Paclitaxel loaded EDC-crosslinked fibroin nanoparticles: a potential approach for colon cancer treatment

Drug Deliv Transl Res. 2020 Apr;10(2):413-424. doi: 10.1007/s13346-019-00682-7.

Abstract

Colon cancer is one of the most life-threatening cancers with high incidence and mortality rates. Current first-line treatments are ineffective and possess many unwanted effects. The off-label use of paclitaxel encapsulated in nanoparticles proves an innovative approach. In this study, we reported novel paclitaxel loaded EDC-crosslinked fibroin nanoparticles (PTX-FNPs) for anticancer purpose. The particles were formulated using desolvation method and the physicochemical properties were controlled favorably, including the particle size (300-500 nm), zeta potential (- 15 to + 30 mV), drug entrapment efficiency (75-100%), crystallinity, drug solubility (1- to 10-fold increase), dissolution profiles, stability (> 24 h in intravenous diluent and > 6 months storage at 4 °C). In in vitro study, all formulations showed no toxicity on the red blood cells, whereas retained the paclitaxel cytotoxicity on MCF-7 breast cancer and Caco-2 colon cancer cells. Interestingly, PTX-FNPs can be uptaken rapidly by the Caco-2 cells, consequently increased paclitaxel potency up to 10-fold compared to the free drug. Graphical abstract.

Keywords: Cancer; Colon; Crosslinked; EDC; Fibroin; Nanoparticles; Paclitaxel.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents, Phytogenic / chemistry
  • Antineoplastic Agents, Phytogenic / pharmacology*
  • Bombyx / metabolism
  • Caco-2 Cells
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • Colonic Neoplasms / drug therapy*
  • Drug Compounding
  • Ethyldimethylaminopropyl Carbodiimide / chemistry*
  • Fibroins / chemistry*
  • Humans
  • MCF-7 Cells
  • Nanoparticles
  • Paclitaxel / chemistry
  • Paclitaxel / pharmacology*
  • Particle Size

Substances

  • Antineoplastic Agents, Phytogenic
  • Fibroins
  • Paclitaxel
  • Ethyldimethylaminopropyl Carbodiimide