Encapsulation of didanosine within polymeric particles for enhanced oral bioavailability in HIV: Spray-drying versus coaxial electrohydrodynamic atomization

SEREMETA, KP; SOSNIK, A

Edimburgo

Encuentro; 2015 Controlled Release Society Annual Meeting; 2015

Controlled Release Society

The goal of this study was to comparatively investigate two technologies, spray-drying (SD) and coaxial electrohydrodynamic atomization (CEHDA) to encapsulate the water-soluble anti-HIV didanosine (ddI) within poly(epsilon-caprolactone) (PCL) microparticles and stabilize it in the gastric medium, where drug undergoes fast acid degradation. Both methods led to high encapsulation efficiency. Pharmacokinetics studies in rats showed that ddI-loaded microparticles (MPs) led to a statistically significant increase of the oral bioavailability with respect to a ddI aqueous solution. In case of SD the increase was of 2.5-fold whereas that in CEHDA was of 3.8-fold. In addition, the half-life was prolonged 1.4- and 2-fold respectively. On the other hand, SD resulted in significantly greater yield. While both technologies are promising to encapsulate water-soluble drugs within polymeric particles, additional optimization stages would be critical for scale up and bench-to-bedside translation.