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透明质酸修饰洛伐他汀仿生高密度脂蛋白载药系统的制备与表征

发表时间:2015-09-15  浏览量:1801  下载量:670
全部作者: 刘莉莎,张文丽,何泓良,张梦媛,张双双,刘建平
作者单位: 中国药科大学药学院
摘 要: 目的:以透明质酸(hyaluronic acid,HA)为修饰材料,制备一种新型稳定的长循环洛伐他汀(loading lovastation,LT)仿生高密度脂蛋白(reconstituted high density lipoprotein,rHDL)载药系统,并考察其理化性质及体外释药行为。方法:首先采用薄膜分散法制备LT纳米脂质载体(nanostructured lipid carriers, LT-NLC),单因素研究处方多成分对LT-NLC性质的影响,采用实验室前期优化的胆酸钠介导法,将载脂蛋白AI(apolipoprotein-AI,Apo-AI)插入LT-NLC中形成洛伐他汀仿生高密度脂蛋白纳米粒(reconstituted high density lipoprotein loading with lovastatin,LT-rHDL),最后通过静电吸附法,将HA修饰于LT-rHDL表面,单因素优化HA的修饰条件,制得HA-LT-rHDL. 采用粒度仪测定HA-LT-rHDL的粒径与Zeta电位,透射电镜(transmission electron microscope,TEM)观察其微观形态,微柱离心法测定HA-LT-rHDL的包封率(entrapment efficiency,EE)和载药量(drug loading content,DL),透析法考察其体外释放行为。结果:HA-LT-rHDL平均粒径为(152.9±2.4)nm,Zeta电位为(-25.66±0.65)mV,EE达90.21%,DL为(4.34±0.59)%. TEM观察发现HA-LT-rHDL具有明显的核壳结构。体外释放考察结果表明HA-LT-rHDL在72 h的累积药物释放量仅为40%左右,显示出良好的缓释效果。结论:采用上述方法制备的HA-LT-rHDL具有明显的核壳结构,实现了载体的有效包封,同时表现出良好的缓释特性。
关 键 词: 药剂学;仿生高密度脂蛋白;洛伐他汀;纳米脂质载体
Title: Preparation and characterization of hyaluronic acid-coated lovastatin reconstituted high density lipoprotein drug delivery system
Author: LIU Lisha, ZHANG Wenli, HE Hongliang, ZHANG Mengyuan, ZHANG Shuangshuang, LIU Jianping
Organization: College of Pharmacy, China Pharmaceutical University
Abstract: Objective: Considering hyaluronic acid (HA) as coating material, the primary purpose of this study was to prepare a newly stable reconstituted high density lipoprotein (rHDL) loading lovastatin (LT) with long circulation and investigate its physic-chemical properties as well as in vitro drug release behavior. Methods: Firstly, LT loaded with nanostructured lipid carriers (LT-NLC) was prepared through thin film dispersion method and optimized by the single factor experiment. Then LT loaded with rHDL (LT-rHDL) and Apo-AI was prepared through cholate sodium mediation according to the previous study. Next, the optimal formulation of HA-LT-rHDL was prepared by electrostatic absorption and screened by the single factor experiment. The particle size, Zeta potential and morphology of HA-LT-rHDL was observed. Entrapment efficiency (EE) and drug loading content (DL) was determined under micro-column centrifugation. In vitro drug release test was studied through dialysis method. Results: In vitro characterizations indicated that the mean size and Zeta potential of HA-LT-rHDL were (152.9±2.4) nm and (-25.66±0.65) mV, respectively. EE was 90.21 % and DL was (4.34±0.59)%. Transmission electron microscope (TEM) photographs revealed that HA-LT-rHDL presented the obvious core-shell structure. In vitro drug release test showed that the cumulative drug release at 72 h of HA-LT-rHDL was merely 40%, which presented obvious sustained- release behavior. Conclusion: HA-LT-rHDL exhibited the obvious core-shell structure with effective encapsulation and sustained release behavior.
Key words: pharmaceutics; reconstituted high density lipoprotein; lovastatin; nanostructured lipid carriers
发表期数: 2015年9月第17期
引用格式: 刘莉莎,张文丽,何泓良,等. 透明质酸修饰洛伐他汀仿生高密度脂蛋白载药系统的制备与表征[J]. 中国科技论文在线精品论文,2015,8(17):1824-1831.
 
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