Lactosylated gramicidin-based lipid nanoparticles (Lac-GLN) for targeted delivery of anti-miR-155 to hepatocellular carcinoma

Mengzi Zhang, Xiaoju Zhou, Bo Wang, Bryant C. Yung, Ly J. Lee, Kalpana Ghoshal, Robert J. Lee

Research output: Contribution to journalArticlepeer-review


Lactosylated gramicidin-containing lipid nanoparticles (Lac-GLN) were developed for delivery of anti-microRNA-155 (anti-miR-155) to hepatocellular carcinoma (HCC) cells. MiR-155 is an oncomiR frequently elevated in HCC. The Lac-GLN formulation contained N-lactobionyl-dioleoyl phosphatidylethanolamine (Lac-DOPE), a ligand for the asialoglycoprotein receptor (ASGR), and an antibiotic peptide gramicidin A. The nanoparticles exhibited a mean particle diameter of 73 nm, zeta potential of + 3.5 mV, anti-miR encapsulation efficiency of 88%, and excellent colloidal stability at 4 C. Lac-GLN effectively delivered anti-miR-155 to HCC cells with a 16.1- and 4.1-fold up-regulation of miR-155 targets C/EBPβ and FOXP3 genes, respectively, and exhibited significant greater efficiency over Lipofectamine 2000. In mice, intravenous injection of Lac-GLN containing Cy3-anti-miR-155 led to preferential accumulation of the anti-miR-155 in hepatocytes. Intravenous administration of 1.5 mg/kg anti-miR-155 loaded Lac-GLN resulted in up-regulation of C/EBPβ and FOXP3 by 6.9- and 2.2-fold, respectively. These results suggest potential application of Lac-GLN as a liver-specific delivery vehicle for anti-miR therapy.

Original languageEnglish (US)
Pages (from-to)251-261
Number of pages11
JournalJournal of Controlled Release
Issue number3
StatePublished - May 9 2013
Externally publishedYes


  • Asialoglycoprotein receptor
  • Drug targeting
  • Gramicidin
  • Hepatocellular carcinoma
  • Nanoparticles

ASJC Scopus subject areas

  • Pharmaceutical Science


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