Characterization and trypanocidal activity of a β-lapachone-containing drug carrier.
Journal
PloS one
ISSN: 1932-6203
Titre abrégé: PLoS One
Pays: United States
ID NLM: 101285081
Informations de publication
Date de publication:
2021
2021
Historique:
received:
22
09
2020
accepted:
26
01
2021
entrez:
4
3
2021
pubmed:
5
3
2021
medline:
27
8
2021
Statut:
epublish
Résumé
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.
Identifiants
pubmed: 33661933
doi: 10.1371/journal.pone.0246811
pii: PONE-D-20-29893
pmc: PMC7932091
doi:
Substances chimiques
Drug Carriers
0
Naphthoquinones
0
Trypanocidal Agents
0
beta-lapachone
6N4FA2QQ6A
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
e0246811Déclaration de conflit d'intérêts
The authors have declared that no competing interests exist.
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