%0 Journal Article
%T Self-microemulsifying drug-delivery system for improved oral bioavailability of pranlukast hemihydrate: preparation and evaluation
%A Baek MK
%A Lee JH
%A Cho YH
%A Kim HH
%A Lee GW
%J International Journal of Nanomedicine
%D 2013
%I 
%R http://dx.doi.org/10.2147/IJN.S37338
%X roemulsifying drug-delivery system for improved oral bioavailability of pranlukast hemihydrate: preparation and evaluation Original Research (875) Total Article Views Authors: Baek MK, Lee JH, Cho YH, Kim HH, Lee GW Published Date January 2013 Volume 2013:8 Pages 167 - 176 DOI: http://dx.doi.org/10.2147/IJN.S37338 Received: 24 August 2012 Accepted: 11 October 2012 Published: 07 January 2013 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 work Abstract: 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.
%K pranlukast hemihydrates
%K PLH
%K SMEDDS
%K bioavailability
%K solubility
%U https://www.dovepress.com/self-microemulsifying-drug-delivery-system-for-improved-oral-bioavail-peer-reviewed-article-IJN