Characterization and trypanocidal activity of a β-lapachone-containing drug carrier

Abstract

The treatment of Chagas disease (CD), a neglected parasitic condition caused by Trypanosoma cruzi, is still based on only two drugs, nifurtimox (Nif) and benznidazole (Bz), both of which have limited efficacy in the late chronic phase and induce severe side effects. This scenario justifies the continuous search for alternative drugs, and in this context, the natural naphthoquinone β-lapachone (β-Lap) and its derivatives have demonstrated important trypanocidal activities. Unfortunately, the decrease in trypanocidal activity in the blood, high toxicity to mammalian cells and low water solubility of β-Lap limit its systemic administration and, consequently, clinical applications. For this reason, carriers as drug delivery systems can strategically maximize the therapeutic effects of this drug, overcoming the above mentioned restrictions. Accordingly, the aim of this study is to investigate the in vitro anti-T. cruzi effects of β-Lap encapsulated in2-hydroxypropyl-β-cyclodextrin (2HP-β-CD) and its potential toxicity to mammalian cells.

Preparation and Synergistic Anti-Tumor Effect of Iridium Oxide Nanocomposites under Microscope

“…The average particle size was determined to be 120 nm by a dynamic light scattering instrument, which provided a certain experimental basis for the development of passive targeting formulation of actalide [ 9 ]. Barbosa used a hydrazone bond to connect doxorubicin and chitosan derivatives, prepared a pH-sensitive drug carrier, and studied its in vitro release performance [ 10 ]. The drug carrier can exist stably in the physiological environment with a pH value of 7.4, and the drug is basically not released.…”

Natural Products and Synthetic Derivatives as Promising Candidates Against Neglected Tropical Diseases

“…In general, naphthoquinones, such as lapachone, have been studied for 40 years since they are promising prototypes of new leishmanicidal and trypanocidal agents mainly due to their oxidizing properties. In addition, the bioactivities have been associated with redox cycling, DNA fragmentation, DNA topoisomerase I and II inhibition, bioreductive alkylation via generation of quinone metides, arylation of thiol groups of proteins and generation of free radicals [94].…”