INTEC (Universidad Nacional del Litoral - CONICET), 3450 Güemes, 3000, Santa Fe, Argentina.
INTEC (Universidad Nacional del Litoral - CONICET), 3450 Güemes, 3000, Santa Fe, Argentina.
Carbohydr Polym. 2020 Apr 15;234:115922. doi: 10.1016/j.carbpol.2020.115922. Epub 2020 Jan 31.
Ceftiofur is a third-generation cephalosporin approved to treat numerous infections in production animals. Its commercial formulations are administered daily due to the mean life time, leading to several inconveniences, like operative challenges and non-uniform plasma levels. The objective of this work was to microencapsulate ceftiofur in chitosan particles using spray drying technology to extend the delivery and consequently reduce the dosage frequency. The effect of formulation factors on particle features was studied using a multilevel factorial design. In addition, ceftiofur thermal stability was assayed by differential scanning calorimetry and microbiological assays. Finally, a pharmacokinetic model was developed to predict theoretical plasma concentration in goats. Results showed that ceftiofur thermal stability increased after microencapsulation, indicating a protective effect of chitosan particles. Besides, MIC, IC50 and inhibition halos against E. coli and S. aureus were similar than those of the commercial product. In addition, suitable plasma levels can be theoretically maintained in goats during 48 h with a single injection. These findings suggest that chitosan microparticles could be a good vehicle for ceftiofur administration.
头孢噻呋是一种第三代头孢菌素，被批准用于治疗生产动物的多种感染。由于其平均半衰期较长，其商业制剂需要每天给药，这导致了一些不便，如操作挑战和非均匀的血浆水平。本工作的目的是使用喷雾干燥技术将头孢噻呋微囊化到壳聚糖颗粒中，以延长其释放时间，从而减少给药频率。使用多级析因设计研究了制剂因素对颗粒特征的影响。此外，还通过差示扫描量热法和微生物测定法测定了头孢噻呋的热稳定性。最后，建立了一个药代动力学模型来预测山羊的理论血浆浓度。结果表明，头孢噻呋的热稳定性在微囊化后增加，表明壳聚糖颗粒具有保护作用。此外，MIC、IC50 和对大肠杆菌和金黄色葡萄球菌的抑制晕环与商业产品相似。此外，单次注射可在 48 小时内理论上维持山羊的合适血浆水平。这些发现表明壳聚糖微球可能是头孢噻呋给药的良好载体。
