Güncüm E, Bakırel T, Anlaş C, Ekici H, Işıklan N
Department of Pharmacology and Toxicology, Faculty of Veterinary Medicine, Kırıkkale University, Yahşihan, Kırıkkale, Turkey.
Department of Pharmacology and Toxicology, Faculty of Veterinary Medicine, Istanbul University, Avcılar, Istanbul, Turkey.
J Vet Pharmacol Ther. 2018 Aug;41(4):588-598. doi: 10.1111/jvp.12505. Epub 2018 Mar 31.
Amoxicillin is used in the treatment and prevention of a wide range of diseases in poultry breeding. However, its short half-life and low bioavailability restrict its clinical application in these species. Entrapment of drugs into polymeric nanoparticles (nps) presents a means to improve gastrointestinal absorption and oral bioavailability of drugs. This study was aimed to overcome limitation of amoxicillin use in poultry breeding. Amoxicillin was loaded into sodium alginate-polyvinyl alcohol (NaAlg-PVA) blend nps, and characterization of the prepared nps was performed. For pharmacokinetic study, commercial male broilers were used and comparative pharmacokinetics of free and nanoparticle form of amoxicillin were investigated. Twenty-one broilers were divided into three groups. All groups received 10 mg/kg drug. Blood samples were collected, and drug plasma concentrations were determined by HPLC. The results demonstrated that the particle size, zeta potential, encapsulation efficiency, and loading capacity of the nps were 513.96 ± 19.46 nm, -45.36 ± 1.35 mV, 43.66 ± 3.30, and 12.06 ± 0.83%, respectively. In vitro drug release exhibited a biphasic pattern with an initial burst release of 18% within 2 hr followed by a sustained release over 22 hr. The pharmacokinetic results showed that amoxicillin nps have higher bioavailability and longer plasma half-life (p < .01) than free amoxicillin. These results indicate that amoxicillin nano formulation is suitable for oral administration in broilers.
阿莫西林用于家禽养殖中多种疾病的治疗和预防。然而，其半衰期短和生物利用度低限制了它在这些物种中的临床应用。将药物包封于聚合物纳米颗粒（NPs）中是提高药物胃肠道吸收和口服生物利用度的一种方法。本研究旨在克服阿莫西林在家禽养殖应用中的局限性。将阿莫西林载入海藻酸钠-聚乙烯醇（NaAlg-PVA）混合纳米颗粒中，并对所制备的纳米颗粒进行表征。为进行药代动力学研究，使用了商品雄性肉鸡，并研究了游离和纳米颗粒形式阿莫西林的比较药代动力学。21只肉鸡被分为三组。所有组均接受10mg/kg药物。采集血样，并通过高效液相色谱法测定药物血浆浓度。结果表明，纳米颗粒的粒径、zeta电位、包封率和载药量分别为513.96±19.46nm、-45.36±1.35mV、43.66±3.30和12.06±0.83%。体外药物释放呈现双相模式，最初2小时内突发释放18%，随后在22小时内持续释放。药代动力学结果表明，阿莫西林纳米颗粒比游离阿莫西林具有更高的生物利用度和更长的血浆半衰期（p<0.01）。这些结果表明，阿莫西林纳米制剂适用于肉鸡口服给药。
