Amorphous Solid Dispersions and the Contribution of Nanoparticles to In Vitro Dissolution and In Vivo Testing: Niclosamide as a Case Study

We developed an amorphous solid dispersion (ASD) of the poorly water-soluble molecule niclosamide that achieved a more than two-fold increase in bioavailability. Notably, this ASD formulation increased apparent drug solubility about 60-fold relative to crystalline material due generation nanoparticles. Niclosamide is weakly acidic drug, Biopharmaceutics Classification System (BCS) class II, and poor glass former with low bioavailability vivo. Hot-melt extrusion high-throughput manufacturing method commonly used development ASDs for increasing compounds. utilized polymer poly(1-vinylpyrrolidone-co-vinyl acetate) (PVP–VA) manufacture by extrusion. Samples were analyzed based on their microscopic macroscopic behavior intermolecular interactions, using differential scanning calorimetry (DSC), X-ray diffraction (XRD), nuclear magnetic resonance (NMR), Fourier-transform infrared (FTIR), dynamic light scattering (DLS). The generated nanoparticles mean particle size 100 nm FaSSIF media. In side-by-side diffusion test, these produced four-fold diffusion. successfully manufactured extrudates showed remarkable vitro dissolution performance. These tests translated rat model also oral