Oral delivery system prolongs blood circulation of docetaxel nanocapsules via lymphatic absorption

Significance Oral drug delivery is the most convenient administration route for patients. Docetaxel, a potent anticancer drug, elicits severe side effects following intravenous administration. Furthermore, oral docetaxel absorption is prevented by biochemical barriers in the intestine. An oral formulation of docetaxel nanocapsules (NCs) embedded in microparticles was developed and elicited higher plasma docetaxel concentrations than intravenous administration of the commercial product. These unexpected results were explained by the penetration of the docetaxel NCs within the enterocytes, circumventing the barriers, where their coating was reinforced prior reaching, intact, the circulation via the lymphatic system. The oral formulation significantly improves docetaxel anticancer efficacy. This delivery concept has potential for clinical translation, allowing docetaxel chemotherapy to be switched from intravenous to oral delivery.