Nanoparticulate drug combination inhibits DNA damage repair and PD-L1 expression in BRCA-mutant and wild type triple-negative breast cancer

J Control Release. 2025 Jan 10:377:661-674. doi: 10.1016/j.jconrel.2024.11.061. Epub 2024 Nov 30.

Abstract

The high mortality rate associated with metastatic breast cancer presents a significant global challenge. Inherent and chemotherapy-induced DNA damage repair, alongside immunosuppression, drastically contribute to triple-negative breast cancer (TNBC) relapse and metastasis. While poly (ADP-ribose) polymerase (PARP) inhibitors such as olaparib show effectiveness against BRCA1-mutant TNBC, they may lead to drug resistance and reduced efficacy due to increased programmed death-ligand 1 (PD-L1) expression. Our study explored the use of polymer-lipid nanoparticles (PLN) loaded with doxorubicin (DOX) and oligomeric hyaluronic acid (oHA), functionalized iRGD-peptide for integrins targeting (iRGD-DOX-oHA-PLN), to prevent TNBC immunosuppression, DNA repair, and metastasis. The results demonstrate that the iRGD-DOX-oHA-PLNs efficiently downregulated single and double-strand DNA repair proteins and enhanced DNA damage while decreasing PD-L1 expression compared to olaparib. Accordingly, iRGD-DOX-oHA-PLN treatment showed significantly higher efficiency in reducing levels of primary tumor growth and numbers of metastases to the lung and liver compared to olaparib in vitro and in vivo in both BRCA1-mutant and wild type TNBC orthotopic xenograft models.

Keywords: BRCA mutation; DNA damage repair; Drug combination; Multitargeting nanoparticles; PD-L1 expression; Triple-negative breast cancer.

MeSH terms

  • Animals
  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use
  • B7-H1 Antigen* / genetics
  • BRCA1 Protein* / genetics
  • Cell Line, Tumor
  • DNA Damage* / drug effects
  • DNA Repair* / drug effects
  • Doxorubicin* / administration & dosage
  • Doxorubicin* / pharmacology
  • Female
  • Humans
  • Hyaluronic Acid / chemistry
  • Liposomes
  • Mice
  • Mice, Nude
  • Mutation
  • Nanoparticles* / administration & dosage
  • Nanoparticles* / chemistry
  • Phthalazines* / administration & dosage
  • Phthalazines* / pharmacology
  • Piperazines / administration & dosage
  • Piperazines / pharmacology
  • Piperazines / therapeutic use
  • Poly(ADP-ribose) Polymerase Inhibitors / administration & dosage
  • Poly(ADP-ribose) Polymerase Inhibitors / pharmacology
  • Triple Negative Breast Neoplasms* / drug therapy
  • Triple Negative Breast Neoplasms* / genetics
  • Triple Negative Breast Neoplasms* / pathology

Substances

  • B7-H1 Antigen
  • CD274 protein, human
  • Phthalazines
  • olaparib
  • BRCA1 Protein
  • Doxorubicin
  • Hyaluronic Acid
  • BRCA1 protein, human
  • Lipid Nanoparticles
  • Piperazines
  • Poly(ADP-ribose) Polymerase Inhibitors
  • Antineoplastic Agents
  • Liposomes