Topical delivery of cyclosporin A: an in vitro study using monoolein as a penetration enhancer.
Topical delivery of cyclosporin A (CysA) is of great interest for the treatment of autoimmune skin disorders, but it is frequently ineffective due to poor drug penetration in the skin. The present study was aimed at investigating whether the presence of monoolein (a lipidic penetration enhancer) in a preparation of propylene glycol can improve CysA delivery to the skin. CysA was incorporated in a propylene glycol preparation containing 5-70% (w/w) of monoolein. The topical (to the skin) and transdermal (across the skin) delivery of CysA were evaluated in vitro using porcine ear skin mounted in a Franz diffusion cell. CysA was quantified by UV-HPLC. At 5%, monoolein increased only the transdermal delivery of CysA. At 10%, it increased both topical and transdermal delivery. When the concentration of monoolein was further increased (20-70% w/w), an interesting phenomenon was observed: the topical delivery of CysA was still elevated but its transdermal delivery was substantially reduced. It was concluded that monoolein (in propylene glycol formulations) can promote the topical delivery of CysA, with reduced transdermal delivery.
Lopes
Luciana B
LB
Department of Pharmaceutical Sciences, Faculty of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Ribeirão Preto, SP, Brazil.
Collett
John H
JH
Bentley
M Vitória L B
MV
D000279:Administration, Cutaneous; D000287:Administration, Topical; D000818:Animals; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D016572:Cyclosporine / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D004058:Diffusion; D005079:Excipients; D005989:Glycerides / Q000494:pharmacology*; D007166:Immunosuppressive Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D066298:In Vitro Techniques; D008055:Lipids / Q000737:chemistry; D008297:Male; D012869:Skin Absorption / Q000187:drug effects*; D012995:Solubility; D013552:Swine
D005079:Excipients; D005989:Glycerides; D007166:Immunosuppressive Agents; D008055:Lipids; D016572:Cyclosporine; C005953:monoolein