In Vivo Bone-Targeting of Bis(phosphonate)-Conjugated Double Helical RNA Monitored by Positron Emission Tomography

Mol Pharm. 2016 Jul 5;13(7):2588-95. doi: 10.1021/acs.molpharmaceut.6b00261. Epub 2016 Jun 6.

Abstract

A bis(phosphonate) conjugate of 2'-O-methyl oligoribonucleotide (microRNA-21) was synthesized and used as a bone-targeting carrier in the systemic delivery of a (68)Ga-1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA)-chelated 2'-O-methyl oligoribonucleotide (anti-microRNA-21). The whole-body biodistribution of the double helical RNA was monitored by positron emission tomography (PET), which verified the expected bis(phosphonate)-induced bone accumulation in healthy rats.

Keywords: 68Ga-labeled oligonucleotides; bis(phosphonate); bone targeting; in vivo PET imaging; siRNA.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Chelating Agents / chemistry
  • Gallium Radioisotopes / chemistry*
  • Heterocyclic Compounds / chemistry
  • Male
  • Positron-Emission Tomography / methods*
  • RNA / analysis*
  • RNA, Small Interfering / chemistry
  • Rats
  • Rats, Sprague-Dawley

Substances

  • Chelating Agents
  • Gallium Radioisotopes
  • Heterocyclic Compounds
  • RNA, Small Interfering
  • 1,4,7-triazacyclononane
  • RNA