Evaluation of soluble fentanyl microneedles for loco-regional anti-nociceptive activity

Abstract

The use of opioids for treating acute and chronic pain condition is a common clinical practice. When delivered systemically, the analgesic activity is mediated through the central pathway, which although effective, leads to various adverse effects such as dependence, abuse and respiratory depression. Fentanyl is an opioid analgesic that is available as injection and transdermal patch products for the management of acute and chronic pain. These products require stringent regulatory controls and label warnings on disposal due to the abuse potential associated. This research project evaluated the regional antinociceptive efficacy of fentanyl delivered from soluble microneedles. The microneedle patches were formulated with relatively less drug loading as compared to patches intended for systemic delivery and were tested for their antinociceptive activity in rats by measuring the paw withdrawal latency when exposed to a thermal stimulus. The results indicate that regional delivery of fentanyl mediated through soluble microneedles provides an effective antinociceptive activity. The onset of analgesic activity was faster with microneedle patch (0.5 h) when compared to the adhesive dermal patch (6 h). This study thus demonstrates the effectiveness of microneedle mediated pain management for immediate pain relief.