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

用于局部递送抗炎药物的纳米乳液型凝胶:体外和体内评价

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作者:Dalia A Gaber, Amal M Alsubaiyel, Alanoud K Alabdulrahim, Hanan Z Alharbi, Rama M Aldubaikhy, Rawan S Alharbi, Wades K Albishr, Heba A Mohamed

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.

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 Cmax 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.

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