Octreotide Nanoparticles Showed Affinity for In Vivo MIA Paca-2 Inducted Pancreas Ductal Adenocarcinoma Mimicking Pancreatic Polypeptide-Secreting Tumor of the Distal Pancreas (PPoma)

Pharm Res. 2019 Aug 5;36(10):143. doi: 10.1007/s11095-019-2678-4.

Abstract

Purpose: Pancreatic Polypeptide-secreting tumor of the distal pancreas (PPoma) is a rare, difficult and indolent type of cancer with a survival rate of 5-year in only 10% of all cases. The PPoma is classified as a neuroendocrine tumor (NET) not functioning that overexpresses SSTR 2 (somatostatin receptor subtype 2). Thus, in order to improve the diagnosis of this type of tumor, we developed nanoparticulate drug carriers based on poly-lactic acid (PLA) polymer loaded with octreotide and radiolabeled with Technetium-99 m (99mTc).

Methods: PLA/PVA octreotide nanoparticles were developed by double-emulsion technique. These nanoparticles were characterized by Atomic Force Microscopy (AFM) and Dynamic Light Scattering (DLS) and radiolabeled with 99mTc by the direct via forming 99mTc-PLA/PVA octreotide nanoparticles. The safety of these nanosystems was evaluated by the MTT cell toxicity assay and their in vivo biodistribution was evaluated in xenografted inducted animals.

Results: The results showed that a 189 nm sized nanoparticle were formed with a PDI of 0,097, corroborating the monodispersive behavior. These nanoparticles were successfully radiolabeled with 99mTc showing uptake by the inducted tumor. The MTT assay corroborated the safety of the nanosystem for the cells.

Conclusion: The results support the use of this nanosystem (99mTc-PLA/PVA octreotide nanoparticles) as imaging agent for PPoma. Graphical Abstract Polypeptide-Secreting Tumor of the Distal Pancreas (PPoma) Radiolabeled Nanoparticles for Imaging.

Keywords: PPoma; imaging agent; nanoradiopharmaceuticals; octreotide; radiopharmacy.

MeSH terms

  • Animals
  • Carcinoma, Pancreatic Ductal / diagnostic imaging*
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Humans
  • Male
  • Mice, Inbred BALB C
  • Mice, Nude
  • Nanoparticles / chemistry*
  • Nanoparticles / metabolism
  • Octreotide / chemistry*
  • Octreotide / metabolism
  • Pancreas / diagnostic imaging
  • Pancreas / metabolism
  • Pancreatic Neoplasms / diagnostic imaging*
  • Pancreatic Neoplasms / metabolism
  • Pancreatic Polypeptide / metabolism*
  • Particle Size
  • Polyesters / chemistry*
  • Radionuclide Imaging / methods
  • Radiopharmaceuticals / chemistry*
  • Radiopharmaceuticals / metabolism
  • Receptors, Somatostatin / genetics
  • Receptors, Somatostatin / metabolism
  • Technetium / chemistry*
  • Tissue Distribution

Substances

  • Polyesters
  • Radiopharmaceuticals
  • Receptors, Somatostatin
  • SSTR2 protein, human
  • poly(lactide)
  • Pancreatic Polypeptide
  • Technetium
  • Octreotide