Mechanochemical preparation of nano-sized pharmaceutical drugs for potential application in cancer therapy (2):Evaluation of realgar and orpiment as a promising cancer therapeutic agent

摘要

Recently arsenic sulfur compounds (AsxSy) have been a research focus because of its promising anticancer effects especially in the treatment of leukemia after successful application of arsenic oxide. The arsenic compounds, realgar (As4S4) and orpiment (As2S3) have long been used as a therapeutic agent to treat some diseases in ancient China and Europe. In general, its poor water-solubility unfortunately results in poor bioavailability and hampers it from being studied and used for possible clinical application. In this study, the apparent solubility of each test sample was examined based on the primary particle size and pH in solution medium. The identified phenomena - polymorphous transformation, new surface area formation as well as man-sized particles preparation are expected to have good correlation with solubility. The bioavailability of two realgar and orpiment as a potential new pharmaceutical drug for leukemia treatment could not be confirmed due to very low solubility. The basic research for other dosage forms including the enhancement of solubility might be required.