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硫醇盐:形式、功能及其在纳米医学中的应用

Thiomers: forms, functions and applications to nanomedicine.

作者信息

Albrecht Karin, Bernkop-Schnürch Andreas

机构信息

Leopold-Franzens-University Innsbruck, Institute of Pharmacy, Josef-Möller-Haus, Innrain 52, 6020 Innsbruck, Austria.

出版信息

Nanomedicine (Lond). 2007 Feb;2(1):41-50. doi: 10.2217/17435889.2.1.41.

Abstract

Thiolated polymers or designated thiomers are gained by immobilization of sulhydryl-bearing ligands on the polymeric backbone of well established polymers, such as chitosan and poly(acrylates). This functionalization leads to significantly improved properties compared with the corresponding unmodified polymers. Mucoadhesive properties are strongly improved by the formation of disulfide bonds between thiol groups of the thiomer and cysteine-rich glycoproteins of the mucus gel layer. Moreover, enzyme- and efflux-pump inhibiting, as well as significantly improved permeation-enhancing properties, are advantages of polymer thiolization. Thiomer micro- and nano-particlulate delivery systems can be generated via different techniques, such as in situ gelation and subsequent covalent crosslinking, radical emulsion polymerization, emulsification/solvent evaporation or air jet milling. As thiomer micro- and nano-particles were shown to exhibit the same features as thiolated polymers per se, they might be useful tools for the delivery of various types of challenging drugs.

摘要

硫醇化聚合物或特定的硫醚聚合物是通过将含巯基的配体固定在已成熟聚合物(如壳聚糖和聚丙烯酸酯)的聚合物主链上而获得的。与相应的未改性聚合物相比,这种功能化导致性能显著改善。硫醚聚合物的巯基与黏液凝胶层富含半胱氨酸的糖蛋白之间形成二硫键,从而大大增强了黏膜黏附性能。此外,聚合物硫醇化还具有抑制酶和外排泵以及显著改善渗透增强性能等优点。硫醚聚合物微米和纳米颗粒递送系统可通过不同技术制备,如原位凝胶化及随后的共价交联、自由基乳液聚合、乳化/溶剂蒸发或气流粉碎。由于硫醚聚合物微米和纳米颗粒本身表现出与硫醇化聚合物相同的特性,它们可能是递送各类挑战性药物的有用工具。

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