摘要
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 prepare temozolomide polybutylcyanoacrylate nanoparticles （TMZ-PBCA-NP） with optimized process. METHODS TMZ-PBCA-NP was prepared by emulsion polymerization with the α-butylcyanoacrylate（BCA） as its carrier and the surface of the nanoparticles was modified with PluronicF-68. Single factor test and orthogonal design were car ried out to optimize the preparing technology according to the particle size and the entrapment efficiency of TMZ-PBCA-NP. RESULTS The optimal conditions for the preparation of TMZ-PBCA-NP was pH 2.5, 1.0% PluronicF-68 （w/v）, 0. 1 mL BCA monomer and 5 mg temozolomide; on the basis of the above conditions, the mean particle size of the NP was （135.8 ± 11.3） nrn and the polydispersity index（PDI） was 0. 19, the surface charge was （ - 24. 8 ± 2. 2）mV, the average entrapment efficiency and drug loading was （44. 23 ± 2. 04）% and （2. 80 ± 0. 05） %, respectively. CONCLUSION An optimized nanoparticle drug delivery system is obtained by emulsion polymerization and it provides a new direction for temozolomide dosage forms in clinic.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2011年第20期1689-1693,共5页
Chinese Journal of Hospital Pharmacy
基金
福建省自然科学基金项目(编号:2006J0188)
厦门市科技局基金项目(编号:3502Z20064013)
