Bioavailability enhancement of nanostructured microparticles of carvedilol

• DOI: 10.1016/j.jddst.2021.102780
• Publication Date: 2021-08-20T06:49:27Z
• Authors: C. Prieto; Z. Evtoski; M. Pardo-Figuerez; J.M. Lagaron
• Keywords: Carvedilol; Biopharmaceutics; Microparticle

A high throughput encapsulation technique termed as electrospraying assisted by pressurized gas technology (EAPG) was used to produce nano-within-micro structures of a Biopharmaceutics Classification System (BCS) Class II model drug. Carvedilol is lipid soluble compound, poorly absorbed in the gastrointestinal tract. The produced formulations were characterized terms morphology, crystallinity, vitro dissolution test, Caco-2 cells permeability and vivo pharmacokinetics rats. Spherical microparticles with carvedilol loading 80% sizes around 4 μm. DLS TEM suggested that released form nanoparticles controlled size when are put solution, WAXS DSC confirmed an amorphous state. In tests showed dissolved 4-fold faster than commercial first 30 min. apparent approximately 2.5-fold higher carvedilol. preliminary pharmacokinetic assay reduction 2 h Cmax for prepared formulations, but due variability observed, results need be further studies. This work potential nanostructured API via EAPG increase rate hence bioavailability BCS