Dutt M, Khuller G K
Department of Biochemistry, Postgraduate Institute of Medical Education & Research, Chandigarh 160 012, India.
Indian J Exp Biol. 2000 Sep;38(9):887-94.
Poly (DL-lactide-co-glycolide) polymers were investigated as carriers for the first line antitubercular drug rifampicin. Different formulations of PLG microparticles viz. porous, non porous and hardened exhibited sustained release of rifampicin up to 7 weeks in vitro. However, hardened PLG microparticles exhibited the most sustained release in vivo in different organs up to 6 weeks. In case of free rifampicin, release was detected in vivo only up to 48 hr. In addition, no hepatotoxicity was observed on a biochemical basis (levels of SGPT, ALP and total bilirubin) in comparison to control animals. Taken together, these results suggest that polymer encapsulated antitubercular drug rifampicin may serve as an ideal therapeutic approach for treatment of tuberculous infections.
聚(DL-丙交酯-乙交酯)聚合物被研究作为一线抗结核药物利福平的载体。不同配方的PLG微粒,即多孔的、无孔的和硬化的,在体外可实现利福平长达7周的持续释放。然而,硬化的PLG微粒在体内不同器官中表现出最长达6周的持续释放。对于游离利福平,在体内仅在48小时内检测到释放。此外,与对照动物相比,在生化指标(SGPT、ALP和总胆红素水平)方面未观察到肝毒性。综上所述,这些结果表明聚合物包裹的抗结核药物利福平可能是治疗结核感染的理想治疗方法。