Cholesterol-Rich Nanoemulsions (LDE) for Drug Targeting of Cholesteryl-Succinyl-5-Fluorouracil Conjugate
Fars K. Alanazi, Nazrul Haq, Awwad A. Radwan, Ibrahim A. Alsarra and Faiyaz Shakeel
The aim of present investigation was to develop and evaluate cholesterol-rich nanoemulsions (LDE) of cholesteryl-succinyl-5-fluorouracil (CS-5-FU conjugate) in order to improve therapeutic efficacy and to reduce adverse effects of the treatment. LDE formulations of CS-5-FU conjugate were developed by high energy emulsification technique and developed formulations were physicochemically characterized for droplet size, polydispersity index, zeta potential, surface morphology and refractive index. In vitro drug release studies of CS-5FU conjugate from LDE nanoemulsions were performed using dialysis membrane. The droplet size (42.2 nm), polydispersity index (0.119), zeta potential (-29.65 mV), viscosity (35.22 cp) and refractive index (1.337) were found to be lowest for optimized formulation LDE5 (containing CS-5-FU-6 mg/cholesterol-0.5 mg/Triolein-1 mg/phosphatidylcholine-20 mg/cholesteryloleate-40 mg/Tween-80-0.3 ml/Labrasol-0.3 ml). Optimized formulation LDE5 also showed best drug release profile (98.4%) through dialysis membrane after 24 h of study. These preliminary studies indicated that developed LDE nanoemulsions could be applied for targeting of CS-5-FU conjugate to cancer cells.
Cholesteryl-succinyl-5-fluorouracil, droplet size, cholesterol-rich nanoemulsion, drug release, surface morphology
Kayyali Chair for Pharmaceutical Industry, Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia.