4.7 Article

Integrin alpha(2)beta(1) Targeting DGEA-Modified Liposomal Doxorubicin Enhances Antitumor Efficacy against Breast Cancer

期刊

MOLECULAR PHARMACEUTICS
卷 18, 期 7, 页码 2634-2646

出版社

AMER CHEMICAL SOC
DOI: 10.1021/acs.molpharmaceut.1c00132

关键词

integrin alpha(2)beta(1); breast cancer; DGEA; liposome; doxorubicin

资金

  1. National Natural Science Foundation of China [81803447, 81690261]
  2. China Postdoctoral Science Foundation [2018M633388]
  3. Fundamental Research Funds for the Central Universalities of China [2018SCU12025]
  4. Sichuan University postdoctoral interdisciplinary Innovation Fund (2018)

向作者/读者索取更多资源

The DGEA-Lipo-DOX platform demonstrated improved antitumor ability in breast cancer treatment through enhanced blood circulation and drug accumulation at tumor sites. Targeting integrin alpha(2)beta(1) by DGEA may represent a potentially safer alternative therapeutic strategy for breast cancer treatment.
Breast cancer was the leading cause of newly diagnosed cases of tumors in 2020, ranking as the second highest cause of female death. Chemotherapy remains the conventional treatment of choice for breast tumors in most clinical cases. However, it is often accompanied by a poor prognosis and severe side effects, resulting from an insufficient accumulation of the drug at tumor sites and an unsystematic distribution of the drug across the body. Inspired by the fact that breast tumor cells overexpress integrin alpha(2)beta(1) on the surface, we designed and constructed an integrin alpha(2)beta(1) targeting DGEA-modified liposomal doxorubicin (DGEA-Lipo-DOX) platform for application in breast cancer therapy. The DGEA-Lipo-DOX was stable with a uniform particle size of 121.1 +/- 3.8 nm and satisfactory drug encapsulation. Demonstrated in vitro and in vivo, the constructed platform exhibited improved antitumor ability. The DGEA-Lipo-DOX showed 4-fold enhanced blood circulation and 6-fold increased accumulation of DOX at the tumor sites compared to those of free DOX, resulting in a significantly enhanced antitumor efficacy in tumor-bearing mice. A preliminary safety evaluation suggested that the systemic toxicity of DOX was relieved by DGEA-Lipo delivery. Collectively, binding integrin alpha(2)beta(1) by DGEA may represent an alternative therapeutic strategy for potentially safer breast cancer treatment.

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