Development of novel galactosylated PLGA nanoparticles for hepatocyte targeting using molecular modelling

Detalhes bibliográficos
Autor(a) principal: Raposo, Cláudia D.
Data de Publicação: 2020
Outros Autores: Costa, Rita, Petrova, Krasimira T., Brito, Catarina, Scotti, Marcus T., Cardoso, M. Margarida
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
Texto Completo: http://hdl.handle.net/10362/105365
Resumo: FCT/MEC (UID/QUI/50006/2019). ERDF under the PT2020 Partnership Agreement (POCI-01-0145-FEDER-007265).
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spelling Development of novel galactosylated PLGA nanoparticles for hepatocyte targeting using molecular modellingDoxorubicin deliveryGalactosylated nanoparticlesHepatocyte targeting nanoparticlesMolecular modelling for drug targetingSurface modified plga nanoparticlesChemistry(all)Polymers and PlasticsFCT/MEC (UID/QUI/50006/2019). ERDF under the PT2020 Partnership Agreement (POCI-01-0145-FEDER-007265).Doxorubicin-loaded PLGA nanoparticles conjugated with a new galactose-based ligand for the specific recognition by human hepatoma cellular carcinoma cells (Hep G2) were successfully produced. The new targeting compound was selected using molecular docking combined with quantum chemical calculations for modelling and comparing molecular interactions among the H1 subunit of the asialoglycoprotein receptor containing the carbohydrate recognition domain and the ligand. The ligand, bis(1-O-ethyl-β-D-galactopyranosyl)amine, was synthetized, characterized, and subsequently linked to PLGA. Unloaded (PLGA-di-GAL NP) and doxorubicin-loaded (DOX-PLGA-di-GAL NP) nanoparticles were prepared using an emulsion method and characterized. The produced DOX-PLGA-di-GAL NP are spherical in shape with a size of 258 ± 47 nm, a zeta potential of-62.3 mV, and a drug encapsulation efficiency of 83%. The in vitro drug release results obtained show a three-phase release profile. In vitro cell studies confirmed the interaction between Hep G2 cells and PLGA-di-GAL NP. Cell cytotoxicity tests showed that unloaded NP are nontoxic and that DOX-PLGA-di-GAL NP caused a decrease of around 80% in cellular viability. The strategy used in this work to design new targeting compounds represents a promising tool to develop eective hepatocyte targeting drug delivery systems and can be applied to other tissues/organs.DQ - Departamento de QuímicaLAQV@REQUIMTEInstituto de Tecnologia Química e Biológica António Xavier (ITQB)RUNRaposo, Cláudia D.Costa, RitaPetrova, Krasimira T.Brito, CatarinaScotti, Marcus T.Cardoso, M. Margarida2020-10-09T22:47:44Z2020-01-042020-01-04T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleapplication/pdfhttp://hdl.handle.net/10362/105365eng1618-7229PURE: 17108233https://doi.org/10.3390/polym12010094info:eu-repo/semantics/openAccessreponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãoinstacron:RCAAP2024-03-11T04:50:36Zoai:run.unl.pt:10362/105365Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-20T03:40:26.352Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãofalse
dc.title.none.fl_str_mv Development of novel galactosylated PLGA nanoparticles for hepatocyte targeting using molecular modelling
title Development of novel galactosylated PLGA nanoparticles for hepatocyte targeting using molecular modelling
spellingShingle Development of novel galactosylated PLGA nanoparticles for hepatocyte targeting using molecular modelling
Raposo, Cláudia D.
Doxorubicin delivery
Galactosylated nanoparticles
Hepatocyte targeting nanoparticles
Molecular modelling for drug targeting
Surface modified plga nanoparticles
Chemistry(all)
Polymers and Plastics
title_short Development of novel galactosylated PLGA nanoparticles for hepatocyte targeting using molecular modelling
title_full Development of novel galactosylated PLGA nanoparticles for hepatocyte targeting using molecular modelling
title_fullStr Development of novel galactosylated PLGA nanoparticles for hepatocyte targeting using molecular modelling
title_full_unstemmed Development of novel galactosylated PLGA nanoparticles for hepatocyte targeting using molecular modelling
title_sort Development of novel galactosylated PLGA nanoparticles for hepatocyte targeting using molecular modelling
author Raposo, Cláudia D.
author_facet Raposo, Cláudia D.
Costa, Rita
Petrova, Krasimira T.
Brito, Catarina
Scotti, Marcus T.
Cardoso, M. Margarida
author_role author
author2 Costa, Rita
Petrova, Krasimira T.
Brito, Catarina
Scotti, Marcus T.
Cardoso, M. Margarida
author2_role author
author
author
author
author
dc.contributor.none.fl_str_mv DQ - Departamento de Química
LAQV@REQUIMTE
Instituto de Tecnologia Química e Biológica António Xavier (ITQB)
RUN
dc.contributor.author.fl_str_mv Raposo, Cláudia D.
Costa, Rita
Petrova, Krasimira T.
Brito, Catarina
Scotti, Marcus T.
Cardoso, M. Margarida
dc.subject.por.fl_str_mv Doxorubicin delivery
Galactosylated nanoparticles
Hepatocyte targeting nanoparticles
Molecular modelling for drug targeting
Surface modified plga nanoparticles
Chemistry(all)
Polymers and Plastics
topic Doxorubicin delivery
Galactosylated nanoparticles
Hepatocyte targeting nanoparticles
Molecular modelling for drug targeting
Surface modified plga nanoparticles
Chemistry(all)
Polymers and Plastics
description FCT/MEC (UID/QUI/50006/2019). ERDF under the PT2020 Partnership Agreement (POCI-01-0145-FEDER-007265).
publishDate 2020
dc.date.none.fl_str_mv 2020-10-09T22:47:44Z
2020-01-04
2020-01-04T00:00:00Z
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://hdl.handle.net/10362/105365
url http://hdl.handle.net/10362/105365
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv 1618-7229
PURE: 17108233
https://doi.org/10.3390/polym12010094
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.source.none.fl_str_mv reponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
instacron:RCAAP
instname_str Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
instacron_str RCAAP
institution RCAAP
reponame_str Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
collection Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
repository.name.fl_str_mv Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
repository.mail.fl_str_mv
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