载羟基喜树碱双嵌段共聚物纳米粒的制备与评价  

Preparation and evaluation of HCPT-loaded amphiphilic block copolymer nanoparticles

作　　者：谢黎崖[1] 常迪[2] 侯振清[2] 许浩云[1] 柯金珍[1] 

机构地区：[1]厦门大学附属第一医院,厦门361003 [2]厦门大学生物医学工程研究中心,厦门361005

出　　处：《中国新药杂志》2016年第17期2021-2026,共6页Chinese Journal of New Drugs

基　　金：福建省医学创新课题资助项目(2014-CXB-35)

摘　　要：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 prepare and evaluate hydroxycamptothecin （HCPT）-loaded amphiphilic block eopolymer nanoparticles（NPs）. Methods： Improved dialysis method was used with HCPT as the model drug to prepare the MePEG [ methoxyl poly （ ethylene glycol） ] -PLGA [ poly （ lactic-co-glycolic acid）] -HCPT amphiphilic block copolymer NPs. Its quality was evaluated and in vitro drug release experiments were carried out. Results： MePEG-PLGA-HCPT-NPs exhibited a solid spherical shape, fairly uniform size, good dispersibility, and relatively smooth surface with core-shell structure. The average particle diameter was （120.1 ± 2.4） nm,the polydispersity coefficient was （0. 057 ± 0. 021 ）, and the Zeta potential was （ -31. 2 ± 0. 98） inV. The drug-loading and entrapment efficiency were （7.42 ± 0.23 ） % and （44.5 ± 0.84） % , respectively. HCPT uniformly distributed in the NPs in a crystalline state. The release behavior in vitro showed biphasic characteristics of burst releasing and sustained releasing. The higher the pH value, the faster the release of HCPT from the NPs, and HCPT could sustainedly release drug over 30 days. Conclusion：The prepared MePEG-PLGA-HCPT-NPs with sustained release property showed a promising potential for application in clinical treatment of tumors.

关 键 词：双嵌段共聚物 羟基喜树碱 甲氧基封端的聚乙二醇-聚乳酸聚乙醇酸 纳米粒 

分 类 号：R979.1[医药卫生—药品]