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Topical activity of ascorbic acid: from in vitro optimization to in vivo efficacy.
Skin Pharmacol Physiol. 2004 Jul-Aug; 17(4):200-6.SP

Abstract

We present here a new cosmetic formula system containing 3% ascorbic acid based on an optimized oil-in-water (O/W) emulsion. This formulation demonstrated a good long-term stability of the active ingredient and also of the emulsion itself. It could be deduced from in vitro release studies that this O/W emulsion enabled a better release of the hydrophilic active agent than an alternative W/O emulsion. By measuring the ultraweak photon emission, which is a well-established parameter for the oxidative stress in the skin, the high in vivo antioxidant capacity of 3% ascorbic acid was demonstrated after 1 week of product application. This placebo-controlled study also proved that ascorbic acid in an O/W cream reduced oxidative stress in human skin significantly better than the derivative sodium ascorbyl-2-phosphate, a more stable vitamin C replacement commonly used in cosmetic formulations. With increasing age, the number of papillae in the epidermal-dermal junction zone in human skin are reduced. This implies a possible consequence of reduced mechanical resistance of the skin and impaired supply of the epidermis with nutrients. In a 1-month placebo-controlled study on 25 human volunteers, a significant increase in the number of dermal papillae after application of the 3% ascorbic acid cream was demonstrated, using a confocal laser scanning microscope. Fine lines and wrinkles are a characteristic sign of aged and especially photo-aged skin. Application of 3% ascorbic acid in a 12-week placebo-controlled usage study indicated a significant reduction of facial wrinkles. Altogether, 3% ascorbic acid in a cosmetic O/W emulsion has been shown to be appropriately stable and to enable a good release of the active agent in vitro as a precondition for a high efficacy in vivo. Application in vivo resulted in a significant reduction of oxidative stress in the skin, an improvement of the epidermal-dermal microstructure and a reduction of fine lines and wrinkles in aged skin. These results were received within a relatively short period of time of product application.

Authors+Show Affiliations

Beiersdorf AG, Research & Development Cosmed, Hamburg, Germany. Thomas.Raschke@Beiersdorf.comNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Clinical Trial
Controlled Clinical Trial
Journal Article

Language

eng

PubMed ID

15258452

Citation

Raschke, T, et al. "Topical Activity of Ascorbic Acid: From in Vitro Optimization to in Vivo Efficacy." Skin Pharmacology and Physiology, vol. 17, no. 4, 2004, pp. 200-6.
Raschke T, Koop U, Düsing HJ, et al. Topical activity of ascorbic acid: from in vitro optimization to in vivo efficacy. Skin Pharmacol Physiol. 2004;17(4):200-6.
Raschke, T., Koop, U., Düsing, H. J., Filbry, A., Sauermann, K., Jaspers, S., Wenck, H., & Wittern, K. P. (2004). Topical activity of ascorbic acid: from in vitro optimization to in vivo efficacy. Skin Pharmacology and Physiology, 17(4), 200-6.
Raschke T, et al. Topical Activity of Ascorbic Acid: From in Vitro Optimization to in Vivo Efficacy. Skin Pharmacol Physiol. 2004 Jul-Aug;17(4):200-6. PubMed PMID: 15258452.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Topical activity of ascorbic acid: from in vitro optimization to in vivo efficacy. AU - Raschke,T, AU - Koop,U, AU - Düsing,H-J, AU - Filbry,A, AU - Sauermann,K, AU - Jaspers,S, AU - Wenck,H, AU - Wittern,K-P, PY - 2003/12/15/received PY - 2004/04/30/accepted PY - 2004/7/20/pubmed PY - 2004/10/23/medline PY - 2004/7/20/entrez SP - 200 EP - 6 JF - Skin pharmacology and physiology JO - Skin Pharmacol Physiol VL - 17 IS - 4 N2 - We present here a new cosmetic formula system containing 3% ascorbic acid based on an optimized oil-in-water (O/W) emulsion. This formulation demonstrated a good long-term stability of the active ingredient and also of the emulsion itself. It could be deduced from in vitro release studies that this O/W emulsion enabled a better release of the hydrophilic active agent than an alternative W/O emulsion. By measuring the ultraweak photon emission, which is a well-established parameter for the oxidative stress in the skin, the high in vivo antioxidant capacity of 3% ascorbic acid was demonstrated after 1 week of product application. This placebo-controlled study also proved that ascorbic acid in an O/W cream reduced oxidative stress in human skin significantly better than the derivative sodium ascorbyl-2-phosphate, a more stable vitamin C replacement commonly used in cosmetic formulations. With increasing age, the number of papillae in the epidermal-dermal junction zone in human skin are reduced. This implies a possible consequence of reduced mechanical resistance of the skin and impaired supply of the epidermis with nutrients. In a 1-month placebo-controlled study on 25 human volunteers, a significant increase in the number of dermal papillae after application of the 3% ascorbic acid cream was demonstrated, using a confocal laser scanning microscope. Fine lines and wrinkles are a characteristic sign of aged and especially photo-aged skin. Application of 3% ascorbic acid in a 12-week placebo-controlled usage study indicated a significant reduction of facial wrinkles. Altogether, 3% ascorbic acid in a cosmetic O/W emulsion has been shown to be appropriately stable and to enable a good release of the active agent in vitro as a precondition for a high efficacy in vivo. Application in vivo resulted in a significant reduction of oxidative stress in the skin, an improvement of the epidermal-dermal microstructure and a reduction of fine lines and wrinkles in aged skin. These results were received within a relatively short period of time of product application. SN - 1660-5527 UR - https://www.unboundmedicine.com/medline/citation/15258452/Topical_activity_of_ascorbic_acid:_from_in_vitro_optimization_to_in_vivo_efficacy_ L2 - https://www.karger.com?DOI=10.1159/000078824 DB - PRIME DP - Unbound Medicine ER -