In the current study, we have focused on the design, development and in-vitro evaluation of d-α-tocopheryl polyethylene glycol 1000 succinate modified amphotericin B (AmB) and paromomycin (PM) loaded solid lipid nanoparticles (TPGS-SLNPs) by emulsion-solvent evaporation method. The optimized TPGS-SLNPs had a mean particle size of 199.4 ± 18.9 nm with a polydispersity index of 0.22 ± 0.14 and entrapment efficiency for AmB and PM was found to be 94 ± 1.5 % and 89 ± 0.50 % respectively. The prepared lipid nanoparticles were characterized by Powdered X-ray diffraction study, Fourier transform infrared spectroscopy, Nuclear magnetic resonance spectroscopy to confirm the absence of any interaction between lipids and drugs. The developed formulation showed a sustained drug release over a period of 48 h and were stable at different temperatures. Finally, TPGS-SLNPs (1 μg/mL) was found to significantly (P < 0.001) mitigate the intra-cellular amastigote growth compared to free AmB. The results obtained suggest TPGS-SLNPs could be an efficient carrier for delivering poorly water-soluble drugs and efficiently enhance its therapeutic potential.

在当前的研究中，我们专注于d的设计，开发和体外评估-α-生育酚聚乙二醇1000琥珀酸酯修饰的两性霉素B（AmB）和巴龙霉素（PM）负载的固体脂质纳米颗粒（TPGS-SLNPs）通过乳液-溶剂蒸发法制备。优化的TPGS-SLNPs的平均粒径为199.4±18.9 nm，多分散指数为0.22±0.14，AmB和PM的包封效率分别为94±1.5％和89±0.50％。通过粉末X射线衍射研究，傅立叶变换红外光谱，核磁共振光谱对制备的脂质纳米颗粒进行表征，以确认脂质与药物之间不存在任何相互作用。所开发的制剂在48小时内显示出持续的药物释放，并且在不同温度下稳定。最后，发现TPGS-SLNPs（1μg/ mL）显着（P <0。001）与游离AmB相比，可减轻细胞内鞭毛体的生长。所获得的结果表明，TPGS-SLNPs可能是递送水溶性差的药物并有效增强其治疗潜力的有效载体。