BACKGROUND: Early detection of cancer is critical and is expected to contribute significantly to the success of cancer therapy and improvement of patient survival rates.

MATERIAL AND METHODS: A biocompatible, reconstituted, high-density lipoprotein (rHDL)-based nano-system containing calcium carbonate and near-infrared fluorescence dye (NIRF), methylene blue (MB), was fabricated and characterized by particle size, zeta potential, and morphology observation. The safety profile was confirmed by bovine serum albumin (BSA) challenge assay, hemolysis test, MTT assay, and in vivo long-term toxicity assay. The tumor targetability was assessed by cellular uptake, competitive inhibition experiments, and in vivo imaging assay.

RESULTS: The self-assembled rHDL/MB/CCPs exhibited desirable and homogenous particle size, neutral surface charges, high bovine serum albumin stability, low hemolytic activity, and negligible cytotoxicity in vitro. The results obtained from confocal scanning laser microscopy and flow cytometry indicated that SR-BI coating exerted tumor-targeting function, which induced high and specific cellular uptake of rHDL/MB/CCPs. In vivo investigation in an A549 tumor xenografts-bearing mouse model revealed that rHDL/MB/CCPs possessed strong tumor targetability.

CONCLUSIONS: rHDL/MB/CCPs could be a safe tumor-targeting probe for cancer detection.

Keywords: Biocompatible Materials - chemistry, Drug Delivery Systems, Fluorescent Dyes - chemistry, Hemolysis, Lipoproteins, HDL - chemistry, Lung Neoplasms - genetics, Nanoparticles - chemistry, Nanotechnology - methods, Neoplasm Transplantation, Particle Size, Proteins - chemistry, Serum Albumin, Bovine - chemistry, Spectroscopy, Near-Infrared