Yu Jie, Wang Mingwei, Ahmed Rizwan, Zhao Hongyang, Cohen Stuart Martien A, Wang Junyou
Shanghai Key Laboratory of Multiphase Materials Chemical Engineering, School of Chemical Engineering, East China University of Science and Technology, Shanghai 200237, People's Republic of China.
ACS Omega. 2020 Dec 7;5(50):32366-32372. doi: 10.1021/acsomega.0c04314. eCollection 2020 Dec 22.
As one of the effective broad-spectrum antimicrobial and anti-inflammatory drugs, tilmicosin (TIM) is applied extensively in a wide range of veterinary treatments. However, the low bioavailability typically leads to overuse of TIM in practical applications, which can cause residual accumulation in the environment and contamination of foodstuffs. Here, we report a precipitation method that allows us to prepare TIM-loaded poly(methyl methacrylate--methacrylic acid) (P(MMA--MAA)) nanoparticles. Specifically, TIM and biocompatible P(MMA--MAA) are dissolved in methanol and then water is introduced as an antisolvent, which triggers the co-precipitation and leads to well-controlled nanoparticles. Depending on the drug/polymer mass ratio and the total concentration of drug and polymer, the formed nanoparticles display a tunable radius from 27 to 80 nm with a narrow size distribution, a high drug loading content, and a controlled release of TIM. The encapsulation does not interrupt the antibacterial function of TIM while reducing its cytotoxicity enormously. Moreover, the formed nanoparticles could be dried to powder through freeze-drying, and the redispersion of the particles hardly disturbs the particle size, size distribution, and drug loading content. Our study developed a facile and robust precipitation method for the controlled construction of TIM-loaded polymeric nanoparticles with tunable properties and functions, as well as improved biocompatibility, which shall improve the bioavailability of TIM and enhance the practical applications.
作为一种有效的广谱抗菌和抗炎药物，替米考星（TIM）广泛应用于各种兽医治疗中。然而，低生物利用度通常导致在实际应用中过度使用替米考星，这可能会导致环境中的残留积累和食品污染。在此，我们报告了一种沉淀方法，该方法使我们能够制备负载替米考星的聚（甲基丙烯酸甲酯-甲基丙烯酸）（P（MMA-MAA））纳米颗粒。具体而言，将替米考星和生物相容性P（MMA-MAA）溶解在甲醇中，然后引入水作为反溶剂，引发共沉淀并形成尺寸可控的纳米颗粒。根据药物/聚合物质量比以及药物和聚合物的总浓度，形成的纳米颗粒的半径可在27至80nm之间调节，尺寸分布窄，药物负载量高，并且替米考星具有控释性能。包封不会中断替米考星的抗菌功能，同时极大地降低了其细胞毒性。此外，形成的纳米颗粒可以通过冷冻干燥干燥成粉末，颗粒的再分散几乎不会干扰粒径、尺寸分布和药物负载量。我们的研究开发了一种简便且稳健的沉淀方法，用于可控构建具有可调性质和功能以及改善的生物相容性的负载替米考星的聚合物纳米颗粒，这将提高替米考星的生物利用度并增强其实际应用。
