Hyperbranched poly(amido amine)s (HPAAs) containing different amounts of β-cyclodextrin (β-CD) (HPAA-CDs) were synthesized in one-pot by Michael addition copolymerization of N,N'-methylene bisacrylamide, 1-(2-aminoethyl)piperazine, and mono-6-deoxy-6-ethylenediamino-β-CD. In comparison to pure HPAA, the fluorescence intensity of HPAA-CDs was enhanced significantly while the cytotoxicity became lower. Ascribed to plenty of amino groups and strong photoluminescence, HPAA-CDs could be used as nonviral gene delivery vectors, and the corresponding gene transfection was evaluated. The experimental results indicated that HPAA-CDs condensed the plasmid DNA very well. By utilizing the fluorescent properties of HPAA-CDs, the cellular uptake and gene transfection processes were tracked by flow cytometry and confocal laser scanning microscopy without any fluorescent labeling. The transfection efficiencies of HPAA-CDs were similar to that of pure HPAA. In addition, the inner cavities of β-CDs in HPAA-CDs could be used to encapsulate drugs through host--guest interaction. Therefore, the HPAA-CDs may have potential application in the combination of gene therapy and chemotherapy.
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Chen et al. (2011) studied this question.
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