Nano-Spanlastics Loaded Mucoadhesive Lyophilized Wafer of Calcium-Channel Antagonist Felodipine

Background A dihydropyridine Ca2 + channel antagonist, felodipine (FDP) is used to treat hypertension and angina pectoris. The low solubility of FDP causes it to undergo pre-systemic metabolism when taken orally, resulting in a 15% reduction in bioavailability. Objective To minimize pre-systemic metabolism, increase drug absorption, and improve pharmacological impact, the researchers in this work encapsulated FDP, a model for an anti-hypertensive drug, in nano-spanlastics (SL) and then incorporated it into a 1% Carboxy methyl cellulose wafer for mucoadhesive buccal drug administration in turn facilitating hypertension treatment without invasive surgery. Methods The ethanol injection technique was employed to create FDP-loaded nano-SL (FDP-SL) using a 2³ factorial design. The properties of the SL formulations were evaluated. The optimized formulation (SL-7) containing 30% Tween 80 was characterized based on particle size, entrapment efficiency, deformability index, flux (Jmax), and stability. In vitro permeation studies assessed trans-buccal delivery, while SL-7 was incorporated into CMC wafers for mucoadhesive application. In vivo studies evaluated the effects on blood pressure, lipid profiles, oxidative stress markers, and heart health. Histopathological studies compared the protection of cardiac tissues between the SL-7 wafer and Plendil®. Results The optimized SL-7 demonstrated an entrapment efficiency (95.38 ± 0.96%), a deformability index (12.46 ± 0.46 g), and a Jmax (28.51 ± 0.21 g/cm²/h), with a 4.72-fold enhancement. The formulation exhibited excellent stability and superior in vitro permeation. In vivo studies showed significant improvements in blood pressure, lipid profiles, and oxidative stress markers, with no adverse effects. Histopathological analysis indicated that the SL-7 wafer provided better protection of cardiac tissues compared to Plendil®. Conclusion Encapsulating FDP in Tween 80-based SL and delivering it via mucoadhesive buccal wafers significantly enhances its bioavailability and therapeutic efficacy. This non-invasive approach offers a promising strategy for improved hypertension management.