title: 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.
abstract: Surface-modified solid lipid nanoparticles (SLNs) containing retinyl palmitate (Rpal) were prepared by the hot-melt method using Gelucire 50/13(®) and Precirol ATO5(®). 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.
authors.affiliation: College of Pharmacy, Chung-Ang University, 221 Heuksuk-dong, Dongjak-gu, Seoul 156-756, Republic of Korea.
authors.forename: Ho Seong
authors.initials: HS
authors.lastname: Jeon
authors.forename: Jo Eun
authors.initials: JE
authors.lastname: Seo
authors.forename: Min Soo
authors.initials: MS
authors.lastname: Kim
authors.forename: Mean Hyung
authors.initials: MH
authors.lastname: Kang
authors.forename: Dong Ho
authors.initials: DH
authors.lastname: Oh
authors.forename: Sang Ok
authors.initials: SO
authors.lastname: Jeon
authors.lastname: Seong Hoon Jeong
authors.forename: Young Wook
authors.initials: YW
authors.lastname: Choi
authors.forename: Sangkil
authors.initials: S
authors.lastname: Lee
mesh_terms: D000180:Acrylic Resins / Q000737:chemistry; D000818:Animals; D000975:Antioxidants / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D003931:Diacetyl / Q000031:analogs & derivatives* / Q000737:chemistry; D004075:Diglycerides / Q000737:chemistry; D004224:Diterpenes; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D005223:Fats / Q000737:chemistry; D005260:Female; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D008812:Mice, Hairless; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry*; D009821:Oils / Q000737:chemistry; D009943:Organophosphorus Compounds / Q000737:chemistry; D010316:Particle Size; D051381:Rats; D017207:Rats, Sprague-Dawley; D000084562:Retinyl Esters; D012867:Skin / Q000187:drug effects / Q000378:metabolism; D012869:Skin Absorption / Q000187:drug effects; D015595:Skin Aging / Q000187:drug effects; D013499:Surface Properties; D014801:Vitamin A / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics
chemical_list: D000180:Acrylic Resins; D000975:Antioxidants; D004075:Diglycerides; D004224:Diterpenes; D004337:Drug Carriers; D005223:Fats; D009821:Oils; D009943:Organophosphorus Compounds; D000084562:Retinyl Esters; D014801:Vitamin A; C071184:Gelucire 50-13; C014794:retinol palmitate; C006903:carbopol 940; C005146:diacetyl phosphate; C009032:precirol; D003931:Diacetyl