Construction of amphiphilic copolymer nanoparticles based on hyperbranched poly (amine-ester) and 1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine as drug carriers for cancer therapy

Novel amphiphilic copolymer nanoparticles (HPAE-co-PLA-DPPE) composed of hyperbranched poly (amine-ester), polylactide and 1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine (DPPE) segments were designed and synthesized that provided high encapsulation efficiency. These nanoparticles (NPs) were used to encapsulate an antitumor model drug, doxorubicin (DOX). The resulting NPs exhibited high encapsulation efficiency to DOX under an appropriate condition. In vitro release experiments revealed that the release of DOX from NPs was faster at pH 4.5 than that at pH 7.4 or pH 6.0. Confocal microscopy observation indicated that the DOX-loaded NPs can enter cells and localize in lysosomes that can be released quickly into the cytoplasm. The DOX-loaded NPs showed comparable anticancer efficacy with the free drug both in vivo and in vitro. These results demonstrate a feasible application of the hyperbranched copolymer, HPAE-co-PLA-DPPE, as a promising nanocarrier for intracellular delivery of antitumor drugs. FROM THE CLINICAL EDITOR: In this paper, the development of novel amphiphilic copolymer nanoparticles is discussed with the goal of establishing high encapsulation efficiency for chemotherapy drugs.