DEVELOPMENT OF POLYETHOXYLATED RETINAMIDE AS AN ANTl-AGINC AGENT

A novel retinol derivative, polyethoxylated retinamide (Medimin A) was synthesized, as an anti-aging agent. Collagen synthesis, skin permeation, stability, and toxicity of Medimin A were evaluated and compared with those of retinol and retinyl palmitate. In vitro collagen synthesis was evaluated by quantitative assay of [$^3H$]-proline incorporation into collagenase sensitive protein in fibroblast cultures. For in vitro skin permeation experiments, Franz diffusion cells (effective diffusion area: $1, 766{\;}\textrm{cm}^2$) and the excised skin of female hairless mouse aged 8 weeks were used The stabilities of retlnoids were evaluated at two different temperature ($25{\;}^{\circ}C$ and $40{\;}^{\circ}C$) and under UV in solubilized state and in OW emulsion. To estimate the safety, acute oral toxicity, acute dermal toxicity, primary skin irritation, acute eye irritation and human patch test were performed The effect of Medimin A on collagen synthesis was similar to that of retinol. The skin permeability of Medimin A was higher than those of retinol and retinyl palmitate. The Medimin A was more stable than retinol and retinyl palmitate. Medimin A was nontoxic in various toxicological tests. These results suggest that Medimin A would be a good anti-aging agent for enhancing bioavailability and stability.