维生素E TPGS的医药应用

A. M. Jasim, M. Jawad
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引用次数: 3

摘要

d -生育酚基聚乙二醇琥珀酸酯(维生素E TPGS)已被FDA批准为一种安全的药物佐剂,并已开发出几种基于TPGS的给药系统(DDS)。本文综述了TPGS作为P-gp抑制剂、增溶剂/吸收剂和渗透增强剂在药物传递中的性能,以及TPGS在纳米晶体、纳米悬浮液、片剂/固体分散体、疫苗系统佐剂、营养补充剂、薄膜增塑剂、抗癌试剂等相关制剂中的应用。因此,TPGS可以抑制atp依赖性p -糖蛋白活性,并作为一种有效的赋形剂,促进药物的递送效率和治疗效果。P-gp的抑制是通过线粒体依赖性的P-gp泵抑制而发生的。许多最新的研究解决了在纳米药物或其他配方的制造中,将TPGS用于许多水溶性或渗透性差的药物。此外,有报道称,TPGS在低浓度下可显著改善乳糜微粒分泌,改善肠道淋巴运输,从而提高药物吸收潜力。这也表明基于TPGS的纳米药物的临床转化仍面临许多问题,需要更深入地评估TPGS的性质和基于未来的递送方法。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Pharmaceutical Applications of Vitamin E TPGS
D-tocopheryl polyethylene glycol succinate (Vitamin E TPGS) has been approved as a safe pharmaceutical adjuvant by FDA, and several drug delivery systems (DDS) based on TPGS have been developed. TPGS properties as a P-gp inhibitor, solubilizer/absorption and permeation enhancer in drug delivery and TPGS-related formulations such as nanocrystals, nanosuspensions, tablets/solid dispersions, vaccine system adjuvant, nutritional supplement, film plasticizer, anticancer reagent, and so on, are discussed in this review. Consequenly, TPGS can inhibit ATP-dependent P-glycoprotein activity and act as a potent excipient that promotes the efficiency of delivery and the therapeutic effect of drugs. Inhibition of P-gp occurs through mitochondria-dependent inhibition of the P-gp pump. Many of the latest studies address the use of TPGS for many poorly water-soluble or permeable drugs in the manufacture of nanodrugs or other formulations. In addition, it has been reported that TPGS shows a robust improvement in chylomicron secretion at low concentrations and improves intestinal lymphatic transport, which would also boost the potential of drug absorption. It also indicates that there are still many problems facing clinical translation of TPGS-based nanomedicines, requiring a more deep evaluation of TPGS properties and a future-based delivery method.
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