Synthesis and characterization of pH-responsive and folated nanoparticles based on self-assembled brush-like PLGA/PEG/AEMA copolymer with targeted cancer therapy properties: A comprehensive kinetic study

In this study, a novel nanocarrier was synthesized based on methacrylated poly(lactic-co-glycolic acid) (mPLGA) as a lipophilic domain, acrylated methoxy poly(ethylene glycol) (aMPEG) as hydrophilic part and N-2-[(tert-butoxycarbonyl)amino] ethyl methacrylamide (Boc-AEMA) as pH-responsive segment. Radical polymerization of the above-mentioned three modified monomers produces amphiphilic brush-like copolymer. The protecting amine group (Boc) was selectively deprotected and the latter targeted copolymer was produced through the reaction of this copolymer with activated folic acid. Nanoprecipitation method was used to prepare quercetin-loaded nanoparticles. Dynamic light scattering (DLS) analysis showed that the produced nanoparticles had nanometric size (<100 nm) and low polydispersity in size at different pHs. Higuchi and Korsmeyer–Peppas models were applied to evaluate release mechanisms and kinetics. Based on in-vitro degradation study, we found that the brush-like copolymer underwent a rapid weight loss in acidic pH.

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► Amphiphilic brush-like copolymer was prepared from PEG and PLGA macromers.
► The linkage of this copolymer to amine-terminated groups made it pH-responsive.
► Conjunction of folic acid to the copolymer structure produced targetable component.
► Quercetin as anti-cancer drug was entrapped in the core of nanoparticles.
► A self-assembled nanoparticle for tumor targeting and therapeutic was produced.