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目的:优化工艺制备替莫唑胺聚氰基丙烯酸正丁酯纳米粒(TMZ-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TMZ-PBCA-NP,并以PluronicF-68作为表面活性剂,通过考察粒径大小和包封率2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TMZ-PBCA-NP的优化条件为反应体系pH2.5,用1%PluronicF-68作为表面活性剂,TMZ用量5 mg,BCA单体用量0.1 mL,按优化条件所制备的TMZ-PBCA-NP平均粒径(135.8±11.3)nm,多分散系数为0.19,表面电位(-24.8±2.2)mV,包封率(44.23±2.04)%,载药量(2.80±0.05)%。结论:通过优化处方和制备工艺,采用乳化聚合法可制备出TMZ-PBCA-NP,对拓展TMZ临床给药新剂型提供一定的参考。
Objective: To optimize the preparation of temozolomide polybutylcyanoacrylate nanoparticles (TMZ-PBCA-NP). Methods: TMZ-PBCA-NP was prepared by emulsification polymerization using n-butyl α-cyanoacrylate (BCA) as carrier, and Pluronic F-68 was used as surfactant. The particle size and encapsulation efficiency On the basis of single factor experiment, the orthogonal design method was used to optimize the prescription and preparation process. Results: The optimal conditions for the preparation of TMZ-PBCA-NP were as follows: pH2.5, 1% Pluronic F-68 as surfactant, TMZ as 5 mg, BCA as monomer, 0.1 mL and TMZ-PBCA (135.8 ± 11.3) nm, polydispersity 0.19, surface potential (-24.8 ± 2.2) mV, encapsulation efficiency (44.23 ± 2.04)% and drug loading capacity (2.80 ± 0.05)% respectively. Conclusion: TMZ-PBCA-NP can be prepared by the emulsion polymerization method through the optimization of prescription and preparation process, which will provide some reference for the development of TMZ new dosage form.