Development of a dry powder formulation for pulmonary delivery of azithromycin-loaded nanoparticles

Detalhes bibliográficos
Autor(a) principal: Sani, Alison Tatiana Madrid
Data de Publicação: 2024
Outros Autores: Rocha, Khellida Loiane V. Ramos, Sarcinelli, Michelle Alvares, Chaves, Marcelo Henrique da Cunha, Rocha, Helvécio Vinícius Antunes, Léo, Patrícia, Cerize, Natália Neto Pereira, Zanin, Maria Helena Ambrosio, Feitosa, Valker Araujo, Yagui, Carlota de Oliveira Rangel
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Institucional da FIOCRUZ (ARCA)
Texto Completo: https://arca.fiocruz.br/handle/icict/70554
Resumo: Wethank Dr. Danae Lopes Francisco for collaboration with MEVimagesandMSc.KellyCristina Manhani for the support in quantification analyses. We also grateful to pharmaceutical companies Laboratório Cristália (Brazil), Lipid Ingredients (Brazil), and DFE Pharma (Germany) for kindly providing azithromycin dehydrated, soybean lecithin S75, and lactose monohydrated LH206, respectively.
id CRUZ_acc4fc7cf4385f78e970d59f81ba1cd6
oai_identifier_str oai:arca.fiocruz.br:icict/70554
network_acronym_str CRUZ
network_name_str Repositório Institucional da FIOCRUZ (ARCA)
repository_id_str 2135
spelling Sani, Alison Tatiana MadridRocha, Khellida Loiane V. RamosSarcinelli, Michelle AlvaresChaves, Marcelo Henrique da CunhaRocha, Helvécio Vinícius AntunesLéo, PatríciaCerize, Natália Neto PereiraZanin, Maria Helena AmbrosioFeitosa, Valker AraujoYagui, Carlota de Oliveira Rangel2025-05-22T15:43:11Z2025-05-22T15:43:11Z2024SANI, Alison Tatiana Madrid et al. Development of a dry powder formulation for pulmonary delivery of azithromycin-loaded nanoparticles. Journal of Pharmacy & Pharmaceutical Sciences. v.14, n. 27, p.1-15, 2024.1482-1826https://arca.fiocruz.br/handle/icict/70554Wethank Dr. Danae Lopes Francisco for collaboration with MEVimagesandMSc.KellyCristina Manhani for the support in quantification analyses. We also grateful to pharmaceutical companies Laboratório Cristália (Brazil), Lipid Ingredients (Brazil), and DFE Pharma (Germany) for kindly providing azithromycin dehydrated, soybean lecithin S75, and lactose monohydrated LH206, respectively.TheCOVID-19pandemichasraisedconcernregardingrespiratory systemdiseases and oral inhalation stands out as an attractive non-invasive route of administration for pulmonary diseases such as chronic bronchitis, cystic fibrosis, COVID-19 and community-acquiredpneumonia.Inthiscontext,weencapsulatedazithromycin in polycaprolactone nanoparticles functionalized with phospholipids rich in dipalmitoylphosphatidylcholine and further produced a fine powder formulation by spray drying with monohydrated lactose. Nanoparticles obtained by the emulsion/solvent diffusion-evaporation technique exhibited a mean hydrodynamic diameter around 195–228 nm with a narrow monomodal size distribution (PdI < 0.2). Nanoparticle dispersions were spray-dried at different inlet temperatures, atomizing air-flow,aspirator air flow,andfeedrate,using lactoseasa drying aid, resulting in a maximal process yield of 63% and an encapsulation efficiency of 83%. Excipients and the dry powder formulations were characterized in terms of morphology, chemical structure, thermal analyses and particle size by SEM, FTIR, DSC/TGA and laser light diffraction. The results indicated spherical particles with 90% at 4.06 µm or below, an adequate size for pulmonary delivery. Aerosolization performance in a NGI confirmed good aerodynamic properties. Microbiological assays showed that the formulation preserves AZM antimicrobial effect against Staphylococcus aureus and Streptococcus pneumoniae strains, with halos above 18 mm. In addition, no formulation-related cytotoxicity was observed against the human cell lines BEAS-2B (lung epithelial), HUVEC (endothelial) and HFF1 (fibroblasts). Overall, the approach described here allows the production of AZM-PCL nanoparticles incorporated into inhalable microparticles, enabling more efficient pulmonary therapy of lung infections.The author(s) declare that financial support was received for the research, authorship, and/or publication of this article. The authors declare that this study received support from Laboratório Cristália (Brazil), Lipid Ingredients (Brazil), and DFE Pharma (Germany). The companies were not involved in the study design, collection, analysis, interpretation of data, the writing of this article or the decision to submit it for publication. Financial support from CAPES (88887.506666/ 2020-00) is greatly acknowledged.Technological Research Institute. Bionanomanufacturing Center. São Paulo, SP, Brasil / University of São Paulo. Department of Biochemical and Pharmaceutical Technology. SãoPaulo, SP, Brasil.Technological Research Institute. Bionanomanufacturing Center. São Paulo, SP, Brasil / University of São Paulo. Department of Biochemical and Pharmaceutical Technology. SãoPaulo, SP, Brasil.Fundação Oswaldo Cruz. Farmanguinhos . Laboratório de Micro e Nanotecnologia. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Farmanguinhos . Laboratório de Micro e Nanotecnologia. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Farmanguinhos . Laboratório de Micro e Nanotecnologia. Rio de Janeiro, RJ, Brasil.Technological Research Institute. Bionanomanufacturing Center. São Paulo, SP, Brasil.Technological Research Institute. Bionanomanufacturing Center. São Paulo, SP, Brasil.Technological Research Institute. Bionanomanufacturing Center. São Paulo, SP, Brasil.University of São Paulo. Department of Biochemical and Pharmaceutical Technology. SãoPaulo, SP, Brasil.University of São Paulo. Department of Biochemical and Pharmaceutical Technology. SãoPaulo, SP, Brasil.engCSPSDevelopment of a dry powder formulation for pulmonary delivery of azithromycin-loaded nanoparticlesinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleSpray-dryingPolycaprolactoneAzithromycinDry powder inhalerPulmonary diseasesCOVID-19Secagem por AtomizaçãoAzitromicinaInaladores de Pó SecoPneumopatiasCOVID-19info:eu-repo/semantics/openAccessreponame:Repositório Institucional da FIOCRUZ (ARCA)instname:Fundação Oswaldo Cruz (FIOCRUZ)instacron:FIOCRUZLICENSElicense.txtlicense.txttext/plain; charset=utf-82991https://arca.fiocruz.br/bitstreams/cd285443-97da-4eb9-bc3c-e49b0bec921c/download5a560609d32a3863062d77ff32785d58MD51falseAnonymousREADORIGINALve_Alison_Sani_et al_Presidencia_2024.pdfve_Alison_Sani_et al_Presidencia_2024.pdfapplication/pdf2453493https://arca.fiocruz.br/bitstreams/6c5456f5-5027-4ff0-b412-cc8354aa0201/downloadd893546bf0100f8326df576a376af696MD52trueAnonymousREADTHUMBNAILcapa_development_dry_powder.jpgcapa_development_dry_powder.jpgimage/jpeg81615https://arca.fiocruz.br/bitstreams/336e844c-ecea-4984-9d6a-daf51fb24cf8/download82e6089727b1fc6be146626bc9e32694MD53falseAnonymousREADve_Alison_Sani_et al_Presidencia_2024.pdf.jpgve_Alison_Sani_et al_Presidencia_2024.pdf.jpgGenerated Thumbnailimage/jpeg4881https://arca.fiocruz.br/bitstreams/835e80ba-2dbf-485e-a461-6016649d492c/download2dcf79b8d9e5e161c8a249def40250a0MD59falseAnonymousREADTEXTve_Alison_Sani_et al_Presidencia_2024.pdf.txtve_Alison_Sani_et al_Presidencia_2024.pdf.txtExtracted texttext/plain71635https://arca.fiocruz.br/bitstreams/117aeabb-14e1-43f8-b68c-08f750ef073c/download40522f0774e7f1fa0e5a0be5b3952834MD58falseAnonymousREADicict/705542025-07-29 19:56:20.678open.accessoai:arca.fiocruz.br:icict/70554https://arca.fiocruz.brRepositório InstitucionalPUBhttps://www.arca.fiocruz.br/oai/requestrepositorio.arca@fiocruz.bropendoar:21352025-07-29T22:56:20Repositório Institucional da FIOCRUZ (ARCA) - Fundação Oswaldo Cruz (FIOCRUZ)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
dc.title.none.fl_str_mv Development of a dry powder formulation for pulmonary delivery of azithromycin-loaded nanoparticles
title Development of a dry powder formulation for pulmonary delivery of azithromycin-loaded nanoparticles
spellingShingle Development of a dry powder formulation for pulmonary delivery of azithromycin-loaded nanoparticles
Sani, Alison Tatiana Madrid
Spray-drying
Polycaprolactone
Azithromycin
Dry powder inhaler
Pulmonary diseases
COVID-19
Secagem por Atomização
Azitromicina
Inaladores de Pó Seco
Pneumopatias
COVID-19
title_short Development of a dry powder formulation for pulmonary delivery of azithromycin-loaded nanoparticles
title_full Development of a dry powder formulation for pulmonary delivery of azithromycin-loaded nanoparticles
title_fullStr Development of a dry powder formulation for pulmonary delivery of azithromycin-loaded nanoparticles
title_full_unstemmed Development of a dry powder formulation for pulmonary delivery of azithromycin-loaded nanoparticles
title_sort Development of a dry powder formulation for pulmonary delivery of azithromycin-loaded nanoparticles
author Sani, Alison Tatiana Madrid
author_facet Sani, Alison Tatiana Madrid
Rocha, Khellida Loiane V. Ramos
Sarcinelli, Michelle Alvares
Chaves, Marcelo Henrique da Cunha
Rocha, Helvécio Vinícius Antunes
Léo, Patrícia
Cerize, Natália Neto Pereira
Zanin, Maria Helena Ambrosio
Feitosa, Valker Araujo
Yagui, Carlota de Oliveira Rangel
author_role author
author2 Rocha, Khellida Loiane V. Ramos
Sarcinelli, Michelle Alvares
Chaves, Marcelo Henrique da Cunha
Rocha, Helvécio Vinícius Antunes
Léo, Patrícia
Cerize, Natália Neto Pereira
Zanin, Maria Helena Ambrosio
Feitosa, Valker Araujo
Yagui, Carlota de Oliveira Rangel
author2_role author
author
author
author
author
author
author
author
author
dc.contributor.author.fl_str_mv Sani, Alison Tatiana Madrid
Rocha, Khellida Loiane V. Ramos
Sarcinelli, Michelle Alvares
Chaves, Marcelo Henrique da Cunha
Rocha, Helvécio Vinícius Antunes
Léo, Patrícia
Cerize, Natália Neto Pereira
Zanin, Maria Helena Ambrosio
Feitosa, Valker Araujo
Yagui, Carlota de Oliveira Rangel
dc.subject.en.none.fl_str_mv Spray-drying
Polycaprolactone
Azithromycin
Dry powder inhaler
Pulmonary diseases
COVID-19
topic Spray-drying
Polycaprolactone
Azithromycin
Dry powder inhaler
Pulmonary diseases
COVID-19
Secagem por Atomização
Azitromicina
Inaladores de Pó Seco
Pneumopatias
COVID-19
dc.subject.decs.none.fl_str_mv Secagem por Atomização
Azitromicina
Inaladores de Pó Seco
Pneumopatias
COVID-19
description Wethank Dr. Danae Lopes Francisco for collaboration with MEVimagesandMSc.KellyCristina Manhani for the support in quantification analyses. We also grateful to pharmaceutical companies Laboratório Cristália (Brazil), Lipid Ingredients (Brazil), and DFE Pharma (Germany) for kindly providing azithromycin dehydrated, soybean lecithin S75, and lactose monohydrated LH206, respectively.
publishDate 2024
dc.date.issued.fl_str_mv 2024
dc.date.accessioned.fl_str_mv 2025-05-22T15:43:11Z
dc.date.available.fl_str_mv 2025-05-22T15:43:11Z
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.citation.fl_str_mv SANI, Alison Tatiana Madrid et al. Development of a dry powder formulation for pulmonary delivery of azithromycin-loaded nanoparticles. Journal of Pharmacy & Pharmaceutical Sciences. v.14, n. 27, p.1-15, 2024.
dc.identifier.uri.fl_str_mv https://arca.fiocruz.br/handle/icict/70554
dc.identifier.issn.none.fl_str_mv 1482-1826
identifier_str_mv SANI, Alison Tatiana Madrid et al. Development of a dry powder formulation for pulmonary delivery of azithromycin-loaded nanoparticles. Journal of Pharmacy & Pharmaceutical Sciences. v.14, n. 27, p.1-15, 2024.
1482-1826
url https://arca.fiocruz.br/handle/icict/70554
dc.language.iso.fl_str_mv eng
language eng
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.publisher.none.fl_str_mv CSPS
publisher.none.fl_str_mv CSPS
dc.source.none.fl_str_mv reponame:Repositório Institucional da FIOCRUZ (ARCA)
instname:Fundação Oswaldo Cruz (FIOCRUZ)
instacron:FIOCRUZ
instname_str Fundação Oswaldo Cruz (FIOCRUZ)
instacron_str FIOCRUZ
institution FIOCRUZ
reponame_str Repositório Institucional da FIOCRUZ (ARCA)
collection Repositório Institucional da FIOCRUZ (ARCA)
bitstream.url.fl_str_mv https://arca.fiocruz.br/bitstreams/cd285443-97da-4eb9-bc3c-e49b0bec921c/download
https://arca.fiocruz.br/bitstreams/6c5456f5-5027-4ff0-b412-cc8354aa0201/download
https://arca.fiocruz.br/bitstreams/336e844c-ecea-4984-9d6a-daf51fb24cf8/download
https://arca.fiocruz.br/bitstreams/835e80ba-2dbf-485e-a461-6016649d492c/download
https://arca.fiocruz.br/bitstreams/117aeabb-14e1-43f8-b68c-08f750ef073c/download
bitstream.checksum.fl_str_mv 5a560609d32a3863062d77ff32785d58
d893546bf0100f8326df576a376af696
82e6089727b1fc6be146626bc9e32694
2dcf79b8d9e5e161c8a249def40250a0
40522f0774e7f1fa0e5a0be5b3952834
bitstream.checksumAlgorithm.fl_str_mv MD5
MD5
MD5
MD5
MD5
repository.name.fl_str_mv Repositório Institucional da FIOCRUZ (ARCA) - Fundação Oswaldo Cruz (FIOCRUZ)
repository.mail.fl_str_mv repositorio.arca@fiocruz.br
_version_ 1839715939806871552