Abstract
Background:
Apigenin (APG), a natural bioactive flavonoid has multiple pharmacological
effects. However, its poor aqueous solubility hinders its clinical benefits.
Objective and Methods:
The work aimed to develop novel apigenin-loaded niosomes (APG-NIO) with
ecological probe sonication techniques. The formulation was statistically optimized by Box-Behnken
design (BBD) and the independent variables were selected as Span 80(X1), Poloxamer 188(X2), and
Tween 80(X3) at three levels, and the dependent variables were identified as: particle size (Y1), polydispersity
index (Y2), and % entrapment efficiency (Y3). The formulation was characterized for various
parameters such as vesicle shape, size, PDI, %EE, solubility, in vitro drug release, and antioxidant potential.
Results:
The optimized APG-NIO formulation was found to have a spherical shape with homogenous
distribution and a low polydispersity index. It has a particle size of 425.77 nm, zeta potential -17.1±0.9
mV, and % EE of 89.63. The aqueous solubility of APG-NIO was found approximately 45 times higher
than that of pure APG. The formulation showed a higher drug release rate as compared to pure APG in
phosphate buffer pH 7.4 and followed the Higuchi release model with a non-Fickian transport mechanism.
The stability was found at 4°C for 3 months. The antioxidant potential of APG-NIO was significantly
increased in comparison to the pure drug suspension in the DPPH• assay.
Conclusion:
These findings suggest that the probe sonication technique is an alternative, cost-effective,
simple, and green method for the development of niosomes, and BBD is a useful optimization tool for
identifying the effect of formulation variables.