776 Optimized Vitamin C prodrug for controlled release and antioxidant activity

Abstract

Vitamin C (vitC) plays key roles in many biological processes and it is a powerful anti-oxidant which protect the skin against UV exposure. Nevertheless, vitC is unstable under oxidative conditions. A pro-vitamin C, Ascorbic acid 2-glucoside (AA2G) was developed to stabilize vitC. The purpose of the study was to assess skin delivery, metabolism and antioxidant effect of AA2G compared to two concurrent products with 5% of encapsulated vitC or with 15% of free vitC. Skin delivery and metabolism studies were performed on human skin explants by UHPLC/UV. For anti-oxidative protection, three parameters were evaluated by measuring superoxide dismutase, catalase following UV exposure and malondialdehyde by GC/MS. We demonstrated prodrug concept with a good stability of AA2G and release of vitC. A better bioavailability was observed with prodrug compare to encapsulated vitC and equivalent to free vitC. A reservoir effect of AA2G in the SC was also observed which allows a controlled release of vitC according to the needs of the skin. These results are in accordance with a better anti-oxidant activity of the prodrug compare to the encapsulated vitC and equivalent to the free vitC with a lower percentage in the formulation 1,8% of prodrug versus 15% of free vitC.