Oral andrographolide nanocrystals protect liver from paracetamol induced injury in mice

Andrographolide (AG) is a labdane di-terpenoid obtained from aerial parts of Andrographis paniculata. Though known as a potent bioactive in a myriad of biological conditions, the applications of AG in translational medicine are mostly limited due to its low aqueous solubility and poor bioavailability. Nanocrystal technology was envisaged as a possible solution. Andrographolide nanocrystals (AGNC) were prepared through solvent-diffusion followed by homogenization. AGNC hydrodynamic diameter of 630 +/- 12 nm and crystallinity changes led to significant increase of aqueous solubility and intestinal permeation ex vivo. Pharmacodynamic studies on mice showed that AGNC exerted hepatoprotective activity at a lower dose against paracetamol induced liver injury, in comparison to crude AG. The work highlighted that nanocrystal technology can be considered as one platform for circumventing the biopharmaceutical limitations of AG. This also ensures significant successes in biological applications.