This study aimed to enhance the dissolution rate and bioavailability of the poorly water-soluble drug raloxifene hydrochloride (RLX) by developing a stable nanosuspension-loaded buccal patch. RLX nanosuspension was formulated using high pressure homogenization, with Tween 20 and Poloxamer 188 as stabilizers. The nanosuspension was characterized for size distribution, zeta potential and morphology. The optimized nanosuspension was then incorporated into a buccal patch, which was prepared using a mucoadhesive layer and a backing membrane composed of ethyl cellulose/Eudragit RL100 via solvent casting. The resulting buccal patch was evaluated for physical, mechanical, bioadhesive properties, as well as in-vitro and in-vivo parameters. The RLX nanosuspension showed a particle size of 416.8 nm, a PDI of 0.256 and a zeta potential of +4.89 mV, with 86.955% drug release in-vitro. The nanosuspension-loaded buccal patch exhibited a particle size of 481.7 nm, a thickness of 0.173 mm and a weight of 0.163±0.004 g. It showed excellent folding endurance (>250), a surface pH of 6.63 and a swelling index of 255.30±0.19% at 6 hours. In-vitro drug release was 78.7±0.1% within 6 hours and the mucoadhesion strength was 13.5±0.10 g. In-vivo studies in a rat model revealed a 349.91% increase in relative bioavailability compared to the RLX suspension, likely due to bypassing gastrointestinal degradation and first-pass hepatic metabolism. Prepared RLX nanosuspension-loaded buccal patch significantly improves bioavailability and offers potential for drugs vulnerable to gastrointestinal degradation and first-pass metabolism.
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