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 / Preparation and release effect of vascular endothelialgrowth factor receptor targeting paclitaxelmicelles
- Resource Type
- Academic Journal
- Authors
- 郭盼; 李淑娟; 于世慧; 潘卫三; 杨星钢; Guo Pan; Li Shujuan; Yu Shihui; Pan Weisan; Yang Xinggang
- Source
- 中国科技论文 / China Sciencepaper. (6):720-724
- Subject
- 药剂学
紫杉醇
聚乳酸聚乙醇酸共聚物-聚乙二醇
胶束
血管内皮生长因子受体
pharmaceutics
paclitaxel
PLGA-PEG
micelles
vascular endothelial growth factor receptor
- Language
- Chinese
- ISSN
- 2095-2783
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。
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.