Lipokon™ is an innovative technology platform delivers the enhancement of oral bioavailability, stability and protection across nutraceuticals with differing solubility and physicochemical profiles through molecular-level encapsulation and amorphization. This research applies the Lipokon™ platform for four nutraceutically diverse actives: berberine, caffeine, curcumin, and resveratrol, and comprehensively evaluates the resulting formulations with respect to solid-state behavior, colloidal properties, and in vitro performance. All formulations exhibited homogeneous appearance, physiologically compatible pH, and controlled moisture content, ensuring physical and chemical stability. Powder X-ray diffraction (XRD) and Differential Scanning Calorimetry (DSC) revealed a dramatic transition from crystalline raw materials to predominantly amorphous states. Particle size analysis revealed nanometric lipid assemblies with Z-average values ranging up to 200 nm. All formulations demonstrated high structural uniformity (Polydispersity Index (PdI): NMT 0.5) and maintained stable negative zeta potentials with lower negative values, ensuring colloidal integrity through effective electrostatic and steric stabilization. Field emission scanning electron microscopy (SEM) and transmission electron microscopy (TEM) showed morphological transformation from angular crystalline particles to uniform nanostructured spherical particles. Energy-dispersive X-ray spectroscopy confirmed molecular-level encapsulation through elevated oxygen content and persistent phospholipid signatures, indicating successful lipid matrix integration. Attenuated Total Reflectance Fourier Transform Infrared (ATR-FTIR) Spectroscopy validated amorphization while confirming chemical integrity without degradation. In vitro dissolution studies demonstrated superior and nearly complete release performance for Lipokon™ Caffeine, which achieved in immediately, while Lipokon™ Resveratrol exhibited controlled biphasic release. These comprehensive findings establish Lipokon™ as a robust, scalable delivery platform capable of transforming crystalline actives into bioavailable formulations while maintaining adaptability across chemically diverse molecules, offering significant potential for enhanced therapeutic efficacy and clinical application.
Patil et al. (Thu,) studied this question.