快速膜乳化与喷雾干燥联用制备汉防己甲素纳米复合粒子及其表征  

Preparation and characterization of tetrandrine-loaded PLGA nanocomposite particles by premix membrane emulsification coupled with spray-drying method

作　　者：胡涛[1,2] 朱华旭[1,2] 郭立玮[1,2] 潘林梅[1,2] 李博[1,2] 石飞燕[1,2] 陆瑾[1,2] 

机构地区：[1]南京中医药大学江苏省中药资源产业化过程协同创新中心,江苏南京210023 [2]南京中医药大学药学院江苏省植物药深加工工程研究中心,江苏南京210023

出　　处：《药学学报》2014年第11期1607-1613,共7页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目(81072749;81303230;30873450;30873449);江苏省抗肿瘤验方研究与产业化工程实验室开放课题;南京中医药大学校级创新团队资助;江苏省高校优势学科建设工程资助项目

摘　　要：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。For effective inhalable dry-powder drug delivery,tetrandrine-PLGA（polylactic-co-glycolic acid） nanocomposite particles have been developed to overcome the disadvantages of nanoparticles and microparticles. The primary nanoparticles were prepared by using premix membrane emulsification method. To prepare second particles,they were spray dried. The final particles were characterized by scanning electron microscopy（SEM）,dry laser particle size analysis,high performance liquid chromatography（HPLC）,X-ray diffraction（XRD）,differential scanning calorimetry（DSC）,infrared analysis（IR） and confocal laser scanning microscope（CLSM）. The average size of the primary particles was（337.5 ± 6.2） nm,while that second particles was（3.675 ± 0.16） μm which can be decomposed into primary nanoparticles in water. And the second particles were solid sphere-like with the drug dispersed as armorphous form in them. It is a reference for components delivery to lung in a new form.

关 键 词：汉防己甲素 快速膜乳化 纳米粒 喷雾干燥 纳米复合粒子 

分 类 号：R943[医药卫生—药剂学]