甲氨蝶呤－聚乳酸复合微球的制备与表征.docVIP

  甲氨蝶呤－聚乳酸复合微球的制备与表征# 陈爱政1,2，杨月梅2，王士斌1,2，刘源岗1,2，党婷婷2，康永强2* （1. 华侨大学化工学院, 福建厦门 361021； 5 10 2. 华侨大学生物材料与组织工程研究所, 福建厦门 361021） 摘要：基于超临界二氧化碳技术制备的甲氨蝶呤纳米粒为小分子模型药物，采用高压静电抗 溶剂法制备甲氨蝶呤-聚乳酸复合微球。用扫描电镜（SEM）、傅立叶红外光谱仪（FTIR） 对该载药复合微球进行表征，并研究其载药量、包封率和药物释放曲线。实验结果表明：甲 氨蝶呤-聚乳酸复合微球表面光滑，粒径分布范围在 10 μm-50 μm 之间；FTIR 表明，在高压 静电抗溶剂过程中聚乳酸化学结构无变化，有利于其作为药物载体；随着理论载药量增加 （2.5%，5%，10%），包封率减少（18.0%，7.1%，2.3%）；甲氨蝶呤从聚乳酸微球中释放 具有长效缓释的性能，无突释效应。 关键词：高压静电抗溶剂；甲氨喋呤；聚乳酸；长效缓释 中图分类号：R318 15 Preparation of methotrexate-loaded PLLA microspheres by a high-voltage electrostatic antisolvent process CHEN Aizheng1,2, YANG Yuemei2, WANG Shibin1,2, LIU Yuangang1,2, DANG Tingting2, KANG Yongqiang2 20 25 30 35 40 (1. College of Chemical Engineering, Huaqiao University, Xiamen, 361021; 2. Institute of Biomaterials and Tissue Engineering, Huaqiao University, Xiamen, 361021) Abstract: Using the supercritical CO2 technology-based methotrexate (MTX) nanoparticles as small molecular drug model, the MTX-loaded poly (L-lactide) (PLLA) microspheres were prepared by a high-voltage electrostatic antisolvent process. The resulting MTX-loaded PLLA microspheres were characterized by scanning electronic microscopy (SEM) and Fourier transform infrared spectrophotometry (FTIR), and their drug load, encapsulation efficiency and drug release profiles were also investigated. The results show that the MTX-loaded PLLA microspheres have a smooth surface with a mean size range from 10 μm to 50 μm; Fourier transform-infrared (FTIR) spectra revealed that no alteration of chemical structure occurred during the high-voltage electrostatic antisolvent process, which is favorable for drug carries; with an increase in theoretical drug load (2.5%, 5.0%, and 10.0%), the encapsulation efficiency decreased (18.0%, 7.1%, and 2.3%, respectively); the MTX-loaded PLLA microspheres released the drug with a long sustained-release effect without a burst release. Key words: high-voltage electrostatic antisolvent; methotrexate; poly (L-lactide) microspheres;