Self-emulsifying systems for the oral delivery of anti-sickling agents

Sickle cell disease is the most common genetic disease affecting more than five million people worldwide. For its treatment, compounds such as senicapoc and voxelotor have recently proven their efficacy in clinical studies with sickle cell patients. However, their low aqueous solubility and sensitivity to metabolism make them poorly bioavailable by the oral route. This project aims to develop self-emulsifying systems to increase the aqueous solubility and oral bioavailability of senicapoc and voxelotor. Self-emulsifying systems loaded with senicapoc and voxelotor were developed and optimized. These formulations increased both the aqueous solubility and cellular transport of senicapoc and voxelotor through enterocyte monolayers (Caco-2). The lipid formulation loaded with voxelotor significantly increased its oral bioavailability compared to a suspension.
(BIFA - Sciences biomédicales et pharmaceutiques) -- UCL, 2021