Zhang Jianbin, Lv Yan, Zhao Shan, Wang Bing, Tan Mingqian, Xie Hongguo, Lv Guojun, Ma Xiaojun
Laboratory of Biomedical Material Engineering, Dalian Institute of Chemical Physics, Chinese Academy of Sciences, Dalian, People's Republic of China.
AAPS PharmSciTech. 2014 Jun;15(3):731-40. doi: 10.1208/s12249-014-0096-9. Epub 2014 Feb 20.
The objective of this study is to investigate the effect of lipolysis on the release of poorly water-soluble drug from SMEDDS in the perspective of drug core/shell location. For this purpose, four SMEDDS formulations with various core/shell properties were developed based on long-chain lipid or medium-chain lipid as well as different surfactant/oil ratios. Poorly water-soluble drugs, hymecromone and resveratrol, were significantly solubilized in all SMEDDS formulations and the diluted microemulsions. Fluorescence spectra analysis indicated that hymecromone was mainly located in the shell of microemulsions, while resveratrol was located in the core. The effect of lipolysis on the release rates of drugs with different core/shell locations were investigated by a modified in vitro drug release model. For the drug located in the shell, hymecromone, the release profiles were not affected during the lipolysis process and no significant differences were observed among four formulations. For the drug located in the core, resveratrol, the release rates were increased to various degrees depending on the extent of digestion. In conclusion, the drug core/shell location plays an important role for determining the effect of lipolysis on drug release from SMEDDS formulation.
本研究的目的是从药物核/壳位置的角度研究脂解作用对自自微乳药物传递系统（SMEDDS）中难溶性药物释放的影响。为此，基于长链脂质或中链脂质以及不同的表面活性剂/油比例，开发了四种具有不同核/壳性质的SMEDDS制剂。难溶性药物羟甲香豆素和白藜芦醇在所有SMEDDS制剂和稀释的微乳剂中均有显著增溶。荧光光谱分析表明，羟甲香豆素主要位于微乳剂的壳层，而白藜芦醇位于核层。通过改进的体外药物释放模型研究了脂解作用对不同核/壳位置药物释放速率的影响。对于位于壳层的药物羟甲香豆素，在脂解过程中释放曲线不受影响，四种制剂之间未观察到显著差异。对于位于核层的药物白藜芦醇，释放速率根据消化程度不同程度增加。总之，药物核/壳位置在确定脂解作用对SMEDDS制剂中药物释放的影响方面起着重要作用。
