Ph-responsive fluorescence enhanced nanogel for targeted delivery of aur and cddp against breast cancer

Zhiwen Cao, Wen Li, Rui Liu, Chenxi Li, Yurong Song, Guangzhi Liu, Youwen Chen, Cheng Lu, Aiping LYU*, Yuanyan Liu

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review


Introduction: Auraptene (AUR), a natural bioactive prenyloxy coumarin, is a highly pleiotropic molecule that can bind to the MT1 receptor and can effectively reduce the proliferation and migration of breast cancer cells. Cisplatin (CDDP), as the first synthetic platinum-based anticancer drug, is widely used in the clinic due to its definite mechanism and therapeutic effect on diverse tumors. However, both of AUR and CDDP exhibit some disadvantages when used alone, including poor solubility, low bioavailability, lack of selec-tivity and systemic toxicity when they are used singly. Methods: Therefore, the biodegradable materials hyaluronic acid (HA) and β-cyclodextrin derivative (mono-(6-amino-mono-6-deoxy)-β-CD, CD) were employed as carriers to load AUR and CDDP to form nanogel (CDDPHA-CD@AUR) capable of dual-targeted delivery and synergistic therapy for breast cancer and cell imaging. Results: With the help of the CDDP-crosslinked CD-loaded structure, the newly synthesized nanogel exhibited excellent physiological stability and fluorescence effects. The release of AUR and CDDP was affected by the pH value, which was beneficial to the selective release in the tumor microenvironment. Cell experiments in vitro demonstrated that the nanogel could be selectively internalized by MCF-7 cells and exhibited low cytotoxicity to HK-2 cells. Antitumor experiments in vivo showed that the nanogel have better antitumor effects and lower systemic toxicity. Conclusion: Based on these, the nanogel loaded with AUR and CDDP have the potential for targeted delivery against breast cancer.

Original languageEnglish
Pages (from-to)8369-8382
Number of pages14
JournalInternational Journal of Nanomedicine
Publication statusPublished - 29 Oct 2020

Scopus Subject Areas

  • Biophysics
  • Bioengineering
  • Biomaterials
  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry

User-Defined Keywords

  • Auraptene
  • Cell imaging
  • Cisplatin
  • PH-responsive
  • Tumor targeting


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