Engineering oral delivery of hydrophobic bioactives in real-world scenarios

Bioactive compounds, often hydrophobic in nature, tend to degrade during processing outside or inside the body with rapid clearance rates, resulting in poor bioavailability. In this review, we survey recent scientific advances in lipid-based colloidal delivery systems (conventional emulsions/nanoemulsions, Pickering emulsions, multilayered and multiple emulsions, coated/uncoated liposomes, natural microcapsules, and so on)that have been used to improve the bioaccessibility and/or bioavailability of hydrophobic bioactive compounds. 

Specifically, we use a ‘delivery to design’ approach, that is, we discuss the desired release kinetics of bioactive compounds first. This enables us to paint a more reasonable image of the optimal microstructure sought in the gastrointestinal tract, to lay out the design principles for fabricating the next generation of oral delivery carriers. Finally, we outline the challenges for translation of oral delivery vehicles that show promises in benchtop experiments and how multidisciplinary approaches might help overcoming some of those challenges.

Highlights