CAJ | 학술논문

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。
이용 PLGA-PEG 감단취합물적량친성질제비료3충불동 PEG 분자량적내부포재약물적혈관내피생장인자수체파향효속 APRPG-PEG-M。통과대제제립경분포、zeta 전위、포봉솔급재약량등방면적고찰，학정처방화제비공예，병고찰기제제학성질。제비적파향효속정구형혹류구형，립경109．7～119．9 nm、포봉솔89．2％～91．5％，재체외석약시험중48 h 루적석방량위47．8％～60．0％，표현출명현적완석효과。제비적자삼순파향효속재체외대약물석방구유량호적완석효과。
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.