Formulation and evaluation of self nano-emulsifying drug delivery system of ezetimibe for dissolution rate enhancement

Abstract

The present study was aimed to develop a Self Nano Emulsifying Delivery System of Ezetimibe (EZM) for enhancing its dissolution rate. Ezetimibe is a cholesterol absorption inhibitor, being a lipophilic drug due to its low solubility EZM shows a low dissolution profile. The SNEDDS formulation consisted of excipients Cinnamon oil, Tween 80, PEG 400 as the Oil, Surfactant and Co-surfactant. Twelve formulations with different ratios of Oil, Surfactant and Co-surfactant were prepared. The liquid SNEDDS were then converted into Solid form by adsorption technique using Avicel PH 101 and Aerosil 200 as adsorbents. The liquid SNEDDS was characterised for Particle size, Emulsification time, Dispersibility, percentage transmittance, PCM, Centrifugation, Cloud Point and Freeze thaw cycle. The solid form was characterized for the flow property, SEM, Drug content and in-vitro dissolution. Among the twelve formulations F6 formulation was found to have a particle size of 196 nm and PDI of 0.123. F6 formulation was selected as the best and it was made into solid by adsorption onto solid carriers. The F6 formulation consisted of the 25% Cinnamon oil, 50% tween 80 and 25% PEG 400. The in-vitro dissolution rate of the prepared formulation was compared with the marketed formulation. The in-vitro dissolution data showed that the drug release at the end of 60 mins from marketed formulation was 63.75 % and from SNEDDS formulation was 90.62 %. The dissolution rate of the prepared SNEDDS was increased by 1.42 times than the marketed formulation. The increase in the dissolution rate shows that SNEDDS is a suitable drug delivery system to enhance the rate of dissolution of Ezetimibe.

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“…Phase-contrast microscopy (Leica S40, 230 ± 10V, 5W) was used to determine the morphology of DTG-L-SNEDDS by focussing the lens at 10× and 40×. [8] Cloud point measurement DTG-L-SNEDDS were diluted to 250 ml with distilled water and placed in a water bath with gradually increasing temperature. The temperature was noted visually when there was a sudden appearance of cloudiness.…”

“…The sample absorbance was then measured using a UV spectrophotometer at 257.80 nm. [8,13] Drug release kinetics was studied using 4 different kinetic models (zero-order, first-order, Higuchi, and Weibull equation). A measure of the model's appropriateness was determined by its R 2 value.…”