Macromolecular confinement of therapeutic protein in polymeric particles for controlled release: insulin as a case study
Autor(a) principal: | |
---|---|
Data de Publicação: | 2017 |
Outros Autores: | , , , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Brazilian Journal of Pharmaceutical Sciences |
Texto Completo: | https://www.revistas.usp.br/bjps/article/view/134167 |
Resumo: | Sustained release systems for therapeutic proteins have been widely studied targeting to improve the action of these drugs. Molecular entrapping of proteins is particularly challenging due to their conformational instability. We have developed a micro-structured poly-epsilon-caprolactone (PCL) particle system loaded with human insulin using a simple double-emulsion w/o/w method followed by solvent evaporation method. This formulation is comprised by spheric-shaped microparticles with average size of 10 micrometers. In vitro release showed a biphasic behavior such as a rapid release with about 50% of drug delivered within 2 hours and a sustained phase for up to 48 h. The subcutaneous administration of microencapsulated insulin showed a biphasic effect on glycemia in streptozotocin-induced diabetic mice, compatible with short and intermediate-acting behaviors, with first transition peak at about 2 h and the second phase exerting effect for up to 48h after s.c. administration. This study reveals that a simplified double-emulsion system results in biocompatible human-insulin-loaded PCL microparticles that might be used for further development of optimized sustained release formulations of insulin to be used in the restoration of hormonal levels. |
id |
USP-31_bc94607fd5fd79a2a0a330d54eb33713 |
---|---|
oai_identifier_str |
oai:revistas.usp.br:article/134167 |
network_acronym_str |
USP-31 |
network_name_str |
Brazilian Journal of Pharmaceutical Sciences |
repository_id_str |
|
spelling |
Macromolecular confinement of therapeutic protein in polymeric particles for controlled release: insulin as a case studyHuman insulin/studyMicroparticlesPoly-ε-caprolactoneTherapeutic proteins/study/actionProteins/molecular entrapping Sustained release systems for therapeutic proteins have been widely studied targeting to improve the action of these drugs. Molecular entrapping of proteins is particularly challenging due to their conformational instability. We have developed a micro-structured poly-epsilon-caprolactone (PCL) particle system loaded with human insulin using a simple double-emulsion w/o/w method followed by solvent evaporation method. This formulation is comprised by spheric-shaped microparticles with average size of 10 micrometers. In vitro release showed a biphasic behavior such as a rapid release with about 50% of drug delivered within 2 hours and a sustained phase for up to 48 h. The subcutaneous administration of microencapsulated insulin showed a biphasic effect on glycemia in streptozotocin-induced diabetic mice, compatible with short and intermediate-acting behaviors, with first transition peak at about 2 h and the second phase exerting effect for up to 48h after s.c. administration. This study reveals that a simplified double-emulsion system results in biocompatible human-insulin-loaded PCL microparticles that might be used for further development of optimized sustained release formulations of insulin to be used in the restoration of hormonal levels.Universidade de São Paulo. Faculdade de Ciências Farmacêuticas2017-01-01info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionapplication/pdfhttps://www.revistas.usp.br/bjps/article/view/13416710.1590/s2175-97902017000216039Brazilian Journal of Pharmaceutical Sciences; Vol. 53 Núm. 2 (2017); e16039-Brazilian Journal of Pharmaceutical Sciences; v. 53 n. 2 (2017); e16039-Brazilian Journal of Pharmaceutical Sciences; Vol. 53 No. 2 (2017); e16039-2175-97901984-8250reponame:Brazilian Journal of Pharmaceutical Sciencesinstname:Universidade de São Paulo (USP)instacron:USPenghttps://www.revistas.usp.br/bjps/article/view/134167/129985Copyright (c) 2018 Brazilian Journal of Pharmaceutical Sciences (Impresso)info:eu-repo/semantics/openAccessGuerreiro, Luiz HenriqueSilva, Daniel daGirard-Dias, WendellMascarenhas, Camile MoreiraMiranda, KildareSola-Penna, MauroRicci Júnior, EduardoLima, Luís Mauricio Trambaioli da Rocha e2017-06-29T17:40:27Zoai:revistas.usp.br:article/134167Revistahttps://www.revistas.usp.br/bjps/indexPUBhttps://old.scielo.br/oai/scielo-oai.phpbjps@usp.br||elizabeth.igne@gmail.com2175-97901984-8250opendoar:2017-06-29T17:40:27Brazilian Journal of Pharmaceutical Sciences - Universidade de São Paulo (USP)false |
dc.title.none.fl_str_mv |
Macromolecular confinement of therapeutic protein in polymeric particles for controlled release: insulin as a case study |
title |
Macromolecular confinement of therapeutic protein in polymeric particles for controlled release: insulin as a case study |
spellingShingle |
Macromolecular confinement of therapeutic protein in polymeric particles for controlled release: insulin as a case study Guerreiro, Luiz Henrique Human insulin/study Microparticles Poly-ε-caprolactone Therapeutic proteins/study/action Proteins/molecular entrapping |
title_short |
Macromolecular confinement of therapeutic protein in polymeric particles for controlled release: insulin as a case study |
title_full |
Macromolecular confinement of therapeutic protein in polymeric particles for controlled release: insulin as a case study |
title_fullStr |
Macromolecular confinement of therapeutic protein in polymeric particles for controlled release: insulin as a case study |
title_full_unstemmed |
Macromolecular confinement of therapeutic protein in polymeric particles for controlled release: insulin as a case study |
title_sort |
Macromolecular confinement of therapeutic protein in polymeric particles for controlled release: insulin as a case study |
author |
Guerreiro, Luiz Henrique |
author_facet |
Guerreiro, Luiz Henrique Silva, Daniel da Girard-Dias, Wendell Mascarenhas, Camile Moreira Miranda, Kildare Sola-Penna, Mauro Ricci Júnior, Eduardo Lima, Luís Mauricio Trambaioli da Rocha e |
author_role |
author |
author2 |
Silva, Daniel da Girard-Dias, Wendell Mascarenhas, Camile Moreira Miranda, Kildare Sola-Penna, Mauro Ricci Júnior, Eduardo Lima, Luís Mauricio Trambaioli da Rocha e |
author2_role |
author author author author author author author |
dc.contributor.author.fl_str_mv |
Guerreiro, Luiz Henrique Silva, Daniel da Girard-Dias, Wendell Mascarenhas, Camile Moreira Miranda, Kildare Sola-Penna, Mauro Ricci Júnior, Eduardo Lima, Luís Mauricio Trambaioli da Rocha e |
dc.subject.por.fl_str_mv |
Human insulin/study Microparticles Poly-ε-caprolactone Therapeutic proteins/study/action Proteins/molecular entrapping |
topic |
Human insulin/study Microparticles Poly-ε-caprolactone Therapeutic proteins/study/action Proteins/molecular entrapping |
description |
Sustained release systems for therapeutic proteins have been widely studied targeting to improve the action of these drugs. Molecular entrapping of proteins is particularly challenging due to their conformational instability. We have developed a micro-structured poly-epsilon-caprolactone (PCL) particle system loaded with human insulin using a simple double-emulsion w/o/w method followed by solvent evaporation method. This formulation is comprised by spheric-shaped microparticles with average size of 10 micrometers. In vitro release showed a biphasic behavior such as a rapid release with about 50% of drug delivered within 2 hours and a sustained phase for up to 48 h. The subcutaneous administration of microencapsulated insulin showed a biphasic effect on glycemia in streptozotocin-induced diabetic mice, compatible with short and intermediate-acting behaviors, with first transition peak at about 2 h and the second phase exerting effect for up to 48h after s.c. administration. This study reveals that a simplified double-emulsion system results in biocompatible human-insulin-loaded PCL microparticles that might be used for further development of optimized sustained release formulations of insulin to be used in the restoration of hormonal levels. |
publishDate |
2017 |
dc.date.none.fl_str_mv |
2017-01-01 |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article info:eu-repo/semantics/publishedVersion |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
https://www.revistas.usp.br/bjps/article/view/134167 10.1590/s2175-97902017000216039 |
url |
https://www.revistas.usp.br/bjps/article/view/134167 |
identifier_str_mv |
10.1590/s2175-97902017000216039 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
https://www.revistas.usp.br/bjps/article/view/134167/129985 |
dc.rights.driver.fl_str_mv |
Copyright (c) 2018 Brazilian Journal of Pharmaceutical Sciences (Impresso) info:eu-repo/semantics/openAccess |
rights_invalid_str_mv |
Copyright (c) 2018 Brazilian Journal of Pharmaceutical Sciences (Impresso) |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
application/pdf |
dc.publisher.none.fl_str_mv |
Universidade de São Paulo. Faculdade de Ciências Farmacêuticas |
publisher.none.fl_str_mv |
Universidade de São Paulo. Faculdade de Ciências Farmacêuticas |
dc.source.none.fl_str_mv |
Brazilian Journal of Pharmaceutical Sciences; Vol. 53 Núm. 2 (2017); e16039- Brazilian Journal of Pharmaceutical Sciences; v. 53 n. 2 (2017); e16039- Brazilian Journal of Pharmaceutical Sciences; Vol. 53 No. 2 (2017); e16039- 2175-9790 1984-8250 reponame:Brazilian Journal of Pharmaceutical Sciences instname:Universidade de São Paulo (USP) instacron:USP |
instname_str |
Universidade de São Paulo (USP) |
instacron_str |
USP |
institution |
USP |
reponame_str |
Brazilian Journal of Pharmaceutical Sciences |
collection |
Brazilian Journal of Pharmaceutical Sciences |
repository.name.fl_str_mv |
Brazilian Journal of Pharmaceutical Sciences - Universidade de São Paulo (USP) |
repository.mail.fl_str_mv |
bjps@usp.br||elizabeth.igne@gmail.com |
_version_ |
1800222913260945408 |