Background <p>To meet the needs of local treatment for spinal tuberculosis, this study developed a thermosensitive gel microsphere composite with both anti-tuberculosis and osteogenesis-promoting functions for efficient drug sustained release. The composite consists of anti-tuberculosis drugs (Pretomanid, Pa-824; Moxifloxacin, M; Pyrazinamide, Z) and bone morphogenetic protein-2 (BMP-2) to optimize drug release kinetics and enhance local therapeutic effects.</p> Methods <p>PaMZ/BMP-2 microspheres were prepared using microfluidics and characterized by SEM, particle size analysis, and XRD. LC–MS and ELISA measured drug and BMP-2 release. The thermosensitive gel (P407/P188) ratio was optimized to ensure it remained liquid at room temperature and formed a gel at 37&#xa0;°C for sustained release.</p> Results <p>Microspheres were spherical with an average size of 203.92 ± 27.76&#xa0;μm. Encapsulation rates were 112.69%, 24.15%, and 15.18% for Pa, M, and Z, respectively. In vitro release showed Pa and M sustained release for over 17&#xa0;days, with the gel prolonging drug release.</p> Conclusion <p>This study successfully prepared PaMZ/BMP-2 microspheres with good morphology and drug loading capacity, achieving controlled sustained release through thermosensitive gel. This offers a potential formulation approach for future localized therapy of spinal tuberculosis and lays the foundation for subsequent in vivo experiments and clinical translation.</p>

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Preparation and in vitro sustained release performance of thermosensitive gel microsphere composite loaded with Anti-Tuberculosis drug PaMZ/BMP-2

  • Gui Li,
  • Qianbo Song,
  • Ye Song,
  • Wenxing Liao,
  • Dong Zhao,
  • Binqing Hong,
  • Guangru Cao

摘要

Background

To meet the needs of local treatment for spinal tuberculosis, this study developed a thermosensitive gel microsphere composite with both anti-tuberculosis and osteogenesis-promoting functions for efficient drug sustained release. The composite consists of anti-tuberculosis drugs (Pretomanid, Pa-824; Moxifloxacin, M; Pyrazinamide, Z) and bone morphogenetic protein-2 (BMP-2) to optimize drug release kinetics and enhance local therapeutic effects.

Methods

PaMZ/BMP-2 microspheres were prepared using microfluidics and characterized by SEM, particle size analysis, and XRD. LC–MS and ELISA measured drug and BMP-2 release. The thermosensitive gel (P407/P188) ratio was optimized to ensure it remained liquid at room temperature and formed a gel at 37 °C for sustained release.

Results

Microspheres were spherical with an average size of 203.92 ± 27.76 μm. Encapsulation rates were 112.69%, 24.15%, and 15.18% for Pa, M, and Z, respectively. In vitro release showed Pa and M sustained release for over 17 days, with the gel prolonging drug release.

Conclusion

This study successfully prepared PaMZ/BMP-2 microspheres with good morphology and drug loading capacity, achieving controlled sustained release through thermosensitive gel. This offers a potential formulation approach for future localized therapy of spinal tuberculosis and lays the foundation for subsequent in vivo experiments and clinical translation.