Development of an Oral Drug Delivery System to Improve the Bioactivity of Avocatin B

Abstract

Avocatin B, a lipid-derived from avocado, is identified as a novel anti-cancer agent capable of inducing apoptosis of leukemia and leukemic stem cells. Although this bioactive compound has demonstrated anti-leukemic activity in vitro, there is concern about its poor bioavailability. In this study, we exploited the surface-active properties of avocatin B to design self-emulsifying drug delivery systems (SEDDS) that are potentially suitable for human oral consumption. The formulations were prepared without external energy and using only one surfactant. In vitro cytotoxicity testing of avocatin B-SEDDS in acute myeloid leukemia cell lines indicate significant increases in potency and bioactivity compared to dimethyl sulfoxide-based delivery. A pilot pharmacokinetic evaluation of avocatin B-SEDDS in C57BL/6J mice revealed appreciable accumulation in whole blood and biodistribution in key target tissues. We anticipate that data obtained from this study will provide the framework for the development of avocatin B as therapeutic agents in the clinical setting.