Oral absorption, distribution, metabolism, and excretion of icaritin in rats by Q-TOF and UHPLC-MS/MS. First-in-class immune-modulating small molecule Icaritin in advanced hepatocellular carcinoma: Preliminary results of safety, durable survival and immune biomarkers. In conclusion, the results suggested that the mixed micelles of Soluplus ® and Poloxamer 407 could be a feasible drug delivery system to enhance oral bioavailability of icaritin, and the ABS method might be a promising technology for the preparation of polymeric micelles to encapsulate poorly water-soluble weakly acidic and alkaline drugs.Īcid-base shift method icaritin oral absorption polymeric micelles transmembrane transport.įan Y., Li S., Ding X., Yue J., Jiang J., Zhao H., Hao R., Qiu W., Liu K., Li Y., et al. Transcellular transport studies of IPMs across Caco-2 cell monolayers confirmed that the IPMs were endocytosed in their intact forms through macropinocytosis, clathrin-, and caveolae-mediated pathways. Furthermore, bioavailability of icaritin in IPMs in beagle dogs displayed a 14.9-fold increase when compared with the oil suspension. In vitro release tests confirmed the faster release of icaritin from IPMs compared to an oil suspension. The prepared IPMs were characterized to have a spherical shape with a size of 72.74 ± 0.51 nm, and 13.18% drug loading content. The feasibility of the ABS method was successfully demonstrated by studies of icaritin-loaded polymeric micelles (IPMs). The purpose of this study was to develop mixed polymeric micelles with high drug loading capacity to improve the oral bioavailability of icaritin with Soluplus ® and Poloxamer 407 using a creative acid-base shift (ABS) method, which exhibits the advantages of exclusion of organic solvents, high drug loading and ease of scaling-up.