title: Fluorescent Copolymer-Based Prodrug for pH-Triggered Intracellular Release of DOX.
abstract: A novel water-soluble pH stimuli-responsive fluorescent copolymer of P(PEGMA-b-(MAH-co-Rh6GEAm)) was synthesized by two-step sequential RAFT polymerization. The prodrug with drug content of 0.1560 mg/mg was prepared by coupling doxorubicin (DOX) onto the copolymer via acid-cleavable hydrazone bond, formed between the carbonyl group of DOX and abundant hydrazide functional groups in the copolymer. The amphiphilic DOX-conjugated prodrug (P(PEGMA-b-(MAH-DOX-co-Rh6GEAm))) could easily form a micelle in water with Dh of less than 100 nm. It could be transported into HepG2 cells and release DOX without burst release, while the leakage of DOX can be avoided in the simulated normal physiological media. Furthermore, its fluorescence intensity experienced a reversible change with the transformation of the media pH. The better biocompatibility, pH stimuli-responsiveness, and the strong fluorescence at low pH media make the nanoparticles a potential platform for the controlled release of anticarcinogens and real-time fluorescent imaging of tumor tissues.
authors.affiliation: State Key Laboratory of Applied Organic Chemistry and Key Laboratory of Nonferrous Metal Chemistry and Resources Utilization of Gansu Province, College of Chemistry and Chemical Engineering, Lanzhou University , Lanzhou 730000, China.
authors.forename: Xu
authors.initials: X
authors.lastname: Jia
authors.affiliation: State Key Laboratory of Applied Organic Chemistry and Key Laboratory of Nonferrous Metal Chemistry and Resources Utilization of Gansu Province, College of Chemistry and Chemical Engineering, Lanzhou University , Lanzhou 730000, China.
authors.forename: Xubo
authors.initials: X
authors.lastname: Zhao
authors.affiliation: State Key Laboratory of Applied Organic Chemistry and Key Laboratory of Nonferrous Metal Chemistry and Resources Utilization of Gansu Province, College of Chemistry and Chemical Engineering, Lanzhou University , Lanzhou 730000, China.
authors.forename: Kun
authors.initials: K
authors.lastname: Tian
authors.affiliation: State Key Laboratory of Applied Organic Chemistry and Key Laboratory of Nonferrous Metal Chemistry and Resources Utilization of Gansu Province, College of Chemistry and Chemical Engineering, Lanzhou University , Lanzhou 730000, China.
authors.forename: Tingting
authors.initials: T
authors.lastname: Zhou
authors.affiliation: State Key Laboratory of Applied Organic Chemistry and Key Laboratory of Nonferrous Metal Chemistry and Resources Utilization of Gansu Province, College of Chemistry and Chemical Engineering, Lanzhou University , Lanzhou 730000, China.
authors.forename: Jiagen
authors.initials: J
authors.lastname: Li
authors.affiliation: State Key Laboratory of Applied Organic Chemistry and Key Laboratory of Nonferrous Metal Chemistry and Resources Utilization of Gansu Province, College of Chemistry and Chemical Engineering, Lanzhou University , Lanzhou 730000, China.
authors.forename: Ruinian
authors.initials: R
authors.lastname: Zhang
authors.affiliation: State Key Laboratory of Applied Organic Chemistry and Key Laboratory of Nonferrous Metal Chemistry and Resources Utilization of Gansu Province, College of Chemistry and Chemical Engineering, Lanzhou University , Lanzhou 730000, China.
authors.forename: Peng
authors.initials: P
authors.lastname: Liu
mesh_terms: D001672:Biocompatible Materials / Q000737:chemistry / Q000494:pharmacology; D004317:Doxorubicin / Q000737:chemistry* / Q000494:pharmacology; D004337:Drug Carriers / Q000737:chemistry*; D005453:Fluorescence; D056945:Hep G2 Cells; D006801:Humans; D006835:Hydrazones / Q000737:chemistry; D006863:Hydrogen-Ion Concentration; D008689:Methacrylates / Q000737:chemistry / Q000494:pharmacology; D008823:Micelles; D008970:Molecular Weight; D011092:Polyethylene Glycols / Q000737:chemistry / Q000494:pharmacology; D058105:Polymerization; D011108:Polymers / Q000737:chemistry* / Q000494:pharmacology; D011355:Prodrugs / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D001672:Biocompatible Materials; D004337:Drug Carriers; D006835:Hydrazones; D008689:Methacrylates; D008823:Micelles; D011108:Polymers; D011355:Prodrugs; C524499:polyethylene glycol methacrylate; D011092:Polyethylene Glycols; D004317:Doxorubicin