辣椒素固体脂质纳米粒的制备及初步修饰研究  

Preparation and Modification of Capsaicin Solid Lipid Nanoparticles

作　　者：段炼[1] 卢钧雄[1] 钟询龙[1] 李国锋[2] 

机构地区：[1]广州医科大学附属第二医院,广州510260 [2]南方医科大学南方医院,广州510515

出　　处：《中国药学杂志》2016年第5期386-390,共5页Chinese Pharmaceutical Journal

基　　金：国家自然科学基金资助项目(81403031);广州医科大学博士启动项目(2013c47)

摘　　要：目的制备辣椒素固体脂质纳米粒(CAP-SLNs)考察其相应的理化性质,并将具有良好包封率和稳定性的固体脂质纳米粒用壳聚糖(CTS)进行包裹,通过大鼠体内结肠定位给药考察药动学。方法采用"乳化蒸发-低温固化法"制备辣椒素固体脂质纳米粒,对其外观形态、粒径分布、形态学、包封率等指标进行考察。结果所得辣椒素固体脂质纳米粒平均粒径为(118.89±25.0)nm,平均包封率为(38.56±2.6)%,平均载药量为(6.17±0.21)%;大鼠结肠定位给药显示,壳聚糖修饰的辣椒素固体脂质纳米粒(CTS-CAP-SLNs)的AUC_(0-360 min)为(243.63±61.46)mg·min·L^(-1),ρmax为(1.23±0.18)mg·L^(-1),较原料药辣椒素分别提高了1.81和1.95倍。结论乳化蒸发-低温固化法制备辣椒素固体脂质纳米粒简单易行,稳定性好。用壳聚糖包裹后,在结肠定位给药的相关药动学参数能得到显著提高。OBJECTIVE To prepare capsaicin-solid lipid nanoparticles （CAP-SLNs） and study their physical and chemical prop- erties. Then, the CAP-SLNs were modified with ehitosan （CTS） and the pharmaeokinetics across colon of rats was studied in vivo. METHODS CAP-SLNs were prepared by emulsion-solvent evaporation method. The mean size, encapsulation efficiency and drug loading of the nanopartieles were investigated. RESULTS The average diameter of CAP-SLNs was （ 118.89 ±25.0） nm, the encap- sulation efficiency was （ 38.56 ± 2. 6 ） %, and the drug-loading was （ 6. 17 ± 0. 21 ） %. After colon-specific delivery in rats, the AUC0-360min （243.63 ±61.46） mg .min .L^（-1） andρmax（ 1.23 ±0. 18） mg . L^（ -1） of CTS-CAP-SLNs were 1.81-fold and 1.95-fold higher than CAP. CONCLUSION It is simple and feasible to prepare CAP-SLNs by emulsion-solvent evaporation method. The pharmaeokinetie parameters in rats are improved remarkably compared with CAP.

关 键 词：辣椒素 壳聚糖 固体脂质纳米粒 乳化法 结肠 

分 类 号：R944[医药卫生—药剂学]