Enhanced oral absorption of saquinavir with Methyl-Beta-Cyclodextrin-Preparation and in vitro and in vivo evaluation

European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences
Shriram M PathakNayanabhirama Udupa

Abstract

Saquinavir (SQV) is a weak base compound, whose solubility is strongly influenced by pH variations. Thus, in the present work, we thought it worthy of interest to investigate in-depth the combined effect of pH control and cyclodextrin (CyD) complexation on SQV solubilization. Phase-solubility studies were performed by adding excess drug to buffered (pH from 1.1 to 7.4) aqueous solutions containing increasing concentrations of Methyl-Beta-CyD (M-β-CyD) in order to evaluate the role of the unionized species of SQV in improving solubility by CyD complexation and to be able to select the most suitable conditions for optimizing drug solubilization. Our study reveals that the integrated approach of pH adjustment and CyD complexation can be successfully used for improving the CyD solubilizing power towards an ionizable drug such as SQV, thus allowing a smaller quantity of CyD to solubilize a given amount of drug, offering clear economic and technologic advantages as well. When biopharmaceutics of the optimized cyclodextrin-based formulation of SQV was studied in Wistar rats after intravenous and oral administrations, we found that inclusion of SQV into M-β-CyD could dramatically improve its oral bioavailability and decrease the variat...Continue Reading

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Citations

Jun 12, 2013·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Su-A KimHyo-Kyung Han
Jun 8, 2013·International Journal of Pharmaceutics·Yusuke TakizawaMasahiro Hayashi
Jul 27, 2012·Therapeutic Delivery·Patricia CallejaJuan M Irache
Aug 4, 2011·Expert Opinion on Drug Delivery·Abhishek SinghGuy Van den Mooter
Dec 22, 2015·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Cassiana MendesMarcos Antônio Segatto Silva
Dec 26, 2012·Journal of Controlled Release : Official Journal of the Controlled Release Society·Ana BeloquiVéronique Préat
Sep 13, 2011·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Michael Lee BranhamThirumala Govender
May 27, 2015·Nanomedicine·Julieta C Imperiale, Alejandro D Sosnik
Dec 30, 2014·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Swapnil J DengaleKrishnamurthy Bhat
Dec 5, 2018·BMC Pharmacology & Toxicology·Gabriel Kigen, Geoffrey Edwards
Jun 26, 2020·European Journal of Drug Metabolism and Pharmacokinetics·Yusuke TakizawaMasahiro Hayashi
Apr 4, 2021·Pharmaceutics·Susana Santos BragaFilipe A Almeida Paz
May 6, 2021·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Shaolong HeHuiling Mu
May 27, 2021·Journal of Drug Delivery Science and Technology·László JicsinszkyGiancarlo Cravotto
Sep 17, 2021·The AAPS Journal·Ruchika BajajDeanna L Kroetz

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