紫杉醇聚氰基丙烯酸正丁酯纳米粒制备研究

Preparation of paclitaxel-loaded polybutylcyanoacrylate nanoparticles

目的评价紫杉醇聚氰基丙烯酸正丁酯纳米粒(PTX-PBCA-NPs)的不同制备工艺对紫杉醇的包封率和载药量的影响,优选PTX-PBCA-NPs的制备工艺。方法以包封率和载药量为主要评价指标,分别采用界面缩聚法和乳化聚合法制备PTX-PBCA-NPs,进行对比研究。用正交设计优选处方。结果界面缩聚法、乳化聚合法制备的PTX-PBCA-NPs的包封率范围均在94.39%～99.23%(n=3)之间,界面缩聚法制备的PTX-PBCA-NP的载药量可达(1.07±0.03)%(n=3),而乳化聚合法制备的PTX-PBCA-NP的载药量可达(0.86±0.01)%(n=3)。用正交试验优选出最佳工艺条件,PTX-PBCA-NPs载药量为0.80%,包封率为95.71%,粒径为235.6nm。结论两种制备方法制备出来的PTX-PBCA-NPs的包封率符合药典要求。经比较研究,界面缩聚法可能是提高PTX-PBCA-NPs载药量较好的一种制备方法(P<0.05)。

Objective To evaluate the effect of different preparation methods on the encapsulation efficiency （EE） and drug loading （DL） of paclitaxel-loaded polybutylcyanoacrylate nanoparticles （PTX-PBCA-NPs） and optimize the preparation of PTX-PBCA-NPs.Methods With DL and EE as the major indexes,the qualities of PTX-PBCA-NPs produced by the interfacial polymerization and emulsion polymerization method were compared.The optimized prescription was obtained by orthogonal design.Results The ranges of EE of PTX-PBCA-NPs with the two methods were both 94.39%-99.23%.The highest DL with interfacial polymerization was （1.07±0.03）%,as compared to （0.86±0.01）% with emulsion polymerization.The optimized preparation conditions resuted in the mean size of PTX-PBCA-NPs of 235.6 nm,DL of 0.80%,and EE of 95.71%.Conclusions The EE of PTX-PBCA-NPs prepared by the above two methods is consistent with the requirement of the Pharmacopoeia of China,and PTX-PBCA-NPs containing higher DL can be obtianed via interfacial polymerization.