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. 2022 Mar 28;14(4):726.
doi: 10.3390/pharmaceutics14040726.

Niosomal Nanocarriers for Enhanced Dermal Delivery of Epigallocatechin Gallate for Protection against Oxidative Stress of the Skin

Danhui Li  1 , Nataly Martini  1 , Zimei Wu  1 , Shuo Chen  1 , James Robert Falconer  2 , Michelle Locke  3 , Zhiwen Zhang  4 , Jingyuan Wen  1
Affiliations

Niosomal Nanocarriers for Enhanced Dermal Delivery of Epigallocatechin Gallate for Protection against Oxidative Stress of the Skin

Danhui Li et al. Pharmaceutics. .

Abstract

Among green tea catechins, epigallocatechin gallate (EGCG) is the most abundant and has the highest biological activities. This study aims to develop and statistically optimise an EGCG-loaded niosomal system to overcome the cutaneous barriers and provide an antioxidant effect. EGCG-niosomes were prepared by thin film hydration method and statistically optimised. The niosomes were characterised for size, zeta potential, morphology and entrapment efficiency. Ex vivo permeation and deposition studies were conducted using full-thickness human skin. Cell viability, lipid peroxidation, antioxidant enzyme activities after UVA-irradiation and cellular uptake were determined. The optimised niosomes were spherical and had a relatively uniform size of 235.4 ± 15.64 nm, with a zeta potential of -45.2 ± 0.03 mV and an EE of 53.05 ± 4.46%. The niosomes effectively prolonged drug release and demonstrated much greater skin penetration and deposition than free EGCG. They also increased cell survival after UVA-irradiation, reduced lipid peroxidation, and increased the antioxidant enzymes' activities in human dermal fibroblasts (Fbs) compared to free EGCG. Finally, the uptake of niosomes was via energy-dependent endocytosis. The optimised niosomes have the potential to be used as a dermal carrier for antioxidants and other therapeutic compounds in the pharmaceutical and cosmetic industries.

Keywords: antioxidant activity; catechin; cellular uptake; dermal delivery; niosomes; oxidative stress; penetration; skin barrier.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
(a) Three-dimensional surface plot for EE of EGCG-niosome as a function of the formulation variables. (b) Contour plot for EE of EGCG-niosome as a function of the formulation variables.
Figure 2
Figure 2
Scanning Electron Microscopy (SEM) image of the optimised EGCG niosomes.
Figure 3
Figure 3
(a) Differential Scanning Calorimetry (DSC) thermograms and (b) Fourier Transform Infra-red Spectroscopy (FTIR) spectra of EGCG, Span 60 and EGCG-niosomes.
Figure 4
Figure 4
In vitro drug release of EGCG-niosomes and EGCG solution (mean ± SD, n = 3).
Figure 5
Figure 5
The amount of drug deposited in the human skin layers from EGCG-niosomes and EGCG-solution (mean ± SD, n = 3).
Figure 6
Figure 6
Sections of the full-thickness human skin after been treated with Fluorescein 5(6)-isothiocyanate (FITC) solution (a) and FITC-loaded niosomes (b) after 12 h.
Figure 7
Figure 7
(a) Cellular viability after UVA-irradiation and treatment with EGCG and EGCG-niosomes. The effect of EGCG and EGCG niosomes on (b) intracellular malondialdehyde (MDA) level (b), (c) superoxide dismutase (SOD) and (d) glutathione peroxidase (GSH)-px after UVA-irradiation (mean ± SD, n = 3).
Figure 8
Figure 8
(a) Effects of niosome concentrations and (b) duration of exposure on the uptake of vesicles by Fbs.
Figure 9
Figure 9
Confocal laser scanning microscopy images of Fbs after incubation with FITC-labelled niosomes for 2 h at 37 °C showing perinuclear accumulation of particles. Nuclei: blue (a), FITC-labelled niosomes: green (b), cytoplasm: red (c), merged images (d) confirming uptake of intake niosomes. Eight images of optical sections taken in the vertical axis at interval of 1 µm from the apical surface (e–l) from left to right; top to bottom, depths 0, 1, 2, 3, 4, 5, 6 and 7 μm, demonstrating particle internalisation. Magnification (600×).
See this image and copyright information in PMC

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