Co-encapsulated xanthoxylin (GX-50) and vitamin C (Vc)
microcapsules
(GX-50-Vc-M) were prepared by the combination of a water-in-oil-in-water
(W1/O/W2) double emulsion with complex coacervation.
The W1/O/W2 double emulsion was prepared by
two-step emulsification, and it has a uniform particle size of 8.388
μm and high encapsulation efficiencies of GX-50 (85.95%) and
Vc (67.35%) under optimized process conditions. Complex coacervation
occurs at pHs 4.0–4.7, which has the highest encapsulation
efficiency of GX-50 and Vc at pH 4.5. The complex coacervate with
tannic acid solidifying (namely, wet microcapsules) has better mechanical
properties and also enhances the ability of co-encapsulation of active
ingredients. The resulting microcapsules by freeze-drying of wet microcapsules
were characterized by UV–vis absorbance spectroscopy (UV–vis),
Fourier infrared spectroscopy (FI-IR), confocal laser scanning microscopy
(CLSM), scanning electron microscopy (SEM), X-ray diffraction (XRD),
2,2-diphenyl-1-picrylhydrazyl (DPPH·) radical scavenging,
and in vitro permeation measurements. Under optimal conditions, the
encapsulation efficiency and drug loading of GX-50-Vc-M for GX-50
and Vc are, respectively, 78.38 ± 0.51 and 59.34 ± 0.56%,
and 35.6 ± 0.68 and 29.8 ± 0.92%. A slight shift in the
FTIR peak between single GX-50 or Vc and GX-50-Vc-M confirmed the
successful co-encapsulation of GX-50 and Vc in microcapsules. GX-50-Vc-M
has bridged irregular spherical aggregates, while GX-50 and Vc are,
respectively, encapsulated in hydrophobic and hydrophilic cavities
of microcapsules in an amorphous dissolved state. GX-50-Vc-M has the
highest DPPH· radical scavenging rate of 62.51%,
and the scavenging process of GX-50-Vc-M on DPPH· radicals is more in line with the pseudo-second-order kinetic equation
model. Moreover, the in vitro permeation of GX-50 and Vc in GX-50-Vc-M
can reach maximum values of 40 and 60%, respectively. This concludes
that GX-50-Vc-M is a promising delivery system for the penetration
of the antioxidant into the deeper layers of the skin for the antioxidant
effect.