Preparation of α-Tocopherol based nanoemulsion for efficacious delivery of Methotrexate

The present work dwells upon developing and assessing the efficacy of nanoemulsion (NEm) for Methotrexate (MTX) delivery. Herein, MTX-loaded NEm was prepared using the ultrasonic nano emulsification method by exploiting biocompatible excipients such as alpha-Tocopherol, Miglyol 812, Tween 80, and ethanol. Employing ultrasonic nano emulsification processes leads to the preparation of NEm with smaller droplet sizes and uniform distribution. The physicochemical characterization by transmission electron microscopy confirmed that the blank NEm and MTX-loaded NEm possesses spherical-shaped nano range particles and drug might be present within the droplet or on the surface of the nanoemulsion. The encapsulation efficiency of MTX in NEm was estimated as 52 +/- 0.6%. The recorded cumulative in-vitro release was 54.74 +/- 2.73% in 24 h and using kinetic modeling, its Fickian diffusion release was validated. Higher stability (94.16 +/- 1.51%) and bioaccessibility (96.06 +/- 1.01%) of MTX-loaded NEm were also confirmed. The hemolysis profile was under the tolerance limit (<8%) for all the concentrations of the formulation. The cell viability assay of NEm loaded with MTX showed significant toxicity against the MCF-7 and HeLa cell lines which validated MTX-loaded NEm as a biosafety vehicle.