In vitro and in vivo evaluation of self-microemulsifying drug delivery system of buparvaquone

Drug Development and Industrial Pharmacy
Gantala VenkateshV Navaratnam

Abstract

The aim of this study was to prepare a lipid-based self-microemulsifying drug delivery system (SMEDDS) to increase the solubility and oral bioavailability of a poorly water-soluble compound, buparvaquone (BPQ). The solubility of BPQ was determined in various vehicles, and pseudo-ternary phase diagrams were constructed to determine the microemulsion region. A series of formulations with different compositions were selected in the microemulsion region for assessment of self-emulsification time and droplet size. The optimized SMEDDS formulation was used for in vitro dissolution and pharmacokinetic studies in rabbits. The optimum formulation of SMEDDS consisted of Capryol 90 (9.82%), Cremophor EL (70.72%), Labrasol (17.68%), and BPQ (1.78%). Emulsification time and the mean droplet size were found to be 1 minute and 18.0 +/- 0.25 nm, respectively, for the optimum formulation. The cumulative percentage of drug released in 90 minutes was 100% in both SGF and SIF. The calculated absolute oral bioavailability for BPQ was found to be 40.10%. The optimum SMEDDS formulation was increased the rate and extent of absorption of BPQ. The formulation is suitable for oral administration of BPQ. It would be useful to conduct efficacy studies of B...Continue Reading

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Citations

Nov 28, 2013·Nanomedicine·Flavia Laffleur, Andreas Bernkop-Schnürch
Feb 13, 2014·Drug Development and Industrial Pharmacy·Anuj G AgrawalParaag S Gide
Jan 31, 2012·Drug Development and Industrial Pharmacy·Jae Kuk Ryu, Sun Dong Yoo
Mar 29, 2014·Drug Delivery·Shambhu Dokania, Amita K Joshi
Nov 16, 2010·Drug Development and Industrial Pharmacy·Zhongbin WuJianming Chen
Feb 14, 2013·International Journal of Pharmaceutics·Andreas Niederquell, Martin Kuentz
Nov 20, 2012·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Christopher McConville, David Friend
Jul 15, 2015·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Sunil KambojVikas Rana
Mar 20, 2016·The British Journal of Ophthalmology·Aikaterini LalatsaGeorge M Saleh
Jun 3, 2011·International Journal of Toxicology·Sheela SharmaVernon E Steele
May 16, 2018·Molecular Pharmaceutics·Lindsay SmithAikaterini Lalatsa

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