Effect of crosslinking, additives and particle coating on ceftiofur delivery from chitosan microparticles

IGNACIO HELBLING; CARLOS BUSATTO; FEDERICO KARP; DIANA ESTENOZ; JULIO LUNA

CABA

Simposio; XIII Simposio Argentino de Polímeros - SAP 2019; 2019

Infectious diseases are a serious problem in animal breeding, causing yield reduction and large economic losses. Ceftiofur is widely used to treat numerous animal infections. Actual therapies for production animals require the dairy dosage of the drug dispersed in an oily vehicle during several days. Despite the proven efficacy of the treatment and the extended acceptance, practical complications appear when a large number of animals are handled. In addition, the indiscriminate use of antibiotics causes microbial resistance and harmful effects on the environment. Therefore, the development of new administration systems that overcome some or all of these drawbacks is highly desired.Microparticles prepared from biocompatible and biodegradable polymers appear as a promising delivery system for ceftiofur administration. They present several advantages, such as minimization of the number of required doses, reduction of adverse effects due to high concentrations, drug protection from degradation and/or inactivation, among others. Up to now, only batch processes (typically emulsion methods) have been used to prepare ceftiofur-loaded microparticles, resulting in relatively low encapsulation efficiencies. The spray drying technique is widely used in the pharmaceutical industry to transform liquid feed into dry solid powder in a one-step continuous process. This technique offers a valuable option to the multi-step, time-consuming conventional methods (solvent evaporation, coacervation, freeze-drying) and it is easy to scale up. On the other hand, chitosan is a biopolymer that exhibits interesting characteristics for microparticles preparation, such as biocompatibility, non-toxicity, antimicrobial activity and biodegradability.In this work, the preparation and characterization of ceftiofur-loaded chitosan microparticles by spray drying was investigated. Microparticles were characterized in terms of particle size and morphology, water content, encapsulation efficiency and drug release behaviour. The effect of drug load, crosslinking degree, incorporation of additives and particle coating on the in vitro release profiles were studied and compared with a commercial product.