多柔比星壳聚糖纳米粒的制备及其体外评价

Preparation and in vitro release of Chitosan nanoparticles containing Doxorubicin

目的制备多柔比星壳聚糖纳米粒,并研究其包封情况和控释能力。方法采用离子交联法制备多柔比星壳聚糖纳米粒,激光粒度仪测定粒径的分布,HPLC法测定纳米粒的包封率,透析法测定多柔比星壳聚糖纳米粒的体外释放情况。结果壳聚糖的浓度增加,纳米粒的粒径增加、包封多柔比星的效率也增加;壳聚糖溶液的pH增加,纳米粒的粒径降低而包封多柔比星的效率增加;壳聚糖分子量增加对多柔比星的包封效率影响较小,但粒径增加,多柔比星突释减小,释放速率降低。结论多柔比星可以通过离子交联法制备壳聚糖纳米粒,其粒径、包封率可控,具有缓释效果。

OBJECTIVE To prepare Chitosan nanoparticles containing Doxorubicin （ CS - DOX - NPs） and investigate the characteristics of encapsulation efficiency （EE） and in vitro release. METHODS CS - DOX - NPs were prepared by ionic gelation process. The distribution of particle size of the NPs was determined by Malvern particle size analyzer. The EE was examined by HPLC method. The in vitro release was investigated by dialysis. RESULTS The particle size and EE of chitosan nanoparticles both increased with increased chitosan concentration. With increasing pH value of chitosan solution, the EE increased and the particle size decreased. The molecular weight had little effect on the encapsulation efficiency, but the in vitro release rate decreased with increasing molecular weight of chitosan. CONCLUSION CS - DOX - NPs prepared by ionic gelation method exhibited sustained release in vitro and the particle size and EE were controllable.