Novel ultra-deformable vesicles entrapped with bleomycin and enhanced to penetrate rat skin.
Beta-sitosterol 3-beta-D-glucoside (Sit-G), an absorption enhancer, was incorporated into ultra-deformable vesicles containing bleomycin to attenuate drug toxicity in human keratinocytes. The presence of Sit-G increased drug entrapment and improved in vitro stability of ultra-deformable vesicles. Confocal laser scanning microscopy revealed the extent to which Sit-G facilitated the penetration of ultra-deformable vesicles containing fluorescent probes into rat skin upon non-occlusive topical application. Furthermore, treatment with preparations incorporating Sit-G resulted in elevated epidermal and dermal concentrations of bleomycin. Ultra-deformable formulation contained Sit-G maintained flexibility for penetration through the skin, increased entrapment efficiency of bleomycin and stability in vitro, and significantly increased distribution of bleomycin in epidermis and dermis compared with those without Sit-G.
Hiruta
Yuka
Y
Institute of Medicinal Chemistry, Hoshi University, Ebara 2-4-41, Shinagawa-ku, Tokyo 142-8501, Japan.
Hattori
Yoshiyuki
Y
Kawano
Kumi
K
Obata
Yasuko
Y
Maitani
Yoshie
Y
D000818:Animals; D001761:Bleomycin / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D004305:Dose-Response Relationship, Drug; D004337:Drug Carriers / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D004357:Drug Synergism; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D012869:Skin Absorption / Q000187:drug effects* / Q000502:physiology
D004337:Drug Carriers; D001761:Bleomycin