生物利用度
溶解度
化学
傅里叶变换红外光谱
分散性
溶解
粒径
药物输送
色谱法
核化学
化学工程
药理学
有机化学
物理化学
医学
工程类
作者
Zhenzhen Chen,Wenhao Gao,Xianquan Feng,Guizhi Zhou,Minxin Zhang,Lingjun Zeng,Xiaomu Hu,Fei Liu,Song Hong-tao
标识
DOI:10.1007/s13346-023-01476-8
摘要
Silymarin (SM) exhibits clinical efficacy in treating liver injuries, cirrhosis, and chronic hepatitis. However, its limited water solubility and low bioavailability hinder its therapeutic potential. The primary objective of this study was to compare the in vitro and in vivo characteristics of the four distinct SM solubilization systems, namely SM solid dispersion (SM-SD), SM phospholipid complex (SM-PC), SM sulfobutyl ether-β-cyclodextrin inclusion complex (SM-SBE-β-CDIC) and SM self-microemulsifying drug delivery system (SM-SMEDDS) to provide further insights into their potential for enhancing the solubility and bioavailability of SM. The formation of SM-SD, SM-PC, and SM-SBE-β-CDIC was thoroughly characterized using scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR), and powder X-ray diffractometry (PXRD) techniques to analyze the changes in their microscopic structure, molecular structure, and crystalline state. The particle size and polydispersity index (PDI) of SM-SMEDDS were 71.6 ± 1.57 nm, and 0.13 ± 0.03, respectively. The self-emulsifying time of SM-SMEDDS was 3.0 ± 0.3 min. SM-SMEDDS exhibited an improved in vitro dissolution rate and demonstrated the highest relative bioavailability compared to pure SM, SM-SD, SM-PC, SM-SBE-β-CDIC, and Legalon®. Consequently, SMEDDS shows promise as a drug delivery system for orally administered SM, offering enhanced solubility and bioavailability.
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