RGD-modified multifunctional nanoparticles encapsulating salvianolic acid A for targeted treatment of choroidal neovascularization

Abstract Background The development of alternative anti-angiogenesis therapy for choroidal neovascularization (CNV) remains a great challenge. Nanoparticle systems have emerged as new form drug delivery in ocular diseases. Here, we report the construction and characterization arginine-glycine-aspartic acid (RGD)-conjugated polyethyleneimine (PEI) vehicle to load antioxidant salvianolic A (SAA) targeted CNV. In this study, PEI was consecutively modified with polyethylene glycol (PEG) conjugated RGD segments, 3-(4?-hydroxyphenyl) propionic acid-Osu (HPAO), fluorescein isothiocyanate (FI), followed by acetylation remaining surface amines generate multifunctional PEI.NHAc-FI-HPAO-(PEG-RGD) (for short, RGD-PEI). formed RGD-PEI utilized an effective platform SAA. Results We showed that RGD-PEI/SAA complexes displayed desirable water dispersibility, low cytotoxicity, sustainable release SAA under different pH conditions. It could be specifically taken up retinal pigment epithelium (RPE) cells which highly expressed ? v ? 5 integrin receptors vitro selectively accumulated CNV lesions vivo. Moreover, specific therapeutic efficacy mouse model laser induced CNV, slow elimination vitreous cavity verified SPECT imaging after 131 I radiolabeling. histological examinations further confirmed biocompatibility RGD-PEI/SAA. Conclusions results suggest designed may potential posterior neovascular Graphic abstract