Improvement of Skin Penetration, Antipollutant Activity and Skin Hydration of 7,3',4'-Trihydroxyisoflavone Cyclodextrin Inclusion Complex - PubMed (original) (raw)
Improvement of Skin Penetration, Antipollutant Activity and Skin Hydration of 7,3',4'-Trihydroxyisoflavone Cyclodextrin Inclusion Complex
Pao Hsien Huang et al. Pharmaceutics. 2019.
Abstract
As is known, many antioxidants from plant extracts have been used as additives in skincare products to prevent skin damage following overexposure to environmental pollutants. 7,3',4'-trihydroxyisoflavone (734THIF), an isoflavone compound, possesses various biological activities, including antioxidant, antityrosinase, photodamage protection, and anticancer effects. Unfortunately, 734THIF has poor water solubility, which limits its skin penetration and absorption, and subsequently influences its biological activity. The aim of the present study was to investigate the mechanisms for the improvement in water solubility and skin penetration of 2-hydroxypropyl-β-cyclodextrin (HPBCD) inclusion complex with 734THIF (5-7HP). We also determined its photostability, antipollutant activity in HaCaT keratinocytes, and moisturizing effect in human subjects. Our results showed that 734THIF was embedded into the lipophilic inner cavity of HPBCD and its water solubility and skin penetration were thereby improved through amorphous transformation, surface area enhancement, and hydrogen bonding formation between 734THIF and HPBCD. In addition, 5-7HP inhibited PM-induced ROS generation and then downregulated ROS-mediated COX-2 and MMP9 production and AQP-3 consumption by inhibiting the phosphorylation of MAPKs. Consequently, we suggest that 5-7HP is a safe and photostable topical ingredient to enhance the skin penetration of 734THIF and skin hydration, and therefore 5-7HP may be used as an antipollutant additive in skin care products.
Keywords: 2-Hydroxypropyl-β-cyclodextrin; 7,3′,4′-trihydroxyisoflavone; antioxidant; skin hydration; skin penetration; solubility.
Conflict of interest statement
The authors declare no conflict of interest. The funders had no role in the design of the study; in the collection, analyses, or interpretation of data; in the writing of the manuscript, or in the decision to publish the results.
Figures
Figure 1
Phase solubility diagram of 734THIF-HPBCD system.
Figure 2
The surface morphology of 734THIF, HPBCD and 7HPs was observed by scanning electron microscopy (SEM).
Figure 3
Powder X-ray diffraction patterns of HPBCD, different ratios of 734HP, and raw 734THIF.
Figure 4
FT-IR spectra of 734THIF, HPBCD, and different ratios of 734HP.
Figure 5
1H-NMR spectra and chemical structural formula of 734THIF, HPBCD, and 5-7HP.
Figure 6
The photostability of 5-7HP powder and 5-7HP water solution. Values are mean ± SD (n = 4). * p < 0.05.
Figure 7
The contents of 734THIF delivered from 734THIF and 5-7HP to different skin layers: (A) stratum corneum, (B) epidermis, (C) and dermis. (D) 734THIF amount permeation in epidermis and dermis treated at different times. (E) Percent of 734THIF penetrated into different skin layer. Values are mean ± SD (n = 6). * p < 0.05 compared with raw 734THIF.
Figure 8
The HaCaT cell viability of 734THIF, 5-7HP and HPβCD at 24 and 48 h. All columns are mean ± SD (n = 3); * p < 0.05. HPβCD concentration was calculated by 5-7HP, which means it needs to be multiplied by 5; for example, 10 μM represent 50 μM HPβCD and so on.
Figure 9
The effect of HPBCD, raw 734THIF and 5-7HP on PM-induced ROS generation in human keratinocytes. All samples (10 μM) were dissolved in DMEM solution (n = 6 in each group).
Figure 10
COX-2, MMP-9, AQP-3, and MAPKs protein expressions. Cells were pre-incubated with HPBCD, raw 734THIF, 5-7HP in DMEM solution for 24 h and then treated with PMs for 2 h (p-JNK, p-ERK, and p-p38, B); 6 h (COX-2 and MMP-9, A); 24 h (AQP-3, C). n = 3 in each group; * p < 0.05 compared with the group of PMs.
Figure 11
The skin surface hydration in 21 volunteers before and after treatment with different concentrations of 734THIF of 5-7HP formulation at different times. (A) non-content of 734THIF, (B) 0.3% 734THIF and (C) 1% 734THIF (n = 7 in each group; * p < 0.05 compared with the group of zero weeks).
References
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