Development of effervescent tablets containing benznidazole complexed with cyclodextrin

Abstract

Effervescent tablets produced using an inclusion complex of BNZ with CD suggest a possible improvement in the bioavailability of BNZ, and this could represent a relevant advance in Chagas therapy.

Hot-Melt Extrusion as an Advantageous Technology to Obtain Effervescent Drug Products

“…In fact, the well-known hygroscopicity of effervescent components is one of the main obstacles faced in the production of effervescent drug products, demanding productive areas with strict environmental humidity controls [ 11 , 42 ]. In this sense, the higher resistance of HME extrudates to water uptake is an important industrial advantage of these products.…”

“…Some recent technological advances involving effervescent products have been proposed by means of solvent-consuming and elaborated multistep processes, including freeze-drying, spray-drying, and fluidized bed coating techniques [9][10][11][12][13], which, therefore, are not attractive to the industry.…”

Mini-tablets: a contemporary system for oral drug delivery in targeted patient groups

“…Different approaches exist in term of overcoming this obstacle, with cyclodextrin complexation emerging as one of the most promising. Several studies deal with complexation of poorly soluble actives with cyclodextrins and incorporation of these complexes into large tablets [79,80]. Salustio et al improved the solubility of ibuprofen by complexation with b-cyclodextrin by using various complexation techniques (spray drying, freeze-drying and air-stream drying of complex solution/suspension or kneading ibuprofen: b-cyclodextrin powder mixture with water) and further manually tableted the complexes obtained into 2.5 mm mini-tablets.…”

Benznidazole Nanoformulates: A Chance to Improve Therapeutics for Chagas Disease

“…Their use in obtaining complexes of different drugs with trypanocidal action has been explored. [25][26][27][28][29] The aims of the present work were 1) to determine the in vitro trypanocidal activity of new nanostructured formulations of BNZ:small unilamellar vesicles (SUVs) (conventional nanoLPs and quatsomes [QS], lipid nanoparticles [solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs)]) and nanostructured CD complexes; and 2) to explore the toxicity of these agents in two cultured mammal cell lines.…”