Artemisone is an innovative artemisinin derivative with applications in the treatment of malaria, schistosomiasis and other diseases. However, its low aqueous solubility and tendency to degrade after solubilisation limits the translation of this drug into clinical practice. We developed a self-microemulsifying drug delivery system (SMEDDS), which is easy to produce (simple mixing) with a high drug load. In addition to known pharmaceutical excipients (Capmul MCM, Kolliphor HS15, propylene glycol), we identified Polysorb ID 46 as a beneficial new additional excipient. The physicochemical properties were characterized by dynamic light scattering, conductivity measurements, rheology and electron microscopy. High storage stability, even at 30 °C, was achieved. The orally administrated artemisone SMEDDS formulation was highly active in vivo in S. mansoni infected mice. Thorough elimination of the adult worms, their eggs and prevention of the deleterious granuloma formation in the livers of infected mice was observed even at a relatively low dose of the drug. The new formulation has a high potential to accelerate the clinical use of artemisone in schistosomiasis and malaria.

中文翻译：

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口服青蒿松治疗血吸虫病：配方挑战和体内疗效。

青蒿素是一种创新的青蒿素衍生物，可用于治疗疟疾、血吸虫病等疾病。然而，其低水溶性和溶解后降解的趋势限制了该药物转化为临床实践。我们开发了一种自微乳化药物递送系统（SMEDDS），该系统易于生产（简单混合）且载药量高。除了已知的药物赋形剂（Capmul MCM、Kolliphor HS15、丙二醇）之外，我们还确定 Polysorb ID 46 是一种有益的新型附加赋形剂。通过动态光散射、电导率测量、流变学和电子显微镜来表征物理化学性质。即使在 30 °C 下也能实现高储存稳定性。口服青蒿松 SMEDDS 制剂在曼氏沙门氏菌感染的小鼠体内具有高活性。即使在相对较低剂量的药物下，也能观察到彻底消除成虫及其卵，并防止受感染小鼠肝脏中有害肉芽肿的形成。新制剂具有加速青蒿素治疗血吸虫病和疟疾的临床应用的巨大潜力。