safety, Clin Interv Aging 1(4) 327-48 (2006)
Introduction:
Granactive Retinoid (INCI Name: Dimethyl Isosorbide (and) Hydroxypinacolone Retinoate), is an ester of all-trans retinoic acid.
This skin care active ingredient belongs to a class of chemical compounds called retinoids, which are natural and synthetic derivatives of vitamin A, capable of binding to retinoid receptors.
The binding of retinoid receptors can enhance gene expression, which effectively turns key cellular functions on and off.
When skin cell retinoid receptors are bound with retinoids, a cascade of mechanisms that benefit the skin complexion are switched on. This can result in enhanced cell proliferation, biosynthesis of extracellular proteins and glycans, and improved cellular turnover. Stimulating these age-defying processes in the skin is critical for fighting and reversing signs of aging.
Biological pathways to youthful skin:
Stimulating cell proliferation and cell turnover are important for normalizing cell renewal and repair processes.
As humans age, skin becomes thinner and less elastic, leading to skin with a loose, sagging, and wrinkled appearance.
Granactive Retinoid (now referred to as ‘the novel retinoid’) helps renew skin plumpness, elasticity and hydration to provide a radiant and fresh appearance. Moreover, the novel retinoid stimulates skin cell proliferation; restoring thickness to skin that has become thinner over time. These processes help fill in lines and wrinkles to give a youthful appearance, while safeguarding skin from further wrinkle development.
Vitamin A Chemistry Challenges:
Although the benefits of retinoids have been known for decades, skin irritation, photochemical instability, and toxicity concerns have hindered their use.
Retinoic acid is a topically applied ingredient recognized for its anti-ageing benefits; however, it can be irritating to skin and is sold as a prescription medication. In recent years, milder synthetic and natural derivatives have become popular alternatives to retinoic acid. These derivatives are metabolized to the active form by skin cells.
Retinol (vitamin A) is the most popular topical retinoid used to date, but its skin irritancy and instability to sunlight has limited its scope and appeal.
Retinol esters are often used to lower the irritation potential and increase stability, but a tradeoff is decreased retinoid activity and benefits.
Opportunities in Vitamin A Skin Care:
The novel retinoid is a next-generation anti-aging product, delivering the performance of retinol and retinoid derivatives with significantly lower irritation potential, thus supporting clear, visibly more youthful looking skin with better consumer acceptance.
The mechanism of action of the novel retinoid is advanced compared to retinol derivatives.
To interact with retinoid receptors, retinol must first be metabolized to more active forms, such as retinaldehyde and retinoic acid using several enzymatic steps. The novel retinoid is unique in that it processes innate retinoic activity, binding directly with retinoid receptors without the need for metabolic breakdown to more biologically active forms. The novel retinoid is dermatologically tested to offer less irritation potential than retinol, providing a gentle, safe and effective anti-aging retinoid.
Performance:
Retinoids are widely regarded as being among the most powerful (if not the most powerful) and effective anti-aging active compounds available.
The two primary reasons the use of retinoids is not universal are issues surrounding irritation potential and stability. Addressing these issues without adversely affecting efficacy provides a breakthrough in opportunities with vitamin A in cosmetic formulations.
Retinoids are known to have positive effect on aged skin. The novel retinoid combats the appearance of fine lines and wrinkles for a younger appearance while increasing skin elasticity for firmer, smoother skin texture. This is achieved because retinoids increase the rate of skin turnover, while also reducing the rate of collagen breakdown, leading to plumper, younger looking skin.
The same process improves overall skin clarity, and appearance is enhanced for a healthier complexion. Dark spots and skin imperfections are reduced for a more even skin tone as a result of the retinoid’s promotion of skin cell-sloughing and a slowing effect on melanin production, which gives a brighter and more luminous appearance to skin. Reduction in pore size is observed, leading to an overall increase in skin clarity. The novel retinoid delivers high performance compared to retinol derivatives, but with a significantly lower irritation potential.
Conclusion:
Granactive Retinoid offers formulators the ability to harness the powerful anti-aging properties of retinoid without irritation and stability issues traditionally associated with older generations of vitamin A analogues.
The ingredient can be incorporated into a wide variety of formulations and perfectly fits the global trend towards milder products.
Due to its superior irritation and stability profile, Granactive Retinoid allows new and exciting opportunities with vitamin A, one of the most trusted efficacious anti-aging active ingredients.
ZINC PYRITHIONE
Medi-Zinc cleanser: 2%
Both rosacea and seborrhea cause sensitive red facial skin, and both respond to some of the same treatments.
Lamore SD, Wondrak GT. Zinc pyrithione impairs zinc homeostasis and upregulates stress response gene expression in reconstructed human epidermis. Biometals. 2011;24(5):875-890. doi:10.1007/s10534-011-9441-6
Zinc Pyrithione is a form of Zinc with anti-fungal and anti-bacterial properties. It is used to ttreat dandruff, eczema, psoriasis and many other skin conditions.
Zinc Pyrithione is a FDA-approved microbial agent used worldwide in topical antimicrobials and has also been examined as an investigational therapeutic targeting psoriasis and UVB induced epidermal hyperplasia.
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2. Article: Zinc Pyrithione: A Topical Antimicrobial With Complex Pharmaceutics
J Drugs Dermatol. 2016;15(2):140-144.
and
3. Article: Zinc therapy in dermatology: a review
Gupta M, Mahajan VK, Mehta KS, Chauhan PS. Zinc therapy in dermatology: a review. Dermatol Res Pract. 2014;2014:709152.
Through clinical type observations, it has been determined that a topical application including Zinc is effective in significantly reducing the redness, flushing and inflammation associated with the chronic, incurable adult acne-like skin condition of Rosacea, and with skin erythema in general.
The efficacy of ZPT originates from two attributes. First, it has a very broad antimicrobial spectrum of activity, including fungi, gram-positive and -negative bacteria. Second, the material has very low solubility, resulting in formulation and delivery as a particulate material, which has distinct performance advantages. The particles are deposited and retained on the target skin surfaces even when delivered from rinse-off products.
These particles slowly release molecularly active material to interact with the surface fungal and bacteria cells to control their population, functioning as slow-release reservoirs to provide extended and persistent benefits.
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4. Article: Zinc salts in dermatology
Stéphan F, Revuz J. Sels de zinc en dermatologie [Zinc salts in dermatology]. Ann Dermatol Venereol. 2004;131(5):455-460.
Zinc is an essential trace element for the human organism. It is not teratogenic and can be given during pregnancy.
Many controlled studies have shown an efficacy on inflammatory lesions.
Zinc pyrithione releases zinc ions, which has anti-inflammatory and antioxidant properties. Zinc ions also inhibit 5α-reductase in the skin.
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5. Study: The antifungal mechanism of action of zinc pyrithione
Reeder NL, Xu J, Youngquist RS, Schwartz JR, Rust RC, Saunders CW. The antifungal mechanism of action of zinc pyrithione. Br J Dermatol. 2011;165 Suppl 2:9-12.
Background: Zinc pyrithione (ZPT) is the active ingredient most commonly used in many antidandruff treatments. Despite decades of successful use to treat human scalps, little is understood about the antifungal mechanism of action of ZPT.
Objectives: The objective of this study is to understand the molecular mechanism by which ZPT inhibits fungal growth, the underlying basis for its therapeutic activity.
Methods: Modern systems biology approaches, such as deletion library screening and microarray analysis, were used in combination with traditional measures of metal content, microbial growth and enzyme assays.
Results: It was shown that ZPT inhibits fungal growth through increased cellular levels of copper, damaging iron-sulphur clusters of proteins essential for fungal metabolism.
Conclusions: The molecular basis for the antifungal activity of the commonly used active ZPT has been elucidated, more than 50 years since its introduction, as utilizing a copper toxicity mechanism that targets critical iron-sulphur proteins.
Brandt S. The clinical effects of zinc as a topical or oral agent on the clinical response and pathophysiologic mechanisms of acne: a systematic review of the literature. J Drugs Dermatol. 2013;12(5):542-545.
This article reviews the published literature about the efficacy of oral and topical zinc as treatments for acne vulgaris.
Each published study was assessed for pathophysiologic results and the quality of the clinical evidence the study provided based on Strength of Recommendation Taxonomy (SORT) criteria.
Finally, the body of evidence for using oral or topical zinc in the treatment of acne was assessed, again using SORT criteria.
The preponderance of evidence suggests zinc has antibacterial and anti-inflammatory effects and that it may decrease sebum production.
2. Article: Zinc salts in dermatology
Stéphan F, Revuz J. Sels de zinc en dermatologie [Zinc salts in dermatology]. Ann Dermatol Venereol. 2004;131(5):455-460.
Zinc is an essential trace element for the human organism. It is not teratogenic and can be given during pregnancy.
Its usefulness in acne is based on the anti-inflammatory action. Many controlled studies have shown an efficacy on inflammatory lesions. Zinc pyrithione releases zinc ions, which has anti-inflammatory and antioxidant properties. Zinc ions also inhibit 5α-reductase in the skin.
ZINC PCA
Acne Repair serum: 2%
1. Regulates excessive oil (sebum) production:
- Zinc PCA inhibits the activity of enzyme 5 a-reductase to control excessive sebum production. It controls pores blocking and acne formation.
2. Anti-inflammatory action:
- Zinc possesses anti-inflammatory properties that help to relieve and ease the pain associated with acne.
- Zinc PCA has proven to be effective in reducing inflammation in several other skin problems like eczema, rosacea, and psoriasis etc.
3. Anti - microbial action:
- Zinc PCA inhibits microbial proliferation including Propionibacterium acnes. It is a gram-positive anaerobic human skin bacterium that favors the anaerobic growth conditions and is involved in the pathogenesis of acne.
- Zinc PCA also possesses cytotoxic activity against Pityrosporum ovale (yeast-like fungus) infection.
- Zinc PCA not only fights acne but also provides relief in itching, and irritation associated with fungal manifestations.
- Zinc compounds exert a protective effect against UV damage in keratinocytes and fibroblasts.
- Zinc PCA suppresses activity of collagenase, an enzyme that degrades collagen.
- Research has shown Zinc PCA has anti-aging benefits due to its ability to thwart destructive enzymes in skin that can damage its surface and lead to an aged, wrinkled appearance.
In this study the scientists investigated the effects of zinc on collagen degradation and production in normal human dermal fibroblasts (NHDF's) in order to gather direct data on the subject.
It was found that Zinc PCA suppressed UVA-induced activation of activator protein-1 (AP-1) and reduced matrix metalloproteinase-1 production in these cells, which is thought to be involved in collagen degradation in photoaged skin.
Furthermore, the study found that Zinc PCA was also able to enhance type 1 Collagen synthesis in NHDFs, which suggests its promising effect against not only photo-aged skin, but also for the simple atrophic change of intrinsic skin aging.
Reduced collagen matrix in the dermis constitutes one of the characteristic features of chronologically aged skin, which is further enhanced on the sun-exposed portions of the body by chronic UV irradiation. This induces the unique changes associated with skin photo aging.
It is based on these in vitro findings, that the scientists consider Zinc PCA to be a promising candidate for anti-skin aging agent.
International Journal of Cosmetic Science, February 2012, pages 23-28
ALTEROMONAS FERMENT EXTRACT
Retinol serum: 5%
An exopolysaccharide (high-molecular-weight polymers) secreted by a microorganism living in hydrothermal deep vents. It reduces irritation in sensitive skin, skin reactivity and intolerance.
It increases resistance to mechanical and sun aggressions, protects the skin against UV damage and reduces skin erythema caused by UV.
It has a soothing effect and better healing of "microcuts" caused by shaving and activates skin repair and restructuring processes.
In preventive application, Abyssine® 657 (inci: Alteromonas ferment extract) reduces the expression of ICAM-1, a skin stress marker involved in the skin reactivity cascade. The expression of ICAM-1 is normally at very low concentration but is increased under the effect of stress agents like allergens, various chemicals or physical aggressions.
Abyssine® 657 leads to a reduction of cutaneous reactivity to chemicals (lactic acid) by 25%.
Click here for reference.
Abyssine® 657 provides very effective protection of Langerhans cells, the skin’s immune defence system sentinels, submitted to UVB radiation.
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VITAMIN C: Tetrahexyldecyl Ascorbate
Collagen serum
Excellent Percutaneous Absorption: THDA (BV-OSC) is retained in the epidermis and, to some extent, in the dermis.
The penetration of THDA (BV-OSC) is dose-dependent, and surpasses that of Ascorbic Acid at the same concentration (20µM) by three-fold. THDA (BV-OSC) maintains a higher penetration rate even when the Ascorbic acid is increased by 25 times that of THDA (BV-OSC)
Click here for the reference.
Pure Vitamin C is very unstable. It is sensitive to oxidation and gives finished formulas a yellowish tint.
Note also that pure vitamin C is not the most active form for collagen synthesis and anti-oxidation.
Tetrahexyldecyl ascorbate is a stable, oil-soluble Vitamin C derivative.
Click here for the reference.
Prevention of Lipid peroxidation, Prevention of DNA damage, Prevention of UV induced cell damage.
THDA (BV-OSC) seems to act as a radical scavenger more slowly than Ascorbic Acid.
THDA (BV-OSC) Protects against cell damage.
UVB damage protection: THDA (BV-OSC) has an excellent penetration in keratinocytes. As a result the cytoprotection against UV-B is increased. The cell viability is increased up to 30% when THDA (BV-OSC) is applied compared to pure Vitamin C.
UVA damage protection: The application of THDA (BV-OSC) inhibits the release of 8-OHdG, thereby protecting the cell against UV-A damage.
Click here for the reference.
Cell activation & Acceleration of Collagen synthesis
- THDA (BV-OSC) increase the proliferation of fibroblast cells. Furthermore, the fibroblasts significantly increased collagen synthesis twice as much as the same concentration ascorbic acid.
- THDA inhibit MMP (breakdown of collagen)
Click here for the reference.
Inhibition of Tyrosinase activity & inhibition of melanogenesis.
Inhibition of Melanogenesis in vitro test with THDA (BV-OSC):
In vitro test shows that 0.1% - 0.2% of THDA (BV-OSC) reduces melanogenesis by more than 80%.
Click here for the reference.
AVOBENZONE
Dermdefence SPF 50
Avobenzone is the only globally available chemical sunscreen agent that provides proper UVA protection. It is the global gold standard of UVA protection and is the most used UVA sunscreen in the world. It gives very good protection across the whole UVA range (310-400 nm that is both UVA1 and UVA2) with a peak protection at 360 nm. Avobenzone has a good safety profile. It is non-irritating and shows no estrogenic effect.
TINOSORB S
Dermdefence SPF 50
Tinosorb S is one of the best sunscreen agents known today. It is a broad-spectrum (covers the whole UVB and UVA range, 280-400 nm) chemical sunscreen agent with peak protections at about 310 and 345 nm, and unlike older UV filters, it's very photostable. It hardly deteriorates in the presence of UV light and it's also useful in stabilizing other less stable sunscreen agents, like the famous UVA protector, avobenzone.
It's a new generation sunscreen agent that was specifically designed for high SPF and good UVA protection and based on a 2007 study that compared 18 sunscreen agents available in the EU it really had the best SPF protection.
It is oil-soluble and is not absorbed into the skin too much. This is good news for a sunscreen agent as it needs to be on the surface of the skin to do its job properly. It has a great safety profile and does not show estrogenic activity.
This agent is known to prevent the formation of free radicals induced by UV radiation to a significant level. Further to this Tinosorb S is photostable, it will minimize erythema (redness), and provide excellent anti-aging effects as well as protect the skin's antioxidant defense system. Tinosorb S has no bioaccumulation, thereby exhibiting a good safety profile.Overall, Trinosorb S is one of the best sunscreen options available today.
Ref:
UBIQUINONE
Dermdefence SPF 50
As an antioxidant Ubiquinone is an antioxidant found naturally in human cells where it plays a big role in energy production. Studies have shown Ubiquinone to absorb into the upper layer of the skin and act there like an awesome antioxidant. It not only has preventative effects but might also be able to reduce the depth of wrinkles.
Ref 1: BioFactors 9 (1999) 371–378, Coenzyme Q10, a cutaneous antioxidant and energizer
Ref 2: Leslie Baumann, MD, Cosmetic Dermatology, 2nd edition, Coenzyme Q10 - pages 294-295
VITAMIN E / TOCOPHEROL
- Dermdefence SPF 50
- Collagen serum
Vitamin E is the major fat-soluble antioxidant in our skin. As a strong antioxidant, it’s an A-player in protecting the skin cells from free-radicals that destroy collagen that makes our skin nice and firm. There are lots of studies showing that Vit E has some nice photoprotection properties, meaning it can protect the skin from UV (and in the case of Vit E it’s mainly UVB) rays. If you put it on your skin, it lowers the production of sunburn cells, reduces the damage caused by UVB rays, and inhibits photocarcinogenesis.
Ref: Leslie Baumann, MD, Cosmetic Dermatology, 2nd edition, Vitamin E - pages 293-294
SQUALANE
Dermdefence SPF 50
Squalane is a hydrating moisturizer that smooth skin without being heavy or greasy. Squalane is compatible with all skin types and skin conditions. It is beneficial for acne-prone skin and safe to use even if you have fungi-related skin issues, like seborrhea or fungal acne.
Squalane has anti-inflammatory properties by targeting pro- and anti-inflammatory mediators and pathways to modulate over-activation of neutrophils, monocytes, and macrophages.
Ref: Ana Cárdeno, Marina Aparicio-Soto, Sergio Montserrat-de la Paz, Beatriz Bermudez, Francisco J.G. Muriana, Catalina Alarcón-de-la-Lastra,
Squalene targets pro- and anti-inflammatory mediators and pathways to modulate over-activation of neutrophils, monocytes and macrophages,
Journal of Functional Foods, Volume 14, 2015, Pages 779-790,
GLYCERIN
Dermdefence SPF 50
Glycerin is a natural moisturizer that helps to maintain the healthy state of our skin in several ways. It helps to maintain a healthy state of the cell membranes and intracellular lipids (keeping the lipids in a nice liquid crystal state that is optimal for barrier function).
Ref: Leslie Baumann, MD, Cosmetic Dermatology, 2nd edition, Glycerin- pages 275
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