Preclinical Development and In Vivo Efficacy of Ceftiofur-PLGA Microparticles.

Drug delivery systems based on polymeric microparticles represent an interesting field of development for the treatment of several infectious diseases for humans and animals. In this work, we developed PLGA microparticles loaded with ceftiofur (PLGA-cef), a third- generation cephalosporin that is us...

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Main Authors: Cristian Vilos, Luis A Velasquez, Paula I Rodas, Katherine Zepeda, Soung-Jae Bong, Natalia Herrera, Mario Cantin, Felipe Simon, Luis Constandil
Format: Article
Language:English
Published: Public Library of Science (PLoS) 2015-01-01
Series:PLoS ONE
Online Access:http://europepmc.org/articles/PMC4410948?pdf=render
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author Cristian Vilos
Luis A Velasquez
Paula I Rodas
Katherine Zepeda
Soung-Jae Bong
Natalia Herrera
Mario Cantin
Felipe Simon
Luis Constandil
author_facet Cristian Vilos
Luis A Velasquez
Paula I Rodas
Katherine Zepeda
Soung-Jae Bong
Natalia Herrera
Mario Cantin
Felipe Simon
Luis Constandil
author_sort Cristian Vilos
collection DOAJ
description Drug delivery systems based on polymeric microparticles represent an interesting field of development for the treatment of several infectious diseases for humans and animals. In this work, we developed PLGA microparticles loaded with ceftiofur (PLGA-cef), a third- generation cephalosporin that is used exclusively used in animals. PLGA-cef was prepared by the double emulsion w/o/w method, and exhibited a diameter in the range of 1.5-2.2 μm, and a negative ζ potential in the range of -35 to -55 mV. The loading yield of PLGA-cef was ~7% and encapsulation efficiency was approximately 40%. The pharmacokinetic study demonstrated a sustained release profile of ceftiofur for 20 days. PLGA-cef administrated in a single dose was more effective than ceftiofur non-encapsulated in rats challenged with S. Typhimurium. The in vivo toxicological evaluation showed that PLGA-cef did not affect the blood biochemical, hematological and hemostasis parameters. Overall, the PLGA-cef showed slow in vivo release profile, high antibacterial efficacy, and low toxicity. The results obtained supports the safe application of PLGA-cef as sustained release platform in the veterinary industry.
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spelling doaj.art-3b7551b90d394039a9a5dc745bc990392022-12-22T00:45:30ZengPublic Library of Science (PLoS)PLoS ONE1932-62032015-01-01104e012333510.1371/journal.pone.0123335Preclinical Development and In Vivo Efficacy of Ceftiofur-PLGA Microparticles.Cristian VilosLuis A VelasquezPaula I RodasKatherine ZepedaSoung-Jae BongNatalia HerreraMario CantinFelipe SimonLuis ConstandilDrug delivery systems based on polymeric microparticles represent an interesting field of development for the treatment of several infectious diseases for humans and animals. In this work, we developed PLGA microparticles loaded with ceftiofur (PLGA-cef), a third- generation cephalosporin that is used exclusively used in animals. PLGA-cef was prepared by the double emulsion w/o/w method, and exhibited a diameter in the range of 1.5-2.2 μm, and a negative ζ potential in the range of -35 to -55 mV. The loading yield of PLGA-cef was ~7% and encapsulation efficiency was approximately 40%. The pharmacokinetic study demonstrated a sustained release profile of ceftiofur for 20 days. PLGA-cef administrated in a single dose was more effective than ceftiofur non-encapsulated in rats challenged with S. Typhimurium. The in vivo toxicological evaluation showed that PLGA-cef did not affect the blood biochemical, hematological and hemostasis parameters. Overall, the PLGA-cef showed slow in vivo release profile, high antibacterial efficacy, and low toxicity. The results obtained supports the safe application of PLGA-cef as sustained release platform in the veterinary industry.http://europepmc.org/articles/PMC4410948?pdf=render
spellingShingle Cristian Vilos
Luis A Velasquez
Paula I Rodas
Katherine Zepeda
Soung-Jae Bong
Natalia Herrera
Mario Cantin
Felipe Simon
Luis Constandil
Preclinical Development and In Vivo Efficacy of Ceftiofur-PLGA Microparticles.
PLoS ONE
title Preclinical Development and In Vivo Efficacy of Ceftiofur-PLGA Microparticles.
title_full Preclinical Development and In Vivo Efficacy of Ceftiofur-PLGA Microparticles.
title_fullStr Preclinical Development and In Vivo Efficacy of Ceftiofur-PLGA Microparticles.
title_full_unstemmed Preclinical Development and In Vivo Efficacy of Ceftiofur-PLGA Microparticles.
title_short Preclinical Development and In Vivo Efficacy of Ceftiofur-PLGA Microparticles.
title_sort preclinical development and in vivo efficacy of ceftiofur plga microparticles
url http://europepmc.org/articles/PMC4410948?pdf=render
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