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JOURNAL OF DERMATOLOGICAL TREATMENT · 2024 · IF 2.9

The adjuvant treatment role of ω-3 fatty acids by regulating gut microbiota positively in the acne vulgaris

Yaxin Huang,Fuming Liu,Jindong Lai,Shiyu Jiang,Xiaoqi Tan,Lingna Chen,Yong Xu,Xia Xiong,Yongqiong Deng

Objectives:We aimed to explore the potential role of omega-3 (ω-3) fatty acids on acne vulgaris by modulating gut microbiota.Materials and Methods:We randomly divided the untreated acne patients into two groups with or without ω-3 fatty acids intervention for 12 weeks. The Sprague Dawley (SD) rats with acne model were given isotretinoin, ω-3 fatty acids or their combination respectively. Then the colonic contents samples of the drug intervention SD rats were transferred to the pseudo sterile rats with acne model. The severity of the disease was assessed by the Global Acne Grading System (GAGS) score of the patients, and the swelling rate of auricle and the pathological section of the rat with acne model. The 16S rDNA gene sequencing was performed to detect the alteration of the gut microbiota.Results:ω-3 fatty acids could increase the diversity of the gut microbiota and regulate the flora structure positively both in the patients and rats, increase the abundance of butyric acid producing bacteria and GAGS score in the patients, and alleviate the inflammation and comedones of rats.Conclusion:Supplementation of ω-3 fatty acids could alleviate the inflammation of acne vulgaris by increasing the abundance of butyric acid producing bacteria.

CAS / MDL: 8001-22-7
研究领域: 皮肤科 · 微生物学 · 营养学
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JOURNAL OF ETHNOPHARMACOLOGY · 2025 · IF 5.4

Essential oil of Saposhnikovia divaricata mitigates Cutibacterium acnes-induced inflammatory acne via Nrf2 pathway activation and NF-κB pathway inhibition

Song-Xue Yang,Wei-Lie Xiao,Xing-Jie Zhang

Ethnopharmacological relevance The root of Saposhnikovia divaricata has been traditionally used in Chinese medicine to treat inflammation and immune related skin diseases, such as skin allergy and itchy rash. However, scientific research supporting its efficacy, particularly in curing inflammation from acne, is still scarce. Aim of the study To evaluate the therapeutic effects of essential oil of Saposhnikovia divaricata (EOSD) on Cutibacterium acnes ( C. acnes )-induced acne and investigate its mechanisms. Materials and Methods An acute acne model was established by injecting C. acnes into mouse ears, followed by topical EOSD treatment (0.25 %, 0.5 % and 1 %). Ear tissues were analyzed 24 hours post-treatment. In vitro, C. acnes -stimulated J774A.1 macrophages were treated with EOSD (3, 10 and 30 μg/ml) to assess mitochondrial damage, oxidative stress, and inflammatory responses. Key markers were analyzed using electron microscopy, real-time PCR, immunoblotting, ELISA, and immunofluorescence. Nrf2 knockdown was achieved via siRNA transfection. Results C. acnes suppressed Nrf2 activation, increased ROS levels, and triggered NLRP3 inflammasome activation, leading to inflammation. EOSD restored Nrf2 activity, reduced ROS levels, and inhibited NLRP3 activation. In vitro, EOSD disrupted Nrf2/Keap1 interaction, enhanced Nrf2 nuclear translocation, reduced mitochondrial damage, and suppressed pyroptosis by downregulating IL-1β, Caspase-1, GSDMD, and NF-κB signaling. These effects were reversed by Nrf2 knockdown. Conclusion EOSD alleviates oxidative stress and modulates NLRP3 inflammasome activation through upregulating Nrf2 pathway and inhibiting NF-κB pathway, as well as improving mitochondrial homeostasis and inflammatory responses in acne. These findings suggest that EOSD may be a promising therapeutic agent for the treatment of acne vulgaris.

研究领域: 药理学 · 皮肤科学 · 分子生物学 · 天然药物化学 · 免疫学 · 氧化应激研究 · 信号转导
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Drug Delivery and Translational Research · 2025 · IF 5.5

Microneedle-mediated delivery of hydroxypropyl-β-cyclodextrin-encapsulated Angelica sinensis (Danggui) essential oil for acne treatment: efficacy and mechanisms

Liu Xiaoli,Li Xiaojuan,He Weijun,Han Xiaoyu,Xiao Ting,Guo Shiqi,Jia Yujie,Lin Liqun,Yang Ming,Wang Li,Xu Yuehong

Acne is a multifactorial dermatological condition driven by Propionibacterium acnes ( P. acnes ) infection, inflammation, and sebum dysregulation. While essential oils, such as Angelica sinensis (Danggui) essential oil (AEO), exhibit antimicrobial and anti-inflammatory properties, their clinical application is hindered by poor solubility, stability, and skin penetration. To address these limitations, we developed hydroxypropyl- β -cyclodextrin (HPCD)-complexed AEO-loaded microneedles (AEO@HPCD MNs) using hyaluronic acid for enhanced transdermal delivery. The optimized AEO@HPCD MNs demonstrated superior mechanical strength, rapid dissolution, and efficient cargo release. In vitro studies confirmed potent antibacterial activity against P. acnes , while in vivo experiments revealed significant reductions in acne lesion size and IL-1 β levels. RNA sequencing of treated acne lesions identified key downregulated genes ( Fpr1 , Rarres2 , Cxcl5 , Gbp3 , Hck , Gbp7 , Librb4a , Psmb8 ) and enriched pathways, including innate immunity and inflammatory responses. Notably, AEO@HPCD MNs suppressed 5 α -reductase and fatty acid synthase (FAS) expression, demonstrating—for the first time—AEO’s ability to normalize sebum production. Mechanistically, AEO@HPCD MNs exert multifaceted therapeutic effects: (1) direct antibacterial activity against P. acnes , (2) suppression of inflammatory and immune-related pathways through modulation of Toll-like receptor, NOD-like receptor, and cytokine-cytokine receptor signaling pathways, (3) regulation of sebum production via lipid-metabolic gene expression modulation, and (4) enhanced delivery efficiency and microenvironment modification through the physical action of microneedles, collectively contributing to synergistic acne therapy. This study develops a microneedle delivery platform that addresses both essential oil instability and inclusion complex delivery challenges while targeting multiple acne pathogenic factors. The AEO@HPCD MNs provide a safe, minimally invasive, multifunctional therapeutic strategy for acne treatment.

研究领域: 药剂学 · 皮肤科 · 药理学 · 纳米技术 · 生物信息学 · 微生物学 · 植物学
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JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY · 2024 · IF 4.5

Eutectogel based on multi-functional deep eutectic solvent for acne infection treatment

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.

CAS / MDL: 67-68-5 56-85-9
研究领域: 药学 · 材料科学 · 化学 · 生物技术
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Natural Product Communications · 2022 · IF 1.496

Honokiol Improves Acne-like Lesions in a Rabbit Ear Model by Alleviating Hyperkeratosis and Sebum Secretion

Yuyan Zhu,Lixia Zhang,Xiyuan Zhou

The prevalence of acne vulgaris is high, but the topical retinoids used as the foundation of treatment have teratogenic and photosensitivity properties. Previous studies have suggested that honokiol, a small-molecule compound extracted from Magnolia officinalis, could effectively inhibit Cutibacterium acnes (C acnes) and inflammation in vitro. However, the effect in vivo is unclear. The rabbit ear acne model that we created showed obvious comedones and hyperkeratosis. These lesions were repeatedly measured and recorded by dermatoscopy (ultraviolet light). Compared with the control group, topical 2.5% honokiol cream obviously improved the comedones and hyperkeratosis and effectively reduced sebum secretion, as shown by Oil Red O staining. The effects were equivalent to those of adapalene gel without local side effects. We added honokiol's other functions to acne treatment in addition to antiinflammation, but further studies are needed.

CAS / MDL: 35354-74-6
研究领域: 皮肤病学 · 分子生物学
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FIBERS AND POLYMERS · 2021 ·Vol. 22 ·期 2 ·323-333 · IF 2.153

Fabrication and Characterization of Multiple Herbal Extracts-loaded Nanofibrous Patches for Topical Treatment of Acne Vulgaris

Tang Ying,Liu Lei,Han Jinju,Zhang Zhaolun,Yang Shuyan,Li Shuxian,Fan Zhanhua,Zhao Hua

Herbal extracts have recently received considerable interest in acne therapy owing to their enhanced skin compatibility compared with antibiotics and synthetic agents. In this study, electrospun poly (vinyl alcohol)/chitosan (PVA/CS) fibrous patch incorporating a combination of herbal extracts with complementary mechanisms of action was developed as an alternative acne therapy for patients with resistance to the conventional treatments. The herbal extracts-loaded electrospun fibers displayed uniform and smooth-surfaced nanofibers (dia. 100–300 nm), high drug loading efficiency (89.5–97.7 %) and good water absorbing properties. Results of the in vitro release and antibacterial studies suggest the patches are capable of sustained release of polyphenol-rich extracts, which may, together with the chitosan present in the fiber, endow the patch with potent bacterial inhibition of Propionibacterium acnes . The herbal extracts-loaded patches exhibited pronounced clinical therapeutic efficacy in treating mild-to-moderate facial acne by rapidly reducing inflamed lesions and restoring epidermal barrier. Also, the herbal patches demonstrated improved biocompatibility or tolerability in comparison with the synthetic drug benzoyl peroxide. Overall, the present study has provided a facile approach to develop biocompatible polymers based electrospun fibrous patch for the efficient delivery of herbal extracts for topical skin therapy, opening new perspectives for a new generation of cosmetotextiles.

研究领域: 药学 · 材料科学 · 皮肤科 · 生物技术
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CHROMATOGRAPHIA · 2022 ·Vol. 85 ·期 12 ·1017-1028 · IF 2.213

Simultaneous Determination of 37 Anti-infective Drugs Potentially Illegally Added to Cosmetics that Claimed to have Anti-acne Effects by UHPLC-Q-TOF HRMS

Gao Yanlin,Chen Cen,Wang Ren,Li Zehua,Cheng Qiaoyuan

Currently, illegal addition of anti-infective drugs has been detected in some cosmetics to achieve rapid sterilization and anti-inflammatory effects. However, the abuse of anti-infective drugs may endanger the health of citizens. Thus, methods for the detection and quantitative determinations of such substances should be developed. In this paper, a method combining ultra-high-performance liquid chromatography with quadrupole time-of-flight mass spectrometry (UHPLC-Q-TOF HRMS) was designed. Its significance and potential were verified by the identification, confirmation, and quantification of 37 illegally added anti-infective drugs in cosmetics that claimed to have anti-acne effects. The method validation revealed a satisfactory linear relationship, and each coefficient of determination ( r 2 ) was higher than 0.9943. The LOD and LLOQ results were in the ranges of 0.0003–0.1063 μg g −1 and 0.0012–0.3545 μg g −1 , respectively. The accuracy ranged from 70.8 to 122.8%, whereas the intra- and inter-day precisions were in the ranges of 0.2–12.8% and 0.2–13.8%, correspondingly. The mean recoveries were in the range of 70.1–117.7%, and the matrix effects ranged from 73.0 to 121.4%. Of the 200 batches of cosmetics that claimed to have anti-acne effects, three batches were positive, with chemical components such as metronidazole, lincomycin, clindamycin, tinidazole and miconazole nitrate being discovered. Therefore, the Q-TOF spectrometry could be widely applied in routine screening of adulteration in cosmetics.

CAS / MDL: 1220-83-3
研究领域: 分析化学 · 药学 · 医学
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ACS Applied Materials & Interfaces · 2021 · IF 9.229

Bioresponsive Nanoarchitectonics-Integrated Microneedles for Amplified Chemo-Photodynamic Therapy against Acne Vulgaris

Ting Wen,Zhiyuan Lin,Yiting Zhao,Yixian Zhou,Boyi Niu,Chaonan Shi,Chao Lu,Xinguo Wen,Minmin Zhang,Guilan Quan,Chuanbin Wu,Xin Pan

The excessive colonization of Propionibacterium acnes (P. acnes) is responsible for the genesis of acne vulgaris, a common inflammatory disease of skin. However, the conventional anti-acne therapies are always limited by various side effects, drug resistance, and poor skin permeability. Microneedles (MNs) are emerging topical drug delivery systems capable of noninvasively breaking through the skin stratum corneum barrier to efficiently enhance the transdermal drug penetration. Herein, MNs loaded with intelligent pH-sensitive nanoplatforms were constructed for amplified chemo-photodynamic therapy against acne vulgaris, jointly exerting antimicrobial and anti-inflammatory effects. The photosensitizer indocyanine green (ICG) was loaded into the zeolitic imidazolate framework-8 (ZIF-8) to improve its photostability, which would be triggered by 808 nm laser irradiation to generate cytotoxic reactive oxygen species (ROS) to result in oxidative damage and disturbed metabolic activities of P. acnes. In addition to the efficient drug delivery, the ZIF-8 carrier could selectively degrade in response to the acidic microenvironment of acne lesions, and the released Zn2+ also exhibited a potent antimicrobial activity. The fabricated ZIF-8-ICG@MNs presented an outstanding synergistic anti-acne efficiency both in vitro and in vivo. This bioresponsive microneedle patch is expected to be readily adapted as a generalized, modular strategy for noninvasive therapeutics delivery against superficial skin diseases.

研究领域: 药学 · 纳米技术 · 皮肤病学 · 治疗递送系统
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NANOTECHNOLOGY · 2023 · IF 3.5

Strong infiltrative HHC36 antimicrobial peptide/silver nanoparticles-loaded carboxymethyl chitosan/sodium alginate hydrogel for acne vulgaris therapy

Hongju Liu,Jiezhao Zhan,Ruibin Lin,Ying Yin,Li Ren

Acne is a common chronic skin inflammatory disease closely related to Cutibacterium acnes (C. acnes), which affects the life quality of patients worldwide, especially adolescents and young adults. However, the physical barrier of the skin makes drugs difficult to infiltrate effectively into infected site, causing acne hard to cure and easy to recur. Herein, we developed an antibacterial skin dressing with strong infiltration of antibacterial agents which can co-delivery small-molecular antimicrobial agents through stratum corneum deeply into dermis, achieving high antimicrobial efficacy. The antibacterial dressings were constructed with carboxymethyl chitosan/sodium alginate (CMCS/SA) hydrogel loading with HHC36 (an antimicrobial peptide) and silver nanoparticles (AgNPs) conjugates (Ag-H2/CMCS/SA hydrogel). The released Ag-H2 from Ag-H2/CMCS/SA hydrogel can early infiltrate into dermis, co-delivery HHC36 and AgNPs due to the infiltration and targeting of HHC36, presenting the superior antibacterial effect compared to HHC36 or AgNPs alone and killing 100% C. acnes and 100% Staphylococcus epidermidis (S. epidermidis) at a very low concentration of Ag-H2 (15 μg/mL Ag with 7.1 μg/mL HHC36). Meanwhile, Ag-H2/CMCS/SA hydrogel was biocompatible due to the natural polysaccharides carboxymethyl chitosan and sodium alginate. The HaCaT cells spread well in Ag-H2/CMCS/SA hydrogel extracts. These results indicate that the co-delivery small-molecular antimicrobial agents is a promising strategy and Ag-H2/CMCS/SA hydrogel has a great potential in the therapy of acne.

研究领域: 药学 · 材料科学 · 生物医学工程 · 皮肤科
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CHEMICAL ENGINEERING JOURNAL · 2023 · IF 15.1

A matrine-based supramolecular ionic salt that enhances the water solubility, transdermal delivery, and bioactivity of salicylic acid

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 · 化妆品科学 · 分子生物学
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ACS Applied Materials & Interfaces · 2024 · IF 8.3

Dissolving Hyaluronic Acid-Based Microneedles to Transdermally Deliver Eugenol Combined with Photothermal Therapy for Acne Vulgaris Treatment

Qi Wang,Zhiyang Gan,Xinxin Wang,Xinying Li,Lei Zhao,Derong Li,Zhilang Xu,Changdao Mu,Liming Ge,Defu Li

A microneedle transdermal drug delivery system simultaneously avoids systemic toxicity of oral administration and low efficiency of traditional transdermal administration, which is of great significance for acne vulgaris therapy. Herein, eugenol-loaded hyaluronic acid-based dissolving microneedles (E@P-EO-HA MNs) with antibacterial and anti-inflammatory activities are developed for acne vulgaris therapy via eugenol transdermal delivery integrated with photothermal therapy. E@P-EO-HA MNs are pyramid-shaped with a sharp tip and a hollow cavity structure, which possess sufficient mechanical strength to penetrate the stratum corneum of the skin and achieve transdermal delivery, in addition to excellent in vivo biocompatibility. Significantly, E@P-EO-HA MNs show effective photothermal therapy to destroy sebaceous glands and achieve antibacterial activity against deep-seated Propionibacterium acnes (P. acnes) under near-infrared-light irradiation. Moreover, cavity-loaded eugenol is released from rapidly dissolved microneedle bodies to play a sustained antibacterial and anti-inflammatory therapy on the P. acnes infectious wound. E@P-EO-HA MNs based on a synergistic therapeutic strategy combining photothermal therapy and eugenol transdermal administration can significantly alleviate inflammatory response and ultimately facilitate the repair of acne vulgaris. Overall, E@P-EO-HA MNs are expected to be clinically applied as a functional minimally invasive transdermal delivery strategy for superficial skin diseases therapy in skin tissue engineering.

研究领域: 药学 · 皮肤科 · 纳米技术 · 治疗工程 · 生物医学工程
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JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY · 2025 · IF 4.9

Cyclodextrin-based supramolecular dissolving microneedles for enhanced transdermal delivery of azelaic acid in acne vulgaris treatment

Yuxu Chen,Yuanyu Xu,Jingqing Zhang,Xinjun Xu

Acne vulgaris is a common skin condition affecting individuals of various age groups, significantly impacting their quality of life. Although azelaic acid (AZA) is widely used in acne treatment due to its anti-inflammatory, antibacterial, and tyrosinase inhibitory properties, its low aqueous solubility limits its transdermal absorption and reduces therapeutic efficacy. Dissolving microneedles (DMNs), fabricated from water-soluble materials, have shown great potential as a strategy for improving transdermal drug delivery. However, DMNs face challenges in encapsulating poorly soluble drugs like AZA. In this study, we developed cyclodextrin-based supramolecular DMNs loaded with AZA, in which the microneedles are composed entirely of inclusion complexes to enhance the transdermal delivery efficiency of AZA for treating acne. AZA was encapsulated into hydroxypropyl-β-cyclodextrin (HP-β-CD) and sulfobutylether-β-cyclodextrin (SBE-β-CD) using a solvent evaporation technique, resulting in respective 34.9-fold and 25.4-fold increases in AZA solubility. The inclusion complexes demonstrated superior antibacterial activity in inhibition zone assays and enhanced tyrosinase inhibitory activity compared to free AZA in aqueous solution, suggesting enhanced dispersion and biological activity. The DMNs exhibited excellent mechanical strength and maintained a high drug-loading capacity of AZA, facilitating efficient penetration through the stratum corneum. In vitro permeation test showed 24-h percutaneous permeability rates at 68.69 ± 3.79 % and 73.59 ± 4.23 % for AZA/HP-β-CD DMNs and AZA/SBE-β-CD DMNs, respectively. Additionally, the DMNs demonstrated no cytotoxicity toward L929 cells and displayed hemocompatibility. Overall, the developed supramolecular DMNs system presents a promising approach for enhancing the transdermal delivery of AZA, with the potential to enhance therapeutic outcomes in acne treatment.

CAS / MDL: 9002-10-2
研究领域: 药剂学 · 皮肤病学 · 生物医学工程
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