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目的:制备硫酸长春新碱聚氰基丙烯酸正丁酯纳米粒(VCR-PBCA-NPs)并进行释药动力学研究。方法:采用乳化聚合法制备VCR-PBCA-NPs,考察纳米粒形态和粒径分布,测定包封率和载药量,采用星点设计效应面法优化处方;采用透析法进行体外释放研究,并利用药物释放模型方程拟合释放曲线。结果:制得的纳米粒形态圆整,平均粒径(98.9±3.05)nm,包封率(55.23±0.96)%,载药量(7.87±0.11)%,体外释放曲线符合W e ibu ll方程。结论:本研究制备了VCR-PBCA-NPs,其体外释放速度较慢,具有一定的缓释特征。
OBJECTIVE: To prepare vincristine sulfate polybutylcyanoacrylate nanoparticles (VCR-PBCA-NPs) and to study the release kinetics. Methods: The VCR-PBCA-NPs were prepared by emulsion polymerization. The morphology and particle size distribution of the nanoparticles were investigated. The entrapment efficiency and drug loading were determined. The prescription of response surface methodology was used to optimize the prescription. The dialysis method was used to study the in vitro release. Release profiles were fitted using the drug release model equation. Results: The morphology of nanoparticles was round and the average particle size was (98.9 ± 3.05) nm. The entrapment efficiency was (55.23 ± 0.96)% and drug loading was 7.87 ± 0.11%. The in vitro release curve was in accordance with W e ibu ll equation . Conclusion: VCR-PBCA-NPs were prepared in this study. The in vitro release rate of VCR-PBCA-NPs is slow and has certain sustained release characteristics.