title: A smart drug delivery system from charge-conversion polymer-drug conjugate for enhancing tumor therapy and tunable drug release.
abstract: A smart drug delivery system is prepared by citraconylated polyaspartic acid (PASP) derivate-drug conjugate. The conjugate contains two pH-sensitive groups: citraconic amide and hydrazone linker. Citraconic amide group can enhance tumor therapy efficiency by the extracellular pH-sensitive charge-conversion property. Hydrazone linker between polymer and drug can cleave efficiently in the intracellular pH environment. The resulting conjugate shows dual-pH sensitive properties: extracellular pH-triggered enhanced tumor targeting and intracellular pH-triggered drug release. The results of physicochemical properties, intracellular location, and cytotoxicity of conjugate micelles demonstrate that this novel smart drug delivery system can enhance intracellular delivery of drug at a low pH and then release drug rapidly.
authors.affiliation: Alan G. MacDiarmid Institute of Jilin University, 2699 Qianjin Street, Changchun, 130012, China.
authors.forename: Hailong
authors.initials: H
authors.lastname: Huang
authors.forename: Yapeng
authors.initials: Y
authors.lastname: Li
authors.forename: Zongpeng
authors.initials: Z
authors.lastname: Sa
authors.forename: Yuan
authors.initials: Y
authors.lastname: Sun
authors.forename: Yuzhen
authors.initials: Y
authors.lastname: Wang
authors.forename: Jingyuan
authors.initials: J
authors.lastname: Wang
mesh_terms: D000969:Antinematodal Agents / Q000737:chemistry* / Q000627:therapeutic use; D001672:Biocompatible Materials / Q000737:chemistry / Q000627:therapeutic use; D016503:Drug Delivery Systems; D065546:Drug Liberation; D006801:Humans; D006863:Hydrogen-Ion Concentration; D009369:Neoplasms / Q000188:drug therapy*; D010455:Peptides / Q000737:chemistry / Q000627:therapeutic use; D011108:Polymers / Q000737:chemistry* / Q000627:therapeutic use
chemical_list: D000969:Antinematodal Agents; D001672:Biocompatible Materials; D010455:Peptides; D011108:Polymers; C017645:polyaspartate
keywords: amphiphiles; biomaterials; charge transfer; conjugated polymers; drug delivery systems