Shah Kifayat Ullah, Shah Shefaat Ullah, Dilawar Naz, Khan Gul Majid, Gibaud Stéphane
a Department of Pharmacy , Quaid-e-Azam University , Islamabad , Pakistan.
b Department of Pharmaceutics, Faculty of Pharmacy , Gomal University , D.I.Khan , Pakistan.
Expert Opin Drug Deliv. 2017 May;14(5):601-610. doi: 10.1080/17425247.2016.1227787. Epub 2016 Sep 6.
Thiomers are the product of the immobilization of sulfhydryl-bearing ligands onto the polymer backbone of a conventional polymer, which results in a significant improvement in mucoadhesion; in situ gelation and efflux inhibition compare with unchanged polymers. Because of thiol groups, thiomers have more reactivity and enhanced protection against oxidation. Since the late 1990s, extensive work has been conducted on these promising polymeric excipients in the pharmaceutical field. Areas covered: This review covers thiomers, their classification and their different properties. Various techniques for the synthesis, purification and characterization of thiomers are described in detail. This review also encompasses their various properties such as mucoadhesion, permeation enhancement, in situ gelation and efflux inhibition, as well as different formulations based on thiomers. In addition to the use of thiomers as multifunctional excipients, this review also encompasses their use as drugs. Expert opinion: The synthesis is realized by linkage of sulfhydryl-bearing ligands but reported methods give low yields. Higher degrees of modification are not necessary and would probably lead to extreme changes in properties. Nevertheless, an accurate characterization of the final product is important. The scale-up procedure for industrial manufacturing has been adapted to produce GMP materials; Lacrimera® eye drops have already entered the European market.
硫醇聚合物是将含巯基配体固定在传统聚合物主链上的产物，这使得粘膜粘附性显著提高；与未改性的聚合物相比，其具有原位凝胶化和外排抑制作用。由于含有硫醇基团，硫醇聚合物具有更高的反应活性和更强的抗氧化保护能力。自20世纪90年代末以来，人们在制药领域对这些有前景的聚合物辅料进行了广泛研究。涵盖领域：本综述涵盖硫醇聚合物、其分类及其不同性质。详细描述了硫醇聚合物的各种合成、纯化和表征技术。本综述还包括它们的各种性质，如粘膜粘附性、渗透增强、原位凝胶化和外排抑制，以及基于硫醇聚合物的不同制剂。除了将硫醇聚合物用作多功能辅料外，本综述还包括它们作为药物的用途。专家观点：合成是通过含巯基配体的连接来实现的，但报道的方法产率较低。不需要更高程度的改性，而且这可能会导致性质发生极端变化。然而，对最终产品进行准确表征很重要。工业生产的放大工艺已进行调整以生产符合GMP标准的材料；Lacrimera®眼药水已进入欧洲市场。
