RGD-peptide conjugated inulin-ibuprofen nanoparticles for targeted delivery of Epirubicin

• PH-dependent RGD conjugated EPB loaded inulin-ibuprofen nanoparticles were fabricated.
• Nanoparticles increased the cellular uptake and cytotoxicity.
• Nanoparticles show superior tumor growth inhibition and reduced systemic toxicity.
• RGD conjugated EPB loaded inulin-ibuprofen nanoparticles have a great potential in chemo-therapy.

Recently, chemotherapy-based polymeric nanoparticles have been extensively investigated for solid tumor treatment. Tumor targeted nanoparticles demonstrated great potential for improved accumulation in the tumor tissue, superior anticancer activity and reduced side effects. Thus, inulin-ibuprofen polymer was synthesized by esterification between inulin and ibuprofen, and RGD targeted epirubicin (EPB) loaded nanoparticles were prepared by the self-assembly of inulin-ibuprofen polymer and in situ encapsulation of EPB. RGD conjugated EPB loaded nanoparticles were characterized by dynamic light scattering (DLS) and transmission electron microscope (TEM). The EPB release from the nanoparticles showed pH-dependent profile and accelerated by the decreased pH value, which would favor the effective drug delivery in vivo. Intracellular uptake analysis suggested that RGD conjugated nanoparticles could be easily internalized by the cancer cells. In vitro cytotoxicity revealed that RGD conjugated EPB loaded nanoparticles exhibited the better antitumor efficacy compared with non-conjugated nanoparticles. More importantly, RGD conjugated EPB loaded nanoparticles showed superior anticancer effects and reduced toxicity than free EPB and non-conjugated nanoparticles by in vivo antitumor activity, EPB biodistribution and histology analysis.

RGD conjugated EPB loaded inulin-ibuprofen nanoparticles were prepared to enhance tumor accumulation and reduce the systemic toxicity.Figure optionsDownload as PowerPoint slide