Hyperbranched amphiphilic polymer with folate mediated targeting property

Abstract: Hyperbranched amphiphilic polymer PG6–PLA–PEG was synthesized through grafting hydrophobic poly(d,l-lactide) (PLA) segments and hydrophilic poly(ethylene glycol) (PEG) blocks to hydrophilic hyperbranched polyglycerol core (PG6), subsequently. To achieve cell targeting property, folic acid (FA) was further incorporated to the hyperbranched polymer to obtain PG6–PLA–PEG–FA. The polymers were characterized by 1H NMR, UV–vis spectroscopy and combined size-exclusion chromatography and multiangle laser light scattering (SEC-MALLS) analysis. Due to the amphiphilicity, PG6–PLA–PEG and PG6–PLA–PEG–FA could self-assemble to form nanoparticles in aqueous solutions. Antineoplastic drug, paclitaxel (PTX), was encapsulated into the nanoparticles. The nanoparticles were observed by transmission electron microscopy (TEM). The targeting property of PG6–PLA–PEG–FA was evaluated in vitro. The results showed that the PTX loaded PG6–PLA–PEG–FA nanoparticles exhibited enhanced inhibition on folate receptor positive tumor cells due to the folate mediated targeting. [Copyright &y& Elsevier]