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 hours, while for microparticles obtained by emulsification technique the total release of CEF did not exceed 34% after 312 hours. 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.