Improvising anti-leishmanial activity of amphotericin B and paromomycin using co-delivery in d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) tailored nano-lipid carrier system. (September 2020)

• Record Type: Journal Article
• Authors: Parvez, Shabi; Yadagiri, Ganesh; Singh, Aakriti; Karole, Archana; Singh, Om Prakash; Sundar, Shyam; Mudavath, Shyam Lal
• Is Part Of: Chemistry and physics of lipids. Volume 231(2020)
• Publication Date: 2020-09
• Subjects: Amphotericin B -- Paromomycin -- Solid lipid nanoparticles -- d-α-Tocopheryl polyethylene glycol 1000 succinate; Lipids -- Periodicals; Lipids -- Periodicals; Lipides -- Périodiques; Lipids; Periodicals; Electronic journals; 547.77
• DOI: 10.1016/j.chemphyslip.2020.104946
• Languages: English
• ISSNs: 0009-3084

Abstract

Highlights: We aimed to design, develop and evaluate ( in-vitro ) a novel 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 TPGS-SLNPs were characterized by FTIR, NMR, XRD, SEM, and TEM analysis. The formulation showed time-dependent internalization in J774A.1 cells. TPGS-SLNPs showed an initial burst release followed by a sustained drug release over a period of 48 h. 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. Abstract: 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.