Ethosome represents a smart transdermal vehicle suitable for solubilization and cutaneous application of drugs. Coenzyme Q10 is an endogenous antioxidant whose supplementation can counteract many cutaneous disorders and pathologies. In this respect, the present study describes the production, characterization, and cutaneous protection of phosphatidylcholine based ethosomes as percutaneous delivery systems for coenzyme Q10. CoQ10 entrapment capacity in ethosomes was almost 100%, vesicles showed the typical ‘fingerprint’ structure, while mean diameters were around 270 nm, undergoing an 8% increase after 3 months from production. An ex-vivo study, conducted by transmission electron microscopy, could detect the uptake of ethosomes in human skin fibroblasts and the passage of the vesicles through 3D reconstituted human epidermis. Immunofluorescence analyses were carried on both on fibroblasts and 3D reconstituted human epidermis treated with ethosomes in the presence of H₂O₂ as oxidative stress challenger, evaluating 4-hydroxynonenal protein adducts which is as a reliable biomarker for oxidative damage. Notably, the pretreatment with CoQ10 loaded in ethosomes exerted a consistent protective effect against oxidative stress, in both models, fibroblasts and in reconstituted human epidermis respectively.

中文翻译：

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用于辅酶 Q10 皮肤给药的醇质体：从设计到 3D 皮肤组织评估。


Ethosome 是一种智能透皮载体，适用于药物的溶解和皮肤应用。辅酶 Q10 是一种内源性抗氧化剂，补充它可以对抗许多皮肤疾病和病理。在这方面，本研究描述了基于磷脂酰胆碱的乙醇体作为辅酶 Q10 经皮递送系统的生产、表征和皮肤保护。 CoQ10在醇质体中的包封率几乎为100%，囊泡呈现典型的“指纹”结构，平均直径在270 nm左右，生产3个月后增加了8%。通过透射电子显微镜进行的离体研究可以检测人体皮肤成纤维细胞对醇质体的摄取以及囊泡通过 3D 重建人体表皮的情况。在 H ₂ O ₂作为氧化应激挑战物的情况下，对用醇质体处理的成纤维细胞和 3D 重建人表皮进行了免疫荧光分析，评估了 4-羟基壬烯醛蛋白加合物，它是氧化损伤的可靠生物标志物。值得注意的是，在两种模型、成纤维细胞和重建的人表皮中，用乙醇体中负载的 CoQ10 进行预处理分别对氧化应激产生了一致的保护作用。