Abstract Nanotechnology has been applied in the medicine field to improve the treatment of a wide range of diseases. However, to reach the nanomedicines delivery to desirable target tissue for promote an enhancement of pharmacological activity, these nanomedicines must overcome biological barriers, such as mucus gel, skin, corneal and blood-brain barriers. Aiming the increase nanomedicines permeation through these barriers, surface modifications of nanocarriers with permeation enhancers and/or specific ligands for cellular receptors have been widely investigated. Among these modifications, d-α-Tocopheryl polyethylene glycol 1000 succinate (TPGS) is a biocompatible macromolecule that has been evaluated as a permeation enhancer. TPGS is a non-ionic surfactant composed by the natural vitamin E bonded with polyethylene glycol 1000 (PEG) and its composition have been responsible to enhance cellular internalization and permeation of nanomedicines through biological barriers. In addition, this molecule has acted as solubilizer, emulsifier, stabilizer and P-glycoprotein (P-gp) inhibitor, that are important features to manufacture nanomedicines with suitable to overcome barriers and multidrug resistance (MDR) mechanisms. This review will address the TPGS physicochemical and biological features and its most recent application in nanomedicine field to overcome biological barriers.

中文翻译：

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在药物递送系统中使用 TPGS 克服生物障碍

摘要 纳米技术已应用于医学领域，以改善对多种疾病的治疗。然而，为了将纳米药物输送到所需的靶组织以促进药理活性的增强，这些纳米药物必须克服生物屏障，如粘液凝胶、皮肤、角膜和血脑屏障。为了通过这些屏障增加纳米药物的渗透，已经广泛研究了具有渗透增强剂和/或细胞受体特异性配体的纳米载体的表面修饰。在这些修饰中，d-α-生育酚聚乙二醇 1000 琥珀酸酯 (TPGS) 是一种生物相容性大分子，已被评估为渗透促进剂。TPGS 是一种非离子表面活性剂，由与聚乙二醇 1000 (PEG) 结合的天然维生素 E 组成，其成分负责通过生物屏障增强纳米药物的细胞内化和渗透。此外，该分子还起到增溶剂、乳化剂、稳定剂和 P-糖蛋白 (P-gp) 抑制剂的作用，这些是制造适合克服障碍和多药耐药 (MDR) 机制的纳米药物的重要特征。本综述将讨论 TPGS 的理化和生物学特征及其在纳米医学领域的最新应用，以克服生物障碍。稳定剂和 P-糖蛋白 (P-gp) 抑制剂，这是制造适合克服障碍和多药耐药 (MDR) 机制的纳米药物的重要特征。本综述将讨论 TPGS 的理化和生物学特征及其在纳米医学领域的最新应用，以克服生物障碍。稳定剂和 P-糖蛋白 (P-gp) 抑制剂，这是制造适合克服障碍和多药耐药 (MDR) 机制的纳米药物的重要特征。本综述将讨论 TPGS 的理化和生物学特征及其在纳米医学领域的最新应用，以克服生物障碍。