Compounding Insight: Pain Management with Transdermal NSAIDs
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The International Association for the Study of Pain defines pain as “An unpleasant sensory and emotional experience associated with, or resembling that associated with, actual or potential tissue damage”.¹ The sensation of pain alerts us that there is something (actually or potentially) wrong and there are generally thought to be two broad categories of pain. Acute pain has a defined organic cause, which means it was caused by something - it could be because of an injury as in getting a sprain while playing football, it could come from a disease, post-surgical procedure and may or may not be accompanied by inflammation. Alternatively, pain could also be the second type - chronic, which means the pain persists beyond the normally expected recovery period with or without a readily identifiable organic causative agent.²
With the increasing recognition of the need for optimal pain management, steps have been taken to advance our methods to get more effective and efficient results. Many pharmacological therapies have been developed to treat pain; one of the most popular solutions is the non-steroidal anti-inflammatory (NSAID) class of medications.
It has been well established that NSAID’s work to decrease acute and chronic pain and inflammation, and they do so by inhibiting the formation of prostaglandins. NSAID’s primarily inhibit intracellular cyclo-oxygenase (COX) enzymes – a crucial step in the formation and propagation of prostaglandins.³ NSAIDs are most often recommended to be taken orally, however, because they typically cause unwanted gastrointestinal side effects, therefore have patient non-compliance due to intolerability of side effects, which can be a significant problem. In an effort to improve the effectiveness of NSAID therapy for their patients, prescribers started to lean towards alternate routes of administration. Transdermal application of NSAIDs overcome patient non-compliance by reducing or eliminating the typical gastrointestinal adverse effects most often associated with oral therapy. Of all the NSAID molecules, Ketoprofen is an excellent topical NSAID drug therapy and it has been shown to be significantly better in relieving moderate to severe pain as compared to the more traditional NSAID’s such as ibuprofen or diclofenac.⁴
The transdermal application of medications
Transdermal drug delivery is defined as the non-invasive, painless delivery of APIs (active pharmaceutical ingredients) or medications through the skin. It has proven to be advantageous as it can be applied directly on the site of pain, therefore having a more rapid effect, and there is easy customization or titration to meet patient needs through compounding.
The first widely recognized transdermal base was the Pluronic Lecithin Organogel (PLO) which is an oil and aqueous emulsion that was introduced in the ‘90s.¹ The PLO is still considered one of the most common vehicles for delivering pain medications topically, however, as technology keeps on advancing, we have come up with new and even better versions have now been introduced to successfully deliver APIs for pain management, such as the TD Lipo Base which can deliver higher percentages of multiple APIs. Cannabase™ is another excellent example of a lipid-based transdermal delivery system for pain management. Cannabase™ is specially developed for the transdermal delivery of lipophilic phytoceuticals such as Phytocannabinoid that have synergistic anti-inflammatory and analgesic effects.⁵
In veterinary use
In a recent study, a transdermal formulation of Ketoprofen provided effective analgesia in cattle undergoing surgical animal husbandry procedures. To reduce the pain caused by such procedures, animal handlers are required to provide pain relief to the animals. It is more common for the analgesics to be administered intramuscularly, however, this study shows the transdermal application of NSAIDs to animals is just as effective as its injectable counterpart, but with improved compliance.⁶ Topical NSAIDs are an excellent choice for many different types of pain control and are effective across species both domesticated and exotic. Topical formulations allow the prescriber multiple treatment options for their non-human patients.
In conclusion, compounded transdermal NSAIDs offer a viable treatment to pain as an alternative dosage form of drug therapy with similar effectiveness to oral/injectable formulations and show decreased side effects. Xenex Labs have many different topical formulations available with your online account or contact customer service for more information.
- Srinivasa et. al. The revised International Association for the Study of Pain definition of pain: concepts, challenges, and compromises. PAIN: September 2020 - Volume 161 - Issue 9 - p 1976-1982
- Williams K. D. (2010). Managing pain with transdermal ketoprofen. International journal of pharmaceutical compounding, 14(3), 204–206.
- Ghlichloo, I. (2021, May 12). Nonsteroidal anti-inflammatory drugs (NSAIDs). StatPearls [Internet]. Retrieved January 27, 2022, from https://www.ncbi.nlm.nih.gov/books/NBK547742/
- U.S. National Library of Medicine. (1970, January 1). Efficacy of Ketoprofen vs Ibuprofen and Diclofenac: A systematic review of the literature and meta-analysis. Database of Abstracts of Reviews of Effects (DARE): Quality-assessed Reviews [Internet]. Retrieved January 27, 2022, from https://www.ncbi.nlm.nih.gov/books/NBK190381/
- “CANNABASE CREAM BASE.” Transderma Pharmaceuticals Inc., www.transderma.com/product/td-cannabase/. Accessed 10 Feb. 2022
- Mills, P. C., Ghodasara, P., Satake, N., Alawneh, J., Fraser, B., Kopp, S., & McGowan, M. (2020, December 20). A novel transdermal ketoprofen formulation provides effective analgesia to calves undergoing amputation dehorning. MDPI. Retrieved January 27, 2022, from https://www.mdpi.com/2076-2615/10/12/2442
Reviewed by: Paul Gibbons B.Sc. Pharm. RPh.
February 8th, 2022
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