Beijing Key Laboratory of Plant Resources Research and Development, College of Chemistry and Materials Engineering, Beijing Technology and Business University, Beijing 100048, China.
State Key Laboratory of Chemical Resource Engineering, College of Chemistry, Beijing University of Chemical Technology, Beijing 100029, China.
Int J Pharm. 2022 Jul 25;623:121903. doi: 10.1016/j.ijpharm.2022.121903. Epub 2022 Jun 11.
This paper presents a facile approach to develop palygorskite (Pal), a fibrous clay mineral, as a delivery system of tea tree oil (TTO) for topical acne therapy. The obtained TTO-Pal composite showed an efficient loading of TTO (27.4%) with a selective accumulation of terpine-4-ol and 1,8-cineole (two major antimicrobial TTO constituents), sustained release of TTO at skin physiological conditions (pH5.4, 32 °C) and superior skin sebum (2.2 g/g) absorbability. In vitro toxicological assessments showed that the Pal incorporation strategy significantly reduced the acute contact toxicity of TTO. The antimicrobial results revealed a preferable bacteriostatic effect for the TTO-Pal system towards opportunistic dermal pathogens (Escherichia coli, Staphylococcus aureus and Propionibacterium acnes) over the beneficial bacterium (Staphylococcus epidermis). Moreover, TTO-Pal based formulations exhibited pronounced clinical therapeutic efficacy in treating facial acne by rapidly reducing inflamed lesions, modulating skin sebum overproduction and restoring barrier function. This is the first report of using fibrous clay as a biocompatible nanocarrier system for topical delivery of essential oils in efficient management of facial acne with both in vitro and in vivo evidences, which may open perspectives for fibrous clay-drug delivery system in topical application and expand the high added value development of this mineral resource in the advanced healthcare fields.
本文提出了一种简便的方法，即用纤维状粘土矿物坡缕石（Pal）作为茶树油（TTO）的输送系统，用于局部痤疮治疗。所得的 TTO-Pal 复合材料对 TTO 具有高效的负载能力（27.4%），对萜品-4-醇和 1,8-桉树脑（两种主要的抗菌 TTO 成分）具有选择性积累，在皮肤生理条件（pH5.4，32°C）下可实现 TTO 的持续释放，并且对皮肤皮脂（2.2g/g）具有优异的吸收能力。体外毒理学评估表明，Pal 的掺入策略显著降低了 TTO 的急性接触毒性。抗菌结果表明，与有益菌（表皮葡萄球菌）相比，TTO-Pal 体系对机会性皮肤病原体（大肠杆菌、金黄色葡萄球菌和痤疮丙酸杆菌）具有更好的抑菌作用。此外，基于 TTO-Pal 的制剂在治疗面部痤疮方面表现出显著的临床治疗效果，可迅速减少炎症病变，调节皮脂过度生成并恢复屏障功能。这是首次报道将纤维状粘土作为生物相容性的纳米载体系统，用于通过体外和体内证据高效管理面部痤疮的精油的局部递送，这可能为纤维状粘土-药物传递系统在局部应用方面开辟前景，并扩大这种矿物资源在高级医疗保健领域的高附加值开发。
