Nano-Emulsion Based Gel for Topical Delivery of an Anti-Inflammatory Drug: In vitro and in vivo Evaluation

INTRODUCTION: Arthritic disorder is a common disease in elderly patients and the most common cause of joint dysfunction. This study aims to design Piroxicam-loaded nanoemulsion (PXM-NE) formulations to enhance the analgesic and anti-inflammatory activity of the drug for topical use. METHODS: The nanoemulsion preparations were designed based on a high-pressure homogenization technique and were characterized for particle size (PS), poly dispersity index (Pi), zeta potential (ZP), drug content, and the selected formula was investigated for its topical analgesic activity and pharmacokinetic parameters. RESULTS: The characterizations showed that the PS was 310.20±19.84 nm, Pi was 0.15±0.02, and ZP was −15.74±1.6 mV for the selected formula. A morphology study showed that the PXM-NE droplets were spherical with a uniform size distribution. The in vitro release study showed a biphasic release pattern with a rapid release within the first 2 hours followed by a sustained release pattern. The analgesic activity for optimal formula was 1.66 times higher than the commercial gel with a double duration of analgesic activity. The C(max) was 45.73±9.95 and 28.48±6.44 ng/mL for the gel form of the selected formula and the commercial gel respectively. The relevant bioavailability of the selected formula was 2.41 higher than the commercial gel. CONCLUSION: The results showed good physicochemical properties, higher bioavailability, and a longer analgesic effect of PXM from nanoemulsion gel, as compared to the commercial product.