Synthesis of folic acid-containing imidazolium copolymers for potential gene delivery applications

Michael H. Allen, Kelsea N. Day, Sean T. Hemp, Timothy Edward Long*

*この研究の対応する著者

研究成果: Article査読

13 被引用数 (Scopus)

抄録

Folic acid conjugation onto poly(1-vinylimidazole) generates imidazolium copolymers for potential receptor-mediated nonviral gene delivery. Homopolymer quaternization with various tBoc-protected bromoalkylamines imparts a permanent charge for DNA complexation. Incorporation of primary amine groups provides a site for folic acid conjugation onto imidazolium copolymers. DNA binding, cytotoxicity, and in vitro transfection in HeLa cells reveal structure-property-transfection relationships for the imidazolium copolymers. Luciferase expression assays establish that primary amine conjugation onto imidazolium copolymers up to 30 mol% fails to improve transfection efficiency. In sharp contrast, incorporation of folic acid onto the copolymers improves transfection efficiency 250-fold. Synthesis of amine-containing imidazolium copolymers with folic acid generates macromolecules for nonviral gene delivery. Low incorporation of folic acid onto the copolymers remains ideal for nonviral gene delivery as large concentrations produce water-insoluble copolymers. The incorporation of folic acid offers a safe and effective avenue to tailor imidazolium copolymer gene delivery.

本文言語English
ページ(範囲)797-805
ページ数9
ジャーナルMacromolecular Chemistry and Physics
214
7
DOI
出版ステータスPublished - 2013 4月 12
外部発表はい

ASJC Scopus subject areas

  • 材料化学
  • ポリマーおよびプラスチック
  • 有機化学
  • 物理化学および理論化学
  • 凝縮系物理学

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