Abstract
Purpose: To prepare transdermal films of ketorolac tromethamine (KT) and study the effect of turpentine oil as a penetration enhancer for the drug. Methods: Transdermal films of KT were prepared with Carbopol-934 and ethyl cellulose, with turpentine oil as the penetration enhancer, using solvent evaporation method. The films were characterized for physicochemical properties, ex vivo permeation, as well as in vivo anti-inflammatory and analgesic activities in Wistar rats. Results: The transdermal films were uniform in weight and thickness, flat, with high drug content (93.9 to 98.5 %) and of high folding endurance (134.0 to 180.0). Drug permeation through excised rat abdominal skin was prolonged, with the total drug release ranging from 58.88 to 88.98 % in 24 h. The films containing penetration enhancer showed higher drug permeation than the one without the enhancer; furthermore, drug permeation increased with increase in the concentration of the enhancer. The films were non-irritant to the skin. The transdermal films prepared with permeation enhancers showed greater anti-inflammatory activity (87.55 ± 2.50 and 83.24 ± 2.29 % inhibition of rat paw edema at the end of 12 h for formulations F2 and F3, respectively, compared to that of the formulation without enhancer with 69.99 %) as well as greater analgesic activity (quicker onset of analgesia in 1.5 h with longer duration of 10 to 12 h). Conclusion: Transdermal films of ketorolac have a potential for use in the treatment of pain andinflammation. Incorporation of turpentine oil in the films enhances not only drug flux but also analgesic and anti-inflammatory activities in rats.
Highlights
Spinal cord injury (SCI) can be very devastating
Nonsteroidal anti-inflammatory drugs (NSAIDs) are frequently suggested for musculoskeletal pain, while opioid and nonopioid analgesics are used for both types of pain [3]
The conventional systemic delivery of NSAIDs is generally associated with the high incidence of serious gastrointestinal disturbances, more peripheral distribution of drug leading to higher plasma levels and more adverse effects [4,5]
Summary
To repair the initial tissue damage, SCI leads to complex cellular and molecular interactions within the central nervous system [1,2]. Pain and inflammation drastically affect the quality of life after SCI. The conventional systemic delivery of NSAIDs is generally associated with the high incidence of serious gastrointestinal disturbances, more peripheral distribution (rather than the localized delivery for analgesia and anti-inflammatory effect) of drug leading to higher plasma levels and more adverse effects [4,5]. Transdermal drug delivery systems (TDDS) of NSAIDs are potential alternative measure of drug delivery with the added advantage of higher site specific delivery with low plasma concentration (leading to less adverse effects), circumventing of hepatic first pass effect, avoidance of gastric irritation/discomfort, no drug-drug interaction, prolonged drug release, controlled therapeutic responses and improved patient compliance [68]
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