title: Effect of lipolysis on drug release from self-microemulsifying drug delivery systems (SMEDDS) with different core/shell drug location.
abstract: 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.
authors.affiliation: Laboratory of Biomedical Material Engineering, Dalian Institute of Chemical Physics, Chinese Academy of Sciences, Dalian, People's Republic of China.
authors.forename: Jianbin
authors.initials: J
authors.lastname: Zhang
authors.forename: Yan
authors.initials: Y
authors.lastname: Lv
authors.forename: Shan
authors.initials: S
authors.lastname: Zhao
authors.forename: Bing
authors.initials: B
authors.lastname: Wang
authors.forename: Mingqian
authors.initials: M
authors.lastname: Tan
authors.forename: Hongguo
authors.initials: H
authors.lastname: Xie
authors.forename: Guojun
authors.initials: G
authors.lastname: Lv
authors.forename: Xiaojun
authors.initials: X
authors.lastname: Ma
mesh_terms: D002626:Chemistry, Pharmaceutical; D004337:Drug Carriers; D004655:Emulsions; D057927:Hydrophobic and Hydrophilic Interactions; D006923:Hymecromone / Q000737:chemistry*; D007700:Kinetics; D008055:Lipids / Q000737:chemistry*; D008066:Lipolysis; D010194:Pancreatin / Q000737:chemistry; D000077185:Resveratrol; D012995:Solubility; D013050:Spectrometry, Fluorescence; D013267:Stilbenes / Q000737:chemistry*; D013501:Surface-Active Agents / Q000737:chemistry; D013678:Technology, Pharmaceutical / Q000379:methods
chemical_list: D004337:Drug Carriers; D004655:Emulsions; D008055:Lipids; D013267:Stilbenes; D013501:Surface-Active Agents; D006923:Hymecromone; D010194:Pancreatin; D000077185:Resveratrol