title: Tunable pH-sensitive poly(β-amino ester)s synthesized from primary amines and diacrylates for intracellular drug delivery.
abstract: The pH sensitivity of a series of PbAEs synthesized from primary amines and diacrylates is studied. By changing alkyl groups of the amine monomers, the pKb can be tuned across a broad range (from 3.5 to 7.2). Micelles formed from a PEG-PbAE block copolymer retain the pH sensitivity of PbAE and can stably load hydrophobic molecules under neutral pH, while quickly dissociate and release their cargoes at pH ≈ 6.0. When the chemotherapy drug DOX is loaded, the micelles show efficient cell proliferation inhibition to HeLa cells and fast intracellular release. Thus, the primary-amine-based PbAEs are shown to be promising in the construction of intracellular targeting drug delivery systems.
authors.affiliation: Key Laboratory of Polymer Ecomaterials, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, China.
authors.forename: Wantong
authors.initials: W
authors.lastname: Song
authors.forename: Zhaohui
authors.initials: Z
authors.lastname: Tang
authors.forename: Mingqiang
authors.initials: M
authors.lastname: Li
authors.forename: Shixian
authors.initials: S
authors.lastname: Lv
authors.forename: Haiyang
authors.initials: H
authors.lastname: Yu
authors.forename: Lili
authors.initials: L
authors.lastname: Ma
authors.forename: Xiuli
authors.initials: X
authors.lastname: Zhuang
authors.forename: Yubin
authors.initials: Y
authors.lastname: Huang
authors.forename: Xuesi
authors.initials: X
authors.lastname: Chen
mesh_terms: D000179:Acrylates / Q000737:chemistry*; D000588:Amines / Q000737:chemistry*; D000903:Antibiotics, Antineoplastic / Q000008:administration & dosage* / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D004317:Doxorubicin / Q000008:administration & dosage* / Q000494:pharmacology; D004337:Drug Carriers / Q000138:chemical synthesis*; D004339:Drug Compounding; D004952:Esters; D005456:Fluorescent Dyes; D006367:HeLa Cells; D006801:Humans; D006863:Hydrogen-Ion Concentration; D057927:Hydrophobic and Hydrophilic Interactions; D009682:Magnetic Resonance Spectroscopy; D008823:Micelles; D010078:Oxazines; D011092:Polyethylene Glycols / Q000737:chemistry*; D058105:Polymerization
chemical_list: D000179:Acrylates; D000588:Amines; D000903:Antibiotics, Antineoplastic; D004337:Drug Carriers; D004952:Esters; D005456:Fluorescent Dyes; D008823:Micelles; D010078:Oxazines; D011092:Polyethylene Glycols; D004317:Doxorubicin; C044808:nile red