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)、fCnu 20 Mg、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。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 carrier 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 entrapment 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.福建省自然科学基金(2006J0188);厦门市科技局基金(3502Z20064013
