A retinyl palmitate-loaded solid lipid nanoparticle system: Effect of surface modification with dicetyl phosphate on skin permeation in vitro and anti-wrinkle effect in vivo

Surface-modified solid lipid nanoparticles (SLNs) containing retinyl palmitate (Rpal) were prepared by the hot-melt method using Gelucire 50/13 (R) and Precirol ATO5 (R). Dicetyl phosphate (DCP) was added to negatively charge the surfaces of the SLNs and thereby enhance the skin distribution properties of Rpal. In vitro skin permeation and in vivo anti-aging studies were performed using SLNs dispersed in a hydrogel. The SLNs were under 100 nm in size with an even polydispersity index (PDI), and the high absolute zeta-potential value was sufficient to maintain the colloidal stability of the SLNs. DCP-modified negative SLNs (DCPmod-SLNs) enhanced the skin distribution of Rpal 4.8-fold and delivered Rpal to a greater depth than did neutral SLNs. The in vivo anti-wrinkle effect of the DCPmod-SLN formulation was Rpal dose-dependent. However, the anti-wrinkle effects of the DCPmod-SLN formulations were significantly different from that of the negative control and effectively prevented the reduction of elastin and superoxide dismutase by UV irradiation. In conclusion, the DCPmod-SLN system presented is a good candidate for topical Rpal delivery. (C) 2013 Elsevier B. V. All rights reserved.