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Evaluation of ceftiofur–PHBV microparticles in rats

机译:头孢噻呋–PHBV微粒在大鼠中的评估

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Abstract: Despite the high number of antibiotics used for the treatment of infectious disease in animals, the development of slow release formulations presents a significant challenge, particularly in using novel biomaterials with low cost. In this report, we studied the pharmacokinetics, toxicity, and therapeutic activity of ceftiofur–PHBV (ceftiofur–poly(3-hydroxybutyrate-co-3-hydroxyvalerate)) in rats. The pharmacokinetic study demonstrated a sustained release of ceftiofur into the bloodstream, with detectable levels over the minimum inhibitory concentration for at least 17 days after a single intramuscular injection of ceftiofur–PHBV (10 mg/kg weight). In addition, the toxicological evaluation of biochemical, hematological, and coagulation blood parameters at the therapeutic dose demonstrated the safety of ceftiofur–PHBV, with no adverse effects. In addition, ceftiofur–PHBV exhibited a therapeutic effect for a longer time period than the nonencapsulated ceftiofur in rats challenged with Salmonella Typhimurium. The slow release of ceftiofur from the ceftiofur–PHBV, its low toxicity in the blood parameters evaluated, and the efficacy in the rats infected with Salmonella Typhimurium make ceftiofur–PHBV a strong candidate for biotechnological applications in the veterinary industry.
机译:摘要:尽管用于治疗动物传染病的抗生素数量众多,但缓释制剂的开发仍是一项重大挑战,特别是在使用低成本的新型生物材料中。在本报告中,我们研究了头孢噻呋-PHBV(头孢噻呋-聚(3-羟基丁酸酯-co-3-羟基戊酸酯))的药代动力学,毒性和治疗活性。药代动力学研究表明头孢噻呋持续释放到血液中,单次肌注头孢噻呋–PHBV(10 mg / kg体重)后,在至少最小抑制浓度下可检测到的水平至少达到17天。此外,在治疗剂量下对生化,血液学和凝血血液参数的毒理学评估证明了头孢噻呋– PHBV的安全性,没有副作用。此外,在鼠伤寒沙门氏菌攻击的大鼠中,头孢噻呋–PHBV比未包封的头孢噻呋具有更长的治疗效果。头孢噻呋从头孢噻呋–PHBV中缓慢释放,其对血液参数的低毒性以及在鼠伤寒沙门氏菌感染的大鼠中的功效,使头孢噻呋–PHBV成为在兽药工业中生物技术应用的强大候选者。

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