Pyrazinoic acid-poly(malic acid) biodegradable nanoconjugate for efficient intracellular delivery.
Autor(a) principal: | |
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Data de Publicação: | 2019 |
Outros Autores: | , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Institucional da UFOP |
Texto Completo: | http://www.repositorio.ufop.br/handle/123456789/12246 https://doi.org/10.33218/prnano2(3).190523.1 |
Resumo: | Tuberculosis is an infectious disease affecting mostly lungs, that is still considered a health global problem as it causes millions of deaths worldwide. Current treatment is effective but associated with severe adverse effects due to the high doses of each anti-tuberculosis drug daily administrated by oral therapy. For the first time, a pyrazinoic acid (PA) biodegradable nanoconjugate was synthesized and developed for pulmonary administration in an attempt to reduce the administered doses by achieving a high drug payload and controlled release at the target site. The conjugate was synthesized by coupling pyrazinoic acid on carboxylic groups of poly(malic acid), which is a biodegradable and biocompatible polymer, and posteriorly self-assembled into nanoconjugates. Characterization confirmed the formation of nanometric, spherical and negatively charged pyrazinoic acid nanoconjugate (NC-PA). NC-PA was stable for 60 days at 4 and 37°C and able to deliver PA in a sustained release manner over time. On macrophages, they exhibited no cell toxicity for a wide range of concentrations (from 1 to 100 µg/mL), demonstrating the safety of NC-PA. In addition, the nanoconjugate was efficiently taken up by RAW 264.7 cells over 6 hours reaching a maximum value after 3 hours of incubation. In conclusion, innovative nanoconjugates are a promising alternative to deliver drugs directly to the lungs and contributing to improving tuberculosis therapy. |
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Carneiro, Simone PintoMoine, LaurenceTessier, BarbaraValérie, NicolasSantos, Orlando David Henrique dosFattal, Elias2020-05-22T16:52:30Z2020-05-22T16:52:30Z2019CARNEIRO, S. P. et al. Pyrazinoic acid-poly(malic acid) biodegradable nanoconjugate for efficient intracellular delivery. Precision Nanomedicine, v. 2, n. 3, p. 303-317, jul. 2019. Disponível em: <https://precisionnanomedicine.com/article/9660-pyrazinoic-acid-poly-malic-acid-biodegradable-nanoconjugate-for-efficient-intracellular-delivery>. Acesso em: 10 fev. 2020.2639-9431http://www.repositorio.ufop.br/handle/123456789/12246https://doi.org/10.33218/prnano2(3).190523.1Tuberculosis is an infectious disease affecting mostly lungs, that is still considered a health global problem as it causes millions of deaths worldwide. Current treatment is effective but associated with severe adverse effects due to the high doses of each anti-tuberculosis drug daily administrated by oral therapy. For the first time, a pyrazinoic acid (PA) biodegradable nanoconjugate was synthesized and developed for pulmonary administration in an attempt to reduce the administered doses by achieving a high drug payload and controlled release at the target site. The conjugate was synthesized by coupling pyrazinoic acid on carboxylic groups of poly(malic acid), which is a biodegradable and biocompatible polymer, and posteriorly self-assembled into nanoconjugates. Characterization confirmed the formation of nanometric, spherical and negatively charged pyrazinoic acid nanoconjugate (NC-PA). NC-PA was stable for 60 days at 4 and 37°C and able to deliver PA in a sustained release manner over time. On macrophages, they exhibited no cell toxicity for a wide range of concentrations (from 1 to 100 µg/mL), demonstrating the safety of NC-PA. In addition, the nanoconjugate was efficiently taken up by RAW 264.7 cells over 6 hours reaching a maximum value after 3 hours of incubation. In conclusion, innovative nanoconjugates are a promising alternative to deliver drugs directly to the lungs and contributing to improving tuberculosis therapy.License: CC BY-NC-SA 4.0. Fonte: o próprio artigo.info:eu-repo/semantics/openAccessTuberculosisPyrazinoic acid-poly(malic acid) biodegradable nanoconjugate for efficient intracellular delivery.info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleengreponame:Repositório Institucional da UFOPinstname:Universidade Federal de Ouro Preto (UFOP)instacron:UFOPLICENSElicense.txtlicense.txttext/plain; charset=utf-8924http://www.repositorio.ufop.br/bitstream/123456789/12246/2/license.txt62604f8d955274beb56c80ce1ee5dcaeMD52ORIGINALARTIGO_PyrazinoicAcidPoly.pdfARTIGO_PyrazinoicAcidPoly.pdfapplication/pdf1150976http://www.repositorio.ufop.br/bitstream/123456789/12246/1/ARTIGO_PyrazinoicAcidPoly.pdff2fed6a0ce821f8caf65438fae814eeeMD51123456789/122462020-05-22 12:52:30.509oai:localhost: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ório InstitucionalPUBhttp://www.repositorio.ufop.br/oai/requestrepositorio@ufop.edu.bropendoar:32332020-05-22T16:52:30Repositório Institucional da UFOP - Universidade Federal de Ouro Preto (UFOP)false |
dc.title.pt_BR.fl_str_mv |
Pyrazinoic acid-poly(malic acid) biodegradable nanoconjugate for efficient intracellular delivery. |
title |
Pyrazinoic acid-poly(malic acid) biodegradable nanoconjugate for efficient intracellular delivery. |
spellingShingle |
Pyrazinoic acid-poly(malic acid) biodegradable nanoconjugate for efficient intracellular delivery. Carneiro, Simone Pinto Tuberculosis |
title_short |
Pyrazinoic acid-poly(malic acid) biodegradable nanoconjugate for efficient intracellular delivery. |
title_full |
Pyrazinoic acid-poly(malic acid) biodegradable nanoconjugate for efficient intracellular delivery. |
title_fullStr |
Pyrazinoic acid-poly(malic acid) biodegradable nanoconjugate for efficient intracellular delivery. |
title_full_unstemmed |
Pyrazinoic acid-poly(malic acid) biodegradable nanoconjugate for efficient intracellular delivery. |
title_sort |
Pyrazinoic acid-poly(malic acid) biodegradable nanoconjugate for efficient intracellular delivery. |
author |
Carneiro, Simone Pinto |
author_facet |
Carneiro, Simone Pinto Moine, Laurence Tessier, Barbara Valérie, Nicolas Santos, Orlando David Henrique dos Fattal, Elias |
author_role |
author |
author2 |
Moine, Laurence Tessier, Barbara Valérie, Nicolas Santos, Orlando David Henrique dos Fattal, Elias |
author2_role |
author author author author author |
dc.contributor.author.fl_str_mv |
Carneiro, Simone Pinto Moine, Laurence Tessier, Barbara Valérie, Nicolas Santos, Orlando David Henrique dos Fattal, Elias |
dc.subject.por.fl_str_mv |
Tuberculosis |
topic |
Tuberculosis |
description |
Tuberculosis is an infectious disease affecting mostly lungs, that is still considered a health global problem as it causes millions of deaths worldwide. Current treatment is effective but associated with severe adverse effects due to the high doses of each anti-tuberculosis drug daily administrated by oral therapy. For the first time, a pyrazinoic acid (PA) biodegradable nanoconjugate was synthesized and developed for pulmonary administration in an attempt to reduce the administered doses by achieving a high drug payload and controlled release at the target site. The conjugate was synthesized by coupling pyrazinoic acid on carboxylic groups of poly(malic acid), which is a biodegradable and biocompatible polymer, and posteriorly self-assembled into nanoconjugates. Characterization confirmed the formation of nanometric, spherical and negatively charged pyrazinoic acid nanoconjugate (NC-PA). NC-PA was stable for 60 days at 4 and 37°C and able to deliver PA in a sustained release manner over time. On macrophages, they exhibited no cell toxicity for a wide range of concentrations (from 1 to 100 µg/mL), demonstrating the safety of NC-PA. In addition, the nanoconjugate was efficiently taken up by RAW 264.7 cells over 6 hours reaching a maximum value after 3 hours of incubation. In conclusion, innovative nanoconjugates are a promising alternative to deliver drugs directly to the lungs and contributing to improving tuberculosis therapy. |
publishDate |
2019 |
dc.date.issued.fl_str_mv |
2019 |
dc.date.accessioned.fl_str_mv |
2020-05-22T16:52:30Z |
dc.date.available.fl_str_mv |
2020-05-22T16:52:30Z |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article |
format |
article |
status_str |
publishedVersion |
dc.identifier.citation.fl_str_mv |
CARNEIRO, S. P. et al. Pyrazinoic acid-poly(malic acid) biodegradable nanoconjugate for efficient intracellular delivery. Precision Nanomedicine, v. 2, n. 3, p. 303-317, jul. 2019. Disponível em: <https://precisionnanomedicine.com/article/9660-pyrazinoic-acid-poly-malic-acid-biodegradable-nanoconjugate-for-efficient-intracellular-delivery>. Acesso em: 10 fev. 2020. |
dc.identifier.uri.fl_str_mv |
http://www.repositorio.ufop.br/handle/123456789/12246 |
dc.identifier.issn.none.fl_str_mv |
2639-9431 |
dc.identifier.doi.pt_BR.fl_str_mv |
https://doi.org/10.33218/prnano2(3).190523.1 |
identifier_str_mv |
CARNEIRO, S. P. et al. Pyrazinoic acid-poly(malic acid) biodegradable nanoconjugate for efficient intracellular delivery. Precision Nanomedicine, v. 2, n. 3, p. 303-317, jul. 2019. Disponível em: <https://precisionnanomedicine.com/article/9660-pyrazinoic-acid-poly-malic-acid-biodegradable-nanoconjugate-for-efficient-intracellular-delivery>. Acesso em: 10 fev. 2020. 2639-9431 |
url |
http://www.repositorio.ufop.br/handle/123456789/12246 https://doi.org/10.33218/prnano2(3).190523.1 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.rights.driver.fl_str_mv |
License: CC BY-NC-SA 4.0. Fonte: o próprio artigo. info:eu-repo/semantics/openAccess |
rights_invalid_str_mv |
License: CC BY-NC-SA 4.0. Fonte: o próprio artigo. |
eu_rights_str_mv |
openAccess |
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reponame:Repositório Institucional da UFOP instname:Universidade Federal de Ouro Preto (UFOP) instacron:UFOP |
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