Bioconjugation and Applications of Amino Functional Fluorescence Polymers

Macromol Biosci. 2017 Mar;17(3). doi: 10.1002/mabi.201600232. Epub 2016 Sep 30.

Abstract

Synthesis and novel applications of biofunctional polymers for diagnosis and therapy are promising area involving various research domains. Herein, three fluorescent polymers, poly(p-phenylene-co-thiophene), poly(p-phenylene), and polythiophene with amino groups (PPT-NH2 , PPP-NH2 , and PT-NH2 , respectively) are synthesized and investigated for cancer cell targeted imaging, drug delivery, and radiotherapy. Polymers are conjugated to anti-HER2 antibody for targeted imaging studies in nontoxic concentrations. Three cell lines (A549, Vero, and HeLa) with different expression levels of HER2 are used. In a model of HER2 expressing cell line (A549), radiotherapy experiments are carried out and results show that all three polymers increase the efficacy of radiotherapy. This effect is even more increased when conjugated to anti-HER2. In the second part of this work, one of the selected polymers (PT-NH2 ) is conjugated with a drug model; methotrexate via pH responsive hydrazone linkage and a drug carrier property of PT-NH2 is demonstrated on neuroblastoma (SH-SY5Y) cell model. Our results indicate that, PPT-NH2 , PPP-NH2 , and PT-NH2 have a great potential as biomaterials for various bioapplications in cancer research.

Keywords: bioconjugation; biofunctional polymers; cell imaging; drug release; fluorescent polymers.

MeSH terms

  • A549 Cells
  • Drug Delivery Systems*
  • Gene Expression Regulation, Neoplastic / drug effects
  • HeLa Cells
  • Humans
  • Neoplasms / drug therapy*
  • Neoplasms / pathology
  • Neoplasms / radiotherapy*
  • Polymers / administration & dosage*
  • Polymers / chemistry
  • Radiation Tolerance / drug effects
  • Radiation-Sensitizing Agents / administration & dosage
  • Radiation-Sensitizing Agents / chemistry
  • Receptor, ErbB-2 / biosynthesis
  • Thiophenes / administration & dosage
  • Thiophenes / chemistry

Substances

  • Polymers
  • Radiation-Sensitizing Agents
  • Thiophenes
  • polythiophene
  • ERBB2 protein, human
  • Receptor, ErbB-2