Levan nanoparticles with intrinsic CD44-targeting ability for tumor-targeted drug delivery.

Existing anticancer therapeutics exhibit short half-lives, non-specificity, and severe side effects. To address this, active-targeting nanoparticles have been developed; however, the complex fabrication procedures, scale-up, and low reproducibility delay FDA approval, particularly for functionalized nanoparticles. We developed levan nanoparticles via simple one-pot nanoprecipitation for specific anticancer drug delivery. Levan is a plant polysaccharide which has a binding affinity to CD44 receptors and amphiphilicity. The nanoparticles are self-assembled and enable active-targeting without chemical modifications. The paclitaxel-loaded levan nanoparticles (PTX@LevNP) demonstrated a sustained PTX release and long-term stability. The LevNP can bind CD44 receptors on cancer cells, and PTX@LevNP showed enhanced anticancer activity in CD44-positive cells (SCC7 cells). In SCC7 tumor-bearing mice, the accumulation of LevNP in tumor tissue was 3.7 times higher than that of the free-dye, resulting in improved anticancer efficacy of PTX@LevNP. This new strategy using levan can produce nanoparticles for effective cancer treatment without complex fabrication procedures.