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Preclinical Evaluation of Polymeric Nanocomposite Containing Pregabalin for Sustained Release as Potential Therapy for Neuropathic Pain

This study offers a novel oral pregabalin (PG)-loaded drug delivery system based on chitosan and hypromellose phthalate-based polymeric nanocomposite in order to treat neuropathic pain (PG-PN). PG-PN has a particle size of 432 ± 20 nm, a polydispersity index of 0.238 ± 0.001, a zeta potential of +19...

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Autores principales: Rodrigues, Rafaela Figueiredo, Nunes, Juliana Barbosa, Agostini, Sandra Barbosa Neder, dos Santos, Paloma Freitas, Cancino-Bernardi, Juliana, Placido, Rodrigo Vicentino, Moraes, Thamyris Reis, Freitas, Jennifer Tavares Jacon, Pereira, Gislaine Ribeiro, Carvalho, Flávia Chiva, Galdino, Giovane, Boralli, Vanessa Bergamin
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8587775/
https://www.ncbi.nlm.nih.gov/pubmed/34771392
http://dx.doi.org/10.3390/polym13213837
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author Rodrigues, Rafaela Figueiredo
Nunes, Juliana Barbosa
Agostini, Sandra Barbosa Neder
dos Santos, Paloma Freitas
Cancino-Bernardi, Juliana
Placido, Rodrigo Vicentino
Moraes, Thamyris Reis
Freitas, Jennifer Tavares Jacon
Pereira, Gislaine Ribeiro
Carvalho, Flávia Chiva
Galdino, Giovane
Boralli, Vanessa Bergamin
author_facet Rodrigues, Rafaela Figueiredo
Nunes, Juliana Barbosa
Agostini, Sandra Barbosa Neder
dos Santos, Paloma Freitas
Cancino-Bernardi, Juliana
Placido, Rodrigo Vicentino
Moraes, Thamyris Reis
Freitas, Jennifer Tavares Jacon
Pereira, Gislaine Ribeiro
Carvalho, Flávia Chiva
Galdino, Giovane
Boralli, Vanessa Bergamin
author_sort Rodrigues, Rafaela Figueiredo
collection PubMed
description This study offers a novel oral pregabalin (PG)-loaded drug delivery system based on chitosan and hypromellose phthalate-based polymeric nanocomposite in order to treat neuropathic pain (PG-PN). PG-PN has a particle size of 432 ± 20 nm, a polydispersity index of 0.238 ± 0.001, a zeta potential of +19.0 ± 0.9 mV, a pH of 5.7 ± 0.06, and a spherical shape. Thermal and infrared spectroscopy confirmed nanocomposite generation. PG-PN pharmacokinetics was studied after a single oral dose in male Wistar rats. PG-PN showed greater distribution and clearance than free PG. The antinociceptive effect of PG-PN in neuropathic pain rats was tested by using the chronic constriction injury model. The parameter investigated was the mechanical nociceptive threshold measured by the von Frey filaments test; PG-PN showed a longer antinociceptive effect than free PG. The rota-rod and barbiturate sleep induction procedures were used to determine adverse effects; the criteria included motor deficit and sedative effects. PG-PN and free PG had plenty of motors. PG-PN exhibited a less sedative effect than free PG. By prolonging the antinociceptive effect and decreasing the unfavorable effects, polymeric nanocomposites with pregabalin have shown promise in treating neuropathic pain.
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spelling pubmed-85877752021-11-13 Preclinical Evaluation of Polymeric Nanocomposite Containing Pregabalin for Sustained Release as Potential Therapy for Neuropathic Pain Rodrigues, Rafaela Figueiredo Nunes, Juliana Barbosa Agostini, Sandra Barbosa Neder dos Santos, Paloma Freitas Cancino-Bernardi, Juliana Placido, Rodrigo Vicentino Moraes, Thamyris Reis Freitas, Jennifer Tavares Jacon Pereira, Gislaine Ribeiro Carvalho, Flávia Chiva Galdino, Giovane Boralli, Vanessa Bergamin Polymers (Basel) Article This study offers a novel oral pregabalin (PG)-loaded drug delivery system based on chitosan and hypromellose phthalate-based polymeric nanocomposite in order to treat neuropathic pain (PG-PN). PG-PN has a particle size of 432 ± 20 nm, a polydispersity index of 0.238 ± 0.001, a zeta potential of +19.0 ± 0.9 mV, a pH of 5.7 ± 0.06, and a spherical shape. Thermal and infrared spectroscopy confirmed nanocomposite generation. PG-PN pharmacokinetics was studied after a single oral dose in male Wistar rats. PG-PN showed greater distribution and clearance than free PG. The antinociceptive effect of PG-PN in neuropathic pain rats was tested by using the chronic constriction injury model. The parameter investigated was the mechanical nociceptive threshold measured by the von Frey filaments test; PG-PN showed a longer antinociceptive effect than free PG. The rota-rod and barbiturate sleep induction procedures were used to determine adverse effects; the criteria included motor deficit and sedative effects. PG-PN and free PG had plenty of motors. PG-PN exhibited a less sedative effect than free PG. By prolonging the antinociceptive effect and decreasing the unfavorable effects, polymeric nanocomposites with pregabalin have shown promise in treating neuropathic pain. MDPI 2021-11-06 /pmc/articles/PMC8587775/ /pubmed/34771392 http://dx.doi.org/10.3390/polym13213837 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Rodrigues, Rafaela Figueiredo
Nunes, Juliana Barbosa
Agostini, Sandra Barbosa Neder
dos Santos, Paloma Freitas
Cancino-Bernardi, Juliana
Placido, Rodrigo Vicentino
Moraes, Thamyris Reis
Freitas, Jennifer Tavares Jacon
Pereira, Gislaine Ribeiro
Carvalho, Flávia Chiva
Galdino, Giovane
Boralli, Vanessa Bergamin
Preclinical Evaluation of Polymeric Nanocomposite Containing Pregabalin for Sustained Release as Potential Therapy for Neuropathic Pain
title Preclinical Evaluation of Polymeric Nanocomposite Containing Pregabalin for Sustained Release as Potential Therapy for Neuropathic Pain
title_full Preclinical Evaluation of Polymeric Nanocomposite Containing Pregabalin for Sustained Release as Potential Therapy for Neuropathic Pain
title_fullStr Preclinical Evaluation of Polymeric Nanocomposite Containing Pregabalin for Sustained Release as Potential Therapy for Neuropathic Pain
title_full_unstemmed Preclinical Evaluation of Polymeric Nanocomposite Containing Pregabalin for Sustained Release as Potential Therapy for Neuropathic Pain
title_short Preclinical Evaluation of Polymeric Nanocomposite Containing Pregabalin for Sustained Release as Potential Therapy for Neuropathic Pain
title_sort preclinical evaluation of polymeric nanocomposite containing pregabalin for sustained release as potential therapy for neuropathic pain
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8587775/
https://www.ncbi.nlm.nih.gov/pubmed/34771392
http://dx.doi.org/10.3390/polym13213837
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