Erythrocyte membrane nanoparticles improve the intestinal absorption of paclitaxel

Biochem Biophys Res Commun. 2017 Jun 24;488(2):322-328. doi: 10.1016/j.bbrc.2017.05.042. Epub 2017 May 8.

Abstract

Paclitaxel (PTX) is a cytotoxic chemotherapy drug with encouraging activity in human malignancies. However, free PTX has a very low oral bioavailability due to its low aqueous solubility and the gastrointestinal drug barrier. In order to overcome this obstacle, we have designed erythrocyte membrane nanoparticles (EMNP) using sonication method. The permeability of PTX by EMNP was 3.5-fold (Papp = 0.425 nm/s) and 16.2-fold (Papp = 394.1 nm/s) higher than free PTX in MDCK-MDR1 cell monolayers and intestinal mucosal tissue, respectively. The in vivo pharmacokinetics indicated that the AUC0-t (μg/mL·h) and Cmax (μg/mL) of EMNP were 14.2-fold and 6.0-fold higher than that of free PTX, respectively. In summary, the EMNP appears to be a promising nanoformulation to enhance the oral bioavailability of insoluble and poorly permeable drugs.

Keywords: Drug delivery; Erythrocyte membrane; Oral route; Paclitaxel.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents, Phytogenic / administration & dosage*
  • Antineoplastic Agents, Phytogenic / chemistry
  • Antineoplastic Agents, Phytogenic / pharmacology*
  • Cell Survival / drug effects
  • Dose-Response Relationship, Drug
  • Erythrocyte Membrane / chemistry*
  • Erythrocyte Membrane / metabolism
  • Intestinal Absorption / drug effects*
  • Nanoparticles / chemistry*
  • Nanoparticles / metabolism
  • Paclitaxel / administration & dosage*
  • Paclitaxel / chemistry
  • Paclitaxel / pharmacology*
  • Particle Size
  • Rats
  • Rats, Sprague-Dawley
  • Structure-Activity Relationship
  • Surface Properties

Substances

  • Antineoplastic Agents, Phytogenic
  • Paclitaxel