title: Enhancement of follicular delivery of finasteride by liposomes and niosomes 1. In vitro permeation and in vivo deposition studies using hamster flank and ear models.
abstract: Finasteride is indicated orally in the treatment of androgenetic alopecia and some other pilosebaceous unit (PSU) disorders. We wished to investigate whether topical application of finasteride-containing vesicles (liposomes and niosomes) could enhance drug concentration at the PSU, as compared to finasteride hydroalcoholic solution (HA). Liposomes consisted of phospholipid (dimyristoyl phosphatidylcholine (DMPC) or egg lecithin):cholesterol:dicetylphosphate (8:2:1, mole ratio). Niosomes were comprising non-ionic surfactant (polyoxyethylene alkyl ethers (Brij series) or sorbitan monopalmitate):cholesterol:dicetylphosphate (7:3:1, mole ratio). Vesicles were prepared by the film hydration technique and characterized with regard to the size, drug entrapment efficiency and gel-liquid transition temperature (T(c)). In vitro permeation of (3)H-finasteride through hamster flank skin was faster from hydroalcoholic solution (0.13 microg/cm(2)h) compared to vesicles (0.025-0.058 microg/cm(2)h). In vivo deposition of (3)H-finasteride vesicles in hamster ear showed that liquid-state vesicle, i.e. those made of DMPC or Brij97:Brij76 (1:1), were able to deposit 2.1 or 2.3% of the applied dose to the PSU, respectively. This was significantly higher than drug deposition by gel-state vesicles (0.35-0.51%) or HA (0.76%). Both in vitro permeation and in vivo deposition studies, demonstrated the potentials of liquid-state liposomes and niosomes for successful delivery of finasteride to the PSU.
authors.affiliation: Department of Pharmaceutics, School of Pharmacy and Isfahan Pharmaceutical Sciences Research Center, Isfahan University of Medical Sciences, Isfahan, Iran. tabbakhian@pharm.mui.ac.ir
authors.forename: Majid
authors.initials: M
authors.lastname: Tabbakhian
authors.forename: Naser
authors.initials: N
authors.lastname: Tavakoli
authors.forename: Mahmoud Reza
authors.initials: MR
authors.lastname: Jaafari
authors.forename: Saeid
authors.initials: S
authors.lastname: Daneshamouz
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D002784:Cholesterol / Q000737:chemistry; D006224:Cricetinae; D004337:Drug Carriers; D016503:Drug Delivery Systems / Q000379:methods*; D004431:Ear, External / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D018120:Finasteride / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D008081:Liposomes; D008297:Male; D008647:Mesocricetus; D010755:Organophosphates / Q000737:chemistry; D010316:Particle Size; D010713:Phosphatidylcholines / Q000737:chemistry; D010938:Plant Oils / Q000737:chemistry; D011092:Polyethylene Glycols / Q000737:chemistry; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption
chemical_list: D004337:Drug Carriers; D004791:Enzyme Inhibitors; D008081:Liposomes; D010755:Organophosphates; D010713:Phosphatidylcholines; D010938:Plant Oils; C002290:dicetylphosphate; D011092:Polyethylene Glycols; D018120:Finasteride; C033084:polyethylene glycol oleyl ether; D002784:Cholesterol