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 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.
Center for Integrative Medicine and Innovative Science (CIMIS), Universidad Andres Bello, Facultad de Medicina, Santiago, Chile; Centro para el Desarrollo de la Nanociencia y Nanotecnología, (CEDENNA). Universidad de Santiago de Chile, Santiago, Chile.
Cristian
C
Vilos
Center for Integrative Medicine and Innovative Science (CIMIS), Universidad Andres Bello, Facultad de Medicina, Santiago, Chile; Centro para el Desarrollo de la Nanociencia y Nanotecnología, (CEDENNA). Universidad de Santiago de Chile, Santiago, Chile.
Luis A
LA
Velasquez
Center for Integrative Medicine and Innovative Science (CIMIS), Universidad Andres Bello, Facultad de Medicina, Santiago, Chile.
Paula I
PI
Rodas
Center for Integrative Medicine and Innovative Science (CIMIS), Universidad Andres Bello, Facultad de Medicina, Santiago, Chile.
Katherine
K
Zepeda
Center for Integrative Medicine and Innovative Science (CIMIS), Universidad Andres Bello, Facultad de Medicina, Santiago, Chile.
Soung-Jae
SJ
Bong
Center for Integrative Medicine and Innovative Science (CIMIS), Universidad Andres Bello, Facultad de Medicina, Santiago, Chile.
Natalia
N
Herrera
CIMA, Department of Integral Dentistry, Faculty of Dentistry, Universidad de La Frontera, Temuco, Chile; Center of Research in Biomedical Sciences, Universidad Autónoma de Chile, Temuco, Chile.
Mario
M
Cantin
Laboratorio de Fisiopatología Integrativa, Departamento de Ciencias Biológicas, Facultad de Ciencias Biológicas and Facultad de Medicina, Universidad Andrés Bello, Santiago, Chile.
Felipe
F
Simon
Centro para el Desarrollo de la Nanociencia y Nanotecnología, (CEDENNA). Universidad de Santiago de Chile, Santiago, Chile; Laboratorio de Neurobiología, Departamento de Biología, Facultad de Química y Biología, Universidad de Santiago de Chile, Santiago, Chile.
Luis
L
Constandil
D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D002214:Capsules / Q000737:chemistry; D002511:Cephalosporins / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D004353:Drug Evaluation, Preclinical; D065546:Drug Liberation; D019344:Lactic Acid / Q000737:chemistry*; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D051381:Rats; D017207:Rats, Sprague-Dawley; D012480:Salmonella Infections / Q000188:drug therapy
D000900:Anti-Bacterial Agents; D002214:Capsules; D002511:Cephalosporins; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; C053503:ceftiofur