Solid lipid nanoparticles as drug carriers for topical glucocorticoids.
Recent investigations both in vitro and in human subjects proved the benefit/risk ratio of prednicarbate (PC) to exceed those of halogenated topical glucocorticoids about 2-fold. To obtain a further highly desired increase by drug targeting to viable epidermis, PC was incorporated into solid lipid nanoparticles (SLN). Keratinocyte and fibroblast monolayer cultures, reconstructed epidermis and excised human skin served to evaluate SLN toxicity and PC absorption. Well-tolerated preparations (e.g. cellular viability 94.5% following 18 h incubation of reconstructed epidermis) were obtained. PC penetration into human skin increased by 30% as compared to PC cream, permeation of reconstructed epidermis increased even 3-fold. The present study shows the great potential of SLN to improve drug absorption by the skin.
Maia
C S
CS
Department of Pharmacology and Toxicology, Freie Universität Berlin, D-14195, Berlin, Germany.
Mehnert
W
W
Schäfer-Korting
M
M
D000287:Administration, Topical; D000893:Anti-Inflammatory Agents / Q000737:chemistry* / Q000493:pharmacokinetics; D002470:Cell Survival / Q000187:drug effects; D004337:Drug Carriers / Q000737:chemistry; D004339:Drug Compounding; D004817:Epidermis / Q000187:drug effects / Q000378:metabolism; D005347:Fibroblasts / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D005938:Glucocorticoids; D006801:Humans; D015603:Keratinocytes / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D008055:Lipids / Q000737:chemistry*; D009824:Ointments; D010316:Particle Size; D011239:Prednisolone / Q000031:analogs & derivatives / Q000737:chemistry / Q000493:pharmacokinetics; D012869:Skin Absorption / Q000187:drug effects
D000893:Anti-Inflammatory Agents; D004337:Drug Carriers; D005938:Glucocorticoids; D008055:Lipids; D009824:Ointments; D011239:Prednisolone; C035287:prednicarbate