Drug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University, 399 Royal Parade, Parkville, VIC, 3052, Australia.
Pharm Res. 2023 Jan;40(1):245-263. doi: 10.1007/s11095-022-03424-6. Epub 2022 Nov 14.
Liposomes are sphere-shaped vesicles that can capture therapeutics either in the outer phospholipid bilayer or inner aqueous core. Liposomes, especially when surface-modified with functional materials, have been used to achieve many benefits in drug delivery, including improving drug solubility, oral bioavailability, pharmacokinetics, and delivery to disease target sites such as cancers. Among the functional materials used to modify the surface of liposomes, the FDA-approved non-ionic surfactant D-alpha-tocopheryl polyethylene glycol succinate (TPGS) is increasingly being applied due to its biocompatibility, lack of toxicity, applicability to various administration routes and ability to enhance solubilization, stability, penetration and overall pharmacokinetics. TPGS decorated liposomes are emerging as a promising drug delivery system for various diseases and are expected to enter the market in the coming years. In this review article, we focus on the multifunctional properties of TPGS-coated liposomes and their beneficial therapeutic applications, including for oral drug delivery, vaccine delivery, ocular administration, and the treatment of various cancers. We also suggest future directions to optimise the manufacture and performance of TPGS liposomes and, thus, the delivery and effect of encapsulated diagnostics and therapeutics.
脂质体是呈球形的囊泡，可以将治疗剂包裹在磷脂双层的外部或内部水相中。脂质体，特别是经过功能材料表面修饰后，已被用于实现药物输送的许多益处，包括提高药物溶解度、口服生物利用度、药代动力学以及递送至疾病靶标部位，如癌症。在用于修饰脂质体表面的功能材料中，由于其生物相容性、低毒性、适用于各种给药途径以及能够增强增溶、稳定性、穿透性和整体药代动力学，已越来越多地应用经 FDA 批准的非离子表面活性剂 D-α-生育酚聚乙二醇琥珀酸酯（TPGS）。TPGS 修饰的脂质体作为一种有前途的药物输送系统，正在各种疾病的治疗中得到应用，并有望在未来几年进入市场。在这篇综述文章中，我们重点介绍了 TPGS 涂层脂质体的多功能特性及其在治疗中的有益应用，包括口服药物输送、疫苗输送、眼部给药以及各种癌症的治疗。我们还提出了未来的方向，以优化 TPGS 脂质体的制造和性能，从而改善封装的诊断和治疗剂的输送和效果。
