Novel ultra-deformable vesicles entrapped with bleomycin and enhanced to penetrate rat skin
Novel ultra-deformable vesicles entrapped with bleomycin and enhanced to penetrate rat skin
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DOI：
10.1016/j.jconrel.2006.04.016
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发表时间：
2006-06-28
影响因子：
10.8
通讯作者：
Maitani, Yoshie
中科院分区：
文献类型：
--
作者：
Hiruta, Yuka;Hattori, Yoshiyuki;Maitani, Yoshie
将吸收促进剂β-谷甾醇3-β-D-葡萄糖苷（Sit-G）掺入含有博来霉素的超变形囊泡中，以减轻药物对人角质形成细胞的毒性。Sit-G的存在增加了药物包封率，并提高了超变形囊泡的体外稳定性。共聚焦激光扫描显微镜揭示了Sit-G促进含有荧光探针的超变形囊泡在非封闭性局部应用后渗透到大鼠皮肤中的程度。此外，治疗制剂纳入Sit-G导致博莱霉素的表皮和真皮浓度升高。与不含Sit-G的超变形制剂相比，含Sit-G的超变形制剂保持了通过皮肤的柔性，提高了博莱霉素的包封率和体外稳定性，并显著增加了博莱霉素在表皮和真皮中的分布。(c)2006 Elsevier B.V保留所有权利。
Beta-sitosterol 3-beta-D-glucoside (Sit-G), an absorption enhancer, was incorporated into ultra-deform able 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. (c) 2006 Elsevier B.V All rights reserved.