Affiliation:
1. L'Oreal Chevilly‐Larue Chevilly‐Larue France
2. Innovation Domain ‐ADME Aulnay‐sous‐Bois France
3. L'Oreal USA Clark Clark New jersey USA
Abstract
AbstractObjectiveRetinol (Vitamin A) is one of the most effective molecules for the treatment of skin aging. However, it degrades rapidly under the influence of light, oxygen, metal ions, and oxidizing agents. To prevent this, stabilizing systems are used commonly. Notably, butylated hydroxytoluene (2,6‐di‐tert‐butyl‐p‐cresol) (BHT) and ethylenediaminetetraacetic acid (EDTA) salts exhibit excellent antioxidant and metal‐chelating properties but are not eco‐friendly. In this study, our goal was to develop a new eco‐friendly stabilization system for retinol‐based formulations such that the system does not interfere with retinol skin absorption, nor its clinical efficacy.MethodsAn evaluation tool called the Sustainable Product Optimization Tool (SPOT) was used to assess the environmental performance of formulations containing retinol and the various stabilizers investigated. Accelerated stability tests were performed on formulations stored for 2 months at 4 and 45°C (ISO/TR Standard 18811 2018 directives). Long‐term stability evaluation was done on formulations stored for 24‐months at room temperature. Retinol skin absorption was assessed by the Franz cell method using human skin explants (OECD guideline 428). Finally, a clinical study was performed to evaluate the cosmetic performance of a 0.3% stabilized retinol formulation.ResultsN,N’‐ethylenediamine disuccinic acid ([S,S]‐EDDS isomer) and pentaerythritol tetrakis(3,5‐di‐tert‐butyl‐4‐hydroxyhydrocinnamate) (PBHC) showed higher biodegradability and a reduced water footprint compared with those of BHT and EDTA. The SPOT simulation gave [S,S]‐EDDS + PBHC a score of 10 versus 8.84 for EDTA + BHT. Moreover, [S,S]‐EDDS + PBHC better controlled the chemical degradation of retinol compared with EDTA + BHT. Retinol skin absorption was also achieved in the case of a formulation containing [S,S]‐EDDS + PBHC, and several skin attributes improved significantly after 12 weeks of product use, with over 75% of the panel perceiving benefits.ConclusionRegarding retinol stabilization, the PBHC + [S,S]‐EDDS combination is an eco‐friendlier and more effective alternative to BHT + EDTA.
Subject
Colloid and Surface Chemistry,Dermatology,Drug Discovery,Pharmaceutical Science,Aging,Chemistry (miscellaneous)