Preparation and Characterization of Isradipine as Surfactant Free Emulsion

Isradipine is a calcium channel blocker, it’s the drug of choice for oral therapy of severe hypertension and urgent hypertension crises in pediatrics. It belongs to the BCS class II. Its oral bioavailability will be approximately 15 to 24 %. This study aims to prepare a stable, low-toxic, eco-friendly, surfactant-free oral oil-in-water emulsion of Isradipine for pediatric patients and enhance dosing accuracy. Isradipine surfactants–free emulsions (SFE) were prepared to protect this ester drug from hydrolysis, oxidation, photosensitivity, increasing its solubility and absorption, thereby improving its bioavailability. The study used corn and grape oil to prepare SFE for solubilizing Isradipine. The SFE was stabilized by different percentages of β-cyclodextrin to encapsulate oil droplets. Twelve formulas were prepared using a homogenizer and mixed for 5 minutes at 10,000 rpm and 25ºC. The SFE formulas were evaluated for organoleptic attributes, thermodynamic stability, dilution test, viscosity, pH, drug content, droplet size distribution, and in-vitro dissolution. Among all the prepared SFE formulas, F3 containing 8g of β-CD and 15g of Corn oil, was chosen as the optimum SFE formula due to its small particle size range1451±0.01 nm, respectable pH, good organoleptic attributes, excellent thermodynamic stability, acceptable viscosity (1869.5±1.54), acceptable drug content percentage, and highest dissolution rate. F3 was further tested for drug excipient compatibility using Fourier Transform Infrared Spectroscopy (FTIR) and Scanning Electron Microscopy (SEM), showing complexation between the drug and oil droplets, and spherical droplets of Corn oil surrounded by β-CD.