PCP copolymers grafted with RGD enhance the rates of RGD-PCP micelles internalized into cells

Abstract

RGD-PCP copolymers were fabricated by grafting Arg-Gly-Asp (RGD) peptide to poly(ε-caprolactone)-b-chitooligosaccharide-b–poly(ethylene glycol) (PCP) copolymers and the rate of internalization of RGD-PCP micelles by PC 12 cells were examined. Increasing intensity of the absorbance of amine groups in FT-IR spectra of RGD-PCP copolymers compared with those of PCP copolymers indicated the presence of RGD in new copolymers. Moreover, the grafting efficiency and molar ratio of RGD peptides to PCP copolymers were 88.2% and 0.45, respectively, analysed with HPLC. The RGD-PCP copolymers self-assemble to micelles at the critical micelle concentration (CMC) of 0.018 wt% (178 mg L⁻¹) and with a mean diameter of 90 nm using a dynamic light-scattering (DLS) analyser. Interestingly, the internalization of DPH-loaded RGD-PCP micelles into PC 12 cells is much faster (e.g. within 5 min) than that of PCP micelles. The new RGD-PCP micelles may potentially be used in cellular drug delivery.

• RGD
• RGD-PCP micelles
• cellular internalization
• drug delivery