Binary and ternary inclusion complexes of dapsone in cyclodextrins and polymers: preparation, characterization and evaluation
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2012-08-01
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Dapsone (DAP) is a synthetic sulfone drug with bacteriostatic activity, mainly against Mycobacterium leprae. in this study we have investigated the interactions of DAP with cyclodextrins, 2-hydroxypropyl-beta-cyclodextrin (HP beta CD) and beta-cyclodextrin (beta CD), in the presence and absence of water-soluble polymers, in order to improve its solubility and bioavailability. Solid systems DAP/HP beta CD and DAP/beta CD, in the presence or absence of polyvinylpyrrolidone (PVP K30) or hydroxypropyl methylcellulose (HPMC), were prepared. the binary and ternary systems were evaluated and characterized by SEM, DSC, XRD and NMR analysis as well as phase solubility assays, in order to investigate the interactions between DAP and the excipients in aqueous solution. This study revealed that inclusion complexes of DAP and cyclodextrins (HP beta CD and beta CD) can be produced in order to improve DAP solubility and bioavailability in the presence or absence of polymers (PVP K30 and HPMC). the more stable inclusion complex was obtained with HP beta CD, and consequently HP beta CD was more efficient in improving DAP solubility than beta CD, and the addition of polymers had no influence on DAP solubility or on the stability of the DAP/CDs complexes.
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Journal of Inclusion Phenomena and Macrocyclic Chemistry. Dordrecht: Springer, v. 73, n. 1-4, p. 467-474, 2012.