Cholesterol-Rich Nanoemulsions (LDE) for Drug Targeting of Cholesteryl-Succinyl- 5-Fluorouracil Conjugate
Fars K. Alanazi,
Awwad A. Radwan,
Ibrahim A. Alsarra,
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.
Keywords: Cholesterol-rich nanoemulsion, cholesteryl-succinyl-5-fluorouracil, droplet size, drug release, surface morphology.
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