Focused ultrasound mediated drug delivery from temperature-sensitive liposomes: in-vitro characterization and validation

Phys Med Biol. 2013 Nov 21;58(22):8135-51. doi: 10.1088/0031-9155/58/22/8135.

Abstract

Nanomedicine-based delivery with non-invasive techniques is a promising approach to increase local drug concentration and to reduce systemic side effects. Focused ultrasound (FUS) has become a promising strategy for non-invasive local drug delivery by mild hyperthermia. In this study, traditional temperature-sensitive liposomes (TTSLs) encapsulating doxorubicin (DOX) were evaluated for FUS-mediated drug delivery with an in-vitro FUS setup. In-vitro studies showed quantitative release of the DOX from the lumen of the temperature-sensitive liposomes when heated to 42 °C with FUS using 1 MHz sinusoidal waves at 1.75 MPa for 10 min. No release was observed when heated at 37 °C. Moreover, we showed that DOX released from TTSLs by FUS is as efficiently internalized by glioblastoma cells as free DOX at 37 °C. In-vitro therapeutic evaluation showed that exposure of a cell monolayer to FUS-activated TTSLs induced a 60% and a 50% decrease in cell viability compared to cell medium and to TTSLs preheated at 37 °C, respectively. Using an in-vitro 3D cell culture model, the results showed that after FUS-mediated hyperthermia, preheated liposomes induced a 1.7-fold decrease in U-87 MG spheroid growth in comparison to the preheated liposomes at 37 °C. In conclusion, our results show that in-vitro FUS allows the evaluation of TTSLs and does not modify the cellular uptake of the released DOX nor its cytotoxic activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Biological Transport
  • Cell Death / drug effects
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • Doxorubicin / administration & dosage
  • Doxorubicin / chemistry
  • Doxorubicin / metabolism
  • Doxorubicin / pharmacology
  • Drug Delivery Systems / methods*
  • Glioblastoma / pathology
  • Humans
  • Liposomes
  • Reproducibility of Results
  • Spheroids, Cellular / drug effects
  • Spheroids, Cellular / pathology
  • Temperature*
  • Ultrasonics*

Substances

  • Liposomes
  • Doxorubicin