Development of Mesalamine Self Nanoemulsifying Drug Delivery System to Improve Solubility and Permeability

The present study was to formulate and evaluate a solid self-nanoemulsifying drug delivery system (SNEDDS) for Mesalamine. Mesalamine was classified as BCS IV, exhibits limited solubility and permeability.

The formulation of liquid SNEDDS was constructed by a pseudoternary phase diagram, which was optimized by the application of a Box-Behnken experimental design. Liquid SNEDDS were then prepared using oleic acid, Tween 80, and PEG 200 at concentrations given by design of experiments (DoE). The liquid SNEDDS were subsequently converted into solid SNEDDS by adsorption technique using Aerosil 200 as the adsorbent agent. The solid SNEDDS were filled into hard gelatine capsules, and further characterization was carried out.

The formulated SNEDDS has a zeta potential of -17 mV and a mean globule size of 107 nm. The efficacy of the formulation was verified by dispersibility, dilution, viscosity, drug content analysis, % transmittance, dye solubility, cloud point, and in vitro drug release studies. The solid SNEDDS underwent physical and micromeritic property evaluations, in vitro dissolution studies, and morphological characterization via Field Emission Scanning Electron Microscopy (FE-SEM). Solid-state characterization showed that Mesalamine was dissolved in the matrix system by (DSC), existed in an amorphous state (PXRD), and had well-separated particles (FE-SEM). The in vitro dissolution study revealed that the optimized SNEDDS had a higher drug release rate than plain Mesalamine.

The study concluded that solid SNEDDS improved solubility, absorption, and permeability of Mesalamine, suggesting enhanced drug delivery and therapeutic efficacy.