In this study, we have developed a novel carrier, micelle-type bioconjugated PLGA-4-arm-PEG
branched polymeric nanoparticles (NPs), for the detection and treatment of pancreatic
cancer. These NPs contained 4-arm-PEG as corona, and PLGA as core, the particle
surface was conjugated with cyclo(arginine–glycine–aspartate) (cRGD) as ligand for
in vivo tumor targeting. The hydrodynamic size of the NPs was determined to be
150–180 nm and the critical micellar concentration (CMC) was estimated to be
10.5 mg l − 1. Our in vitro study shows that these NPs by themselves had negligible cytotoxicity to human
pancreatic cancer (Panc-1) and human glioblastoma (U87) cell lines. Near infrared (NIR)
microscopy and flow cytometry demonstrated that the cRGD conjugated PLGA-4-arm-PEG
polymeric NPs were taken up more efficiently by U87MG glioma cells, over-expressing the
αvβ3
integrin, when compared with the non-targeted NPs. Whole body imaging showed that the
cRGD conjugated PLGA-4-arm-PEG branched polymeric NPs had the highest
accumulation in the pancreatic tumor site of mice at 48 h post-injection. Physical,
hematological, and pathological assays indicated low in vivo toxicity of this NP formulation.
These studies on the ability of these bioconjugated PLGA-4-arm-PEG polymeric NPs
suggest that the prepared polymeric NPs may serve as a promising platform for detection
and targeted drug delivery for pancreatic cancer.