Acid-Activatable Theranostic Unimolecular Micelles Composed of Amphiphilic Star-like Polymeric Prodrug with High Drug Loading for Enhanced Cancer Therapy

作者：Shi, Xiaoxiao; Hou, Meili; Bai, Shuang; Ma, Xiaoqian; Gao, Yong-E; Xiao, Bo; Xue, Peng; Kang, Yuejun^*; Xu, Zhigang^*; Li, Chang Ming

来源：Molecular Pharmaceutics, 2017, 14(11): 4032-4041.

DOI：10.1021/acs.molpharmaceut.7b00704

• acid-activatable
• polymeric prodrug
• unimolecular micelles
• drug delivery
• cancer therapy

Stimuli-responsive nanomedicine with theranostic functionalities with reduced side-effects has attracted growing attention, although there are some major obstacles to overcome before clinical applications. Herein, we present an acid-activatable theranostic unimolecular micelles based on amphiphilic star-like polymeric prodrug to systematically address typical existing issues. This smart polymeric prodrug has a preferable size of about 35 nm and strong micellar stability in aqueous solution, which is beneficial to long-term blood circulation and efficient extravasation from tumoral vessels. Remarkably, the polymeric prodrug has a high drug loading rate up to 53.1 wt%, which induces considerably higher cytotoxicity against tumor cells (HeLa cells and MCF-7 cells) than normal cells (HUVEC cells) suggesting a spontaneous tumor-specific targeting capability. Moreover, the polymeric prodrug can serve as a fluorescent nanoprobe activated by the acidic microenvironment in tumor cells, which can be used as a promising platform for tumor diagnosis. The superior antitumor effect in this in vitro study demonstrates the potential of this prodrug as a promising platform for drug delivery and cancer therapy.

• 出版日期2017-11
• 单位西南大学