Chagas disease: pharmaceutical nanovehicles encapsulating benznidazole

MURACA, G.; ISLAN, G.A.; RUIZ, M.E.; SCIOLI MONTOTO, S.; PESCE, G.O.; CASTRO, G.R.; TALEVI, A.

Mar del Plata

Congreso; REUNIÓN ANUAL DE SOCIEDADES DE BIOCIENCIA 2019; 2019

SAIC - SAFE - SAB - SAP - AACYTAL - NANOMED-ar

Chagas disease is an endemic parasitosis in Latin America whose etiologic agent is Trypanosoma cruzi. Benznidazole, the first-line therapy, eliminates trypanosomes in the circulatory system but seemingly does not fully eliminate parasites in tissue reservoirs, presenting a low cure rate in the chronic stage of the disease. An interesting approach to be considered is antichagasic drug delivery in novel nanotechnological vehicles. In other pathologies, nano systems are known to modify drug pharmacokinetics, improve delivery to target cells, increase drug concentration in tissues and protect circulating drug from elimination mechanisms, enhancing the drug safety profile and promoting adherence to the treatment. Our project aimed to obtain and evaluate pharmaceutical nanovehicles encapsulating benznidazole, taking advantage of the previously mentioned advantages. Here, nanoparticles were synthesized by the homogenization/ultrasonication method using two distinct matrixes: one lipidic (fatty esters) and one polymeric (ethyl acrylate, methyl methacrylate). This were evaluated in terms of drug loading and other physicochemical characteristics, with interest on developing future hybrid particles. Both types of nanoparticles presented spherical shape and encapsulation efficiencies of approximately 60 %. Mean diameter size was measured by DLS and TEM. Polymeric and lipidic particles sizes were 156.5 and 153.8 nm, respectively. Polydispersity index was around 0.2 which indicates an adequate size distribution to perform biological assays. In vitro drug release assays showed controlled release profiles in different dissolution mediums (phosphate buffer, hydroalcoholic solution and lauryl sulfate solution), with and average release of around 80 % of the drug load at 24 hours. As the next step in our research, thermal and spectroscopical methods will be included, as well as cell permeability/toxicity assays, and evaluation of trypanocidal effects in cell models.