Poloxamer micellar system for intra-articular injection of 15-deoxy-Δ12,14-prostaglandin J2 with improved bioavailability and anti-inflammatory properties in the temporomandibular joint of rats
Autor(a) principal: | |
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Data de Publicação: | 2020 |
Outros Autores: | , , , , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Institucional da UNESP |
Texto Completo: | http://dx.doi.org/10.1016/j.ijpharm.2020.119383 http://hdl.handle.net/11449/201725 |
Resumo: | Painful conditions of the temporomandibular joint (TMJ) are challenging to manage and most attempts often result in unsatisfactory outcomes. In such context, nanocarrier systems, such as polymeric micelles, have been showing encouraging results in solving therapeutic limitations. Poloxamers are widely used, especially PL 407, because of their high biocompatibility and approval by the Food and Drug Administration (FDA) for clinical use. 15-deoxy-Δ12,14-prostaglandin J2 (15d-PGJ2) has shown important antinociceptive and anti-inflammatory activity. The present study evaluated the efficacy and viability of the micellar system of PL-15dPGJ2 in a formalin-induced acute pain model in the temporomandibular joint of rats. The PL-15dPGJ2 was prepared and characterized. The animals were pretreated with an intra-articular injection of PL-15dPGJ2 followed by the formalin challenge. The nociceptive response was evaluated at different time-periods and the periarticular tissue and articular wash were collected for analysis. We found that intra-articular injection of PL-15d-PGJ2 produced pain relief at lower concentrations and in a sustained manner compared with free 15d-PGJ2. Moreover, a strong anti-inflammatory effect was observed with decreased levels of key pro-inflammatory cytokines and modulation of the leukocyte migration process. Our findings suggest that 15d-PGJ2 combined with a poloxamer micellar system provided clinical relevance in terms of bioavailability, long-lasting effect, and safe dosage. The formulation investigated herein is a promising micellar carrier system for managing pain conditions of the TMJ. |
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Poloxamer micellar system for intra-articular injection of 15-deoxy-Δ12,14-prostaglandin J2 with improved bioavailability and anti-inflammatory properties in the temporomandibular joint of rats15d-PGJ2PainPoloxamer micellar systemTemporomandibular jointPainful conditions of the temporomandibular joint (TMJ) are challenging to manage and most attempts often result in unsatisfactory outcomes. In such context, nanocarrier systems, such as polymeric micelles, have been showing encouraging results in solving therapeutic limitations. Poloxamers are widely used, especially PL 407, because of their high biocompatibility and approval by the Food and Drug Administration (FDA) for clinical use. 15-deoxy-Δ12,14-prostaglandin J2 (15d-PGJ2) has shown important antinociceptive and anti-inflammatory activity. The present study evaluated the efficacy and viability of the micellar system of PL-15dPGJ2 in a formalin-induced acute pain model in the temporomandibular joint of rats. The PL-15dPGJ2 was prepared and characterized. The animals were pretreated with an intra-articular injection of PL-15dPGJ2 followed by the formalin challenge. The nociceptive response was evaluated at different time-periods and the periarticular tissue and articular wash were collected for analysis. We found that intra-articular injection of PL-15d-PGJ2 produced pain relief at lower concentrations and in a sustained manner compared with free 15d-PGJ2. Moreover, a strong anti-inflammatory effect was observed with decreased levels of key pro-inflammatory cytokines and modulation of the leukocyte migration process. Our findings suggest that 15d-PGJ2 combined with a poloxamer micellar system provided clinical relevance in terms of bioavailability, long-lasting effect, and safe dosage. The formulation investigated herein is a promising micellar carrier system for managing pain conditions of the TMJ.Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Drug Research Academy, Københavns UniversitetLefkofsky Family FoundationFaculdade São Leopoldo Mandic Instituto São Leopoldo Mandic Laboratory of Neuroimmune Interface of PainFaculdade São Leopoldo Mandic de ArarasDepartment of Physiology Sciences Piracicaba Dental School University of CampinasCenter of Human and Natural Sciences Federal University of ABCDepartment of Environmental Engineering São Paulo State University (UNESP)Department of Environmental Engineering São Paulo State University (UNESP)Laboratory of Neuroimmune Interface of PainFaculdade São Leopoldo Mandic de ArarasUniversidade Estadual de Campinas (UNICAMP)Federal University of ABCUniversidade Estadual Paulista (Unesp)Abdalla, Henrique B.Napimoga, Marcelo H.Macedo, Cristina G.Bonfante, RicardoDe Araujo, Daniele.R.de Mello, Nathalie F.S.Carvalho, Lucas B. [UNESP]Fraceto, Leonardo F. [UNESP]Clemente-Napimoga, Juliana T.2020-12-12T02:40:13Z2020-12-12T02:40:13Z2020-06-15info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articlehttp://dx.doi.org/10.1016/j.ijpharm.2020.119383International Journal of Pharmaceutics, v. 583.1873-34760378-5173http://hdl.handle.net/11449/20172510.1016/j.ijpharm.2020.1193832-s2.0-85084150900Scopusreponame:Repositório Institucional da UNESPinstname:Universidade Estadual Paulista (UNESP)instacron:UNESPengInternational Journal of Pharmaceuticsinfo:eu-repo/semantics/openAccess2021-10-22T21:09:40Zoai:repositorio.unesp.br:11449/201725Repositório InstitucionalPUBhttp://repositorio.unesp.br/oai/requestopendoar:29462024-08-05T13:55:57.302607Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)false |
dc.title.none.fl_str_mv |
Poloxamer micellar system for intra-articular injection of 15-deoxy-Δ12,14-prostaglandin J2 with improved bioavailability and anti-inflammatory properties in the temporomandibular joint of rats |
title |
Poloxamer micellar system for intra-articular injection of 15-deoxy-Δ12,14-prostaglandin J2 with improved bioavailability and anti-inflammatory properties in the temporomandibular joint of rats |
spellingShingle |
Poloxamer micellar system for intra-articular injection of 15-deoxy-Δ12,14-prostaglandin J2 with improved bioavailability and anti-inflammatory properties in the temporomandibular joint of rats Abdalla, Henrique B. 15d-PGJ2 Pain Poloxamer micellar system Temporomandibular joint |
title_short |
Poloxamer micellar system for intra-articular injection of 15-deoxy-Δ12,14-prostaglandin J2 with improved bioavailability and anti-inflammatory properties in the temporomandibular joint of rats |
title_full |
Poloxamer micellar system for intra-articular injection of 15-deoxy-Δ12,14-prostaglandin J2 with improved bioavailability and anti-inflammatory properties in the temporomandibular joint of rats |
title_fullStr |
Poloxamer micellar system for intra-articular injection of 15-deoxy-Δ12,14-prostaglandin J2 with improved bioavailability and anti-inflammatory properties in the temporomandibular joint of rats |
title_full_unstemmed |
Poloxamer micellar system for intra-articular injection of 15-deoxy-Δ12,14-prostaglandin J2 with improved bioavailability and anti-inflammatory properties in the temporomandibular joint of rats |
title_sort |
Poloxamer micellar system for intra-articular injection of 15-deoxy-Δ12,14-prostaglandin J2 with improved bioavailability and anti-inflammatory properties in the temporomandibular joint of rats |
author |
Abdalla, Henrique B. |
author_facet |
Abdalla, Henrique B. Napimoga, Marcelo H. Macedo, Cristina G. Bonfante, Ricardo De Araujo, Daniele.R. de Mello, Nathalie F.S. Carvalho, Lucas B. [UNESP] Fraceto, Leonardo F. [UNESP] Clemente-Napimoga, Juliana T. |
author_role |
author |
author2 |
Napimoga, Marcelo H. Macedo, Cristina G. Bonfante, Ricardo De Araujo, Daniele.R. de Mello, Nathalie F.S. Carvalho, Lucas B. [UNESP] Fraceto, Leonardo F. [UNESP] Clemente-Napimoga, Juliana T. |
author2_role |
author author author author author author author author |
dc.contributor.none.fl_str_mv |
Laboratory of Neuroimmune Interface of Pain Faculdade São Leopoldo Mandic de Araras Universidade Estadual de Campinas (UNICAMP) Federal University of ABC Universidade Estadual Paulista (Unesp) |
dc.contributor.author.fl_str_mv |
Abdalla, Henrique B. Napimoga, Marcelo H. Macedo, Cristina G. Bonfante, Ricardo De Araujo, Daniele.R. de Mello, Nathalie F.S. Carvalho, Lucas B. [UNESP] Fraceto, Leonardo F. [UNESP] Clemente-Napimoga, Juliana T. |
dc.subject.por.fl_str_mv |
15d-PGJ2 Pain Poloxamer micellar system Temporomandibular joint |
topic |
15d-PGJ2 Pain Poloxamer micellar system Temporomandibular joint |
description |
Painful conditions of the temporomandibular joint (TMJ) are challenging to manage and most attempts often result in unsatisfactory outcomes. In such context, nanocarrier systems, such as polymeric micelles, have been showing encouraging results in solving therapeutic limitations. Poloxamers are widely used, especially PL 407, because of their high biocompatibility and approval by the Food and Drug Administration (FDA) for clinical use. 15-deoxy-Δ12,14-prostaglandin J2 (15d-PGJ2) has shown important antinociceptive and anti-inflammatory activity. The present study evaluated the efficacy and viability of the micellar system of PL-15dPGJ2 in a formalin-induced acute pain model in the temporomandibular joint of rats. The PL-15dPGJ2 was prepared and characterized. The animals were pretreated with an intra-articular injection of PL-15dPGJ2 followed by the formalin challenge. The nociceptive response was evaluated at different time-periods and the periarticular tissue and articular wash were collected for analysis. We found that intra-articular injection of PL-15d-PGJ2 produced pain relief at lower concentrations and in a sustained manner compared with free 15d-PGJ2. Moreover, a strong anti-inflammatory effect was observed with decreased levels of key pro-inflammatory cytokines and modulation of the leukocyte migration process. Our findings suggest that 15d-PGJ2 combined with a poloxamer micellar system provided clinical relevance in terms of bioavailability, long-lasting effect, and safe dosage. The formulation investigated herein is a promising micellar carrier system for managing pain conditions of the TMJ. |
publishDate |
2020 |
dc.date.none.fl_str_mv |
2020-12-12T02:40:13Z 2020-12-12T02:40:13Z 2020-06-15 |
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.uri.fl_str_mv |
http://dx.doi.org/10.1016/j.ijpharm.2020.119383 International Journal of Pharmaceutics, v. 583. 1873-3476 0378-5173 http://hdl.handle.net/11449/201725 10.1016/j.ijpharm.2020.119383 2-s2.0-85084150900 |
url |
http://dx.doi.org/10.1016/j.ijpharm.2020.119383 http://hdl.handle.net/11449/201725 |
identifier_str_mv |
International Journal of Pharmaceutics, v. 583. 1873-3476 0378-5173 10.1016/j.ijpharm.2020.119383 2-s2.0-85084150900 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
International Journal of Pharmaceutics |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.source.none.fl_str_mv |
Scopus reponame:Repositório Institucional da UNESP instname:Universidade Estadual Paulista (UNESP) instacron:UNESP |
instname_str |
Universidade Estadual Paulista (UNESP) |
instacron_str |
UNESP |
institution |
UNESP |
reponame_str |
Repositório Institucional da UNESP |
collection |
Repositório Institucional da UNESP |
repository.name.fl_str_mv |
Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP) |
repository.mail.fl_str_mv |
|
_version_ |
1808128291468476416 |