Development and characterization of ceftriaxone-loaded P3HB-based microparticles for drug delivery

Abstract

In this study, polymer-based microparticles are used to improve the therapeutic properties of ceftriaxone (CEF) and render them safer. Poly-3-hydroxybutyrate (P3HB) and poly-3-hydroxybutyrate/polyethylene glycol (P3HB-PEG)-based microparticles were prepared by two methods: a double emulsification technique and spray-drying. The microparticles were characterized in terms of size and zeta potential, morphology, total drug loading and drug release. The microparticles had spherical shapes with diameters of a size range from 0.74 to 1.55 µm (emulsification technique) and from 3.84 to 6.51 µm (spray-drying); CEF encapsulation efficiency was around 63% and 49% for these methods respectively. The CEF release from microparticles obtained by spray-drying reached 100% after 150 h, while for microparticles obtained by emulsification technique the total release of CEF did not exceed 34% after 312 h. The release profiles could be best explained by Zero order kinetics model, Higuchi and Korsmeyer-Peppas models, as the plots showed high linearity. Antibacterial activity of the microparticles was evaluated against gram-positive and gram-negative bacterial strains. In general, CEF encapsulation in polymeric microparticles preserves the therapeutic efficacy of the CEF and provides its prolonged effect.

Keywords:

• Ceftriaxone
• P3HB-microparticles
• emulsification technique
• spray-drying
• drug release
• microbiological evaluation

Acknowledgments

The authors would like to thank Ivan Nemtsev (Federal Research Center Krasnoyarsk Scientific Center of the Siberian Branch of the RAS) for their support with SEM.

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This work was supported by the state budget allocated to the fundamental research at the Russian Academy of Sciences: [Project no. AAAA-A17- 117013050028-8].