博莱霉素脂质体凝胶的制备和体外透皮性比较

目的：研制博莱霉素（BLM）脂质体凝胶，并对其皮肤靶向性进行体外评价。方法：采用逆相蒸发-冻融法制备BLM脂质体，再用卡渡姆940为基质制成BLM脂质体凝胶；以离心法测定BLM脂质体的包封率；以体外透皮渗透释药法，比较BLM脂质体凝胶与BLM普通凝胶的透过作用。结果：BLM脂质体平均粒径为（885．20±12．08）nm，平均包封率为（66．80±1．38）％。在24h内，BLM脂质体凝胶累积透过量（Q）及稳态透皮速率（J）与BLM普通脂质体相比，均明显提高，而在皮肤中的滞留药量也显著提高（P〈0．05）。结论：BLM脂质体凝胶在体外可显著增加BLM的透皮吸收，增加皮肤中的滞留量，值得进一步研究。

Preparation and Skin Permeation Evaluation in Vitro of Bleomycin Lipogel

Objective： To prepare bleomycin （BLM） lipogel and to evaluate its skin targeting ability in vitro. Method： The BLM liposomes were prepared by the reverse-phase evaporation and freeze-thawing method. Carbopol 940 was used as a base for the preparation of the lipogel. Encapsulation efficiency was determined by centrifugation and the accumulative permeation amount of BLM lipogel was assessed by Franz-diffiusion cells compared with that of the BLM common gel. Result： The mean diameter of the BLM liposomes was 885.2 ±12.08 nm and the average encapsulation efficiency was （66.80± 1.38 ） %. Compared with those of the BLM common gels,the accumulative permeation amount （Q） and steady permeation rate （J） of lipogel was increased and the drug amount in skin was also increased significantly in 24 h （P 〈 0.05 ）. Conclusion ： The BLM lipogel can enhance BLM transdermal absorption and promote BLM amount in skin in vitro. It is valuable to be study further in vivo.