title: Ceramide-2 nanovesicles for effective transdermal delivery: development, characterization and pharmacokinetic evaluation.
abstract: Abstract Context: The vesicles based on skin lipid have a drug localization effect and its main lipid, ceramide provides protective and regenerative effects while oleic acid (OA) is a penetration enhancer, however, it causes slight irritation, so we have formulated formulation incorporating both of these to develop a transdermal formulation for better permeation.
  
  
  OBJECTIVE
  Present study investigated the preparation and characterization of physicochemical properties and permeation of nanovesicles of ceramide-2 containing OA and palmitic acid (PA) respectively and a commercial gel.
  
  
  METHODS
  The vesicles were made using ceramide 2, cholesterol (Chol), cholesteryl sulfate (CS) and OA or PA, respectively, using film hydration method. The vesicles were characterized for physicochemical properties, ex vivo permeation using human skin and pharmacokinetic parameters and anti-inflammatory activity in rats.
  
  
  RESULTS
  The vesicles showed size at 102-125 nm while PDI was 0.11-0.13 and negative zeta potential. OV-3 showed highest entrapment efficiency. The drug fluxes were 92.02 and 8.920 μg/cm(2)/h, respectively, for OV-3 and PV-1. The Cmax were 7.91 and 4.01 μg/ml at 4 and 6 h for OV-3 (2.5 mg) and PV-1 (10 mg), respectively. OV-3 and PV-1 showed 98.8% and 77.36% edema inhibition, respectively, at 3 h.
  
  
  CONCLUSIONS
  Both formulations showed similar physical parameters and different permeation since OA get incorporated in vesicles and increases its permeability and ceramide makes sure that vesicles can rapidly traverse the stratum corneum.
  
  
  CONCLUSIONS
  OV-3 containing 3% OA showed optimum physical parameters and good permeation with maximum anti-inflammatory activity.
authors.affiliation: Faculty of Pharmaceutical Sciences, Jodhpur National University, Narnadi, 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*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004008:Diclofenac / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D004195:Disease Models, Animal; D016503:Drug Delivery Systems; D005079:Excipients / Q000737:chemistry*; D006801:Humans; D007249:Inflammation / Q000188:drug therapy / Q000473:pathology; D008297:Male; D053758:Nanoparticles; D019301:Oleic Acid / Q000737:chemistry; D019308:Palmitic Acid / Q000737:chemistry; D010316:Particle Size; D051381:Rats; D017208:Rats, Wistar; D012869:Skin Absorption
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D002518:Ceramides; D005079:Excipients; D004008:Diclofenac; D019301:Oleic Acid; D019308:Palmitic Acid