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(FT-IR)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10-50μm之间;FT-IR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%和10%),包封率减少(18.0%、7.1%和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。
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 (FT-IR), 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 50μm; Fourier transform-in- frared (FT-IR) 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.