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  • Receptor-mediated, tumor-targeted gene delivery using folate-terminated polyrotaxanes.

Receptor-mediated, tumor-targeted gene delivery using folate-terminated polyrotaxanes.

Molecular pharmaceutics (2012-04-10)
Yi Zhou, He Wang, Chengxi Wang, Yueshan Li, Wenfeng Lu, Shuifang Chen, Jiandong Luo, Yongnan Jiang, Jianhai Chen
ABSTRACT

Safe and effective gene delivery is essential to the success of gene therapy. We synthesized and characterized a novel nonviral gene delivery system in which folate (FA) molecules were functioned as blockers on cationic polyrotaxanes (PR) composed of poly(ethylenimine) (PEI)(600)-grafted α-cyclodextrin rings linearized on polyethylene glycol to form FA-terminated PR-PEI(600) (FPP). The FA terminal caps of FPP target cell surfaces abundant in FA receptor (FR), a common feature of tumor cells. The structure of FPP was characterized by using (1)H nuclear magnetic resonance ((1)H NMR). The delivery particle was composed of chemically bonded PEG (4000), α-cyclodextrins (CD), and PEI (600 Da) at a molar ratio of 1:17:86.7, and the particle size and zeta potential of FPP/pDNA polyplexes were measured using dynamic light scattering. FPP/pDNA exhibited a lower cytotoxicity, strong specificity to FR, and high efficiency of delivering DNA to target cells in vitro and in vivo with the reporter genes. Furthermore, the FPP/DNA complex showed an enhanced antitumor effect in the nude mice compared with other delivery systems, such as PEI-25K. Together, these results suggest that FPP may be useful for gene therapy.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
α-Cyclodextrin, ≥98%
Sigma-Aldrich
α-Cyclodextrin, purum, ≥98.0% (HPLC)
Sigma-Aldrich
α-Cyclodextrin, powder, BioReagent, suitable for cell culture, ≥98%
Sigma-Aldrich
α-Cyclodextrin, Produced by Wacker Chemie AG, Burghausen, Germany, Life Science, 98.0-101.0% cyclodextrin basis (HPLC)
Sigma-Aldrich
α-Cyclodextrin, produced by Wacker Chemie AG, Burghausen, Germany, ≥99.0% (HPLC)