Abstract 382: In-vivo imaging of lung cancer using tumor homing peptide coated nanoparticles

Purpose: Lung cancer is one of the leading cause of death (1.3 million deaths annually) worldwide and non-small cell lung cancer (NSCLC) accounts for 85 % of all lung cancers. Vascular endothelial growth factor (VEGF) over-expression (61% to 92% of NSCLC) is associated with poor survival. Recently, new approaches in the treatment of lung cancer with novel drugs that selectively inhibit tumor blood supply thus controlling cancer cell survival, proliferation and/or metastasis in combination with conventional anticancer or antiangiogenic drugs have generated clinical interest, e.g. DIM-C-pPhC6H5 (DIM-P); a c-substituted diindolylmethanes which is novel anti-cancer agent. Objective of this study are: 1) to formulate tumor homing pegylated CREKA peptide coated nanoparticle of DIM-P (PCNCs-D)/ D-luciferin (PCNCs-DL)/ XenolightDiR (PCNCs-Di), 2) In-vivo imaging of tumor progression / tumor vasculature and tracking of PCNCs-Di. Methods: Nanoparticles were prepared with DIM-P (NCs-D)/ D-luciferin (NCs-DL)/XenolightDiR(NCs-Di), Compritol, Miglyol, DOGS-NTA-Ni and sodium taurocholate using high pressure homogenizer (Nano-DeBEE). PCNCs-D and PCNCs-DL/PCNCs-Di were prepared by conjugating NCs-D and NCs-DL/ NCs-Di with 6His-PEG2K-CREKA peptide and characterized for physical properties, clot binding assay and tube formation assay. Pharmacokinetic parameters of formulations were evaluated in BALB/c mice. In-vivo imaging of tumor and tracking of nanoparticles was carried out with IVIS® Spectrum CT (Caliper life Sciences) by using fluorescent dye (Xenolight DIR) and bioluminescence (luciferin) following intravenous and inhalation delivery of nanoparticles. Results: Particle size of PCNCs-D was 190-210 nm. The PCNCs-D formulation showed an initial burst release followed by a slow release up to 72 hr (90%) of DIM-P. PCNCs-D showed (p