CHEMICAL ENGINEERING JOURNAL
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2023
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IF 15.1
Mi Wang,Zhenyuan Wang,Jichuan Zhang,Liguo Zhang,Wei Wang,Jingbo Zhan,Ya Liao,Chengyu Wu,Wen Yu,Jiaheng Zhang
Salicylic acid (H[Sal]) is an attractive bionic acid that is widely used in cosmetics and drugs for the treatment of skin diseases, owing to its excellent anti-acne, anti-inflammatory, antibacterial, oil-control, stratum-corneum-conditioning, and anti-photoaging abilities. However, H[Sal] is a relatively strong irritant and cannot be used on sensitive skin, and its poor water solubility limits the amounts that can be included in formulas, resulting in poor transdermal efficiency and bioavailability. In this study, we develop matrinium salicylate ([Mat][Sal]), a supramolecular ionic salt that is less cytotoxic and irritates the skin less than H[Sal], while exhibiting enhanced water-solubility, transdermal-delivery, and bioactivity properties. The anticancer, antioxidant, anti-inflammatory, and antibacterial properties of [Mat][Sal] are found to be superior or comparable to those of H[Sal]. The molecular structure of [Mat][Sal] is thoroughly investigated, including through single-crystal structure refinement, to gain an in-depth understanding of its properties. Moreover, in-vitro skin penetration experiments show that forming a salt with matrine increase the transdermal efficiency of H[Sal] while not damaging the skin barrier. The transdermal mechanisms of H[Sal] and [Mat][Sal] are studied both experimentally and using molecular dynamics simulations, which show that, compared to H[Sal], [Mat][Sal] reacts more strongly with the skin, and [Sal] − diffuses more rapidly in the skin owing to its higher water solubility and the ion-pair effect. Furthermore, [Mat][Sal] exhibits satisfactory anti-acne capabilities in a clinical-efficacy trial, highlighting its great potential for use in biomedical and cosmetics applications.
研究领域:
药理学
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化妆品科学
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分子生物学
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF MOLECULAR STRUCTURE
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2025
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IF 4.7
Zhenyuan Wang,Tianqi Liu,Beibei Lu,Jichuan Zhang,Jingbo Zhan,Xiangli Liu,Mi Wang,Jiaheng Zhang
Caffeic acid (CA) is a sustainable bioactive compound with abundant skincare benefits; however, its poor solubility and stability make its clinical application challenging. In this study, a salt with abundant supramolecular interactions (SupCA) was prepared from CA and matrine to address these issues. The structure-activity relationship of SupCA was systematically studied using density functional theory, molecular docking, and molecular dynamics simulations. The supramolecular interactions in SupCA modified the electronic distribution of CA, leading to enhanced water solubility, stability, antioxidant ability, and affinity for key proteins in inflammatory signaling pathways. The skincare benefits of SupCA were comprehensively tested and compared with those of a mixture of CA and matrine to further investigate the impact of supramolecular interactions on the bioactivity of SupCA. A 28-day treatment with a SupCA emulsion reduced facial redness, a* value, fine lines under the eyes, and crow's feet wrinkles in participants by 65.62 %, 13.27 %, 45.07 %, and 38.09 %, respectively, which were significantly superior to those of the mixture emulsion. This demonstrated the vital role of supramolecular interactions in enhancing bioactivity, consistent with the calculation findings. In addition, SupCA exhibited excellent anti-acne, skin repair, and whitening properties, with no adverse responses and 100 % user satisfaction, making it a safe, versatile, and efficient ingredient in cosmetics.
研究领域:
化妆品科学
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超分子化学
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皮肤科学研究
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计算化学
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天然产物
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
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2024
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IF 4.5
Qinghua Yang,Zhuoni Liu,Tianxiang Yin,Xiaoyong Wang,Jing Yuan
Deep eutectic solvents (DESs), as a new type of green and easily designable solvent, showed great potential applications in various fields. In this work, a novel deep eutectic solvent based on active pharmaceutical ingredient matrine and lauric acid was developed. The structure, thermal stability, and cytotoxicity were investigated by various technologies. The prepared DES displayed excellent ability on enhancing the solubility of curcumin, and the curcuim showed high stability in DES. Moreover, DES as well as curcumin-contained DES possessed good antioxidant and anti- P. acne activity. More importantly, the prepared DES can act as a gelator to form eutectogel in water, which was confirmed from the rheological behavior and scanning electron microscope (SEM) measurement. The curcumin-contained eutectogel displayed good injectable and permeation ability. Therefore, the prepared multi-functional DES (i.e. antioxidant, antibacterial agent, solvent and stabilizer of curcumin, and gelator) provides a new strategy to construct transdermal delivery system that displays potential application on treatment of acne infection.
研究领域:
药学
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材料科学
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化学
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生物技术
✓ 已验证
产品关联
DOI
高影响因子
CARBOHYDRATE POLYMERS
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2024
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IF 10.7
Noor Ul Ain,Bibimaryam Khan,Kehan Zhu,Wen Ji,He Tian,Xiaoxiao Yu,Lin Yi,Duxin Li,Zhenqing Zhang
Glycyrrhizae Radix et rhizome/licorice is a precious herb in traditional Chinese medicine (TCM). TCM's polysaccharides are medicinally active. But herbal polysaccharides pose some limitations for topical applications. Therefore, this study aimed to utilize licorice polysaccharide via mesoporous silica nanoparticles (MSN) for anti-acne efficacy in topical delivery. The polysaccharide (GGP) was extracted with a 10 % NaOH solution. Chemical characterization suggested that GGP possesses an Mw of 267.9 kDa, comprised primarily of Glc (54.1 %) and Ara (19.12 %), and probably 1,4-linked Glc as a backbone. Then, MSN and amino-functionalized MSN were synthesized, GGP entrapped, and coated with polydopamine (PDA) to produce nanoparticle cargo. The resulted product exhibited 76 % entrapment efficiency and an in vitro release of 89 % at pH 5, which is usually an acne-prone skin's pH. Moreover, it significantly increased Sebocytes' cellular uptake. GGP effectively acted as an anti-acne agent and preserved its efficacy in synthesized nanoparticles. In vivo , the results showed that a 20 % gel of MSN-NH 2 -GGP@PDA could mediate an inflammatory response via inhibiting pro-inflammatory cytokines and regulating anti-inflammatory cytokines. The MSN-NH 2 -GGP@PDA inhibited TLR2-activated-MAPK and NF-κB pathway triggered by heat-killed P. acnes . In conclusion, fabricated MSN entrapped GGP for biomimetic anti-acne efficacy in topical application.
研究领域:
药学
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纳米技术
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皮肤科
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传统中药
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Journal of Functional Foods
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2020
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IF 3.701
ShiFa Ruan,ShiJian Xiang,WenFeng Wu,SiWei Cao,QunQun Du,ZhuXian Wang,TingTing Chen,Qun Shen,Li Liu,HuoJi Chen,LiDong Weng,HongXia Zhu,Qiang Liu
We applied a label-free proteomic method to explore the mechanisms of Licorice flavonoid anti-acne effects in rat. Acne model was established in the back of rats as model group (MDL), then treated with licorice flavonoid (LCF), while none treated rats as control groups (CTR). In MDL, 314 differentially expressed proteins (DEPs) and 27 significantly differentially expressed proteins (SDEPs) were identified compared to what was identified in CTR. While in LCF, 359 DEPs and 15 SDEPs were identified in comparison to MDL. Bioinformatics analysis showed that pathways related to metabolism, tight junction, PI3K-Akt signaling, focal adhesion, regulation of actin cytoskeleton, and leukocyte transendothelial migration were activated. The results of proteomics data were validated by qRT-PCR and western blot. Transdermal administration of LCF may exert anti-acne effects by inhibiting PI3K-Akt signaling pathway and mitochondrial activity. Hence, our results elucidated the underlying mechanisms of LCF anti-acne effect.
研究领域:
药理学
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皮肤科
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蛋白质组学
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分子生物学
✓ 已验证
产品关联
DOI
高影响因子
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
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2021
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IF 4.384
Mengzhen Xing,Guozhong Yang,Suohui Zhang,Yunhua Gao
To overcome the poor solubility, skin irritation, and low permeability of azelaic acid (AZA) existed on the marketed formulations, a co-drug principle via matrine (MAT) was adopted to prepare anti-acne dissolving microneedles (DMNs). The formula was optimized according to the solubility and antibacterial activity of novel ionic salt. The results indicated solubilization of AZA could be achieved at a molar ratio between AZA and MAT was 1:1. Meanwhile, synergistic antibacterial and anti-irritative properties were acquired. The matrix materials were composed of sodium carboxymethyl cellulose (CMC), polyvinylpyrrolidone (PVP), and trehalose. And drug loadings of AZA and MAT in DMNs were 201.88 ± 4.81 µg and 259.71 ± 1.72 µg, respectively. After insertion into porcine skin for 10 h, the cumulative permeability of AZA and MAT were 68.16% ± 3.79% and 57.37 ± 5.17%, respectively, while just 4.13 ± 0.39% ( p < 0.01) was detected for commercially available AZA gel. In vitro antibacterial experiment, bacteriostatic rates of DMNs were all above 95% for Staphylococcus aureus, Staphylococcus epidermidis , and Propionibacterium acnes . Besides, DMNs exhibited no cytotoxicity and skin irritation. In conclusion, combination between AZA and MAT addressed shortcomings of AZA, and made it easier, safer, and more effective in acne treatment.
研究领域:
药学
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皮肤科
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药物递送系统
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化妆品科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）