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

被引:7
作者
Barbosa, Juliana M. C. [1 ]
Nicoletti, Caroline D. [2 ,3 ]
da Silva, Patricia B. [1 ]
Melo, Tatiana G. [4 ]
Futuro, Debora O. [2 ]
Ferreira, Vitor F. [2 ,3 ]
Salomao, Kelly [1 ]
机构
[1] Fundacao Oswaldo Cruz, Lab Biol Celular Inst Oswaldo Cruz, Rio De Janeiro, RJ, Brazil
[2] Univ Fed Fluminense, Inst Quim, Lab Sintese Organ Aplicada, Niteroi, RJ, Brazil
[3] Univ Fed Fluminense, Fac Farm, Niteroi, RJ, Brazil
[4] Fundacao Oswaldo Cruz, Lab Ultraestrutura Celular, Inst Oswaldo Cruz, Rio De Janeiro, RJ, Brazil
来源
PLOS ONE | 2021年 / 16卷 / 03期
关键词
TRYPANOSOMA-CRUZI ACTIVITY; IN-VITRO; NAPHTHOQUINONES; BENZNIDAZOLE; BIOAVAILABILITY; VIVO; CYCLODEXTRINS; SOLUBILITY; STRATEGIES; COMPLEXES;
D O I
10.1371/journal.pone.0246811
中图分类号
O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];
学科分类号
07 ; 0710 ; 09 ;
摘要
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 beta-lapachone (beta-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 beta-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 beta-Lap encapsulated in2-hydroxypropyl-beta-cyclodextrin (2HP-beta-CD) and its potential toxicity to mammalian cells.
引用
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页数:13
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