title: Enhancement of skin permeation of flurbiprofen via its transdermal patches using isopulegol decanoate (ISO-C10) as an absorption enhancer: pharmacokinetic and pharmacodynamic evaluation.
abstract: OBJECTIVE
  The study aimed to prepare a transdermal patch for flurbiprofen using isopulegol decanoate (ISO-C10) as a permeation enhancer, and to evaluate the in-vitro and in-vivo percutaneous permeation of the drug, as well as the pharmacodynamic efficacy of the formulation.
  
  
  METHODS
  The permeation experiments were conducted on rabbit skin, and the pharmacokinetic profiles and synovial fluid drug concentration were measured after in-vivo transdermal administration. A deconvolution approach was employed to analyse the correlation between the in-vitro and in-vivo drug permeation. The anti-inflammatory and analgesic effects were, respectively, assessed using the adjuvant arthritis model and the acetic acid induced pain model.
  
  
  RESULTS
  ISO-C10 could increase the in-vitro permeation of flurbiprofen from 46.22 ± 5.65 μg/cm(2) to 101.07 ± 10.85 μg/cm(2) . The in-vivo absorption of the drug was also improved by the enhancer, and a good linear correlation was observed between the in-vitro and in-vivo drug permeation. Meanwhile, the ISO-C10 contained patches increased the drug disposition in synovial fluid and enhanced the pharmacodynamic efficacy of the formulation.
  
  
  CONCLUSIONS
  ISO-C10 would be a promising permeation enhancer for improving the in-vitro and in-vivo delivery of flurbiprofen from its transdermal patches.
authors.affiliation: Department of Pharmaceutical Science, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, Liaoning, China.
authors.forename: Yang
authors.initials: Y
authors.lastname: Chen
authors.affiliation: Department of Pharmaceutical Science, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, Liaoning, China.
authors.forename: Peng
authors.initials: P
authors.lastname: Quan
authors.affiliation: Department of Pharmaceutical Science, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, Liaoning, China.
authors.forename: Xiaochang
authors.initials: X
authors.lastname: Liu
authors.affiliation: Department of Pharmaceutical Science, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, Liaoning, China.
authors.forename: Wenjia
authors.initials: W
authors.lastname: Guo
authors.affiliation: Department of Pharmaceutical Science, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, Liaoning, China.
authors.forename: Wenting
authors.initials: W
authors.lastname: Song
authors.affiliation: Department of Pharmaceutical Science, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, Liaoning, China.
authors.forename: Dongmei
authors.initials: D
authors.lastname: Cun
authors.affiliation: Department of Pharmaceutical Science, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, Liaoning, China.
authors.forename: Zhongyan
authors.initials: Z
authors.lastname: Wang
authors.affiliation: Department of Pharmaceutical Science, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, Liaoning, China.
authors.forename: Liang
authors.initials: L
authors.lastname: Fang
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D000081005:Cyclohexane Monoterpenes; D003651:Decanoates / Q000737:chemistry*; D003652:Decanoic Acids / Q000494:pharmacology; D004195:Disease Models, Animal; D016503:Drug Delivery Systems / Q000379:methods; D005480:Flurbiprofen / Q000008:administration & dosage* / Q000737:chemistry*; D008297:Male; D051379:Mice; D010146:Pain / Q000139:chemically induced / Q000188:drug therapy; D011817:Rabbits; D012867:Skin / Q000378:metabolism*; D012869:Skin Absorption; D013729:Terpenes / Q000737:chemistry*; D057968:Transdermal Patch
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D000081005:Cyclohexane Monoterpenes; D003651:Decanoates; D003652:Decanoic Acids; D013729:Terpenes; C409816:isopulegol; C031071:decanoic acid; D005480:Flurbiprofen
keywords: flurbiprofen; isopulegol decanoate; pharmacodynamic; pharmacokinetics; transdermal enhancer