聚氰基丙烯酸正丁酯纳米粒载福莫司汀的制备工艺

目的优化工艺制备福莫司汀聚氰基丙烯酸正丁酯纳米粒（FCNU-PBCA—NP）。方法以α-氰基丙烯酸正丁酯（BCA）为载体，采用乳化聚合法制备FCNU-PBCA—NP，并加以聚乙二醇20000（PEG20000）进行表面修饰，通过考察粒径和包封率两个指标，在单因素实验初选的基础上，正交设计法优化处方和制备工艺。结果制备FCNU-PBCA—NP的优化条件为BCA单体体积分数0．8％（V/V）、FCNU20mg、PEG20000浓度2．0％，按优化条件所制备的FCNU-PBCA-NP的粒径为（124．6±5．2）nm，多分散系数（PDI）范围为0．07—0．16，包封率（64．12±2．36）％，载药量（7．28±0．76）％。结论通过优化处方和制备工艺，采用乳化聚合法可制备出FCNU—PBCA—NP,对拓展FCNU临床给药新剂型提供一定的参考。

Preparation of fotemustine-loaded polybutylcyanoacrylate nanoparticles

AIM To prepare fotemustine polybutylcyanoacrylate nanoparticles （FCNU-PBCA-NP） with optimized process. METHODS FCNU-PBCA-NP was prepared by emulsion polymerization with the α-butylcyanoacrylate（BCA） as its cartier and the surface of the nanoparticles was modified with polyethylene glycol 20000 （ PEG20000）. Single factor test and orthogonal design were carried out to optimize the preparing technology according to the particle size and the en- trapment efficiency of FCNU-PBCA-NP. RESULTS The optimal conditions for the preparation of FCNU-PBCA-NP were 0.8% BCA monomer（V/V）, 20 mg fotemustine and 2.0% PEG20000（m/V）. On the basis of the above conditions, the mean particle size of the NP was（ 124.6 ± 5.2）nm and the polydispersity index（PDI） was 0.07- 0.16, the average entrapment efficiency and drug loading was（64.12±2.36）% and（7.28±0.76）%, respectively. CONCLUSION An optimized nanoparticle drug delivery system is obtained by emulsion polymerization and provides a new direction for fotemutine dosage forms in future.