Self-microemulsifying drug-delivery system for improved oral bioavailability of probucol: preparation and evaluation | Zendy

Xiaoling Fang | Zendy

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Self-microemulsifying drug-delivery system for improved oral bioavailability of probucol: preparation and evaluation

Author(s) -

Xiaoling Fang

Publication year - 2012

Publication title -

international journal of nanomedicine

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.245

H-Index - 128

eISSN - 1178-2013

pISSN - 1176-9114

DOI - 10.2147/ijn.s28052

Subject(s) - bioavailability , probucol , pharmacokinetics , chemistry , drug delivery , drug , chromatography , pharmacology , solubility , medicine , biochemistry , cholesterol , organic chemistry

The objective of our investigation was to design a self-microemulsifying drug-delivery system (SMEDDS) to improve the bioavailability of probucol. SMEDDS was composed of probucol, olive oil, Lauroglycol FCC, Cremophor EL, Tween-80, and PEG-400. Droplet sizes were determined. In vitro release was investigated. Pharmacokinetics and bioavailability of probucol suspension, oil solution, and SMEDDS were evaluated and compared in rats. Plasma drug concentration was determined by high-performance liquid chromatography. After administration of probucol suspension, plasma drug concentration was very low. Relative bioavailability of SMEDDS was dramatically enhanced in an average of 2.15- and 10.22-fold that of oil solution and suspension, respectively. It was concluded that bioavailability of probucol was enhanced greatly by SMEDDS. Improved solubility and lymphatic transport may contribute to the enhancement of bioavailability.

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