紫杉醇MPEG-PCL纳米粒的制备、表征及其体外释药行为研究

Paclitaxel/MPEG-PCL Nanoparticles: Preparation, Characterization and in Vitro Release

关键词:  聚乙二醇单甲醚-聚己内酯  纳米粒  紫杉醇  体外释放

Key words:  MPEG-PCL  nanoparticle  paclitaxel  in vitro release

摘要:

目的 以聚乙二醇单甲醚-聚己内酯(MPEG-PCL)为载体制备紫杉醇MPEG-PCL纳米粒并对其体外释放行为进行考察。方法 采用开环聚合法合成MPEG-PCL共聚物，采用核磁共振波谱仪(¹H-NMR)、傅里叶红外光谱仪(FTIR)对其进行表征；通过共沉淀法制备了紫杉醇MPEG-PCL纳米粒，并测定了粒径分布、Zeta电位、结构特征、包封率以及载药量；同时以磷酸盐缓冲溶液(pH=7.4)为释放介质考察其体外释放行为。结果 成功合成了相对分子质量为4 875的MPEG-PCL共聚物。透射电镜结果显示紫杉醇MPEG-PCL纳米粒具有规则的球形结构，纳米粒的平均粒径为(102.3±3.5)nm，PDI=0.102，药物包封率和载药量分别为(95.6±3.2)%和(8.5±0.4)%。体外释放结果显示紫杉醇可以缓慢的从MPEG-PCL纳米粒中释放出来。结论 MPEG-PCL共聚物是紫杉醇的良好载体，所制备的纳米粒具有包封率和载药量高、药物释放缓慢的特点。

Abstract:

OBJECTIVE To develop paclitaxel(PTX)/MPEG-PCL nanoparticles and investigate its in vitro release behavior. METHODS MPEG-PCL block polymer was synthesized by a ring-opeing polymerization method, followed by the characterization with 1H-NMR and FTIR. The PTX/MPEG-PCL nanoparticles was firstly prepared by a coprecipitation method, and then characterized by a DLS, TEM and etc. In vitro release study of PTX/MPEG-PCL nanoparticles as a function with time was performed in PBS solution (pH=7.4) at 37 ℃. RESULTS With the analysis of 1H-NMR and FTIR spectrum, MPEG-PCL block polymer (molecular weight=4 875) was successfully synthesized. With the observation of TEM, the developed PTX/MPEG-PCL nanoparticles showed almost spherical in shape with uniform mean particle size about (102.3±3.5)nm. Drug loading effciency and drug loading capacity of PTX/MPEG-PCL nanoparticles were (95.6±3.2)% and (8.5±0.4)%, respectively. In vitro release study indicated that PTX was released in a sustained-release manner from MPEG-PCL nanoparticles. CONCLUSION MPEG-PCL nanoparticle as an excellent carrier for PTX exhibits high drug loading effciency, drug loading capacity and sustained release progerty.