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<p>Herein, trimethoprim-montmorillonite-polylactic acid microspheres are prepared by an intercalation-encapsulation method. The protection of montmorillonite prevents the degradation of trimethoprim (TMP) by gastric juice and improves the bioavailability of TMP. The TMP content in the microspheres is about 6%. The cumulative release amounts of TMP in artificial gastric juice, PBS and intestinal fluid are 10.2%, 12.8% and 95.0% after 48&#xa0;h. The antibacterial rates against <i>E. coli</i> of microspheres on the first and third days are 100% and 87% at a concentration of 0.05&#xa0;mg/mL. The main antibacterial mechanism is that the TMP released from the microspheres inhibits the activity of the dihydrofolate reductase of bacteria. <i>E. coli</i> in the main organs of the infected mouse model can be completely cleared after oral administration and the liver and kidney functions of the mice are unaffected. The time to reach maximum concentration in mice of the microspheres is only half that of commercially available TMP tablets. The average residence time of the microsphere treatment group is 1.13 times that of the commercially available tablet treatment.</p>

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Montmorillonite Microspheres Enhance Bioavailability and Antibacterial Efficiency of Veterinary Trimethoprim

  • 期刊论文

  • 发表日期：

    2026年7月6日

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  • Ming Niu,
  • Xiaohui Qiao,
  • Jie Zhao,
  • Zhenghua Zhang,
  • Rourou Wang,
  • Haitao Long,
  • Lumei Pu,
  • Weibing Xu,
  • Nuraly S. Akimbekov

摘要

Herein, trimethoprim-montmorillonite-polylactic acid microspheres are prepared by an intercalation-encapsulation method. The protection of montmorillonite prevents the degradation of trimethoprim (TMP) by gastric juice and improves the bioavailability of TMP. The TMP content in the microspheres is about 6%. The cumulative release amounts of TMP in artificial gastric juice, PBS and intestinal fluid are 10.2%, 12.8% and 95.0% after 48 h. The antibacterial rates against E. coli of microspheres on the first and third days are 100% and 87% at a concentration of 0.05 mg/mL. The main antibacterial mechanism is that the TMP released from the microspheres inhibits the activity of the dihydrofolate reductase of bacteria. E. coli in the main organs of the infected mouse model can be completely cleared after oral administration and the liver and kidney functions of the mice are unaffected. The time to reach maximum concentration in mice of the microspheres is only half that of commercially available TMP tablets. The average residence time of the microsphere treatment group is 1.13 times that of the commercially available tablet treatment.