Literature DB >> 9742560

Complexation and solubility behavior of albendazole with some cyclodextrins.

D Díaz1, M J Bernad Bernad, J Gracia Mora, C M Escobar Llanos.   

Abstract

The main purpose of this work was to study the albendazole-cyclodextrins complexation equilibrium and to propose a suitable excipient to improve the solubility behavior and dissolution rate of albendazole. The complexation of albendazole with four cyclodextrins, alpha-CD, beta-CD, gamma-CD, and hydroxypropylated (HP)-beta-CD, has been studied by using electronic absorption spectroscopy and molecular mechanics. The equilibrium was studied at pH 7.5 under various temperature conditions, and at pH 1.8 with HP-beta-CD at 298 K. The albendazole binding constant was the greatest for the HP-beta-CD. Both the un-ionized (Alb) and the ionized species (AlbH+) were shown to interact with HP-beta-CD. The studies at different temperatures suggest that the hydrophobic effect is the most important driving force in these systems. Moreover, the dissolution rate studies with beta- and HP-beta-CDs in the buffered aqueous solution at pH 7.5 have been accomplished and the dissolution rate was observed to increase with the cyclodextrin concentration. The solubility behavior was studied with the Higuchi and Connors method. The phase solubility and direct spectroscopy methods reveal a 1:1 inclusion complex in all of the studied cases. Molecular mechanics data show the most probable structure of the complexes.

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Year:  1998        PMID: 9742560     DOI: 10.3109/10837459809009867

Source DB:  PubMed          Journal:  Pharm Dev Technol        ISSN: 1083-7450            Impact factor:   3.133


  3 in total

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Authors:  Laura Ceballos; Laura Moreno; Juan J Torrado; Carlos Lanusse; Luis Alvarez
Journal:  BMC Vet Res       Date:  2012-05-28       Impact factor: 2.741

2.  Characterization of albendazole-randomly methylated-β-cyclodextrin inclusion complex and in vivo evaluation of its antihelmitic activity in a murine model of Trichinellosis.

Authors:  Agustina García; Darío Leonardi; María D Vasconi; Lucila I Hinrichsen; María C Lamas
Journal:  PLoS One       Date:  2014-11-18       Impact factor: 3.240

3.  Super Aqueous Solubility of Albendazole in β-Cyclodextrin for Parenteral Application in Cancer therapy.

Authors:  Krishna Pillai; Javed Akhter; David Lawson Morris
Journal:  J Cancer       Date:  2017-03-12       Impact factor: 4.207

  3 in total

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