Pharmaceutics Division, Central Drug Research Institute, Lucknow 226001, India.
J Biomed Nanotechnol. 2010 Jun;6(3):293-302. doi: 10.1166/jbn.2010.1121.
The present study was aimed to assess the efficacy of developed transfersome (TF-3) formulation bearing amphotericin B (AmB) against sensitive and resistant clinical isolates of L donovani and compared with conventional liposomal formulation (F-2) and free AmB (F-1). The skin permeation of AmB from TF-3 was performed using Franz diffusion cell using rat skin which showed fickian diffusion across the skin. When tested against L. donovani (intramacrophagic amastigotes), it has been observed that TF was more effective than F-1 and F-2 formulation in sensitive and resistant clinical isolates. The data provides evidences that the TF formulation owing to its fluidized behaviour imparted by sodium deoxycholate, enables to penetrate well in the infected cells and thus provide enhanced activity. The permeation study also supports this data as the flux value of AmB through TF formulation was 1.5 fold higher compared to conventional liposomes suggesting improved penetration and better partitioning in skin layers. Implicit to this preliminary data it is evident that the AmB loaded TF formulation has potential as alternate chemotherapeutic approach to control of VL. Potential utilities of novel formulation as a transdermal delivery of AmB for leishmaniasis necessitates further elaborated investigations which is underway in our laboratory.
本研究旨在评估载两性霉素 B（AmB）的新型传递体（TF-3）制剂对敏感和耐药临床分离株利什曼原虫的疗效，并与传统脂质体制剂（F-2）和游离 AmB（F-1）进行比较。采用Franz 扩散池，使用大鼠皮肤进行 AmB 的皮肤渗透研究，结果表明 AmB 呈菲克扩散穿过皮肤。当对利什曼原虫（巨噬细胞内无鞭毛体）进行测试时，观察到 TF 比 F-1 和 F-2 制剂在敏感和耐药的临床分离株中更有效。这些数据提供了证据，表明由于脱氧胆酸钠赋予的流体化行为，TF 制剂能够很好地穿透感染细胞，从而提供增强的活性。渗透研究也支持这一数据，因为 AmB 通过 TF 制剂的通量值比传统脂质体高 1.5 倍，表明渗透和在皮肤层中更好的分配得到改善。根据这些初步数据可以明显看出，载两性霉素 B 的 TF 制剂具有作为控制内脏利什曼病的替代化学治疗方法的潜力。新型制剂作为治疗利什曼病的透皮递送的潜在用途需要进一步详细研究，这是我们实验室正在进行的工作。
