血管内皮生长因子受体靶向的紫杉醇胶束的制备及其缓释效果

摘要

The main objective of this work is to prepare the Ala-Pro-Arg-Pro-Gly (APRPG)-modified vascular endothelial growth factor receptor (VEGFR)targeting micelles loaded with paclitaxel (PCT).Three VEGFR targeting PCT-loaded micelles (AP-RPG-PEG-M)incorporating drug with different PEG molecular weight were prepared by the amphipathic property of block copol-ymer.The prescription and preparation process of micelles were determined based on the investigations on particle size,zeta po-tential,drug encapsulation efficiency (EE)and drug loading capacity (DL).The pharmaceutical properties of APRPG-PEG-M were also investigated.The prepared APRPG-PEG-M show spherical or ellipsoid shape.The mean particle sizes are 109.7-119.9 nm and the entrapment efficiency are in the range of 89.2%-91.5%.The in vitro release experiment shows that only 47.8%-60.0% of PCT is released from micelles up to 48 h,indicating an obvious sustained-release characteristic.The prepared APRPG-PEG-M has a good sustained-release characteristic in vitro.%利用 PLGA-PEG 嵌段聚合物的两亲性质制备了3种不同 PEG 分子量的内部包载药物的血管内皮生长因子受体靶向胶束 APRPG-PEG-M。通过对制剂粒径分布、zeta 电位、包封率及载药量等方面的考察，确定处方和制备工艺，并考察其制剂学性质。制备的靶向胶束呈球形或类球形，粒径109．7～119．9 nm、包封率89．2％～91．5％，在体外释药试验中48 h 累积释放量为47．8％～60．0％，表现出明显的缓释效果。制备的紫杉醇靶向胶束在体外对药物释放具有良好的缓释效果。