Blood-pool multifunctional nanoparticles formed by temperature-induced phase transition for cancer-targeting therapy and molecular imaging

Int J Pharm. 2012 Nov 1;437(1-2):192-202. doi: 10.1016/j.ijpharm.2012.08.028. Epub 2012 Aug 24.

Abstract

Multifunctional nanoparticles (NPs) were prepared based on temperature-induced phase transition in a molten mixture of Lipiodol(®), Tween 80, paclitaxel (PTX), and Pluronic F-68, wherein the Lipiodol(®)/Tween 80 mixture is used as a solubilizer for PTX, and Pluronic F-68 is used for the stabilization of the molten mixture. The morphology and size distribution of optimized multifunctional NPs were observed using transmittance electron microscopy (TEM) and a particle size analyzer. In the optical imaging of tumor-bearing mice using a near-infrared fluorescence (NIRF) imaging system, the multifunctional NPs were evaluated in terms of a time-dependent excretion profile, in vivo biodistribution and tumor-targeting capability compared to free fluorescence dye. In addition, the prolonged circulation of multifunctional NPs was confirmed by enhancement of the blood-pool in live animals using a micro-CT imaging system, because iodine-containing Lipiodol(®) has an X-ray enhancement property. Finally, the anti-tumor efficacy of multifunctional NPs was monitored by injecting the multifunctional NPs into the tail veins of tumor-bearing mice. The multifunctional NPs showed excellent tumor targetability and anti-tumor efficacy in tumor-bearing mice, caused by the enhanced permeation and retention (EPR) effect.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents, Phytogenic / administration & dosage*
  • Antineoplastic Agents, Phytogenic / blood
  • Antineoplastic Agents, Phytogenic / chemistry
  • Antineoplastic Agents, Phytogenic / pharmacokinetics
  • Cell Line, Tumor
  • Ethiodized Oil / chemistry
  • Humans
  • Male
  • Mice
  • Mice, Inbred C3H
  • Molecular Imaging
  • Nanoparticles / administration & dosage*
  • Nanoparticles / chemistry
  • Neoplasms / drug therapy*
  • Neoplasms / pathology
  • Paclitaxel / administration & dosage*
  • Paclitaxel / blood
  • Paclitaxel / chemistry
  • Paclitaxel / pharmacokinetics
  • Phase Transition
  • Poloxamer / chemistry
  • Polysorbates / chemistry
  • Temperature
  • Tumor Burden / drug effects
  • Xenograft Model Antitumor Assays

Substances

  • Antineoplastic Agents, Phytogenic
  • Polysorbates
  • Poloxamer
  • Ethiodized Oil
  • Paclitaxel