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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- co -methacrylic acid) (P(MMA- co -MAA)) nanoparticles. Specifically, TIM and biocompatible P(MMA- co -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.

Facile Preparation of Tilmicosin-Loaded Polymeric Nanoparticle with Controlled Properties and Functions