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TITLE:

TECHNOLOGICAL STRATEGIES TO INCREASE SOLUBILITY OF ALBENDAZOLE: A REVIEW ABOUT INCLUSION COMPLEXES AND SOLID DISPERSIONS

AUTHORS:

Camila Gomes de Melo*, Paulo César Dantas da Silva, Lucas Amadeu Gonzaga da Costa, Lucas José de Alencar Danda, Laysa Creusa Paes Barreto Barros Silva, Marcelo Montenegro Rabello, Victor de Albuquerque Wanderley Sales, Emerson de Oliveira Silva, Taysa Renata Ribeiro Timóteo, Pedro José Rolim Neto

ABSTRACT:

The aim of the present review is to summarize and discuss the main strategies for addressing the poor solubility of Albendazole (ABZ) with pharmaceutical carriers, as well as the most used methodologies for physicochemical characterization of such compounds. ABZ is a benzimidazole-derived drug widely used in the treatment and control of helminths, being the first choice therapy for several parasitic diseases. Since ABZ belongs to the class II in the Biopharmaceutical Classification System, it is poorly absorbed by the oral route and has low bioavailability. This work covers from the formation of inclusion complexes with cyclodextrins (highlighting β-cyclodextrin) to the use of several polymers for the formation of solid dispersions. Techniques such as infrared absorption spectroscopy, thermal analysis, X-ray diffractometry, nuclear magnetic resonance, microscopies, dissolution tests, in vivo studies, among others, are discussed here, highlighting how these drug delivery systems are capable of modulating the crystalline properties of ABZ, which culminates in increased dissolution rate and may improve oral drug bioavailability Keywords: Albendazole. Inclusion complexes. Solid dispersions. Characterization. In vivo studies.

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