N-三甲基壳聚糖对青藤碱脂质体体外性质的影响

Effect of N-trimethyl chitosan on in vitro properties of sinomenine hydrochloride liposomes

目的考察N-三甲基壳聚糖(TMC)对青藤碱(SH)脂质体体外性质的影响。方法采用乙醚注入法制备SH脂质体(SHL),分别用季铵化程度(DQ)为20%、40%及60%的TMC包衣,再对脂质体的形态、粒径、Zeta电位、包封率及体外透皮动力学特性进行考察。结果与未包衣的SHL比较,TMC包衣SHL的粒径及Zeta电位均随着DQ的增大而增大;TMC包衣后,在体外透皮前期,透皮速率较小,呈现一定的时滞,且DQ越大,时滞越短;时滞后,透皮速率明显高于未包衣的SHL,且DQ越大,透皮速率越大;包衣对SHL的包封率的影响无统计学意义。结论 TMC包衣后,SHL的粒径、Zeta电位及体外透皮特性均发生相应的变化,且与TMC的季铵化程度有关。

Objective To study the effect of N-trimethyl chitosan （TMC） on the in vitro sinomenine hydrochloride （SH） liposomes （SHL）. Methods SHL was prepared by ether injeetion method followed by TMC coating with various degrees of quaternization （DQ of 20% ,40% and 60% ）. The morphology, size, Zeta potential, entrapment efficiency and transdermal penetration in vitro of the TMC-coated SHL were studied and compared with those of un-eoated SHL. Results Compared with those of un-coated SHL,the size and Zeta potential of TMC-coated SHL were both increased with the increase of DQ. At the beginning of in vitro transdemlal penetration,TMC-eoated SHL showed notable lag time which was decreased with the increase of DQ. After the lag time, the transdermal penetration rate was enhanced significantly and depended on the increase of DQ. TMC-coating had no significant effect on the entrapment efficiency of SHL. Conclusion After coated by TMC, such in vitro properties of SHL as size, Zeta potential and transdermal penetration showed relative changes,which depended on the DQ of TMC.