Preparation and pharmaceutical evaluation of new tacrolimus-loaded solid self-emulsifying drug delivery system

The purpose of this study was to develop a novel tacrolimus-loaded solid self-emulsifying drug delivery system (SEDDS) using Labrafac as an oil phase. The ternary phase diagram was plotted with Labrafac, Labrasol and Lauroglycol used as an oil, surfactant and co-surfactant, respectively. The liquid...

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Bibliographic Details
Published in:Archives of pharmacal research 2015-02, Vol.38 (2), p.223-228
Main Authors: Seo, Youn Gee, Kim, Dong-Wuk, Cho, Kwan Hyung, Yousaf, Abid Mehmood, Kim, Dong Shik, Kim, Jeong Hoon, Kim, Jong Oh, Yong, Chul Soon, Choi, Han-Gon
Format: Article
Language:English
Subjects:
Animals
Drug Carriers - chemistry
Drug Compounding
Drug Delivery Systems - methods
Emulsions
Glycerides - chemistry
Immunosuppressive Agents - administration & dosage
Immunosuppressive Agents - pharmacokinetics
Laurates - chemistry
Male
Medicine
Pharmacology/Toxicology
Pharmacy
Propylene Glycols - chemistry
Rats, Sprague-Dawley
Research Article
Solubility
Tacrolimus - administration & dosage
Tacrolimus - pharmacokinetics
Triglycerides - chemistry
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Summary:The purpose of this study was to develop a novel tacrolimus-loaded solid self-emulsifying drug delivery system (SEDDS) using Labrafac as an oil phase. The ternary phase diagram was plotted with Labrafac, Labrasol and Lauroglycol used as an oil, surfactant and co-surfactant, respectively. The liquid SEDDS formulated with Labrasol, Lauroglycol and Labrafac (70:15:15, volume ratio) furnished the smallest emulsion globule size. The solid SEDDS was obtained by spray-drying the liquid mixture containing the liquid SEDDS with 5 % tacrolimus and silicon dioxide. Furthermore, dissolution of tacrolimus from the solid SEDDS and pharmacokinetics in rats was studied compared to the commercial product. The solid SEDDS produced relatively larger emulsion globule size than that exhibited by the corresponding liquid SEDDS. However, this size variation was not significantly different. The solid SEDDS with approximately 280 nm emulsion droplet size improved the dissolution of the drug compared to drug power and the commercial product. It resulted in significantly higher plasma concentration, AUC and C max , and shorter T max values than did the commercial product ( p  
ISSN:0253-6269
1976-3786
DOI:10.1007/s12272-014-0459-5