title: Preparation, characterization and permeation studies of a nanovesicular system containing diclofenac for transdermal delivery.
abstract: BACKGROUND
  Transdermal formulations contain permeation enhancer which causes skin damage. Ceramide 2 is natural lipid found in stratum corneum (SC).
  
  
  OBJECTIVE
  Drug-loaded nanovesicles of ceramide-2, cholesterol, palmitic acid, cholesteryl sulfate were formulated and analyzed for physical and biological properties. Diclofenac was used as a model drug.
  
  
  METHODS
  The vesicles were prepared using the film hydration method and characterized for physical parameters, in vitro drug release, accelerated stability studies and formulated into gel. Respective gels were compared with a commercial formulation (CEG) and plain carbopol gel (CG) containing drug for ex vivo, in vivo drug permeation and anti-inflammatory activity.
  
  
  RESULTS
  The vesicles were stable with optimum physical parameters. DCG-1 showed 92.89% in vitro drug release. Ceramide vesicles showed drug release between 18 and 25 μg/cm(2) whereas CG and CEG released 0.33 and 1.35 μg/cm(2) drug, respectively. DCG-1 and CEG showed corresponding Cmax at 6 and 4 h, respectively. DCG-1 showed six times AUC than CEG. DCG-1 inhibited edema by 86.37% by 4th hour of application.
  
  
  CONCLUSIONS
  The presence of ceramide 2 specifically promotes the drug permeation through SC and dermis and also contribute towards stability and non-irritancy.
  
  
  CONCLUSIONS
  The composition of the nanovesicle played an important role in physical properties and drug permeation.
authors.affiliation: Department of Pharmaceutics, Jodhpur National University , Jodhpur, Rajasthan , India.
authors.forename: Praveen Kumar
authors.initials: PK
authors.lastname: Gaur
authors.forename: Suresh
authors.initials: S
authors.lastname: Purohit
authors.forename: Yatendra
authors.initials: Y
authors.lastname: Kumar
authors.forename: Shikha
authors.initials: S
authors.lastname: Mishra
authors.forename: Anil
authors.initials: A
authors.lastname: Bhandari
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D002518:Ceramides / Q000737:chemistry*; D002784:Cholesterol / Q000737:chemistry; D002788:Cholesterol Esters / Q000737:chemistry; D004008:Diclofenac / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D008297:Male; D053769:Nanocapsules / Q000737:chemistry*; D019308:Palmitic Acid / Q000737:chemistry; D051381:Rats; D017208:Rats, Wistar; D012867:Skin / Q000187:drug effects / Q000378:metabolism; D012869:Skin Absorption; D023422:Skin Irritancy Tests
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D002518:Ceramides; D002788:Cholesterol Esters; D053769:Nanocapsules; D004008:Diclofenac; D019308:Palmitic Acid; D002784:Cholesterol; C007045:cholesteryl sulfate