Synthesis and biological evaluation of radiolabeled photosensitizer linked bovine serum albumin nanoparticles as a tumor imaging agent

Int J Pharm. 2012 Jan 17;422(1-2):472-8. doi: 10.1016/j.ijpharm.2011.11.013. Epub 2011 Nov 15.

Abstract

In this study, we reported on the synthesis and biological evaluation of radiolabeled fluorescent dye conjugated bovine serum albumin nanoparticles within the size range 190-210 nm. The bovine serum albumin nanoparticles (BSANPs) were prepared using a desolvation method, and chemical cross-linking was performed using gluteraldehyde. Furthermore, pheophorbide-a (PH-A) was loaded on the BSANPs. The results obtained from dynamic light scattering and electron microscopy have proved that nanoparticles are highly monodisperse and near-spherical shaped. The photo-physical properties of the PH-A-BSANPs were obtained using the spectrophotometric techniques. According to the results, PH-A and BSANPs show high non-covalent interaction. PH-A loaded nanoparticles were labeled with (99m)Tc and the radio-labeling efficiency was determined as 90 ± 1.2%. Biodistribution studies of (99m)Tc labeled PH-A-BSANPs and PH-A were carried out using female Albino Wistar rats, and (99m)Tc-PH-A-BSANPs showed a significantly higher uptake in the breast and uterus than (99m)Tc-PH-A. Cell culture study was carried out in MCF-7 cell line (human breast adenocarcinoma cell line). According to the cell culture studies, (99m)Tc-PH-A-BSANPs showed a higher uptake than (99m)Tc-PH-A. Moreover, PH-A-BSANPs demonstrated good photo-physical properties and BSANPs increased the uptake of PH-A on to the MCF-7 cell line. These results confirm that (99m)Tc labeled PH-A-BSANPs could be utilized for radioimaging.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenocarcinoma / metabolism
  • Adenocarcinoma / pathology
  • Animals
  • Breast Neoplasms / metabolism
  • Breast Neoplasms / pathology
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Chlorophyll / analogs & derivatives*
  • Chlorophyll / chemistry
  • Chlorophyll / pharmacokinetics
  • Chlorophyll / toxicity
  • Cross-Linking Reagents / chemistry
  • Drug Carriers*
  • Female
  • Glutaral / chemistry
  • Humans
  • Light
  • Magnetic Resonance Spectroscopy
  • Mass Spectrometry
  • Microscopy, Electron
  • Microscopy, Fluorescence
  • Molecular Imaging / methods*
  • Nanoparticles*
  • Particle Size
  • Radiation-Sensitizing Agents / chemistry
  • Radiation-Sensitizing Agents / pharmacokinetics*
  • Radiation-Sensitizing Agents / toxicity
  • Radiopharmaceuticals / chemistry
  • Radiopharmaceuticals / pharmacokinetics*
  • Rats
  • Rats, Wistar
  • Scattering, Radiation
  • Serum Albumin, Bovine / chemistry
  • Serum Albumin, Bovine / pharmacokinetics*
  • Spectrophotometry, Ultraviolet
  • Technetium / chemistry
  • Technetium / pharmacokinetics*
  • Tissue Distribution

Substances

  • Cross-Linking Reagents
  • Drug Carriers
  • Radiation-Sensitizing Agents
  • Radiopharmaceuticals
  • Chlorophyll
  • Serum Albumin, Bovine
  • Technetium
  • pheophorbide a
  • Glutaral