title: Thiomers: promising platform for macromolecular drug delivery.
abstract: The application of macromolecules as therapeutic agents holds great promise for several major disorders such as cancer and cardiovascular disease. However, their use is limited by the lack of efficient, safe and specific delivery strategies. A promising strategy to overcome these challenges might be the use of thiolated polymers or designated thiomers. Thiomers are synthesized by immobilization of sulfhydryl bearing ligands on a polymeric backbone of well-established polymers. These multifunctional polymeric excipients show advantages in mucoadhesion, enzyme and efflux pump inhibition in comparison to unmodified polymers. One obstacle in the use of thiomers is that they are prone to oxidation at lower pH but this could be solved by introducing a completely new generation of thiomers, namely, the preactivated thiomer generation. Preactivated thiomers are mixed disulfides, which exhibit oxidation resistance and, beyond that, improved thiomer features. This review summarizes recent findings of polymeric excipients for macromolecular drug delivery as well as their synthesis and distinctive features.
authors.affiliation: Department of Pharmaceutical Technology, Institute of Pharmacy, Center for Chemistry & Biomedicine, University of Innsbruck, Innrain 80/82, 6020 Innsbruck, Austria.
authors.forename: Flavia
authors.initials: F
authors.lastname: Laffleur
authors.forename: Andreas
authors.initials: A
authors.lastname: Bernkop-Schnürch
mesh_terms: D000818:Animals; D004337:Drug Carriers / Q000737:chemistry* / Q000378:metabolism; D016503:Drug Delivery Systems / Q000379:methods*; D005079:Excipients / Q000737:chemistry / Q000378:metabolism; D006801:Humans; D046911:Macromolecular Substances / Q000008:administration & dosage*; D004364:Pharmaceutical Preparations / Q000008:administration & dosage*; D011108:Polymers / Q000737:chemistry* / Q000378:metabolism; D013438:Sulfhydryl Compounds / Q000737:chemistry* / Q000378:metabolism
chemical_list: D004337:Drug Carriers; D005079:Excipients; D046911:Macromolecular Substances; D004364:Pharmaceutical Preparations; D011108:Polymers; D013438:Sulfhydryl Compounds