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用于痤疮治疗的宇宙-营养纳米囊泡:理化特性表征和探索性临床实验。

Cosm-nutraceutical nanovesicles for acne treatment: Physicochemical characterization and exploratory clinical experimentation.

机构信息

Department of Pharmaceutics, Faculty of Pharmacy and Drug Manufacturing, Pharos University in Alexandria, Alexandria, Egypt; Drug Discovery, Delivery and Patient Care (DDDPC) Theme, School of Life Sciences, Pharmacy and Chemistry, Department of Pharmacy, Kingston University London, Kingston upon Thames, Surrey, KT1 2EE, United Kingdom; Department of Chemistry, School of Sciences and Engineering, The American University in Cairo, Egypt.

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.

出版信息

Int J Pharm. 2020 Mar 15;577:119092. doi: 10.1016/j.ijpharm.2020.119092. Epub 2020 Jan 28.

Abstract

The full exploration of the 'nutraceuticals' therapeutic potential in cosmetics has been hindered by their poor stratum corneum permeation. Therefore, the aim of the present study was to formulate a nutraceutical; quercetin, in novel vitamin C based nanovesicles (aspasomes), and to explore their beneficial effects in the treatment of acne. Aspasomes were characterized for their particle size, zeta potential, entrapment efficiency (EE%), 3-months storage stability, skin deposition/permeation, antioxidant potential, and morphology. Aspasomes antibacterial efficacy on Propionibacterium acnes using the zone of inhibition assay was also tested, whilst their safety on skin fibroblastic cells was assessed in vitro using 3T3 CCL92 cell lines. An exploratory clinical trial was conducted in acne patients, and the percentage reduction of inflammatory, non-inflammatory and total acne lesions was taken as the evaluation criterion. Results revealed that quercetin-loaded aspasomes displayed a desirable nanometer size (125-184 nm), negative charge with good storage stability, and high skin deposition reaching 40%. Aspasomes managed to preserve the antioxidant activity of quercetin, and exhibited a significantly higher antibacterial effect (15 ± 1.53 mm) against Propionibacterium acnes than quercetin alone (8.25 ± 2.08 mm), and were safe on skin fibroblastic cells. Upon clinical examination in 20 acne patients (14 females, 6 males), quercetin aspasomes exhibited reduction percentages of 77.9%, 11.8% and 55.3% for inflammatory lesions, comedones and total lesions respectively. This opens vast applications of the presented formulation in the treatment of other oxidative skin diseases, and delineates the nutraceuticals and nanoformulations prepared from natural materials as promising dermatological treatment modes.

摘要

“营养保健品”在化妆品中的治疗潜力尚未得到充分开发,原因在于其在角质层中的渗透性较差。因此,本研究的目的是将一种营养保健品(槲皮素)制成新型维生素 C 纳米囊泡(aspasomes),并研究其在治疗痤疮中的有益作用。对 aspasomes 的粒径、zeta 电位、包封效率(EE%)、3 个月储存稳定性、皮肤沉积/渗透、抗氧化能力和形态进行了表征。还通过抑菌圈试验测试了 aspasomes 对痤疮丙酸杆菌的抗菌效果,并用 3T3 CCL92 细胞系评估了其对皮肤成纤维细胞的体外安全性。对痤疮患者进行了探索性临床试验,以炎症性、非炎症性和总痤疮病变的减少百分比作为评估标准。结果表明,载有槲皮素的 aspasomes 显示出理想的纳米尺寸(125-184nm)、带负电荷和良好的储存稳定性,皮肤沉积率达到 40%。aspasomes 成功地保留了槲皮素的抗氧化活性,并且对痤疮丙酸杆菌的抗菌效果明显高于单独使用槲皮素(15±1.53mm),对皮肤成纤维细胞也安全。在 20 名痤疮患者(14 名女性,6 名男性)的临床检查中,槲皮素 aspasomes 对炎症性病变、粉刺和总病变的减少百分比分别为 77.9%、11.8%和 55.3%。这为该制剂在治疗其他氧化皮肤疾病中的应用开辟了广阔的前景,并将来源于天然材料的营养保健品和纳米制剂描绘为有前途的皮肤科治疗模式。

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