A Simple Add-and-Display Method for Immobilisation of Cancer Drug on His-tagged Virus-like Nanoparticles for Controlled Drug Delivery

Sci Rep. 2017 Jul 13;7(1):5303. doi: 10.1038/s41598-017-05525-4.

Abstract

pH-responsive virus-like nanoparticles (VLNPs) hold promising potential as drug delivery systems for cancer therapy. In the present study, hepatitis B virus (HBV) VLNPs harbouring His-tags were used to display doxorubicin (DOX) via nitrilotriacetic acid (NTA) conjugation. The His-tags served as pH-responsive nanojoints which released DOX from VLNPs in a controlled manner. The His-tagged VLNPs conjugated non-covalently with NTA-DOX, and cross-linked with folic acid (FA) were able to specifically target and deliver the DOX into ovarian cancer cells via folate receptor (FR)-mediated endocytosis. The cytotoxicity and cellular uptake results revealed that the His-tagged VLNPs significantly increased the accumulation of DOX in the ovarian cancer cells and enhanced the uptake of DOX, which improved anti-tumour effects. This study demonstrated that NTA-DOX can be easily displayed on His-tagged VLNPs by a simple Add-and-Display step with high coupling efficiency and the drug was only released at low pH in a controlled manner. This approach facilitates specific attachment of any drug molecule on His-tagged VLNPs at the very mild conditions without changing the biological structure and native conformation of the VLNPs.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / metabolism*
  • Cell Line, Tumor
  • Cell Surface Display Techniques / methods*
  • Doxorubicin / metabolism*
  • Drug Carriers*
  • Drug Delivery Systems*
  • Endocytosis
  • Epithelial Cells / metabolism
  • Folic Acid Transporters / metabolism
  • Hepatitis B virus*
  • Humans
  • Hydrogen-Ion Concentration
  • Protein Binding
  • Virosomes*

Substances

  • Antineoplastic Agents
  • Drug Carriers
  • Folic Acid Transporters
  • Virosomes
  • Doxorubicin