Mucoadhesive microspheres of parthenolide nanocrystals for sustained drug delivery and its potential cytotoxic effect against hepatic cancers.

Objective

The current focus in drug delivery system design is Mucoadhesion. Mucoadhesive microspheres are designed to remain at the drug delivery site for a longer period by enhancing contact with the absorption surface, thereby improving the drug's systemic exposure. The study aimed to formulate and assess mucoadhesive microspheres using sodium alginate, guar gum, and carbopol to achieve sustained release of parthenolide nanocrystals, thereby increasing systemic exposure.

Methods

The ionic gelation process was employed to prepare parthenolide-loaded microspheres (PTL-NC-M). The microspheres were characterized for their particle size (P.S.), entrapment efficiency (E.E.), mucoadhesivity, swelling capacity, and drug release profile, as well as by scanning electron microscopy (SEM), X-ray diffraction (XRD), and differential scanning calorimetry (DSC), and an in vitro wash-off test.

Results

The selected formulation F2 has a particle size of 3.10 ± 0.18 µm and a percentage swelling index of 132.67 ± 1.67%. The carbopol content plays a crucial role in mucoadhesion, and the F2 exhibited superior adhesion to the membranes. The entrapment efficiency ranged from 43% to 95%. The SEM analysis revealed continuous polymeric-coated spherical microspheres.

Conclusion

The microspheres demonstrated a prolonged residence time during the in vitro wash-off period, along with the desired drug release profile. The selected microspheres F2 exhibited better and sustained drug release, along with good mucoadhesivity, resulting in an enhanced invitro cytotoxic potential and increased systemic exposure.