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.

穿心莲内酯（AG）是从穿心莲的空中部分获得的一种拉丹烷二萜。尽管在众多生物条件下被称为有效生物活性剂，但由于其水溶性低和生物利用度差，AG在转化医学中的应用受到很大限制。纳米晶体技术被认为是一种可能的解决方案。穿心莲内酯纳米晶体（AGNC）通过溶剂扩散然后均质化制备。AGNC的流体动力学直径为630±12 nm，并且结晶度变化导致离体的水溶性和肠道渗透性显着增加。对小鼠的药效学研究表明，与粗制AG相比，AGNC在较低剂量下对乙酰氨基酚引起的肝损伤具有保肝作用。这项工作着重指出，纳米晶体技术可以看作是一种解决AG的生物制药局限性的平台。这也确保了生物学应用的重大成功。