title: Benznidazole drug delivery by binary and multicomponent inclusion complexes using cyclodextrins and polymers.
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.
authors.affiliation: Pharmaceutical Technology Laboratory, Federal University of Pernambuco, Rua Arthur de Sá, s/n, Cidade Universitária, 50.740-521 Recife, PE, Brazil; Core of Pharmaceutical Technology, Federal University of Piauí, Campus Universitário Ministro Petrônio Portella, s/n, Ininga, 64.049-550 Teresina, PI, Brazil.
authors.forename: José L
authors.initials: JL
authors.lastname: Soares-Sobrinho
authors.affiliation: Pharmaceutical Technology Laboratory, Federal University of Pernambuco, Rua Arthur de Sá, s/n, Cidade Universitária, 50.740-521 Recife, PE, Brazil.
authors.forename: Fabiana L A
authors.initials: FL
authors.lastname: Santos
authors.affiliation: Pharmaceutical Technology Laboratory, Federal University of Pernambuco, Rua Arthur de Sá, s/n, Cidade Universitária, 50.740-521 Recife, PE, Brazil.
authors.forename: Magaly A M
authors.initials: MA
authors.lastname: Lyra
authors.affiliation: Pharmaceutical Technology Laboratory, Federal University of Pernambuco, Rua Arthur de Sá, s/n, Cidade Universitária, 50.740-521 Recife, PE, Brazil.
authors.forename: Lariza D S
authors.initials: LD
authors.lastname: Alves
authors.affiliation: Pharmaceutical Technology Laboratory, Federal University of Pernambuco, Rua Arthur de Sá, s/n, Cidade Universitária, 50.740-521 Recife, PE, Brazil.
authors.forename: Larissa A
authors.initials: LA
authors.lastname: Rolim
authors.affiliation: Pharmaceutical Technology Laboratory, Federal University of Pernambuco, Rua Arthur de Sá, s/n, Cidade Universitária, 50.740-521 Recife, PE, Brazil.
authors.forename: Adley A N
authors.initials: AA
authors.lastname: Lima
authors.affiliation: Core of Pharmaceutical Technology, Federal University of Piauí, Campus Universitário Ministro Petrônio Portella, s/n, Ininga, 64.049-550 Teresina, PI, Brazil.
authors.forename: Lívio C C
authors.initials: LC
authors.lastname: Nunes
authors.affiliation: Pharmaceutical Technology Laboratory, Federal University of Pernambuco, Rua Arthur de Sá, s/n, Cidade Universitária, 50.740-521 Recife, PE, Brazil; Core of Pharmaceutical Technology, Federal University of Piauí, Campus Universitário Ministro Petrônio Portella, s/n, Ininga, 64.049-550 Teresina, PI, Brazil.
authors.forename: Monica F R
authors.initials: MF
authors.lastname: Soares
authors.affiliation: Pharmaceutical Technology Laboratory, Federal University of Pernambuco, Rua Arthur de Sá, s/n, Cidade Universitária, 50.740-521 Recife, PE, Brazil.
authors.forename: Pedro J
authors.initials: PJ
authors.lastname: Rolim-Neto
authors.affiliation: Department of Pharmacy and Pharmaceutical Technology, Facultad de Farmacia, Universidad de Santiago de Compostela, 15782 Santiago de Compostela, Spain.
authors.forename: Juan J
authors.initials: JJ
authors.lastname: Torres-Labandeira
mesh_terms: D016503:Drug Delivery Systems; D057927:Hydrophobic and Hydrophilic Interactions; D065347:Hypromellose Derivatives / Q000737:chemistry; D008745:Methylation; D009593:Nitroimidazoles / Q000737:chemistry*; D011205:Povidone / Q000737:chemistry; D012995:Solubility; D014344:Trypanocidal Agents / Q000737:chemistry*; D047392:beta-Cyclodextrins / Q000737:chemistry*
chemical_list: D009593:Nitroimidazoles; D014344:Trypanocidal Agents; D047392:beta-Cyclodextrins; D065347:Hypromellose Derivatives; D011205:Povidone; C031215:betadex; C009999:benzonidazole