PEGylated ofloxacin nanoparticles render strong antibacterial activity against many clinically important human pathogens.
Autor(a) principal: | |
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Data de Publicação: | 2015 |
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/1822/40267 |
Resumo: | The rise of bacterial resistance against important drugs threatens their clinical utility. Fluoroquinones, one of the most important classes of contemporary antibiotics has also reported to suffer bacterial resistance. Since the general mechanism of bacterial resistance against fluoroquinone antibiotics (e.g. ofloxacin) consists of target mutations resulting in reduced membrane permeability and increased efflux by the bacteria, strategies that could increase bacterial uptake and reduce efflux of the drug would provide effective treatment. In the present study, we have compared the efficiencies of ofloxacin delivered in the form of free drug (OFX) and as nanoparticles on bacterial uptake and antibacterial activity. Although both poly(lactic-co-glycolic acid) (OFX-PLGA) and methoxy poly(ethylene glycol)-b-poly(lactic-co-glycolic acid) (OFX-mPEG-PLGA) nanoformulations presented improved bacterial uptake and antibacterial activity against all the tested human bacterial pathogens, namely, Escherichia coli, Proteus vulgaris, Salmonella typhimurium, Pseudomonas aeruginosa, Klebsiella pneumoniae and Staphylococcus aureus, OFX-mPEG-PLGA showed significantly higher bacterial uptake and antibacterial activity compared to OFX-PLGA. We have also found that mPEG-PLGA nanoencapsulation could significantly inhibit Bacillus subtilis resistance development against OFX. |
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PEGylated ofloxacin nanoparticles render strong antibacterial activity against many clinically important human pathogens.Antibiotic resistanceOfloxacinmPEG-PLGA diblock Co-polymerNanoparticlesAntibacterialBacterial uptakeCiências Médicas::Ciências da SaúdeScience & TechnologyThe rise of bacterial resistance against important drugs threatens their clinical utility. Fluoroquinones, one of the most important classes of contemporary antibiotics has also reported to suffer bacterial resistance. Since the general mechanism of bacterial resistance against fluoroquinone antibiotics (e.g. ofloxacin) consists of target mutations resulting in reduced membrane permeability and increased efflux by the bacteria, strategies that could increase bacterial uptake and reduce efflux of the drug would provide effective treatment. In the present study, we have compared the efficiencies of ofloxacin delivered in the form of free drug (OFX) and as nanoparticles on bacterial uptake and antibacterial activity. Although both poly(lactic-co-glycolic acid) (OFX-PLGA) and methoxy poly(ethylene glycol)-b-poly(lactic-co-glycolic acid) (OFX-mPEG-PLGA) nanoformulations presented improved bacterial uptake and antibacterial activity against all the tested human bacterial pathogens, namely, Escherichia coli, Proteus vulgaris, Salmonella typhimurium, Pseudomonas aeruginosa, Klebsiella pneumoniae and Staphylococcus aureus, OFX-mPEG-PLGA showed significantly higher bacterial uptake and antibacterial activity compared to OFX-PLGA. We have also found that mPEG-PLGA nanoencapsulation could significantly inhibit Bacillus subtilis resistance development against OFX.G.M and C.J.S were supported by FCT – Fundac¸ ão para a Ciên-cia e a Tecnologia, Portugal, grants SFRH/BD/72809/2010 and SFRH/BPD/89493/2012, respectively. The present work was alsosupported by the FCT projects PTDC/AGR-GPL/119211/2010 and UID/AGR/04033/2013.Elsevier Science BVUniversidade do MinhoMarslin, GregoryRevina, A. M.Khandelwal, V. K. M.Balakumar, K.Singh, Caroline Jeya Sheeba Daniel SunderFranklin, Gregory20152015-01-01T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleapplication/pdfhttp://hdl.handle.net/1822/40267engMarslin, G., Revina, A. M., Khandelwal, V. K. M., Balakumar, K., Sheeba, C. J., & Franklin, G. (2015). PEGylated ofloxacin nanoparticles render strong antibacterial activity against many clinically important human pathogens. Colloids and Surfaces B: Biointerfaces, 132, 62-70. doi: 10.1016/j.colsurfb.2015.04.0500927-776510.1016/j.colsurfb.2015.04.05026005932http://www.sciencedirect.com/science/article/pii/S0927776515002696info: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:RCAAP2023-07-21T12:26:50Zoai:repositorium.sdum.uminho.pt:1822/40267Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-19T19:21:19.395945Repositório 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 |
PEGylated ofloxacin nanoparticles render strong antibacterial activity against many clinically important human pathogens. |
title |
PEGylated ofloxacin nanoparticles render strong antibacterial activity against many clinically important human pathogens. |
spellingShingle |
PEGylated ofloxacin nanoparticles render strong antibacterial activity against many clinically important human pathogens. Marslin, Gregory Antibiotic resistance Ofloxacin mPEG-PLGA diblock Co-polymer Nanoparticles Antibacterial Bacterial uptake Ciências Médicas::Ciências da Saúde Science & Technology |
title_short |
PEGylated ofloxacin nanoparticles render strong antibacterial activity against many clinically important human pathogens. |
title_full |
PEGylated ofloxacin nanoparticles render strong antibacterial activity against many clinically important human pathogens. |
title_fullStr |
PEGylated ofloxacin nanoparticles render strong antibacterial activity against many clinically important human pathogens. |
title_full_unstemmed |
PEGylated ofloxacin nanoparticles render strong antibacterial activity against many clinically important human pathogens. |
title_sort |
PEGylated ofloxacin nanoparticles render strong antibacterial activity against many clinically important human pathogens. |
author |
Marslin, Gregory |
author_facet |
Marslin, Gregory Revina, A. M. Khandelwal, V. K. M. Balakumar, K. Singh, Caroline Jeya Sheeba Daniel Sunder Franklin, Gregory |
author_role |
author |
author2 |
Revina, A. M. Khandelwal, V. K. M. Balakumar, K. Singh, Caroline Jeya Sheeba Daniel Sunder Franklin, Gregory |
author2_role |
author author author author author |
dc.contributor.none.fl_str_mv |
Universidade do Minho |
dc.contributor.author.fl_str_mv |
Marslin, Gregory Revina, A. M. Khandelwal, V. K. M. Balakumar, K. Singh, Caroline Jeya Sheeba Daniel Sunder Franklin, Gregory |
dc.subject.por.fl_str_mv |
Antibiotic resistance Ofloxacin mPEG-PLGA diblock Co-polymer Nanoparticles Antibacterial Bacterial uptake Ciências Médicas::Ciências da Saúde Science & Technology |
topic |
Antibiotic resistance Ofloxacin mPEG-PLGA diblock Co-polymer Nanoparticles Antibacterial Bacterial uptake Ciências Médicas::Ciências da Saúde Science & Technology |
description |
The rise of bacterial resistance against important drugs threatens their clinical utility. Fluoroquinones, one of the most important classes of contemporary antibiotics has also reported to suffer bacterial resistance. Since the general mechanism of bacterial resistance against fluoroquinone antibiotics (e.g. ofloxacin) consists of target mutations resulting in reduced membrane permeability and increased efflux by the bacteria, strategies that could increase bacterial uptake and reduce efflux of the drug would provide effective treatment. In the present study, we have compared the efficiencies of ofloxacin delivered in the form of free drug (OFX) and as nanoparticles on bacterial uptake and antibacterial activity. Although both poly(lactic-co-glycolic acid) (OFX-PLGA) and methoxy poly(ethylene glycol)-b-poly(lactic-co-glycolic acid) (OFX-mPEG-PLGA) nanoformulations presented improved bacterial uptake and antibacterial activity against all the tested human bacterial pathogens, namely, Escherichia coli, Proteus vulgaris, Salmonella typhimurium, Pseudomonas aeruginosa, Klebsiella pneumoniae and Staphylococcus aureus, OFX-mPEG-PLGA showed significantly higher bacterial uptake and antibacterial activity compared to OFX-PLGA. We have also found that mPEG-PLGA nanoencapsulation could significantly inhibit Bacillus subtilis resistance development against OFX. |
publishDate |
2015 |
dc.date.none.fl_str_mv |
2015 2015-01-01T00:00:00Z |
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 |
http://hdl.handle.net/1822/40267 |
url |
http://hdl.handle.net/1822/40267 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
Marslin, G., Revina, A. M., Khandelwal, V. K. M., Balakumar, K., Sheeba, C. J., & Franklin, G. (2015). PEGylated ofloxacin nanoparticles render strong antibacterial activity against many clinically important human pathogens. Colloids and Surfaces B: Biointerfaces, 132, 62-70. doi: 10.1016/j.colsurfb.2015.04.050 0927-7765 10.1016/j.colsurfb.2015.04.050 26005932 http://www.sciencedirect.com/science/article/pii/S0927776515002696 |
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 Science BV |
publisher.none.fl_str_mv |
Elsevier Science BV |
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 |
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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1799132679687372800 |