卡波姆包衣姜黄素脂质体的制备及体外黏附性考察

Preparation of carbopol modified curcumin liposomes and study adhesion in vitro

目的探讨提高难溶性药物口服生物利用度的方法。方法采用薄膜分散法制备姜黄素脂质体,采用孵育法对姜黄素脂质体进行卡波姆包衣并考察姜黄素脂质体包衣前后稳定性、包封率及相对包衣率的变化,采用离体大鼠小肠孵育法考察卡波姆包衣姜黄素脂质体体外黏附性。结果卡波姆包衣对脂质体的稳定性影响较大,当卡波姆的质量浓度为5.0 g.L-1时脂质体最稳定;脂质体包衣后包封率略有下降,相对包衣率随着卡波姆质量浓度的增大而增大;质量浓度同为5.0 g.L-1的条件下,卡波姆包衣脂质体的体外生物黏附性比壳聚糖包衣的体外生物黏附性大,未包衣的脂质体体外生物黏附性很小。结论作为药物载体,卡波姆包衣脂质体具备了难溶性药物姜黄素口服给药的条件,将有很好的应用前景。

Objective To discuss the methods of improving oral bioavailability of the insoluble drugs. Methods Carbopol modified curcumin liposomes were prepared by film dispersion and incubation technique. Physical stability, encapsulation efficiency and relative coated rate of curcumin liposomes were determined before and after coated. The small intestine of rats was applied to study the adhesion of carbopol coated curcumin liposomes in vitro. Results Carbopol coating has a great effect on the stability of liposomes; compared to unmodified liposomes, carbopol modified curcumin liposomes possessed a slight decline encapsulation efficiency;relative coated rate increased with the increase of the concentration of carbopol. At the same concentration, the adhesion rate of carbopol modified liposomes were higher than the ones modified with chitosan in vitro. The non-coated liposomes have almost no adhesion. Conclusions Carbopol modified curcumin liposomes, which meet the requirements of insoluble drug curcumin in the oral administration, will have a very good prospect.