Construction of curcumin-loaded micelles and evaluation of the anti-tumor effect based on angiogenesis

Abstract

Objective: Inhibition of tumor angiogenesis has become a new targeted tumor therapy. In this study, we established a micellar carrier with a tumor neovascularization-targeting effect modified by the neovascularization-targeting peptide NGR.

Methods: The targeted polymer poly(ethylene glycol)-b-poly(lactide-co-glycolide) (PEG-PLGA) modified with Asn-Gly-Arg (NGR) peptide was prepared and characterized by ¹H nuclear magnetic resonance and Fourier-transform infrared spectrometry. NGR-PEG-PLGA was used to construct curcumin (Cur)-loaded micelles by the solvent evaporation method. The physicochemical properties of the micelles were also investigated. Additionally, we evaluated the antitumor efficacy of the polymer micelles (PM) using in vitro cytology experiments and in vivo animal studies.

Results: The particle size of Cur-NGR-PM was 139.70β±β2.51 nm, and the drug-loading capacity was 14.37β±β0.06%. In vitro cytological evaluation showed that NGR-modified micelles showed higher cellular uptake through receptor-mediated endocytosis pathways than did unmodified micelles, leading to the apoptosis of tumor cells. Then, in vivo antitumor experiments showed that the modified micelles significantly inhibited tumor growth and were safe.

Conclusions: NGR-modified micelles significantly optimized the therapeutic efficacy of Cur. This strategy offers a viable avenue for cancer treatment.

Keywords

Antitumor therapy / Curcumin (Cur) / Micelles / NGR / Tumor angiogenesis

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