Preparation of bufalin-loaded pluronic polyetherimide nanoparticles, cellular uptake, distribution, and effect on colorectal cancer

Int J Nanomedicine. 2014 Aug 21:9:4035-41. doi: 10.2147/IJN.S64708. eCollection 2014.

Abstract

A large number of studies have shown that bufalin can have a significant antitumor effect in a variety of tumors. However, because of toxicity, insolubility in water, fast metabolism, short half-life, and other shortcomings, its application is limited in cancer therapy. In this study, we explored the anti-metastatic role of bufalin-loaded pluronic polyetherimide nanoparticles on HCT116 colon cancer-bearing mice. Nanoparticle size, shape, drug loading, encapsulation efficiency, and in vitro drug release were studied. Also, cellular uptake of nanoparticles, in vivo tumor targeting, and tumor metastasis were studied. The nanoparticles had a particle size of about 60 nm and an encapsulation efficiency of 75.71%, by weight. The in vitro release data showed that free bufalin was released faster than bufalin-loaded pluronic polyetherimide nanoparticles, and almost 80% of free bufalin was released after 32 hours. Nanoparticles had an even size distribution, were stable, and had a slow release and a tumor-targeting effect. Bufalin-loaded pluronic polyetherimide nanoparticles can significantly inhibit the growth and metastasis of colorectal cancer.

Keywords: bufalin; colon cancer; nanoparticles; tumor target.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacokinetics
  • Antineoplastic Agents / pharmacology
  • Bufanolides / chemistry*
  • Bufanolides / pharmacokinetics
  • Bufanolides / pharmacology
  • Colorectal Neoplasms / metabolism*
  • Colorectal Neoplasms / pathology
  • Drug Carriers / chemistry
  • Drug Carriers / pharmacokinetics
  • HCT116 Cells
  • Humans
  • Liver / chemistry
  • Liver / drug effects
  • Liver / metabolism
  • Male
  • Mice
  • Mice, Nude
  • Nanoparticles / chemistry*
  • Particle Size
  • Poloxamer / chemistry*
  • Polymers / chemistry*
  • Xenograft Model Antitumor Assays

Substances

  • Antineoplastic Agents
  • Bufanolides
  • Drug Carriers
  • Polymers
  • polyetherimide
  • Poloxamer
  • bufalin