Infectious Disease Biology Laboratory, Chemical Biology Unit, Institute of Nano Science & Technology, Habitat Centre, Phase 10, Sector 64, Mohali, Punjab 160062, India.
Department of Biochemistry, Institute of Science, Banaras Hindu University, Varanasi, Uttar Pradesh 221005, India.
Chem Phys Lipids. 2020 Sep;231:104946. doi: 10.1016/j.chemphyslip.2020.104946. Epub 2020 Jul 1.
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.
在本研究中，我们专注于通过乳化-溶剂蒸发法设计、开发和体外评估 d-α-生育酚聚乙二醇 1000 琥珀酸酯修饰的两性霉素 B（AmB）和硫酸巴龙霉素（PM）负载的固体脂质纳米粒（TPGS-SLNPs）。优化的 TPGS-SLNPs 的平均粒径为 199.4 ± 18.9nm，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、傅里叶变换红外光谱、核磁共振波谱对制备的脂质纳米粒进行了表征，以确认脂质和药物之间不存在任何相互作用。所开发的制剂在 48 小时内表现出持续的药物释放，并在不同温度下稳定。最后，与游离 AmB 相比，TPGS-SLNPs（1μg/mL）显著（P<0.001）减轻了细胞内无鞭毛体的生长。结果表明，TPGS-SLNPs 可以作为一种有效的载体，用于输送水溶性差的药物，并有效地提高其治疗潜力。
