Assessment of a Nano emulsion-Based Drug Delivery System for Improving the Solubility of Imatinib Mesylate: In Vitro Evaluation.

Shiva KM, Mohd I, Kavita S, Kajal R and Ranveer S

Published on: 2023-12-12

Abstract

The objective of the present study was to develop a Self-Nano emulsifying Drug Delivery System (SNEDDS) as a means of enhancing the bioavailability, release rate, and solubility of imatinib mesylate, classified as a BCS class II drug for oral administration. The SNEDDS formulation, comprising an isotropic and thermodynamically stable mixture of oil, surfactant, co-solvent/surfactant, and the medication, demonstrated spontaneous emulsification upon application to an aqueous phase with mild agitation. Various combinations of oil, surfactant, and co-surfactant were systematically screened using a ternary phase diagram to identify a more homogeneous mixture.

The SNEDDS formulations underwent evaluation for appearance, mean droplet size, phase separation, in vitro drug release, and oral bioavailability. The screening process identified Labrafil M 2125 CS as the oil, Tween 80 as the surfactant, and Transcutol®P as the co-surfactant, demonstrating the most favourable solubilizing qualities. The optimized SNEDDS exhibited a notable 98.39% drug release, with dissolution behaviour attributed to the oil/surfactant ratios and surfactant phase properties. Moreover, the optimized SNEDDS displayed a threefold increase in the Area under the Curve (AUC) compared to conventional imatinib mesylate.

The study highlights several factors contributing to the effectiveness of SNEDDS over other drug delivery forms, including a larger droplet surface area, enhanced drug solubilisation facilitated by Labrafil M 2125 CS, and the surfactant's impact on mucosal permeability. The findings suggest that SNEDDS could serve as a promising alternative strategy to enhance the solubility and accessibility of orally administered poorly soluble drugs.