Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex

European Journal of Medicinal Chemistry
Gladys E GraneroMarcela R Longhi

Abstract

The aim of our work was to develop a multicomponent inclusion complex of acetazolamide (ACZ) in order to investigate the combined effect of hydroxypropyl-beta-cyclodextrin (HP-beta-CD) and triethanolamine (TEA) on the solubility of ACZ and its possibility of ophthalmic delivery. Phase solubility study was used to evaluate the complexation in solution at 25 degrees C. Complex formation was also evaluated by comparing the infrared (FT-IR) spectra of the solid complexes with a simple physical mixture containing the same amount of ACZ. FT-IR experiments provided data indicating that the carbonamido group of ACZ is involved in the inclusion process. In vitro release data showed that both formulations, containing the freeze-dried ternary complex and the corresponding simple physical mixture of ACZ with HP-beta-CD and TEA presented the fastest release rate of ACZ. These results suggest that the ACZ-HP-beta-CD-TEA complex represents an effective novel formulation to enhance ACZ solubility in water, turning it promising for ophthalmic administration.

Citations

Apr 23, 2013·AAPS PharmSciTech·Ariana ZoppiMarcela Raquel Longhi
Sep 27, 2014·International Journal of Molecular Sciences·Jahamunna A A BarbosaArnóbio A da Silva-Júnior
May 26, 2010·Journal of Drug Targeting·A L Laza-KnoerrP Couvreur
Jun 23, 2010·Expert Opinion on Drug Delivery·Gladys E Granero, Marcela R Longhi
Feb 19, 2010·Journal of Pharmaceutical Sciences·Ariana ZoppiMarcela R Longhi
Jul 10, 2012·International Journal of Pharmaceutics·Sergey V Kurkov, Thorsteinn Loftsson
Mar 1, 2012·Journal of Pharmaceutical and Biomedical Analysis·Claudia GarneroMarcela Longhi
Aug 31, 2013·Carbohydrate Polymers·María J MoraGladys E Granero
Nov 11, 2016·AAPS PharmSciTech·Abd El-Gawad Helmy Abd El-GawadSaeed A S Al-Zuhairy
Feb 10, 2018·Therapeutic Delivery·Javier Adrián CallesSantiago Daniel Palma
Dec 14, 2018·Journal of Materials Science. Materials in Medicine·Atul P Sherje, Mrunal Jadhav
Apr 14, 2020·Materials Science & Engineering. C, Materials for Biological Applications·Julieta Abraham-MirandaMarcela R Longhi
Feb 8, 2021·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Xiu ZhaoLijuan Chen
Jun 17, 2020·Current Drug Targets·Malwina LachowiczMichał Kołodziejczyk

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