title: PEGylated estradiol benzoate liposomes as a potential local vascular delivery system for treatment of restenosis.
abstract: This study was directed towards the preparation and optimization of PEGylated (PEG, poly(ethylene glycol)) estradiol benzoate (ESB)-loaded liposomes to be used for the treatment of restenosis by local vascular delivery. Various liposomal formulations were prepared by thin film hydration method followed by sonication. Response surface methodology was applied to study the influence of three different independent variables, on the response of entrapment efficiency (%EE). Liposomes were characterized in terms of size, zeta potential, %EE and release profile. Incorporation of ESB was higher in egg phosphatidylcholine (EPC) liposomes, whereas the drug was displaced from liposomes, as the cholesterol (Chol) content of liposome increased. The optimum formulation composed of EPC/dioleyloxy trimethylammonium propane/distearoylphosphatidylethanolamine-PEG2000 with a molar proportion of 8.5:1:0.5 had the highest EE. In vivo studies in the balloon-injured rat carotid arteries revealed the potential of ESB-loaded liposomes as efficient local and controlled drug delivery systems to reduce restenosis.
authors: Department of Pharmaceutics, School of Pharmacy, Shaheed Beheshti University of Medical Sciences, Tehran, Iran.
authors: Azadeh
authors: A
authors: Haeri
authors: Saeed
authors: S
authors: Sadeghian
authors: Shahram
authors: S
authors: Rabbani
authors: Maryam Sotoudeh
authors: MS
authors: Anvari
authors: Mohammad
authors: M
authors: Erfan
authors: Simin
authors: S
authors: Dadashzadeh
mesh_terms: D000818:Animals; D001808:Blood Vessels / Q000378:metabolism*; D023921:Coronary Stenosis / Q000188:drug therapy*; D004958:Estradiol / Q000031:analogs & derivatives* / Q000737:chemistry; D006801:Humans; D008081:Liposomes; D008297:Male; D011092:Polyethylene Glycols / Q000737:chemistry*; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D008081:Liposomes; C074283:estradiol 3-benzoate; D011092:Polyethylene Glycols; D004958:Estradiol