Varied Transdermal Delivery Methods for Diclofenac Sodium, the Ultimate NSAID

Varied Transdermal Delivery Methods for Diclofenac Sodium, the Ultimate NSAID

i-microscopeAll compounding pharmacists know that compounding reaches back to the roots of the pharmacy trade, all the way to ancient Egypt and mortars and pestles and the genesis of formulating medicines to treat human ailments. It’s worth remembering, however, that compounding and working on different formulations for medications also represents the future of personalized medicine and innovation in pharmacology.

Consider Michael, a 67-year-old grandfather of six and retired autoworker who had corneal refractive surgery at an Illinois hospital last year. Because pharmacists and researchers have been hard at work in the past few years developing ways to deliver diclofenac sodium ophthalmically using hydroxypropyl methylcellulose films, he was able to recover mostly pain-free and without feeling blinded by regular daylight.1

It’s meant he can get back to playing outdoors with his grandchildren, including his third grandchild, Laurel, who is able to take the diclofenac sodium she needs for her juvenile arthritis without any trouble because pharmacists and researchers have been developing a flexible-dose, slow-release diclofenac sodium pellet for use with pediatric patients.2

Pharmacists can affect the pharmacokinetic properties of adaptable compounds like the versatile NSAID diclofenac sodium. Through consistently innovating the pharmacy practice, pharmacists can ensure that patients receive personalized care while lowering risk of adverse side effects, and make pain-relieving or life-changing medications accessible to all patient populations.

Compounding Diclofenac Sodium for Transdermal Delivery

Diclofenac sodium is non-steroidal anti-inflammatory drug (NSAID) typically used for pain relief, as an anti-inflammatory in the case of swelling or to relieve joint stiffness caused by arthritis. It’s also become more common in recent years as a treatment for pain from migraines, cataract surgery and corneal refractive surgery.3

The properties of diclofenac sodium make it an ideal NSAID for compounding into gels, patches and other transdermal delivery methods. Highly non-water soluble, various formulations of diclofenac sodium have been created and tested for different applications in order to achieve the peak level of local or systemic effect as an alternative to oral administration options.4

One of the most effective and common ways to boost transdermal absorption and effectiveness for diclofenac sodium and other compounds is to add “penetration enhancers” to formulations. These enhancers work with the active compound to promote better drug administration and potentially even reduce toxicity.

For instance, a study published in BioMed Research International worked with elastic vesicles like liposomes, ethosomes and transfersomes to see if any of the penetration enhancers would improve transdermal applications of diclofenac sodium. The idea of a vesicular system of transdermal delivery has long interested researchers, since such a system would allow a hyper-local delivery and concentration of the active drug to the tissue site, while simultaneously preventing drug loss into surrounding tissues. The study concluded that vesicular systems overall had the highest level of permeability for diclofenac sodium preparations, and that among the tested vesicular systems, the addition of ethosomes and transfersomes far outweighed the efficacy of liposomes, which is somewhat contrary to expectations.5

International researchers have also found emulsification and microemulsion systems effective in transdermal delivery of diclofenac sodium. A Saudi study experimented with using emulsification and internal gelation techniques in order to achieve better in vitro release of the active drug. It ultimately concluded that using alginate microparticles loaded with diclofenac sodium allowed for emulsification and internal gelation, meaning that microencapsulation could be achieved simply and cost-effectively. This results in a gel or other transdermal delivery method with a more efficient controlled drug delivery and release.6

Similar conclusions were echoed by a Romanian research team examining physico-chemical properties of various microemulsion systems as delivery systems for diclofenac sodium. These systems included soybean oil, ethanol and other common additions to transdermal gels and patches.7

Ultimately, diclofenac sodium should always be considered an active ingredient that can be used as an effective oral medication and also a highly effective and localized transdermal drug. Delivery methods can always be improved, especially in settings where researchers are looking for ways to contend with systemic side effects that might mar an otherwise highly effective drug.

How Diclofenac Sodium’s Versatility Helps Pharmacists Treat Patients

NSAIDs are a very commonly prescribed drug class, and diclofenac sodium’s versatility is well-known in terms of pharmacists being able to use it in treatments and pain relief for many different conditions. It’s always good to take a moment to think not only about which compound formulation to use for a specific patient, but ways that the formula can be improved without sacrificing effectiveness as a patient treatment.

Compounding pharmacists play a unique role in our health care system. They not only have the chance to treat their patients and relieve painful symptoms and conditions, but are afforded the ability to do so in a way that lessens patient risk of side effects that can be worse than the original condition.

Diclofenac sodium is a versatile NSAID that allows a skilled pharmacist to directly affect the pharmacokinetics of the formulation and therefore directly affect their patient’s treatment experience. Staying educated and continually improving their skills can help pharmacists continue to make meaningful change for their patients using the latest innovations in pharmaceutical research. As specific formulations or uses for diclofenac sodium continue to evolve, pharmacists can work with physicians and patients to see if compound diclofenac sodium can play a part in each patient’s personal health care and treatment plan.

Pharmaceutica North America is a premier provider of high-quality bulk active pharmaceutical ingredients, unit-dose APIs and custom compounding kits, including diclofenac sodium. Contact us to learn more about how our products can help you provide the best possible patient care.

Show 7 footnotes

  1. “Hydroxypropylmethylcellulose films for the ophthalmic delivery of diclofenac sodium,” Feb. 2013, http://www.ncbi.nlm.nih.gov/pubmed/23278686
  2. “Diclofenac sodium pellets for flexible pediatric drug dosing: Preparation, characterization and evaluation,” July 2015, http://scholarsresearchlibrary.com/dpl-vol7-iss1/DPL-2015-7-1-122-133.pdf
  3. “Diclofenac: Diclofenac Sodium Enteric-Coated Tablet,” accessed Jan. 26, 2016, http://www.webmd.com/drugs/2/drug-4284-4049/diclofenac-oral/diclofenacsodiumenteric-coatedtablet-oral/details
  4. “Diclofenac Sodium Pharmacokinetics,” Aug. 27, 2015, http://www.drugs.com/monograph/diclofenac-sodium.html
  5. “Enhanced Transdermal Delivery of Diclofenac Sodium via Conventional Liposomes, Ethosomes and Transfersomes,” 2013, http://www.hindawi.com/journals/bmri/2013/616810/; “Transferosomes – a vesicular transdermal delivery system for enhanced drug permeation,” July 2011, http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3217704/
  6. “Emulsification/internal gelation as a method of preparation of diclofenac sodium–sodium alginate microparticles,” Aug. 4, 2011, http://www.sciencedirect.com/science/article/pii/S131901641100065X
  7. “Topical Delivery of Diclofenac using Microemulsion Systems,” Nov. 30, 2008, http://www.rombio.eu/rbl6vol13/Lucrare%209%20bt.pdf
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