A Stepwise Framework for the Systematic Development of Lipid Nanoparticles
Autor(a) principal: | |
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Data de Publicação: | 2022 |
Outros Autores: | , , , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
Texto Completo: | http://hdl.handle.net/10316/103195 https://doi.org/10.3390/biom12020223 |
Resumo: | A properly designed nanosystem aims to deliver an optimized concentration of the active pharmaceutical ingredient (API) at the site of action, resulting in a therapeutic response with reduced adverse effects. Due to the vast availability of lipids and surfactants, producing stable lipid dispersions is a double-edged sword: on the one hand, the versatility of composition allows for a refined design and tuning of properties; on the other hand, the complexity of the materials and their physical interactions often result in laborious and time-consuming pre-formulation studies. However, how can they be tailored, and which premises are required for a "right at first time" development? Here, a stepwise framework encompassing the sequential stages of nanoparticle production for disulfiram delivery is presented. Drug in lipid solubility analysis leads to the selection of the most suitable liquid lipids. As for the solid lipid, drug partitioning studies point out the lipids with increased capacity for solubilizing and entrapping disulfiram. The microscopical evaluation of the physical compatibility between liquid and solid lipids further indicates the most promising core compositions. The impact of the outer surfactant layer on the colloidal properties of the nanosystems is evaluated recurring to machine learning algorithms, in particular, hierarchical clustering, principal component analysis, and partial least squares regression. Overall, this work represents a comprehensive systematic approach to nanoparticle formulation studies that serves as a basis for selecting the most suitable excipients that comprise solid lipid nanoparticles and nanostructured lipid carriers. |
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A Stepwise Framework for the Systematic Development of Lipid Nanoparticlesdrug formulationlipid nanoparticlesmultivariate analysisNLCsscreeningSLNsLipidsLiposomesParticle SizeDrug CarriersNanoparticlesA properly designed nanosystem aims to deliver an optimized concentration of the active pharmaceutical ingredient (API) at the site of action, resulting in a therapeutic response with reduced adverse effects. Due to the vast availability of lipids and surfactants, producing stable lipid dispersions is a double-edged sword: on the one hand, the versatility of composition allows for a refined design and tuning of properties; on the other hand, the complexity of the materials and their physical interactions often result in laborious and time-consuming pre-formulation studies. However, how can they be tailored, and which premises are required for a "right at first time" development? Here, a stepwise framework encompassing the sequential stages of nanoparticle production for disulfiram delivery is presented. Drug in lipid solubility analysis leads to the selection of the most suitable liquid lipids. As for the solid lipid, drug partitioning studies point out the lipids with increased capacity for solubilizing and entrapping disulfiram. The microscopical evaluation of the physical compatibility between liquid and solid lipids further indicates the most promising core compositions. The impact of the outer surfactant layer on the colloidal properties of the nanosystems is evaluated recurring to machine learning algorithms, in particular, hierarchical clustering, principal component analysis, and partial least squares regression. Overall, this work represents a comprehensive systematic approach to nanoparticle formulation studies that serves as a basis for selecting the most suitable excipients that comprise solid lipid nanoparticles and nanostructured lipid carriers.2022info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articlehttp://hdl.handle.net/10316/103195http://hdl.handle.net/10316/103195https://doi.org/10.3390/biom12020223eng2218-273XBasso, JoãoMendes, MariaCova, TâniaSousa, JoãoPais, AlbertoFortuna, AnaVitorino, RuiVitorino, Carlainfo: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:RCAAP2022-10-20T20:31:47Zoai:estudogeral.uc.pt:10316/103195Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-19T21:20:04.288887Repositório 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 |
A Stepwise Framework for the Systematic Development of Lipid Nanoparticles |
title |
A Stepwise Framework for the Systematic Development of Lipid Nanoparticles |
spellingShingle |
A Stepwise Framework for the Systematic Development of Lipid Nanoparticles Basso, João drug formulation lipid nanoparticles multivariate analysis NLCs screening SLNs Lipids Liposomes Particle Size Drug Carriers Nanoparticles |
title_short |
A Stepwise Framework for the Systematic Development of Lipid Nanoparticles |
title_full |
A Stepwise Framework for the Systematic Development of Lipid Nanoparticles |
title_fullStr |
A Stepwise Framework for the Systematic Development of Lipid Nanoparticles |
title_full_unstemmed |
A Stepwise Framework for the Systematic Development of Lipid Nanoparticles |
title_sort |
A Stepwise Framework for the Systematic Development of Lipid Nanoparticles |
author |
Basso, João |
author_facet |
Basso, João Mendes, Maria Cova, Tânia Sousa, João Pais, Alberto Fortuna, Ana Vitorino, Rui Vitorino, Carla |
author_role |
author |
author2 |
Mendes, Maria Cova, Tânia Sousa, João Pais, Alberto Fortuna, Ana Vitorino, Rui Vitorino, Carla |
author2_role |
author author author author author author author |
dc.contributor.author.fl_str_mv |
Basso, João Mendes, Maria Cova, Tânia Sousa, João Pais, Alberto Fortuna, Ana Vitorino, Rui Vitorino, Carla |
dc.subject.por.fl_str_mv |
drug formulation lipid nanoparticles multivariate analysis NLCs screening SLNs Lipids Liposomes Particle Size Drug Carriers Nanoparticles |
topic |
drug formulation lipid nanoparticles multivariate analysis NLCs screening SLNs Lipids Liposomes Particle Size Drug Carriers Nanoparticles |
description |
A properly designed nanosystem aims to deliver an optimized concentration of the active pharmaceutical ingredient (API) at the site of action, resulting in a therapeutic response with reduced adverse effects. Due to the vast availability of lipids and surfactants, producing stable lipid dispersions is a double-edged sword: on the one hand, the versatility of composition allows for a refined design and tuning of properties; on the other hand, the complexity of the materials and their physical interactions often result in laborious and time-consuming pre-formulation studies. However, how can they be tailored, and which premises are required for a "right at first time" development? Here, a stepwise framework encompassing the sequential stages of nanoparticle production for disulfiram delivery is presented. Drug in lipid solubility analysis leads to the selection of the most suitable liquid lipids. As for the solid lipid, drug partitioning studies point out the lipids with increased capacity for solubilizing and entrapping disulfiram. The microscopical evaluation of the physical compatibility between liquid and solid lipids further indicates the most promising core compositions. The impact of the outer surfactant layer on the colloidal properties of the nanosystems is evaluated recurring to machine learning algorithms, in particular, hierarchical clustering, principal component analysis, and partial least squares regression. Overall, this work represents a comprehensive systematic approach to nanoparticle formulation studies that serves as a basis for selecting the most suitable excipients that comprise solid lipid nanoparticles and nanostructured lipid carriers. |
publishDate |
2022 |
dc.date.none.fl_str_mv |
2022 |
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/10316/103195 http://hdl.handle.net/10316/103195 https://doi.org/10.3390/biom12020223 |
url |
http://hdl.handle.net/10316/103195 https://doi.org/10.3390/biom12020223 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
2218-273X |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
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 |
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Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação |
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RCAAP |
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RCAAP |
reponame_str |
Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
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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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1799134094450229248 |