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解析丁香酸负载亚油酸传递体对痤疮的药物和临床相关性。

Unraveling the pharmaceutical and clinical relevance of the influence of syringic acid loaded linoleic acid transferosomes on acne.

机构信息

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, AinShams University, Monazzamet Elwehda Elafrikeya Street, P.O.B. 11566, Abbaseyya, Cairo, Egypt.

Department of Dermatology, STD's and Andrology, Faculty of Medicine, Minia University, Al-Minya, Egypt.

出版信息

Int J Pharm. 2023 May 25;639:122940. doi: 10.1016/j.ijpharm.2023.122940. Epub 2023 Apr 9.

DOI:10.1016/j.ijpharm.2023.122940
PMID:37040824
Abstract

Natural medicines are promising platforms for competent topical treatment modalities benefiting the cosmetic implementation and proffering solutions to the current remedies. Therefore, the objective of this study was to formulate syringic acid (SA), well-known for its multilateral anti-inflammatory, antimicrobial and antioxidant potentials, in newly developed linoleic acid (LA) transferosomes as an anti-acne nano-form remedy. Herein, LA was incorporated in transferosomes owing to its antimicrobial effect and dermal penetrability. Comprehensive appraisal through physicochemical, antioxidant and dermal deposition investigations was conducted. Clinical assessment was also performed in acne patients and compared with the marketed product (Adapalene® gel). The relevant investigations of the optimum formula indicated stable vesicles with a small-sized diameter (147.46 nm), surface charge (-26.86 mV), spherical architecture, reasonable entrapment (76.63%), considerable antioxidant activity (IC50 = 11.1 µg/mL) and remarkable skin deposition (78.72%).More importantly, LA based transferosomes enclosing SA exhibited inflammation lessening in acne sufferers as manifested by greater reduction in the total count of the acne lesions reaching 79.5% in contrast to Adapalene® gel with only 18.7% reduction in acne lesions. Interestingly, no irritation and erythema were reported for the proposed transferosomes. Inclusively, the cosmetic formulation practice could reap benefits of the development of such vesicles.

摘要

天然药物是一种很有前途的平台,可以为有能力的局部治疗方法提供支持,使美容实施受益,并为当前的治疗方法提供解决方案。因此,本研究的目的是将丁香酸(SA)制成新型的亚油酸(LA)转体纳米痤疮治疗药物,丁香酸以其多方面的抗炎、抗菌和抗氧化潜力而闻名。在此,由于其抗菌作用和皮肤穿透性,将 LA 掺入转体中。通过物理化学、抗氧化和皮肤沉积研究进行了全面评估。还在痤疮患者中进行了临床评估,并与市售产品(阿达帕林凝胶)进行了比较。对最佳配方的相关研究表明,具有小粒径(147.46nm)、表面电荷(-26.86mV)、球形结构、合理包封率(76.63%)、相当大的抗氧化活性(IC50=11.1µg/mL)和显著皮肤沉积率(78.72%)的稳定囊泡。更重要的是,载有 SA 的基于 LA 的转体在痤疮患者中减轻了炎症,表现在痤疮病变的总计数减少了 79.5%,而阿达帕林凝胶仅减少了 18.7%。有趣的是,所提出的转体没有引起任何刺激和红斑。总之,这种囊泡的开发为美容制剂实践带来了好处。

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