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Encapsulation of Acetylshikonin by Polyamidoamine Dendrimers for Preparing Prominent Nanoparticles

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Abstract

Acetylshikonin (AS) has demonstrated antitumor potential. However, the development of therapeutic applications utilizing AS is inhibited by its poor solubility in water. In the present work, polyamidoamine (PAMAM) dendrimers and their PEGylated derivatives were employed to increase the solubility of AS. A distinct color transition was observed during the encapsulation of AS suggesting strong intermolecular forces between PAMAM and AS. Ultraviolet–visible, high-performance liquid chromatography, and 1H NMR were used to verify the interaction between PAMAM and AS. The maximum amount of combined AS to each PAMAM molecule was determined. The cytotoxicity of AS nanoparticles was evaluated against leukemia (K562) and breast cancer (SK-BR-3) cell lines; the AS nanoparticles were shown to effectively inhibit tumor cells.

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Acknowledgments

This work was supported by the Natural Science Foundation of Jiangsu Province grant (no. BK2011771) and the Fundamental Research Funds for the Central Universities (no. JKQ2011019).

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Correspondence to Zhenghong Wu or Zhengrong Li.

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Jianqing Peng, Wen Zhou, and Xinyi Xia contributed equally to this work.

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Peng, J., Zhou, W., Xia, X. et al. Encapsulation of Acetylshikonin by Polyamidoamine Dendrimers for Preparing Prominent Nanoparticles. AAPS PharmSciTech 15, 425–433 (2014). https://doi.org/10.1208/s12249-014-0074-2

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