Characterization and trypanocidal activity of a β-lapachone-containing drug carrier
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 conti...
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| creator | Barbosa, Juliana M C Nicoletti, Caroline D da Silva, Patrícia B Melo, Tatiana G Futuro, Débora O Ferreira, Vitor F Salomão, Kelly |
| description | 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. |
| doi_str_mv | 10.1371/journal.pone.0246811 |
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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.</description><identifier>ISSN: 1932-6203</identifier><identifier>EISSN: 1932-6203</identifier><identifier>DOI: 10.1371/journal.pone.0246811</identifier><identifier>PMID: 33661933</identifier><language>eng</language><publisher>United States: Public Library of Science</publisher><subject>Animals ; Bioavailability ; Biological activity ; Biology and Life Sciences ; Cardiac muscle ; Chagas disease ; Chlorophenol ; Chromatography ; Cytotoxicity ; Drug carriers ; Drug delivery ; Drug dosages ; Embryos ; Experimentation ; Experiments ; Funding ; Infections ; Lapachone ; Medicine and Health Sciences ; Methodology ; Muscles ; Parasites ; Pharmaceutical industry ; Physical Sciences ; Protozoa ; Tropical diseases ; Vector-borne diseases</subject><ispartof>PloS one, 2021-03, Vol.16 (3), p.e0246811-e0246811</ispartof><rights>2021 Barbosa et al. This is an open access article distributed under the terms of the Creative Commons Attribution License: http://creativecommons.org/licenses/by/4.0/ (the “License”), which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited. 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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. 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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.</abstract><cop>United States</cop><pub>Public Library of Science</pub><pmid>33661933</pmid><doi>10.1371/journal.pone.0246811</doi><orcidid>https://orcid.org/0000-0001-5397-718X</orcidid><oa>free_for_read</oa></addata></record> |
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| subjects | Animals Bioavailability Biological activity Biology and Life Sciences Cardiac muscle Chagas disease Chlorophenol Chromatography Cytotoxicity Drug carriers Drug delivery Drug dosages Embryos Experimentation Experiments Funding Infections Lapachone Medicine and Health Sciences Methodology Muscles Parasites Pharmaceutical industry Physical Sciences Protozoa Tropical diseases Vector-borne diseases |
| title | Characterization and trypanocidal activity of a β-lapachone-containing drug carrier |
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