title: Physicochemical characteristics of liposomes are decisive for their antirestenosis efficacy following local delivery.
abstract: OBJECTIVE
  To develop an ameliorated sirolimus (SIR) liposome for intramural delivery, the effects of various carrier physicochemical parameters on the antirestenosis efficacy were evaluated.
  
  
  METHODS
  Different liposomes were prepared, characterized and administered to balloon injured rats (12 animal groups). Their efficacies were investigated using morphometric, immunohistochemical and in vivo computed tomography imaging analyses.
  
  
  RESULTS
  The antirestenosis efficacy of SIR liposomes decreased in the following order: cationic 100 nm vesicles ≥ cationic 60 nm vesicles > neutral 100 nm vesicles ≥ stealth 100 nm vesicles > anionic 100 nm vesicles. The 100 µg SIR loaded in cationic liposomes showed almost no artery stenosis.
  
  
  CONCLUSIONS
  Appropriate modulation of physicochemical characteristics makes it possible to optimize the liposomes for local delivery.
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
authors.forename: Azadeh
authors.initials: A
authors.lastname: Haeri
authors.affiliation: Tehran Heart Center, Tehran University of Medical Sciences, Tehran, Iran.
authors.forename: Saeed
authors.initials: S
authors.lastname: Sadeghian
authors.affiliation: Tehran Heart Center, Tehran University of Medical Sciences, Tehran, Iran.
authors.forename: Shahram
authors.initials: S
authors.lastname: Rabbani
authors.affiliation: Tehran Heart Center, Tehran University of Medical Sciences, Tehran, Iran.
authors.forename: Shapour
authors.initials: S
authors.lastname: Shirani
authors.affiliation: Tehran Heart Center, Tehran University of Medical Sciences, Tehran, Iran.
authors.forename: Maryam Sotoudeh
authors.initials: MS
authors.lastname: Anvari
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran.|Pharmaceutical Sciences Research Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
authors.forename: Simin
authors.initials: S
authors.lastname: Dadashzadeh
mesh_terms: D000818:Animals; D002317:Cardiovascular Agents / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology; D002339:Carotid Arteries / Q000187:drug effects / Q000378:metabolism / Q000473:pathology; D020212:Carotid Artery Injuries / Q000188:drug therapy; D023903:Coronary Restenosis / Q000188:drug therapy*; D019394:Ki-67 Antigen / Q000378:metabolism; D008081:Liposomes / Q000008:administration & dosage* / Q000737:chemistry*; D008297:Male; D058426:Neointima / Q000378:metabolism; D010949:Plasma / Q000737:chemistry; D011136:Polysorbates / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D020123:Sirolimus / Q000008:administration & dosage* / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D002317:Cardiovascular Agents; D019394:Ki-67 Antigen; D008081:Liposomes; D011136:Polysorbates; D020123:Sirolimus
keywords: liposome; local delivery; physicochemical characteristics; restenosis; sirolimus