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针对肺部吸入干粉制剂,为了克服微球和纳米粒各自的缺点,本文以聚乳酸-羟基乙酸共聚物(PLGA)为辅料,汉防己甲素(tetrandrine,TET)为模型药物,采用快速膜乳化法将其制备成聚乳酸-羟基乙酸纳米粒(TET-PLGA NPs),再利用喷雾干燥技术将纳米粒组装成微米级复合粒子。利用扫描电镜(SEM)、激光粒度分析、高效液相色谱(HPLC)、X射线衍射(XRD)、差热扫描(DSC)、红外分析(IR)和激光共聚焦显微镜(CLSM)对复合粒子进行表征。快速膜乳法制备的汉防己甲素纳米粒(一级粒子)的平均粒径为(337.5±6.2)nm、PDI为0.014±0.004。纳米粒经喷雾干燥后,形成平均粒径为(3.675±0.16)μm的实心类球状纳米复合粒子(二级粒子),药物以无定形态分布于载体材料中。该粒子遇水后能重新分散,释放出一级粒子。本实验所采用的快速膜乳化-喷雾干燥联用技术整合了微球和纳米粒的优点,为活性物质递送肺部奠定基础。
In order to overcome the shortcomings of the microspheres and the nanoparticles for the inhalation of dry powder formulations in the lungs, polylactic-co-glycolic acid (PLGA) as the excipient and tetrandrine (TET) as the model drug were used in this study. Method to prepare polylactic acid - glycolic acid nanoparticles (TET-PLGA NPs), and then using spray-drying technology to assemble the nanoparticles into micron-sized composite particles. The composite particles were characterized by scanning electron microscopy (SEM), laser particle size analysis, high performance liquid chromatography (HPLC), X-ray diffraction (XRD), differential scanning calorimetry (DSC), infrared spectroscopy (IR) and laser confocal microscopy (CLSM) Characterization. The average particle size of tetrandrine nanoparticles (primary particles) prepared by rapid membrane emulsions was (337.5 ± 6.2) nm and the PDI was 0.014 ± 0.004. After the nanoparticles were spray-dried, solid spherical nanoparticles (secondary particles) with an average particle size of (3.675 ± 0.16) μm were formed, and the drug was distributed in an amorphous state in the carrier material. The particles redisperse with water and release first-order particles. The rapid membrane emulsification-spray-drying technique used in this experiment integrated the advantages of microspheres and nanoparticles and laid the foundation for the delivery of active substances to the lungs.