Author/Authors :
Soares-Sobrinho، نويسنده , , José L. and Santos، نويسنده , , Fabiana L.A. and Lyra، نويسنده , , Magaly A.M. and Alves، نويسنده , , Lariza D.S. and Rolim، نويسنده , , Larissa A. and Lima، نويسنده , , Adley A.N. and Nunes، نويسنده , , Lيvio C.C. and Soares، نويسنده , , Monica F.R. and Rolim-Neto، نويسنده , , Pedro J. and Torres-Labandeira، نويسنده , , Juan J.، نويسنده ,
Abstract :
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-β-cyclodextrin (RMβCD) and in ternary systems (TS) with BNZ, RMβCD 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.
Keywords :
Benznidazole , Chagas disease , dissolution rate , cyclodextrin , Hydrophilic polymer
