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目的:研究载羟基喜树碱双嵌段共聚物纳米粒的制备方法并进行评价。方法:以可降解聚合物甲氧基封端的聚乙二醇-聚乳酸聚乙醇酸(Me PEG-PLGA)为载体,羟基喜树碱(HCPT)为模型药物,采用改良的透析法制备羟基喜树碱双嵌段共聚物纳米粒。并对其进行质量评价与体外释药试验。结果:Me PEGPLGA-HCPT纳米粒为实心球形壳核结构,表面圆滑,粒径分布均一,分散性好,平均粒径为(120.1±2.4)nm、多分散系数为(0.057±0.021)、Zeta电位为(-31.2±0.98)m V;载药量为(7.42±0.23)%,包封率为(44.5±0.84)%;且HCPT以晶体形状态均匀分布于纳米粒中。其在3种p H条件下的体外释放分为突释和缓释2部分,且随着释放介质p H值的上升,纳米粒释放速率加快,并且药物能缓释30 d以上。结论:MePEG-PLGA-HCPT纳米粒具有缓释的特点,有用于肿瘤临床治疗的潜能。
OBJECTIVE: To study and evaluate the preparation method of hydroxycamptothecin diblock copolymer nanoparticles. METHODS: Hydroxycamptothecin (HCPT) was used as a model drug with Me PEG-PLGA, a methoxy-terminated polyethylene glycol, as a model drug. Hydroxycamptothecine was prepared by modified dialysis Epidermophylline diblock copolymer nanoparticle And its quality evaluation and in vitro release test. Results: Me PEGPLGA-HCPT nanoparticles were spherical spherical core-shell structure with smooth surface, uniform particle size distribution and good dispersibility. The average particle diameter was (120.1 ± 2.4) nm, polydispersity coefficient was (0.057 ± 0.021) (-31.2 ± 0.98) mV. The drug loading was (7.42 ± 0.23)% and the encapsulation efficiency was (44.5 ± 0.84)%. HCPT was uniformly distributed in the nanoparticles in the crystalline state. The in vitro release under three p H conditions was divided into two parts: burst release and sustained release, and with the increase of p H value of release medium, the release rate of nanoparticles was accelerated and the drug could be released for more than 30 days. Conclusion: MePEG-PLGA-HCPT nanoparticles have the characteristics of sustained release, and have the potential for clinical treatment of tumors.