Journal
CARBOHYDRATE POLYMERS
Volume 89, Issue 2, Pages 323-330Publisher
ELSEVIER SCI LTD
DOI: 10.1016/j.carbpol.2012.02.042
Keywords
Benznidazole; Chagas disease; Dissolution rate; Cyclodextrin; Hydrophilic polymer
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Benznidazole (BNZ) is the drug of choice for Chagas disease treatment, which affects about 9.8 million people worldwide. It has low solubility and high toxicity. The present study aimed to develop and characterize inclusion complexes (IC) in binary systems (BS) with BNZ and randomly methylated-beta-cyclodextrin (RM beta CD) and in ternary systems (TS) with BNZ, RM beta CD and hydrophilic polymers. The results showed that the solid BS had a large increase in dissolution rate (Q>80%). For the solid IC obtained, the kneading method, in ratio of 1:0.17 (77.8% in 60 min), appeared to be the most suitable for the development of a solid oral pharmaceutical product, with possible industrial scale-up and low concentration of CD. The solid TS containing 0.1% of hydroxypropylmethylcellulose (HPMC) showed no significant advantages compared to the binary IC in solid state. The use of cyclodextrins proved to be a viable tool for effective. standardized and safe drug delivery. Crown Copyright (C) 2012 Published by Elsevier Ltd. All rights reserved.
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