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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：2507 下载量：846
| 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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