title: Polymeric anticancer drugs with pH-controlled activation.
abstract: Use of macromolecular water-soluble carriers of anti-cancer drugs represents a promising approach to cancer therapy. Release of drugs from the carrier system is a prerequisite for therapeutic activity of most macromolecular anti-cancer conjugates. Incorporation of acid-sensitive spacers between the drug and carrier enables release of an active drug from the carrier in a tumor tissue, either in slightly acidic extracellular fluids or, after endocytosis, in endosomes or lysosomes of cancer cells. This paper reviews advances in development and study of properties of various acid-sensitive macromolecular drug delivery systems, starting from simple polymer-drug conjugates to ending with site-specific antibody-targeted polymer-drug conjugates.
authors.affiliation: Institute of Macromolecular Chemistry, Academy of Sciences of the Czech Republic, Heyrovsky Sq. 2, 162 06 Prague 6, Czech Republic. ulbrich@imc.cas.cz
authors.forename: Karel
authors.initials: K
authors.lastname: Ulbrich
authors.forename: Vladimír
authors.initials: V
authors.lastname: Subr
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D004337:Drug Carriers; D006801:Humans; D006863:Hydrogen-Ion Concentration; D018796:Immunoconjugates / Q000737:chemistry / Q000494:pharmacology; D011108:Polymers / Q000737:chemistry* / Q000494:pharmacology; D011355:Prodrugs / Q000737:chemistry* / Q000494:pharmacology; D012995:Solubility; D014867:Water / Q000737:chemistry
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D018796:Immunoconjugates; D011108:Polymers; D011355:Prodrugs; D014867:Water