Self-microemulsifying drug-delivery system for improved oral bioavailability of pranlukast hemihydrate: preparation and evaluation
Myoung-Ki Baek,1,* Jong-Hwa Lee,2,* Young-Ho Cho,3 Hak-Hyung Kim,4 Gye-Won Lee3 1Life Science R&D Park, SK Biopharmaceuticals Co, LTD, Daejeon, Republic of Korea; 2Toxicology Center, Korea Institute of Toxicology, Daejeon, Republic of Korea; 3Department of Pharmaceutical Engineering, Kon...
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| Formato: | article |
| Lenguaje: | EN |
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Dove Medical Press
2013
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| Acceso en línea: | https://doaj.org/article/0c389c5119554a35a9d426d47e07e673 |
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| Sumario: | Myoung-Ki Baek,1,* Jong-Hwa Lee,2,* Young-Ho Cho,3 Hak-Hyung Kim,4 Gye-Won Lee3 1Life Science R&D Park, SK Biopharmaceuticals Co, LTD, Daejeon, Republic of Korea; 2Toxicology Center, Korea Institute of Toxicology, Daejeon, Republic of Korea; 3Department of Pharmaceutical Engineering, Konyang University, Nonsan, Republic of Korea; 4R&D Center, Pharvis Korea Pharm, Ansan, Republic of Korea *These authors contributed equally to this workAbstract: The purpose of the present investigation was to develop and evaluate a self-microemulsifying drug delivery system (SMEDDS) for improving the oral absorption of a pranlukast hemihydrate (PLH), a very poorly water-soluble drug. An efficient self-microemulsifying vehicle for PLH was selected and optimized using solubility testing and phase diagram construction. The formulations were characterized by assessing self-emulsification performance, droplet size analysis, in vitro drug release characteristics and formulation stability studies. Optimized formulations for in vitro dissolution and bioavailability assessment were Triethylcitrate (TEC; 10%), Tween 20 (50%), Span 20 (25%), triethanolamine (5%), and benzyl alcohol (10%). The SMEDDS readily released the lipid phase to form a fine oil-in-water microemulsion with a narrow distribution size. Saturated solubilities of PLH from SMEDDS in water, pH 4.0 and 6.8, were over 150 times greater than that of plain PLH. The release of 100% PLH from SMEDDS was considerably greater compared to only 1.12% in simulated intestinal fluid (pH 6.8) from plain PLH after 2 hours. The PLH suspension with 0.5% sodium carboxymethylcellulose or 3% PLH-loaded SMEDDS was administrated at a dose of 40 mg/kg as PLH to fasted rats. The absorption of PLH from SMEDDS resulted in about a threefold increase in bioavailability compared with plain PLH aqueous suspension. Our studies illustrated that the potential use of the new SMEDDS can be used as a possible alternative to oral delivery of a poorly water-soluble drug such as PLH.Keywords: pranlukast hemihydrates, PLH, SMEDDS, bioavailability, solubility |
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