Technological innovation strategies for the specific treatment of Chagas disease based on Benznidazole

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

“…Nevertheless, it is still used in the acute phase, with chances of cure, and in the chronic phase, preventing the disease progression. Therefore, as it is a worldwide public health problem, there is a certain urgency for the development of therapeutic alternatives 6 , 10 – 12 .…”

In vitro studies and preclinical evaluation of benznidazole microparticles in the acute Trypanosoma cruzi murine model

“…BNZ, like many other benzimidazole derivatives, is poorly water-soluble and exhibits a low dissolution rate which may require the administration of high doses to achieve therapeutic effects (Buckley et al , 2013). Thus, BNZ belongs to Class II of the Biopharmaceutical Classification System (BCS) (Del Moral Sanchez et al , 2018; Ferraz et al , 2018). However, according to the experimental data provided by Maximiano et al (2011), it is classified as Class IV, which indicate a reduced solubility and permeability with a Log P in distilled water, gastric fluid and enteric fluid of 0.77, 0.78 and 0.76, respectively (Maximiano et al , 2011).…”

“…BNZ is a poorly water-soluble compound (0.4 mg mL −1 ) and, therefore, high doses are needed to reach therapeutic concentrations in blood following oral administration (Quijia Quezada et al , 2019). Thus, reduction of the particle size constitutes a useful strategy to enhance the aqueous solubility/dissolution and improve the bioavailability after oral administration (Maximiano et al , 2011; Ferraz et al , 2018). Generally, micronization methodologies, including spray-drying devices, lead to the development of drug-loading microparticulate systems with desired functionalities (Piccirilli et al , 2014; Al-Khattawi et al , 2018).…”

Facile Synthesis of a Series of Non-Symmetric Thioethers Including a Benzothiazole Moiety and Their Use as Efficient In Vitro anti-Trypanosoma cruzi Agents

“…In this line, American trypanosomiasis or Chagas disease is caused by the hemoflagellate protozoan Trypanosoma cruzi ( T. cruzi ) that is transmitted by vectors, mainly triatomine insects [11]. This parasitic infection is considered neglected and affects mainly countries of tropical zones of Americas, where it is estimated that between 6 to 7 million people are infected with T. cruzi [12], and approximately 100 million people are at risk of infection with this protozoan [13].…”