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Research Article

Self-assembly delivery system based on small-molecule camptothecin prodrug for treatment of colorectal carcinoma

    Jialing Dai

    Department of Pharmaceutics, China Pharmaceutical University, Nanjing 210009, PR China

    ,
    Mo Chen

    Department of Pharmaceutics, China Pharmaceutical University, Nanjing 210009, PR China

    ,
    Dongmei Xu

    Department of Pharmaceutics, China Pharmaceutical University, Nanjing 210009, PR China

    ,
    Huangjuan Li

    Department of Pharmaceutics, China Pharmaceutical University, Nanjing 210009, PR China

    ,
    Yingyu Qiao

    Department of Pharmaceutics, China Pharmaceutical University, Nanjing 210009, PR China

    ,
    Xue Ke

    **Author for correspondence:

    E-mail Address: kexue1973@vip.sina.com

    Department of Pharmaceutics, China Pharmaceutical University, Nanjing 210009, PR China

    &
    Tianyuan Ci

    *Author for correspondence:

    E-mail Address: citianyuan_cpu@163.com

    Department of Pharmaceutics, China Pharmaceutical University, Nanjing 210009, PR China

    Department of Pharmaceutical Sciences, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, PR China

    Published Online:https://doi.org/10.2217/nnm-2020-0453

    The aim of this study was to prepare small-molecule camptothecin (CPT) prodrugs and evaluate their effectiveness in colorectal carcinoma therapy. Prodrug nanoparticles (NPs) were physicochemically characterized and evaluated for their cytotoxicity in human colon cancer (HCT116) cell lines. The antitumor efficacy of the NPs was evaluated in HCT116 tumor-bearing mice. The prepared NPs exhibited high drug loading capacity (32% of CPT w/w) and also kept a high active lactone fraction of CPT (>85%) during circulation. The NPs were internalized into tumor cells efficiently compared with free drug and significantly enhanced the drug's therapeutic efficacy. The developed small-molecule CPT prodrug NPs could be a promising strategy in the clinical therapy of colorectal carcinoma.

    Papers of special note have been highlighted as: • of interest; •• of considerable interest

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