title: Enhanced transdermal drug delivery of zaltoprofen using a novel formulation.
abstract: Zaltoprofen is a non-steroidal anti-inflammatory drug (NSAID) belonging to the propionic acid class. It has strong inhibitory effects on acute and chronic inflammation. Although zaltoprofen is well tolerated orally compared to other NSAIDs, it has to be administered in three to four doses per day and was associated with ulcerogenicity, bellyache and indigestion. This makes administration of zaltoprofen unsuitable for patients with gastric ulcer and is also associated with drug interactions. Therefore, it is important to develop an alternative dosage form which is easier to administer and avoids first-pass metabolism. The transdermal route meets all the above advantages. In this study, zaltoprofen gels were prepared using carbomer with mixture solution of polyethylene glycol (PEG) 400, Tween 80 and (2-hydroxypropyl)-β-cyclodextrin (HPCD) (called as T2), subsequently oleic acid as a penetration enhancer was added. Zaltoprofen gel containing T2 and oleic acid could promote the percutaneous absorption of zaltoprofen and increase AUC by 183% compared to zaltoprofen gel without T2 and oleic acid. Also, there was a finding zaltoprofen gel containing T2 and oleic acid did not cause dermal irritations in an experimental animal.
authors.affiliation: College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, Daejeon 305-764, South Korea.
authors.forename: Jong-Suep
authors.initials: JS
authors.lastname: Baek
authors.forename: Ji-Ho
authors.initials: JH
authors.lastname: Lim
authors.forename: Jong-Seong
authors.initials: JS
authors.lastname: Kang
authors.forename: Sang-Chul
authors.initials: SC
authors.lastname: Shin
authors.forename: Sang-Hun
authors.initials: SH
authors.lastname: Jung
authors.forename: Cheong-Weon
authors.initials: CW
authors.lastname: Cho
mesh_terms: D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000180:Acrylic Resins / Q000737:chemistry; D000279:Administration, Cutaneous; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000737:chemistry* / Q000493:pharmacokinetics; D001578:Benzopyrans / Q000008:administration & dosage* / Q000737:chemistry* / Q000493:pharmacokinetics; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D005782:Gels; D006801:Humans; D008297:Male; D051379:Mice; D019301:Oleic Acid / Q000737:chemistry; D011092:Polyethylene Glycols / Q000737:chemistry; D011136:Polysorbates / Q000737:chemistry; D011422:Propionates / Q000008:administration & dosage* / Q000737:chemistry* / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley; D012867:Skin / Q000187:drug effects; D012882:Skin Tests; D012995:Solubility; D047392:beta-Cyclodextrins / Q000737:chemistry
chemical_list: D000180:Acrylic Resins; D000894:Anti-Inflammatory Agents, Non-Steroidal; D001578:Benzopyrans; D005782:Gels; D011136:Polysorbates; D011422:Propionates; D047392:beta-Cyclodextrins; D000073738:2-Hydroxypropyl-beta-cyclodextrin; C043940:pyranoprofen; D019301:Oleic Acid; D011092:Polyethylene Glycols; C006903:carbopol 940
keywords: Cytotoxicity; Skin irritation; Transdermal drug delivery; Zaltoprofen