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Transdermal Adhesive Patches Loaded with Ketoprofen Evaluated by Dynamic Detection of Percutaneous Absorption

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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 Simultaneously, blood samples were withdrawn over time to obtain the drug absorption in plasma.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 AUC0–8h were 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.

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Acknowledgements

This work was financially supported by the Major New Drug Discovery of Major Science and Technology Projects (2014ZX09507001-009).

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Authors and Affiliations

  1. School of Pharmacy, Shenyang Pharmaceutical University, No103, Wenhua Road, Shenyang, 110016, China

    Menglin Wang, Yinghua Sun, Guixia Ling & Zhonggui He

  2. Research and Development Department, Beijing Wan Sheng Pharmaceutical Co., Ltd., No8, Guangyuan East Street, Tongzhou District, Beijing, 101113, China

    Longwei Li

  3. Pharmaceutical Engineering, Hebei Chemical & Pharmaceutical College, No. 88 Yuhuafangxing Road, Shijiazhuang, 050000, China

    Junxia Xie

Authors
  1. Menglin Wang
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  2. Longwei Li
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  3. Junxia Xie
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  4. Yinghua Sun
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  5. Guixia Ling
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Correspondence to Yinghua Sun or Zhonggui He.

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Wang, M., Li, L., Xie, J. et al. Transdermal Adhesive Patches Loaded with Ketoprofen Evaluated by Dynamic Detection of Percutaneous Absorption. AAPS PharmSciTech 18, 2141–2148 (2017). https://doi.org/10.1208/s12249-016-0695-8

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  • DOI: https://doi.org/10.1208/s12249-016-0695-8

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