title: Titanium dioxide inclusion in backing reduce the photoallergenicity of ketoprofen transdermal patch.
abstract: Ketoprofen (KP) is a widely used transdermal non-steroidal anti-inflammatory drug. However, increasing number of adverse effect case reports suggests that KP transdermal formulation can cause photoallergic reaction. The photoallergic potential of KP is attributable to the instability of KP under UV/visible light and subsequent formation of reactive degradation products. In this study, we investigated whether the inclusion of titanium dioxide (TiO(2)), a well-known mineral sunscreen agent, in the KP transdermal patch can prevent the photodegradation of KP and ultimately, can reduce photoallergic reaction. TiO(2) inclusion in fabric backing effectively decreased the UV transmission through fabric patch throughout all UVA region from 320 to 380 nm and consistently, KP patch with TiO(2) exhibited significantly increased photostability of KP. This enhanced photostability of KP resulted in reduced generation of photodegradation product as determined by HPLC-UV analysis. In a good accordance with these in vitro results, photosensitization test in guinea pig in vivo demonstrated low photoallergic reactions of KP patch with TiO(2) compared to KP patch without TiO(2), indeed. This study demonstrated that KP transdermal patch with TiO(2)-included backing can provide with improved photostability and photosafety over conventional fabric KP patch.
authors.affiliation: Amorepacific Corporation R&D Center, Bora-dong, Giheung-gu, Yongin-si, Republic of Korea.
authors.forename: Yang-Gyu
authors.initials: YG
authors.lastname: Choi
authors.forename: Ji Hae
authors.initials: JH
authors.lastname: Lee
authors.forename: Il-Hong
authors.initials: IH
authors.lastname: Bae
authors.forename: Young-Chang
authors.initials: YC
authors.lastname: Ah
authors.forename: Han-Moe
authors.initials: HM
authors.lastname: Ki
authors.forename: Jun-Ho
authors.initials: JH
authors.lastname: Bae
authors.forename: Young-Ho
authors.initials: YH
authors.lastname: Park
authors.forename: Kang Choon
authors.initials: KC
authors.lastname: Lee
authors.forename: Kyung-Min
authors.initials: KM
authors.lastname: Lim
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000378:metabolism*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D017454:Dermatitis, Photoallergic / Q000209:etiology* / Q000378:metabolism; D006168:Guinea Pigs; D007660:Ketoprofen / Q000378:metabolism; D008297:Male; D011897:Random Allocation; D014025:Titanium / Q000494:pharmacology*; D057968:Transdermal Patch
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; C009495:titanium dioxide; D007660:Ketoprofen; D014025:Titanium