Dual-Arm Nanocapsule Targets Neuropilin-1 Receptor and Microtubule: A Potential Nanomedicine Platform

Mol Pharm. 2019 Jun 3;16(6):2522-2531. doi: 10.1021/acs.molpharmaceut.9b00123. Epub 2019 May 3.

Abstract

A multiarm nanomedicine template has been designed following bottom-up approach, which target neuropilin-1 (Nrp-1) receptor of cancer cells. Through this venture, we discovered that cucurbit [6] uril (CB [6]) binds with tubulin close to binding pocket of vinblastine site and perturbs tubulin polymerization. To increase the specificity of gold nanoparticle (GNP) toward Nrp-1-rich cancer cells, we further modified this GNP with Nrp-1 receptor-specific short peptide (CGNKRTR). Remarkably, we found an interesting self-assembly process upon addition of curcumin into the CB [6] and peptide-functionalized GNP, leading to the formation of a spherical nanocapsule (CGNP·Cur). It can deliver and release significantly higher amounts of anticancer drug curcumin in Nrp-1-rich cancer cells. It causes microtubule depolymerization and significant tumor regression in Nrp-1 overexpressed mice melanoma model. These interesting findings show that nanocapsule has high potential to develop a powerful anticancer nanomedicine and help in its preclinical validation.

Keywords: Nrp-1 receptor; STD NMR; cucurbituril; drug delivery; in vivo model; nanocapsule; tubulin/microtubule.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Apoptosis / drug effects
  • Cell Cycle / drug effects
  • Cryoelectron Microscopy
  • Gold / chemistry
  • Humans
  • Melanoma / drug therapy
  • Melanoma / metabolism
  • Metal Nanoparticles / chemistry*
  • Mice
  • Microtubules / metabolism*
  • Nanocapsules / chemistry*
  • Nanocapsules / therapeutic use*
  • Nanomedicine / methods*
  • Neuropilin-1 / metabolism*
  • Tubulin / metabolism

Substances

  • Nanocapsules
  • Tubulin
  • Neuropilin-1
  • Gold