Preparation and characterization of lung-targeting ceftiofur-loaded gelatin microspheres.

Abstract

BACKGROUND:

Ceftiofur is an effective antibiotic against respiratory infections in livestock. However, ceftiofur concentration that is found in lungs after intravenous injection is not effective. Fortunately, ceftiofur-loaded gelatin microsphere (Cef-MS) enjoys advantages of lung-targeting and can achieve an effective concentration. However, no study has been reported on this modality of drug delivery.

OBJECTIVE:

We investigated the properties of this delivery modality--lung targeting ceftiofur-Cef-MSs.

METHODS:

We prepared Cef-MS and investigated drug loading, stability and release characteristics in vitro and studied tissue distribution patterns and potential lung injury in mice.

RESULTS:

Results showed that the average size and span value are 21.26 μm and 1.07, respectively. Drug loading and loading efficiency were 15.31 and 76.55%, respectively. Cef-MSs were stable in light, heat and humidity, except that agglutinative phenomenon was observed in 90% humidity after 10 days. Cef-MS presented a slower in vitro release pattern compared to ceftiofur. Cef-MS mainly concentrates in lungs after intravenous administration. Furthermore, histopathological studies showed that Cef-MS only induces mild and reversible lung injury and is biologically safe.

CONCLUSION:

Cef-MS is a promising alternative form with high lung-targeting properties for the treatment of respiratory infections.

• Authors: Zhihui Hao, Baohan Qu, Yanling Wang, Shusheng Tang, Gang Wang, Mei Qiu, Ruili Zhang, Yuanyuan Liu, Xilong Xiao
• Journal: Drug development and industrial pharmacy (Drug Dev Ind Pharm) Vol. 37 Issue 12 Pg. 1422-8 (Dec 2011) ISSN: 1520-5762 [Electronic] England
• PMID: 21635137 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Anti-Bacterial Agents
• Cephalosporins
• Drug Carriers
• ceftiofur
• Gelatin

Topics

• Animals
• Anti-Bacterial Agents (administration & dosage, chemistry, pharmacokinetics)
• Cephalosporins (administration & dosage, chemistry, pharmacokinetics)
• Drug Carriers (administration & dosage, chemistry, pharmacokinetics)
• Drug Delivery Systems (methods)
• Female
• Gelatin (administration & dosage, chemistry, pharmacokinetics)
• Injections, Intravenous
• Lung (drug effects)
• Male
• Mice
• Microspheres
• Models, Animal
• Particle Size