Nanoemulsions of sulfonamide carbonic anhydrase inhibitors strongly inhibit the growth of Trypanosoma cruzi

摘要

Sulfonamide carbonic anhydrase (CA, EC 4.2.1.1) inhibitors targeting the α-class enzyme from the protozoan pathogen responsible of Chagas disease, were recently reported. Although many such derivatives showed low nanomolar activity , they were inefficient anti- agents . Here, we show that by formulating such sulfonamides as nanoemulsions in clove ( ) oil, highly efficient anti-protozoan effects are observed against two different strains of . These effects are probably due to an enhanced permeation of the enzyme inhibitor through the nanoemulsion formulation, interfering in this way with the life cycle of the pathogen either by inhibiting pH regulation or carboxylating reactions in which bicarbonate/CO are involved. This type of formulation of sulfonamides with CA inhibitory effects may lead to novel therapeutic approaches against this orphan disease.