Effect of Hydrophilic Polymers on Complexation Efficiency of Cyclodextrins in Enhancing Solubility and Release of Diflunisal

Polymers
Mehreen BashirMuhammad Shahid Iqbal

Abstract

The effects of three hydrophilic polymers, namely, carboxymethyl cellulose sodium (CMC-Na), polyvinyl alcohol (PVA) and poloxamer-188 (PXM-188) on the solubility and dissolution of diflunisal (DIF) in complexation with β-cyclodextrin (βCD) or hydroxypropyl β-cyclodextrin (HPβCD), were investigated. The kneading method was used at different drug to cyclodextrin weight ratios. Increases in solubility and drug release were observed with the DIF/βCD and DIF/HPβCD complexes. The addition of hydrophilic polymers at 2.5, 5.0 and 10.0% w/w markedly improved the complexation and solubilizing efficiency of βCD and HPβCD. Fourier-transform infrared (FTIR) showed that DIF was successfully included into the cyclodextrin cavity. Differential scanning calorimetry (DSC) and X-ray diffractometry (XRD) confirmed stronger drug amorphization and entrapment in the molecular cage of cyclodextrins. The addition of PVA, CMC-Na or PXM-188 reduced further the intensity of the DIF endothermic peak. Most of the sharp and intense peaks of DIF disappeared with the addition of hydrophilic polymers. In conclusion, PXM-188 at a weight ratio of 10.0% w/w was the best candidate in enhancing the solubility, stability and release of DIF.

References

Sep 2, 1998·European Journal of Drug Metabolism and Pharmacokinetics·C Rodríguez-EspinosaM Sánchez
Feb 11, 1999·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·E E SiderisP E Macheras
Mar 7, 2000·Journal of Pharmaceutical and Biomedical Analysis·S O UgwuJ Blanchard
Jun 7, 2000·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·C Leuner, J Dressman
Feb 13, 2001·International Journal of Pharmaceutics·B CappelloM Fabrizio Saettone
Apr 12, 2001·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·P MuraG P Bettinetti
Oct 3, 2002·Biochemical and Biophysical Research Communications·Anupama E GururajBharathi P Salimath
Feb 21, 2003·International Journal of Pharmaceutics·Margarita ValeroLicesio J Rodríguez
Dec 2, 2006·International Journal of Pharmaceutics·Thorsteinn Loftsson, Dominique Duchêne
Jul 3, 2007·Advanced Drug Delivery Reviews·Marcus E Brewster, Thorsteinn Loftsson
Dec 7, 2007·Drug Discovery Today·Teófilo VasconcelosPaulo Costa
Mar 14, 2008·Toxicologic Pathology·Valentino J Stella, Quanren He
Apr 11, 2008·Journal of Pharmaceutical and Biomedical Analysis·R StancanelliV Venuti
Mar 14, 2009·Bioorganic & Medicinal Chemistry·Ana Carolina C AsbahrLetícia N C Rodrigues
Jun 27, 2009·Drug Development and Industrial Pharmacy·Maria Esther ZugastiMaría Cristina Martínez-Ohárriz
Oct 29, 2009·AAPS PharmSciTech·Mowafaq M GhareebMohammed I Noordin
Nov 26, 2009·Drug Development and Industrial Pharmacy·Yi LuShaomin Wang
Jul 26, 2012·ISRN Pharmaceutics·Ketan T SavjaniJignasa K Savjani
Jun 23, 2015·BioMed Research International·Muhammad Tayyab AnsariGhulam Murtaza
Jan 15, 2016·Colloids and Surfaces. B, Biointerfaces·Luana Becker PeresClaudia Sayer
Mar 1, 1983·Pharmacotherapy·T Y Shen
Apr 6, 2019·Materials Science & Engineering. C, Materials for Biological Applications·Ana Isa Pedroso MarcolinoClarice Madalena Bueno Rolim

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