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...

Descripción completa

Guardado en:

Detalles Bibliográficos
Autores principales:	Rafaela Figueiredo Rodrigues, Juliana Barbosa Nunes, Sandra Barbosa Neder Agostini, Paloma Freitas dos Santos, Juliana Cancino-Bernardi, Rodrigo Vicentino Placido, Thamyris Reis Moraes, Jennifer Tavares Jacon Freitas, Gislaine Ribeiro Pereira, Flávia Chiva Carvalho, Giovane Galdino, Vanessa Bergamin Boralli
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	neuropathy polymeric nanoparticles preclinical investigation pharmacokinetics of pregabalin antinociceptive effect induced sleep Organic chemistry QD241-441
Acceso en línea:	https://doaj.org/article/7829cca9daee4d8e95b7582b1cae90af
Etiquetas:	Agregar Etiqueta Sin Etiquetas, Sea el primero en etiquetar este registro!

id	oai:doaj.org-article:7829cca9daee4d8e95b7582b1cae90af
record_format	dspace
spelling	oai:doaj.org-article:7829cca9daee4d8e95b7582b1cae90af2021-11-11T18:48:40ZPreclinical Evaluation of Polymeric Nanocomposite Containing Pregabalin for Sustained Release as Potential Therapy for Neuropathic Pain10.3390/polym132138372073-4360https://doaj.org/article/7829cca9daee4d8e95b7582b1cae90af2021-11-01T00:00:00Zhttps://www.mdpi.com/2073-4360/13/21/3837https://doaj.org/toc/2073-4360This 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.Rafaela Figueiredo RodriguesJuliana Barbosa NunesSandra Barbosa Neder AgostiniPaloma Freitas dos SantosJuliana Cancino-BernardiRodrigo Vicentino PlacidoThamyris Reis MoraesJennifer Tavares Jacon FreitasGislaine Ribeiro PereiraFlávia Chiva CarvalhoGiovane GaldinoVanessa Bergamin BoralliMDPI AGarticleneuropathypolymeric nanoparticlespreclinical investigationpharmacokinetics of pregabalinantinociceptive effectinduced sleepOrganic chemistryQD241-441ENPolymers, Vol 13, Iss 3837, p 3837 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	neuropathy polymeric nanoparticles preclinical investigation pharmacokinetics of pregabalin antinociceptive effect induced sleep Organic chemistry QD241-441
spellingShingle	neuropathy polymeric nanoparticles preclinical investigation pharmacokinetics of pregabalin antinociceptive effect induced sleep Organic chemistry QD241-441 Rafaela Figueiredo Rodrigues Juliana Barbosa Nunes Sandra Barbosa Neder Agostini Paloma Freitas dos Santos Juliana Cancino-Bernardi Rodrigo Vicentino Placido Thamyris Reis Moraes Jennifer Tavares Jacon Freitas Gislaine Ribeiro Pereira Flávia Chiva Carvalho Giovane Galdino Vanessa Bergamin Boralli Preclinical Evaluation of Polymeric Nanocomposite Containing Pregabalin for Sustained Release as Potential Therapy for Neuropathic Pain
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.
format	article
author	Rafaela Figueiredo Rodrigues Juliana Barbosa Nunes Sandra Barbosa Neder Agostini Paloma Freitas dos Santos Juliana Cancino-Bernardi Rodrigo Vicentino Placido Thamyris Reis Moraes Jennifer Tavares Jacon Freitas Gislaine Ribeiro Pereira Flávia Chiva Carvalho Giovane Galdino Vanessa Bergamin Boralli
author_facet	Rafaela Figueiredo Rodrigues Juliana Barbosa Nunes Sandra Barbosa Neder Agostini Paloma Freitas dos Santos Juliana Cancino-Bernardi Rodrigo Vicentino Placido Thamyris Reis Moraes Jennifer Tavares Jacon Freitas Gislaine Ribeiro Pereira Flávia Chiva Carvalho Giovane Galdino Vanessa Bergamin Boralli
author_sort	Rafaela Figueiredo Rodrigues
title	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_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_sort	preclinical evaluation of polymeric nanocomposite containing pregabalin for sustained release as potential therapy for neuropathic pain
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/7829cca9daee4d8e95b7582b1cae90af
work_keys_str_mv	AT rafaelafigueiredorodrigues preclinicalevaluationofpolymericnanocompositecontainingpregabalinforsustainedreleaseaspotentialtherapyforneuropathicpain AT julianabarbosanunes preclinicalevaluationofpolymericnanocompositecontainingpregabalinforsustainedreleaseaspotentialtherapyforneuropathicpain AT sandrabarbosanederagostini preclinicalevaluationofpolymericnanocompositecontainingpregabalinforsustainedreleaseaspotentialtherapyforneuropathicpain AT palomafreitasdossantos preclinicalevaluationofpolymericnanocompositecontainingpregabalinforsustainedreleaseaspotentialtherapyforneuropathicpain AT julianacancinobernardi preclinicalevaluationofpolymericnanocompositecontainingpregabalinforsustainedreleaseaspotentialtherapyforneuropathicpain AT rodrigovicentinoplacido preclinicalevaluationofpolymericnanocompositecontainingpregabalinforsustainedreleaseaspotentialtherapyforneuropathicpain AT thamyrisreismoraes preclinicalevaluationofpolymericnanocompositecontainingpregabalinforsustainedreleaseaspotentialtherapyforneuropathicpain AT jennifertavaresjaconfreitas preclinicalevaluationofpolymericnanocompositecontainingpregabalinforsustainedreleaseaspotentialtherapyforneuropathicpain AT gislaineribeiropereira preclinicalevaluationofpolymericnanocompositecontainingpregabalinforsustainedreleaseaspotentialtherapyforneuropathicpain AT flaviachivacarvalho preclinicalevaluationofpolymericnanocompositecontainingpregabalinforsustainedreleaseaspotentialtherapyforneuropathicpain AT giovanegaldino preclinicalevaluationofpolymericnanocompositecontainingpregabalinforsustainedreleaseaspotentialtherapyforneuropathicpain AT vanessabergaminboralli preclinicalevaluationofpolymericnanocompositecontainingpregabalinforsustainedreleaseaspotentialtherapyforneuropathicpain
_version_	1718431709903454208

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

Ejemplares similares