【摘要】 目的筛选口服槲皮素纳米结构脂质载体的处方和制备工艺,并对其进行体外评价。方法采用溶解度考察和正交优化设计法结合,优选出较优的处方,并通过伪三元相图验证,评价其粒子形态、多分散性、包封率。通过测定不同稀释倍数、不同缓冲液对粒径的影响及药物的体外溶出行为,对槲皮素纳米结构脂质载体进行体外评价。结果最佳处方组成为硬脂酸-Labrafac lipophile WL1349-Cremophor EL-Transcutol P(3:5:5:2),所得纳米结构脂质载体为圆整的类球形粒子,平均粒径为69nm,包封率为89.0%,PDI=0.251。同槲皮素混悬液比较,槲皮素纳米结构脂质载体的体外溶出明显提高。结论口服纳米结构脂质载体释药系统制备工艺简便,粒子性状符合要求,可提高难溶性药物的体外溶出。更多还原

【Abstract】 OBJECTIVE To develop the formulation of quercetin(QU) loaded nanostructured lipid carries(NLC) and evaluate its quality in vitro.METHODS According to the results of the solubility of QU in different oils and surfactants,the formulations were optimized by the orthogonal design.Pseudotertiary phase diagram was used to confirm the emulsion ability of the optimal formulation.The characteristics of the nanoparticles,including size,PDI,encapsulation efficiency were determined.The effects of different dilutions,different buffers on the size and the dissolution in vitro were studied.RESULTS The best formulation was made up of Stearate Labrafac lipophile WL1349-Cremophor EL-Transcutol P(3:5:5:2),which served as solid oil,liquid oil,emulsifier and assistant emulsifier,respectively.The selected formulation had regular spherical surface and a narrow particle size with mean diameter of 69 nm and PDI of 0.251.The encapsulation efficiency was 89.0%.As compared with QU suspension,QU-NLC could improve drug dissolution significantly.CONCLUSION The method for preparing QU-NLC was simple and the properties of nanoparticles were conformed to the requirement of pharmaceutics.Meanwhile,QU-NLC could give rise to the dissolution increase of slightly soluble drug in water in vitro.更多还原