Superficial nociceptive pains such as myalgia (muscular pain) can have a wide range of causes, from bee stings and burns to trauma, muscle overuse or chronic tensions, and is often associated with inflammation and tissue swelling [1]. Generally, a specific group of drugs called nonsteroidal anti-inflammatory drugs (NSAIDs) can be used for the treatment of local muscular pain and inflammation. The NSAIDs inhibit the activity of cyclooxygenase enzymes (COX-1 and COX-2), thereby controlling the synthesis of thromboxanes and prostaglandins [2]. The cyclooxygenase is an enzyme released during pain and inflammation, whereas thromboxanes and prostaglandins are mediators of vasoconstriction and inflammation, respectively [3]. Some commonly used NSAIDs include aspirin, ibuprofen, naproxen and diclofenac.Diclofenac is used for the treatment of mild to moderate muscular pain, as well as for alleviating the symptoms of arthritis, menstrual cramps, toothache and migraines/headaches [4]. However, if it is taken orally for a long period of time in high doses, then it may potentially lead to fatal stomach and intestinal bleeding, and perhaps increase the risk of a heart attack or stroke [5]. Today, patients are becoming more and more conscious of such side effects and hence novel and safer ways of pain management are desirable.Transdermal drug delivery (TDD) can pose as a safer and preferred alternative to oral drug delivery as well as parenteral administration for NSAIDs due to various reasons [6]. One advantage is that the transdermal route avoids the metabolism of the drug inside the liver and its rapid absorption inside the GI tract, thus avoiding the risk of internal bleeding and irritation. Additionally, TDD typically avoids painful administration or other unwanted systemic side effects that may occur with oral administration. TDD systems are designed to deliver a predetermined amount of drug through the stratum corneum and subsequently the systemic circulation [7]. The choice of drug for TDD depends on the size of the drug, as it should efficiently pass through the skin pores. Conventional means of TDD include ointments, creams and gels; however, the major disadvantage of these is the need for frequent application, the inability to determine exact dosage administered and instability. Moreover, strong ointments or their improper usage can potentially lead to skin allergies, dryness, lesions and thinning of the skin [8].Given this, TDD systems, such as drug-loaded patches, backing films, microneedles, thermal, mechanical and electrical ablation, are often preferred [9,10]. Out of these, TDD patches are simple and the most patient-compliant. A few transdermal patches for treating muscular pain are available on the market -most based on either narcotic (Fentanyl) or methyl salicylate (Salonpas), which can cause breathing problems, or toxicity issues [11,12].
Novel diclofenac-loaded TDD patchesIdeally, TDD systems need to facilitate the permeation of drug through the stratum corneum, systematically deliver the drug and mainta...