EVALUATION OF IN VITRO DISSOLUTION OF BENZNIDAZOLE AND BINARY MIXTURES: SOLID DISPERSIONS WITH HYDROXYPROPYLMETHYLCELLULOSE AND Î²-CYCLODEXTRIN INCLUSION COMPLEXES
Keywords:Benznidazole, Solid dispersion, Inclusion complexes, Dissolution
Objective: To increase the solubility/dissolution of benznidazole (BNZ) in water using two systems: solid dispersions (SD) with hydroxypropylmethylcellulose (HPMC) and Î²-cyclodextrin (Î²-CD) inclusion complexes (IC).
Methods: The samples were obtained by physical mixtures (PM), kneading (KN), evaporation (EV) and by spray-dryer (SY) atomization The analysis was based on results of in vitro dissolution and molecular modeling techniques.
Results: Molecular modeling showed that BNZ can form Î²-CD complexes in different ways such as in an aqueous solution or a vacuum. In vitro dissolution showed significant improvement in BNZ solubility in the PM, SD and IC, and also that the Î²-CD IC promoted better solubility than SD with HPMC.
Conclusion: Considering the data obtained, it is possible to consider the technique for the formation of Î²-CD IC as a more effective technique in promoting the improvement of BNZ solubility compared with getting SD with HPMC which, in turn, may increase the bioavailability of the drug and improve their pharmaceutical potential.
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