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首页> 外文期刊>RSC Advances >Dual-sensitive chitosan derivative micelles for site-specific drug release in the treatment of chicken coccidiosis
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Dual-sensitive chitosan derivative micelles for site-specific drug release in the treatment of chicken coccidiosis

机译：双敏感性壳聚糖衍生物胶束可用于定点释放药物，用于治疗球虫病

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Coccidiosis is a widespread and economic disease that deteriorates the growth of infected animals and largely affects our food safety. It has been proved that chitosan and its derivatives could offer outstanding antibacterial and hemostatic capabilities and help increase weight gain in the breeding of poultry. Herein, we put forward a novel strategy for the development of anti-coccidiosis drug formulations, aiming to synthesize 3-carboxyphenylboronic acid (CPBA) modified chitosan (CS) conjugates which could be self-assembled into polymeric micelles together with diclazuril (DIC), a poorly water-soluble coccidiostat drug, for site-specific drug release in the treatment of animal coccidiosis. The CPBA-modified micelles possessed specific glucose and pH dual-responsive capacity. The cumulative release of DIC reached the maximum of 85.0% at pH 6.8 and 50 mM glucose, while only 44.2% at pH 2.0 and no glucose, which allows drug to be released in the intestinal tract with neutral pH and glucose existence. ~(1) H NMR and FTIR confirmed the successful synthesis of amphiphilic polymer; and the optimized DIC-loaded CS–CPBA micelles (DIC/CS–CPBA) shared nanoscale particle size of (118.9 ± 1.1) nm, drug loading of 8.97% and spherical shape. The pharmacokinetic results indicated that the AUC value of DIC/CS–CPBA micelles was 1.7 times than that of drug suspensions. The anti-coccidial efficacy demonstrated that DIC/CS–CPBA micelles improved the anticoccidial efficacy in vivo and reduced intestinal damage. These results indicated that phenylboronic acid-conjugated chitosan micelles provided a promising platform for specific-targeted drug release in the intestinal tract for the treatment of coccidiosis.
机译：球虫病是一种广泛的经济疾病，它使受感染动物的生长恶化，并在很大程度上影响我们的食品安全。事实证明，壳聚糖及其衍生物可以提供出色的抗菌和止血功能，并有助于增加家禽育种的体重。在此，我们提出了一种新的抗球虫病药物制剂开发策略，旨在合成3-羧苯基硼酸（CPBA）改性的壳聚糖（CS）缀合物，该缀合物可以与地克珠利（DIC）一起自组装成聚合物胶束，一种水溶性差的抗球虫药，用于治疗动物球虫病的定点药物释放。 CPBA修饰的胶束具有特定的葡萄糖和pH双重响应能力。在pH 6.8和50 mM葡萄糖条件下，DIC的累积释放最高达到85.0％，而在pH 2.0且没有葡萄糖时，DIC的累积释放最高达到44.2％，这使得药物可以在具有中性pH和葡萄糖存在的肠道中释放。 〜（1）1 H NMR和FTIR证实两亲聚合物的成功合成;优化的载有DIC的CS–CPBA胶束（DIC / CS–CPBA）的纳米级粒径为（118.9±1.1）nm，载药量为8.97％，球形。药代动力学结果表明，DIC / CS-CPBA胶束的AUC值是药物悬浮液的AUC值的1.7倍。抗球虫功效表明，DIC / CS-CPBA胶束可提高体内抗球虫功效并减少肠道损伤。这些结果表明，结合苯基硼酸的壳聚糖胶束为肠道球虫的特异性靶向药物释放提供了有希望的平台。

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