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.

ZIF-8 as a promising drug delivery system for benznidazole: development, characterization, in vitro dialysis release and cytotoxicity

“…Thus, it was possible to build daily calibration curves, based on the method developed by Soares-Sobrinho et al 15 making it possible to calculate the apparent incorporation of BNZ into the ZIF-8 network. The experiment aimed to analyze the drop in drug concentration, justified by its incorporation into the ZIF-8 network.…”

Improved Aqueous Solubility and Antihypercholesterolemic Activity of Ezetimibe on Formulating with Hydroxypropyl-β-Cyclodextrin and Hydrophilic Auxiliary Substances

“…A previously reported method was adopted with modifications [19]. Excess Eze (20 mg) was added to 10 mL acetate buffer solutions of pH 4.5, containing a fixed concentration of HPBCD (2%w/v) and increasing amounts of TPGS (0.01%-0.25%w/v) or AA2G (0.01%-0.5%w/v).…”

Effects of stabilizing agents on the development of myricetin nanosuspension and its characterization: An in vitro and in vivo evaluation

“…Among the mentioned stabilizers, HP-b-CD is an excipient with a relatively high water solubility, low economic cost, and low toxicity, and in the pharmaceutical field, it is usually used to enhance the solubility of insoluble compounds by forming a complex (Tang et al, 2013a). It was recently reported that HP-b-CD reduced the surface tension between dissolution medium and drug (de Freitas et al, 2012;Soares-Sobrinho et al, 2012). Thus, it is a potential surfactant.…”