Formulation of Felodipine lipid nanoparticle-loaded oral fast-dissolving films

Abstract

Felodipine, a calcium channel blocker used to treat hypertension, is a BCS Class II drug characterized by low solubility, high permeability and significant hepatic metabolism, which limits its bioavailability to 15 %. This study focuses on improving the bioavailability of Felodipine by developing oral fast-dissolving films (OFDFs) incorporating lipid nanoparticles. Felodipine loaded lipid nanoparticles were prepared using glyceryl monooleate (GMO) as lipid and Poloxamer 407 as the surfactant, and then incorporated into OFDFs using the solvent casting technique. A Box-Behnken design with Design Expert Stat-Ease® 360 was used to evaluate the impact of GMO, Poloxamer 407 concentration, and sonication time on particle size and entrapment efficiency. The resulting nanoparticle dispersions had particle sizes ranging from 74.92 nm to 112.1 nm and entrapment efficiencies between 80.43 % and 95.23 %. Differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), and X-ray diffraction (XRD) confirmed successful drug encapsulation. The OFDF showed optimal mechanical properties, disintegration within (41.33 ± 3.51) s, and an in-vitro drug release of (89.82 ± 2.75) % in 6 min. Scanning electron microscopy (SEM) revealed a smooth, uniform, porous surface and the films remained stable for three months. The study concludes that Felodipine loaded lipid nanoparticles in fast-dissolving OFDFs improve permeability, dissolution, and onset of action, making them a promising approach for antihypertensive therapy.