title: Formulation and evaluation of cholesterol-rich nanoemulsion (LDE) for drug delivery potential of cholesteryl-maleoyl-5-fluorouracil.
abstract: It has been reported that cholesterol-rich nanoemulsions (LDE) can bind to low density lipoprotein (LDL) receptors which can concentrate anticancer drugs in the tissues via LDL receptor overexpression and reduced the adverse effects of the treatment. Therefore, in this study, LDE nanoemulsions of cholesteryl-maleoyl-5-fluorouracil (5-FU conjugate) were developed and evaluated in vitro. LDE nanoemulsions were prepared by high-energy emulsification technique. Developed formulations were characterized in terms of droplet size, polydispersity index, zeta potential, viscosity and refractive index. Optimized formulation (L5) was also evaluated for surface morphology using transmission electron microscopy (TEM). Developed formulations were subjected to in vitro drug release studies through dialysis membrane. The droplet size (50 nm), polydispersity index (0.109) and viscosity (32.16 cp) were found to be lowest for optimized formulation L5. The results of zeta potential indicated the stable formation of developed LDE nanoemulsions. TEM images of optimized formulation indicated non-spherical shape of droplets. About 97% of conjugate was found to be released from L5 after 24 h of study. Overall, these results indicated that developed LDE nanoemulsions could be successfully used for oral delivery of 5-FU conjugate.
authors.affiliation: Kayyali Chair for Pharmaceutical Industry, Department of Pharmaceutics, College of Pharmacy, King Saud University , Riyadh , Saudi Arabia and.
authors.forename: Fars K
authors.initials: FK
authors.lastname: Alanazi
authors.forename: Nazrul
authors.initials: N
authors.lastname: Haq
authors.forename: Awwad A
authors.initials: AA
authors.lastname: Radwan
authors.forename: Ibrahim A
authors.initials: IA
authors.lastname: Alsarra
authors.forename: Faiyaz
authors.initials: F
authors.lastname: Shakeel
mesh_terms: D000964:Antimetabolites, Antineoplastic / Q000008:administration & dosage* / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods; D002784:Cholesterol / Q000737:chemistry*; D016503:Drug Delivery Systems; D065546:Drug Liberation; D004655:Emulsions; D005472:Fluorouracil / Q000008:administration & dosage* / Q000737:chemistry; D008055:Lipids / Q000737:chemistry; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles; D010316:Particle Size; D013997:Time Factors; D014783:Viscosity
chemical_list: D000964:Antimetabolites, Antineoplastic; D004655:Emulsions; D008055:Lipids; D002784:Cholesterol; D005472:Fluorouracil
keywords: Cholesteryl-maleoyl-5-fluorouracil; droplet size; drug release; nanoemulsion; zeta potential