title: Transdermal Adhesive Patches Loaded with Ketoprofen Evaluated by Dynamic Detection of Percutaneous Absorption.
abstract: Topical delivery has many benefits toward NSAIDs administration, and the best-selling transdermal preparation in 2015 was the NSAID patch MOHRUS®. Herein, we report a ketoprofen adhesive patch (KAP) and evaluate the penetration and absorption compared to MOHRUS®. Microdialysis sampling technique was applied to determine drug penetration in the dermis and subcutaneous tissue. Simultaneously, blood samples were withdrawn over time to obtain the drug absorption in plasma. The ketoprofen concentrations in the dermis, subcutaneous tissue, and plasma were compared with the commercially available patch (MOHRUS®). Based on the detection, pharmacokinetic parameters including Cmax, Tmax, and AUC0-8hwere determined for both the formulations. No significant differences were found in the dermis, subcutaneous tissue, and plasma in rats according to the bioequivalence assessment. The KAP demonstrated multiple therapeutic advantages including the controlled drug release and the sustained drug concentration in the skin as well as in plasma. The pharmacokinetic study coupled with microdialysis sampling provided an effective strategy to evaluate transdermal delivery.
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, No103, Wenhua Road, Shenyang, 110016, China.
authors.forename: Menglin
authors.initials: M
authors.lastname: Wang
authors.affiliation: Research and Development Department, Beijing Wan Sheng Pharmaceutical Co., Ltd., No8, Guangyuan East Street, Tongzhou District, Beijing, 101113, China.
authors.forename: Longwei
authors.initials: L
authors.lastname: Li
authors.affiliation: Pharmaceutical Engineering, Hebei Chemical & Pharmaceutical College, No. 88 Yuhuafangxing Road, Shijiazhuang, 050000, China.
authors.forename: Junxia
authors.initials: J
authors.lastname: Xie
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, No103, Wenhua Road, Shenyang, 110016, China. sunyinghua77@aliyun.com.
authors.forename: Yinghua
authors.initials: Y
authors.lastname: Sun
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, No103, Wenhua Road, Shenyang, 110016, China.
authors.forename: Guixia
authors.initials: G
authors.lastname: Ling
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, No103, Wenhua Road, Shenyang, 110016, China. hezhonggui@vip.163.com.
authors.forename: Zhonggui
authors.initials: Z
authors.lastname: He
mesh_terms: D000269:Adhesives / Q000378:metabolism; D000279:Administration, Cutaneous; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000493:pharmacokinetics; D001682:Biological Availability; D016503:Drug Delivery Systems / Q000379:methods*; D007660:Ketoprofen / Q000008:administration & dosage / Q000493:pharmacokinetics; D008297:Male; D017551:Microdialysis / Q000379:methods; D051381:Rats; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption / Q000502:physiology; D013810:Therapeutic Equivalency; D057968:Transdermal Patch
chemical_list: D000269:Adhesives; D000894:Anti-Inflammatory Agents, Non-Steroidal; D007660:Ketoprofen
keywords: bioequivalence; ketoprofen patch; microdialysis; pharmacokinetics; transdermal penetration