4.8 Article

Liposome-encapsulated anthraquinone improves efficacy and safety in triple negative breast cancer

Journal

JOURNAL OF CONTROLLED RELEASE
Volume 342, Issue -, Pages 31-43

Publisher

ELSEVIER
DOI: 10.1016/j.jconrel.2021.12.001

Keywords

Breast cancer; Liposome; Anthraquinone; Polyethylene glycol

Funding

  1. Taiwan Ministry of Science and Technology [MOST 108-2320-B-038-067]
  2. Taipei Medical Uni-versity [TMU 107-AE1-B27]
  3. Schlumberger Foundation Faculty for the Future program
  4. TMU Laboratory Animal Center
  5. Academia Sinica Cryo-EM Facility [AS-CFII-108-110]
  6. Taiwan Protein Project [AS-KPQ-109-TPP2, AS-KPQ-105-TPP]

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Triple negative breast cancer (TNBC) is a highly aggressive subtype that is challenging to treat, with small molecule-based chemotherapy being the preferred course of treatment. However, these drugs have high toxicity and tumors may develop resistance.
Breast cancer is the most common cancer among women and a leading cause of death worldwide. Triple negative breast cancer (TNBC) is a highly aggressive subtype which is the most challenging to treat. Due to heterogeneity and a lack of specific molecular targets, small molecule-based chemotherapy is the preferred course of treatment. However, these drugs have high toxicity due to off-target effects on healthy tissues, and tumors may develop resistance. Here, we present a polyethylene glycol-modified nanoscale liposomal formulation (LipoRV) of a new anthraquinone derivative which has potent effects on multiple TNBC cell lines. LipoRV readily inhibited the cell cycle, induced cell apoptosis, and reduced long-term proliferative potential of TNBC cells. In a xenograft animal model, LipoRV successfully cleared tumors and demonstrated a good safety profile, without detrimental effects on biochemical markers. Finally, RNA sequencing of LipoRV-treated TNBC cells was carried out, indicating that LipoRV may have immunomodulatory properties. These findings demonstrate that a liposomal anthraquinonebased molecule has excellent promise for TNBC therapy in the future.

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