Expansile nanoparticles: synthesis, characterization, and in vivo efficacy of an acid-responsive polymeric drug delivery system

J Am Chem Soc. 2009 Feb 25;131(7):2469-71. doi: 10.1021/ja807416t.


Nanoparticles are finding increased uses in drug delivery applications as a means to increase treatment efficacy and improve patient care. Here, we report engineered polymeric nanoparticles that undergo a hydrophobic to hydrophilic transition at pH 5 to afford swelling and rapid release of their contents. As our clinical interest lies in the prevention of lung tumor recurrence following resection, the nanoparticles were evaluated in a model mimicking microscopic disease, akin to residual occult tumor that can remain at the resection margin following surgery. Expansile nanoparticles loaded with paclitaxel, a poorly water-soluble anticancer drug, prevent establishment of lung cancer in vivo and are superior to the conventional drug delivery method for paclitaxel using Cremophor EL/ethanol.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Carcinoma, Lewis Lung / drug therapy
  • Carcinoma, Non-Small-Cell Lung / drug therapy
  • Cell Line, Tumor
  • Drug Delivery Systems / methods*
  • Drug Screening Assays, Antitumor
  • Hydrogen-Ion Concentration
  • Hydrophobic and Hydrophilic Interactions
  • Lung Neoplasms / drug therapy
  • Mice
  • Nanoparticles / administration & dosage
  • Nanoparticles / chemistry*
  • Paclitaxel / administration & dosage
  • Paclitaxel / chemistry
  • Polymers / administration & dosage
  • Polymers / chemical synthesis
  • Polymers / chemistry*


  • Polymers
  • Paclitaxel