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 Simultaneously, blood samples were withdrawn over time to obtain the drug absorption in plasma.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 C, T, and AUC 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.

Characterization of ketoprofen‐loaded PEG‐CH semi‐IPN system for wound dressing application

“…This is important in the pharmaceutical industry and for the development process of new drug dosage forms. For instance, Wang et al . studied ketoprofen patches with isopropyl mystirate (6 months, 40 ± 2 °C, relative humidity 5% ± 5%).…”

“…The drug has a half‐life of 2 h, resulting in multiple dosage regimens. The main undesirable side effects include gastrointestinal adverse reactions (ulcerations, abdominal burning, and even gastrointestinal bleeding), renal and hepatic toxicity . In addition, no significant differences have been observed in the percutaneous absorption of ketoprofen, allowing a focal release of the drug and sustained plasma concentration .…”

“…[25][26][27] In addition, no significant differences have been observed in the percutaneous absorption of ketoprofen, allowing a focal release of the drug and sustained plasma concentration. 25 Therefore topical administration could avoid the disadvantages of the oral route. 28 In a study, it was reported that the use of nonsteroidal anti-inflammatory drug s in the form of dressings, such as those produced for wound closure treatments, can reduce the intensity of pain, and accelerate the healing process.…”

Comprehensive Characterisation of the Ketoprofen-β-Cyclodextrin Inclusion Complex Using X-ray Techniques and NMR Spectroscopy

“…KP is used in the form of capsules or tablets in doses up to 300 mg/day, and has a short elimination half-life (1.5–4 h); therefore, it is administered orally four times daily. As a result, chronic use may cause serious gastric side effects, such as ulcerations and even gastrointestinal bleeding [ 6 ]. Therefore, various approaches have been adopted to improving patient compliance by allowing once-daily oral administration of KP.…”

Development of a MD-LC-MS/MS Method to Analyze 3 Bioactive Compounds in Huoxuezhitong Rubber Patch and Application to a Pharmacokinetic Study in Rats

“…To our knowledge, the local pharmacokinetic properties of formula loading pure ingredients have been investigated [22, 23], while there are few studies about the compound prescription, especially following dermal administration. Thus, the study of pharmacokinetic parameters of a standard compound will be helpful to evaluate the efficacy and safety in clinical application.…”