Potential of lipid nanoemulsion for drug delivery of cholesteryl-hexahydrophthaloyl-5-fluorouracil

The present study was undertaken to evaluate lipid nanoemulsions of cholesteryl-hexahydrophthaloyl-5-fluorouracil (CHHP-5-FU) to improve its therapeutic potential and to reduce adverse effects. CHHP-5-FU-loaded lipid nanoemulsions were prepared by high energy emulsification method and evaluated for droplet size, polydispersity index, zeta potential, refractive index and drug release. The drug release was found to be increased significantly by increasing the concentration of surfactants and decreasing droplet size & viscosity of formulations (P<0.05). The values of droplet size (58.4 nm), polydispersity index (0.148), zeta potential (-29.25 mV), viscosity (40.24 cp) and refractive index (1.338) were found to be lowest for formulation F5 (containing CHHP-5-FU-6 mg/cholesteryloleate-40 mg/phosphatidylcholine-20 mg Triolein-1 mg/cholesterol-0.5 mg/ Tween-80-0.3 mL/Labrasol-0.3 mL). Formulation F5 also showed highest drug release profile (92.4%) via dialysis membrane after 24 h. Kinetic studies showed all lipid nanoemulsions followed non-Ficknian diffusion mechanism. Based on these studies, formulation F5 was selected as an optimized lipid nanoemulsion of CHHP-5-FU.