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Effect of lipolysis on drug release from self-microemulsifying drug delivery systems (SMEDDS) with different core/shell drug location.

AAPS PharmSciTech (2014-02-21)
Jianbin Zhang, Yan Lv, Shan Zhao, Bing Wang, Mingqian Tan, Hongguo Xie, Guojun Lv, Xiaojun Ma
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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Maleic acid, ReagentPlus®, ≥99% (HPLC)
Sigma-Aldrich
4-Methylumbelliferone, ≥98%
Sigma-Aldrich
Methylamine solution, 33 wt. % in absolute ethanol ((denatured with 1% toluene))
Sigma-Aldrich
Methylamine solution, 2.0 M in THF
Supelco
Maleic acid, Standard for quantitative NMR, TraceCERT®
Sigma-Aldrich
Methylamine solution, 2.0 M in methanol
Supelco
Maleic acid, Pharmaceutical Secondary Standard; Certified Reference Material
Sigma-Aldrich
Ethyl oleate, 98%
Sigma-Aldrich
4-Bromophenylboronic acid, ≥95.0%
USP
Maleic acid, United States Pharmacopeia (USP) Reference Standard
Sigma-Aldrich
Ethyl oleate, tested according to Ph. Eur.
Sigma-Aldrich
Ethyl oleate, natural, ≥85%
Supelco
Ethyl oleate, analytical standard
Sigma-Aldrich
Ethyl oleate, technical grade, 70%
Sigma-Aldrich
Maleic acid, tested according to Ph. Eur.
Hymecromone, European Pharmacopoeia (EP) Reference Standard