RBC-derived vesicles as a systemic delivery system of doxorubicin for lysosomal-mitochondrial axis-improved cancer therapy

J Adv Res. 2020 Nov 24:30:185-196. doi: 10.1016/j.jare.2020.11.009. eCollection 2021 May.

Abstract

Introduction: Chemotherapeutic drugs are the main intervention for cancer management, but many drawbacks impede their clinical applications. Nanoparticles as drug delivery systems (DDSs) offer much promise to solve these limitations.

Objectives: A novel nanocarrier composed of red blood cell (RBC)-derived vesicles (RDVs) surface-linked with doxorubicin (Dox) using glutaraldehyde (glu) to form Dox-gluRDVs was investigated for improved cancer therapy.

Methods: We investigated the in vivo antineoplastic performance of Dox-gluRDVs through intravenous (i.v.) administration in the mouse model bearing subcutaneous (s.c.) B16F10 tumor and examined the in vitro antitumor mechanism and efficacy in a panel of cancer cell lines.

Results: Dox-gluRDVs can exert superior anticancer activity than free Dox in vitro and in vivo. Distinct from free Dox that is mainly located in the nucleus, but instead Dox-gluRDVs release and efficiently deliver the majority of their conjugated Dox into lysosomes. In vitro mechanism study reveals the critical role of lysosomal Dox accumulation-mediated mitochondrial ROS overproduction followed by the mitochondrial membrane potential loss and the activation of apoptotic signaling for superior anticancer activity of Dox-gluRDVs.

Conclusion: This work demonstrates the great potential of RDVs to serve a biological DDS of Dox for systemic administration to improve conventional cancer chemotherapeutics.

Keywords: Cancer chemotherapy; Doxorubicin; Drug delivery; Lysosome; Mitochondria; Nanoparticle.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents
  • Apoptosis / drug effects
  • Cell Line, Tumor
  • Doxorubicin / administration & dosage*
  • Doxorubicin / chemistry
  • Drug Carriers / chemistry
  • Drug Carriers / therapeutic use
  • Drug Delivery Systems / methods
  • Drug Liberation
  • Erythrocytes / chemistry*
  • Female
  • Fixatives / chemistry
  • Glutaral / chemistry
  • Humans
  • Lysosomes / metabolism*
  • Mice
  • Mice, Inbred C57BL
  • Mitochondria / metabolism*
  • Nanoparticles / chemistry*
  • Nanoparticles / therapeutic use
  • Neoplasms / drug therapy*
  • Neoplasms / metabolism
  • Reactive Oxygen Species

Substances

  • Antineoplastic Agents
  • Drug Carriers
  • Fixatives
  • Reactive Oxygen Species
  • Doxorubicin
  • Glutaral