Preparation and testing of cefquinome-loaded poly lactic-co-glycolic acid microspheres for lung targeting

Drug Deliv. 2017 Nov;24(1):745-751. doi: 10.1080/10717544.2017.1321058.

Abstract

The aim of this study was to prepare cefquinome-loaded poly lactic-co-glycolic acid (PLGA) microspheres and to evaluate their in vitro and in vivo characteristics. Microspheres were prepared using a spry drier and were characterized in terms of morphology, size, drug-loading coefficient, encapsulation ratio and in vitro release. The prepared microspheres were spherical with smooth surfaces and uniform size (12.4 ± 1.2 μm). The encapsulation efficiency and drug loading of cefquinome was 91.6 ± 2.6 and 18.3 ± 1.3%, respectively. In vitro release of cefquinome from the microspheres was sustained for 36 h. In vivo studies identified the lung as the target tissue and the region of maximum cefquinome release. A partial lung inflammation was observed but disappeared spontaneously as the microspheres were removed through in vivo decay. The sustained cefquinome release from the microspheres revealed its applicability as a drug delivery system that minimized exposure to healthy tissues while increasing the accumulation of therapeutic drug at the target site. These results indicated that the spray-drying method of loading cefquinome into PLGA microspheres is a straightforward method for lung targeting in animals.

Keywords: Cefquinome; in vivo; poly lactic-co-glycolic acid microspheres; sustained release; target.

MeSH terms

  • Animals
  • Cephalosporins
  • Glycols
  • Lactic Acid
  • Lung
  • Microspheres*
  • Particle Size
  • Polyglycolic Acid
  • Polylactic Acid-Polyglycolic Acid Copolymer

Substances

  • Cephalosporins
  • Glycols
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polyglycolic Acid
  • Lactic Acid
  • cefquinome