Post-lumpectomy intracavitary retention and lymph node targeting of (⁹⁹m)Tc-encapsulated liposomes in nude rats with breast cancer xenograft

Breast Cancer Res Treat. 2011 Nov;130(1):97-107. doi: 10.1007/s10549-010-1309-x. Epub 2010 Dec 23.

Abstract

Liposomes are recognized drug delivery systems with tumor-targeting capability. In addition, therapeutic or diagnostic radionuclides can be efficiently loaded into liposomes. This study investigated the feasibility of utilizing radiotherapeutic liposomes as a new post-lumpectomy radiotherapy for early-stage breast cancer by determining the locoregional retention and systemic distribution of liposomes radiolabeled with technetium-99m ((⁹⁹m)Tc) in an orthotopic MDA-MB-231 breast cancer xenograft nude rat model. To test this new brachytherapy approach, a positive surgical margin lumpectomy model was set up by surgically removing the xenograft and deliberately leaving a small tumor remnant in the surgical cavity. Neutral, anionic, and cationic surface-charged fluorescent liposomes of 100 and 400 nm diameter were manufactured and labeled with (⁹⁹m)Tc-BMEDA. Locoregional retention and systemic distribution of (⁹⁹m)Tc-liposomes injected into the post-lumpectomy cavity were determined using non-invasive nuclear imaging, ex vivo tissue gamma counting and fluorescent stereomicroscopic imaging. The results indicated that (⁹⁹)Tc-liposomes were effectively retained in the surgical cavity (average retention was 55.7 ± 24.2% of injected dose for all rats at 44 h post-injection) and also accumulated in the tumor remnant (66.9 ± 100.4%/g for all rats). The majority of cleared (⁹⁹m)Tc was metabolized quickly and excreted into feces and urine, exerting low radiation burden on vital organs. In certain animals (⁹⁹m)Tc-liposomes significantly accumulated in the peripheral lymph nodes, especially 100 nm liposomes with anionic surface charge. The results suggest that post-lumpectomy intracavitary administration of therapeutic radionuclides delivered by 100-nm anionic liposome carrier is a potential therapy for the simultaneous treatment of the surgical cavity and the draining lymph nodes of early-stage breast cancer.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Brachytherapy
  • Breast Neoplasms / diagnostic imaging
  • Breast Neoplasms / metabolism*
  • Breast Neoplasms / radiotherapy
  • Cell Line, Tumor
  • Female
  • Humans
  • Liposomes
  • Lymph Nodes / metabolism*
  • Mastectomy, Segmental
  • Microscopy, Fluorescence
  • Multimodal Imaging
  • Positron-Emission Tomography
  • Rats
  • Rats, Nude
  • Technetium / administration & dosage*
  • Technetium / pharmacokinetics
  • Tomography, X-Ray Computed
  • Xenograft Model Antitumor Assays

Substances

  • Liposomes
  • Technetium