Optimization of rifapentine-loaded lipid nanoparticles using a Quality-by-Design strategy
Autor(a) principal: | |
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Data de Publicação: | 2020 |
Outros Autores: | , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
Texto Completo: | https://hdl.handle.net/10216/141458 |
Resumo: | This work aims to optimize and assess the potential use of lipid nanoparticles, namely nanostructured lipid carriers (NLCs), as drug delivery systems of rifapentine (RPT) for the treatment of tuberculosis (TB). A Box-Behnken design was used to increase drug encapsulation efficiency (EE) and loading capacity (LC) of RPT-loaded NLCs. The optimized nanoparticles were fully characterized, and their effect on cell viability was assessed. The quality-by-design approach allowed the optimization of RPT-loaded NLCs with improved EE and LC using the minimum of experiments. Analyses of variance were indicative of the validity of this model to optimize this nanodelivery system. The optimized NLCs had a mean diameter of 242 ± 9 nm, polydispersity index <0.2, and a highly negative zeta potential. EE values were higher than 80%, and differential scanning calorimetry analysis enabled the confirmation of the efficient encapsulation of RPT. Transmission electron microscopy analysis showed spherical nanoparticles, uniform in shape and diameter, with no visible aggregation. Stability studies indicated that NLCs were stable over time. No toxicity was observed in primary human macrophage viability for nanoparticles up to 1000 µg mL-1. Overall, the optimized NLCs are efficient carriers of RPT and should be considered for further testing as promising drug delivery systems to be used in TB treatment. |
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Optimization of rifapentine-loaded lipid nanoparticles using a Quality-by-Design strategyThis work aims to optimize and assess the potential use of lipid nanoparticles, namely nanostructured lipid carriers (NLCs), as drug delivery systems of rifapentine (RPT) for the treatment of tuberculosis (TB). A Box-Behnken design was used to increase drug encapsulation efficiency (EE) and loading capacity (LC) of RPT-loaded NLCs. The optimized nanoparticles were fully characterized, and their effect on cell viability was assessed. The quality-by-design approach allowed the optimization of RPT-loaded NLCs with improved EE and LC using the minimum of experiments. Analyses of variance were indicative of the validity of this model to optimize this nanodelivery system. The optimized NLCs had a mean diameter of 242 ± 9 nm, polydispersity index <0.2, and a highly negative zeta potential. EE values were higher than 80%, and differential scanning calorimetry analysis enabled the confirmation of the efficient encapsulation of RPT. Transmission electron microscopy analysis showed spherical nanoparticles, uniform in shape and diameter, with no visible aggregation. Stability studies indicated that NLCs were stable over time. No toxicity was observed in primary human macrophage viability for nanoparticles up to 1000 µg mL-1. Overall, the optimized NLCs are efficient carriers of RPT and should be considered for further testing as promising drug delivery systems to be used in TB treatment.MDPI20202020-01-01T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleapplication/pdfhttps://hdl.handle.net/10216/141458eng1999-492310.3390/pharmaceutics12010075Magalhães, JChaves, LLVieira, ACSantos, SGPinheiro, MReis, Sinfo: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:RCAAP2023-11-29T13:20:40Zoai:repositorio-aberto.up.pt:10216/141458Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-19T23:38:55.640564Repositório 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 |
Optimization of rifapentine-loaded lipid nanoparticles using a Quality-by-Design strategy |
title |
Optimization of rifapentine-loaded lipid nanoparticles using a Quality-by-Design strategy |
spellingShingle |
Optimization of rifapentine-loaded lipid nanoparticles using a Quality-by-Design strategy Magalhães, J |
title_short |
Optimization of rifapentine-loaded lipid nanoparticles using a Quality-by-Design strategy |
title_full |
Optimization of rifapentine-loaded lipid nanoparticles using a Quality-by-Design strategy |
title_fullStr |
Optimization of rifapentine-loaded lipid nanoparticles using a Quality-by-Design strategy |
title_full_unstemmed |
Optimization of rifapentine-loaded lipid nanoparticles using a Quality-by-Design strategy |
title_sort |
Optimization of rifapentine-loaded lipid nanoparticles using a Quality-by-Design strategy |
author |
Magalhães, J |
author_facet |
Magalhães, J Chaves, LL Vieira, AC Santos, SG Pinheiro, M Reis, S |
author_role |
author |
author2 |
Chaves, LL Vieira, AC Santos, SG Pinheiro, M Reis, S |
author2_role |
author author author author author |
dc.contributor.author.fl_str_mv |
Magalhães, J Chaves, LL Vieira, AC Santos, SG Pinheiro, M Reis, S |
description |
This work aims to optimize and assess the potential use of lipid nanoparticles, namely nanostructured lipid carriers (NLCs), as drug delivery systems of rifapentine (RPT) for the treatment of tuberculosis (TB). A Box-Behnken design was used to increase drug encapsulation efficiency (EE) and loading capacity (LC) of RPT-loaded NLCs. The optimized nanoparticles were fully characterized, and their effect on cell viability was assessed. The quality-by-design approach allowed the optimization of RPT-loaded NLCs with improved EE and LC using the minimum of experiments. Analyses of variance were indicative of the validity of this model to optimize this nanodelivery system. The optimized NLCs had a mean diameter of 242 ± 9 nm, polydispersity index <0.2, and a highly negative zeta potential. EE values were higher than 80%, and differential scanning calorimetry analysis enabled the confirmation of the efficient encapsulation of RPT. Transmission electron microscopy analysis showed spherical nanoparticles, uniform in shape and diameter, with no visible aggregation. Stability studies indicated that NLCs were stable over time. No toxicity was observed in primary human macrophage viability for nanoparticles up to 1000 µg mL-1. Overall, the optimized NLCs are efficient carriers of RPT and should be considered for further testing as promising drug delivery systems to be used in TB treatment. |
publishDate |
2020 |
dc.date.none.fl_str_mv |
2020 2020-01-01T00:00:00Z |
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 |
https://hdl.handle.net/10216/141458 |
url |
https://hdl.handle.net/10216/141458 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
1999-4923 10.3390/pharmaceutics12010075 |
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.publisher.none.fl_str_mv |
MDPI |
publisher.none.fl_str_mv |
MDPI |
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 |
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1799135703624318976 |