Levofloxacin in nanostructured lipid carriers: preformulation and critical process parameters for a highly incorporated formulation

Detalhes bibliográficos
Autor(a) principal: Araújo, Viviane Lucia Beraldo de
Data de Publicação: 2022
Outros Autores: Vicente, Ana Flávia Siqueira, Lima, Marcelo van Vliet, Umerska, Anita, Souto, Eliana Maria Barbosa, Tajber, Lidia, Nascimento, Laura de Oliveira
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
Texto Completo: https://hdl.handle.net/1822/79599
Resumo: Available online 13 September 2022
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spelling Levofloxacin in nanostructured lipid carriers: preformulation and critical process parameters for a highly incorporated formulationPreformulationDesign of experimentsLevofloxacinNanostructured lipid carrierSolid stateDegradationScience & TechnologyAvailable online 13 September 2022The first step of a successful nanoformulation development is preformulation studies, in which the best excipients, drug-excipient compatibility and interactions can be identified. During the formulation, the critical process parameters and their impact must be studied to establish the stable system with a high drug entrapment efficiency (EE). This work followed these steps to develop nanostructured lipid carriers (NLCs) to deliver the antibiotic levofloxacin (LV). The preformulation studies covered drug solubility in excipients and thorough characterization using thermal analysis, X-ray diffraction and spectroscopy. A design of experiment based on the process parameters identified nanoparticles with < 200 nm in size, polydispersity <=0.3, zeta potential -21 to -24 mV, high EE formulations (> 71%) and an acceptable level of LV degradation products (0.37-1.13%). To the best of our knowledge, this is the first time that a drug degradation is reported and studied in work on nanostructured lipids. LV impurities following the NLC production were detected, mainly levofloxacin N-oxide, a degradation product that has no antimicrobial activity and could interfere with LV quantification in spectrophotometric experiments. Also, the achievement of the highest EE in lipid nanoparticles than those described in the literature to date and the apparent protective action of NLC of entrapped-LV against degradation are important findings.This study was part-financed by the Coordenação de Aperfeiçoamento de Pessoal de Nível Superior - Brasil (CAPES) - Finance Code 001, CAPES-PrInt, Santander – Program of International Mobility number 31/2018 and Sao Paulo Research Foundation (FAPESP) grant numbers 2018/03666-3, 2019/09719-4 and 2020/08059-8. LT and AU acknowledge funding from Science Foundation Ireland, grants 15/CDA/3602 and 12/RC/2275_P2.info:eu-repo/semantics/publishedVersionElsevierUniversidade do MinhoAraújo, Viviane Lucia Beraldo deVicente, Ana Flávia SiqueiraLima, Marcelo van VlietUmerska, AnitaSouto, Eliana Maria BarbosaTajber, LidiaNascimento, Laura de Oliveira2022-10-152022-10-15T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleapplication/pdfhttps://hdl.handle.net/1822/79599engAraújo, Viviane; Vicente, Ana Flávia Siqueira; Lima, Marcelo van Vliet; Umerska, Anita; Souto, Eliana B.; Tajber, Lidia; Nascimento, Laura de Oliveira, Levofloxacin in nanostructured lipid carriers: preformulation and critical process parameters for a highly incorporated formulation. International Journal of Pharmaceutics, 626(122193), 20220378-517310.1016/j.ijpharm.2022.12219336108993122193http://www.elsevier.com/locate/issn/03785173info: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:RCAAP2023-07-21T12:50:07Zoai:repositorium.sdum.uminho.pt:1822/79599Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-19T19:48:46.355629Repositório 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 Levofloxacin in nanostructured lipid carriers: preformulation and critical process parameters for a highly incorporated formulation
title Levofloxacin in nanostructured lipid carriers: preformulation and critical process parameters for a highly incorporated formulation
spellingShingle Levofloxacin in nanostructured lipid carriers: preformulation and critical process parameters for a highly incorporated formulation
Araújo, Viviane Lucia Beraldo de
Preformulation
Design of experiments
Levofloxacin
Nanostructured lipid carrier
Solid state
Degradation
Science & Technology
title_short Levofloxacin in nanostructured lipid carriers: preformulation and critical process parameters for a highly incorporated formulation
title_full Levofloxacin in nanostructured lipid carriers: preformulation and critical process parameters for a highly incorporated formulation
title_fullStr Levofloxacin in nanostructured lipid carriers: preformulation and critical process parameters for a highly incorporated formulation
title_full_unstemmed Levofloxacin in nanostructured lipid carriers: preformulation and critical process parameters for a highly incorporated formulation
title_sort Levofloxacin in nanostructured lipid carriers: preformulation and critical process parameters for a highly incorporated formulation
author Araújo, Viviane Lucia Beraldo de
author_facet Araújo, Viviane Lucia Beraldo de
Vicente, Ana Flávia Siqueira
Lima, Marcelo van Vliet
Umerska, Anita
Souto, Eliana Maria Barbosa
Tajber, Lidia
Nascimento, Laura de Oliveira
author_role author
author2 Vicente, Ana Flávia Siqueira
Lima, Marcelo van Vliet
Umerska, Anita
Souto, Eliana Maria Barbosa
Tajber, Lidia
Nascimento, Laura de Oliveira
author2_role author
author
author
author
author
author
dc.contributor.none.fl_str_mv Universidade do Minho
dc.contributor.author.fl_str_mv Araújo, Viviane Lucia Beraldo de
Vicente, Ana Flávia Siqueira
Lima, Marcelo van Vliet
Umerska, Anita
Souto, Eliana Maria Barbosa
Tajber, Lidia
Nascimento, Laura de Oliveira
dc.subject.por.fl_str_mv Preformulation
Design of experiments
Levofloxacin
Nanostructured lipid carrier
Solid state
Degradation
Science & Technology
topic Preformulation
Design of experiments
Levofloxacin
Nanostructured lipid carrier
Solid state
Degradation
Science & Technology
description Available online 13 September 2022
publishDate 2022
dc.date.none.fl_str_mv 2022-10-15
2022-10-15T00:00:00Z
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/1822/79599
url https://hdl.handle.net/1822/79599
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv Araújo, Viviane; Vicente, Ana Flávia Siqueira; Lima, Marcelo van Vliet; Umerska, Anita; Souto, Eliana B.; Tajber, Lidia; Nascimento, Laura de Oliveira, Levofloxacin in nanostructured lipid carriers: preformulation and critical process parameters for a highly incorporated formulation. International Journal of Pharmaceutics, 626(122193), 2022
0378-5173
10.1016/j.ijpharm.2022.122193
36108993
122193
http://www.elsevier.com/locate/issn/03785173
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 Elsevier
publisher.none.fl_str_mv Elsevier
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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