Targeted therapy for glioma using cyclic RGD-entrapped polyionic complex nanomicelles

Abstract

Background:The purpose of this study was to test the efficacy of cyclic Arg-Gly-Asp (RGD) peptide conjugated with polyionic complex nanomicelles as targeted therapy for glioma. Methods: A stable cyclic RGD polyionic complex nanostructure, ie, a c(RGDfC) polyionic complex micelle, was synthesized and its biocompatibility with cultured neurons was assessed using a cell viability assay. Targeted binding to cultured glioma cells was evaluated by the CdTe quantum dot marking technique and a cell viability assay. The inhibitory effect of the nanomicelles against glioma cells was also evaluated, and their targeted migration into rat brain glioma cells and apoptotic effects were traced by the CdTe quantum dot marking and immunohistochemical staining. Results: c(RGDfC) polyionic complex micelles did not affect the growth of neurons but bonded selectively to and inhibited proliferation of glioma cells in vitro. When tested in vivo, the micelles migrated into glioma cells, inducing apoptosis in the rat brain. Conclusion:The c(RGDfC) polyionic complex micelle is an effective targeted therapy against glioma.

RGD-Modified Nanocarrier-Mediated Targeted Delivery of HIF-1α-AA Plasmid DNA to Cerebrovascular Endothelial Cells for Ischemic Stroke Treatment

“…RGD (R, arginine; G, glycine; D, aspartic acid) is a specific ligand for integrin receptors. , The expression levels of integrin receptors are greatly improved in cerebral ischemia, making it easier for nanocarriers containing RGD to enter vascular endothelial cells of the infarcted area by binding to the overexpressed integrins . Therefore, gene carriers conjugated with RGD peptides have recently gained attention as a potential and efficient approach for treating ischemic diseases. , Moreover, many studies have used RGD-modified nanoparticles for the treatment of neurological diseases, and Zhang, L. et al demonstrated that RGD-modified synthetic hyperbranched cationic polymers can cross the blood–brain barrier in vivo. − Consequently, in this study, we selected RGD as a targeting ligand and used it for the targeted therapy of ischemic stroke.…”

Forward Precision Medicine: Micelles for Active Targeting Driven by Peptides

“…cRGD was also exploited by Liu et al to target glioma cells [ 121 ]. They formulated homogeneous polyionic micelles based on maleimide-PEG-g- N -diethanolamine (PDEA) and maleimide-PEG-g-poly(aspartamide) (PAsp), with an average diameter of 60 nm.…”

Effects of arginine–glycine–aspartic acid peptide-conjugated quantum dots-induced photodynamic therapy on pancreatic carcinoma in vivo

“…Integrin plays a critical part in the regulation of the growth, metastasis, and angiogenesis of tumors. [30][31][32] Therefore, creation of RGD-conjugated quantum dots (QDs-RGD) can help to trace and image tumor cells in vivo.…”