In vitro targeting behaviors of Folate-conjugate Pluronic F127/poly (lactic-co-glycolic) nanoparticles

X.Y. Xiong
Jiangxi Science and Technology Normal University,

Keywords: targeted delivery, pluronic, poly (lactic-co-glycolic), nanoparticles, folic acid


Novel Folated Pluronic F127/poly (lactic-co-glycolic) (FA-F127-PLGA) and PLGA-F127-PLGA block copolymer were synthesized and characterized by 1H nuclear magnetic resonance (NMR). Nanoparticles self-assembled from these two copolymers were characterized by dynamic light scattering (DLS) and transmission electron microscope (TEM). Paclitaxel (PTX) was successfully encapsulated in these two nanoparticles. According to in vitro release studies of PTX-loaded nanoparticles, after an initial burst release during the first 11h, the entrapped PTX released slowly in the following 82h. The cytotoxicity studies demonstrated that the in vitro antitumor effect of PTX could be improved by encapsulating PTX into PLGA-F127-PLGA nanoparticles. Moreover, folate-targeted FA-F127-PLGA nanoparticles were more effective than PLGA-F127-PLGA when delivering PTX in folate receptor overexpressing OVCAR-3 cells, which could be due to the FA-receptor-meditated endocytosis. As the treatment time became longer, the targeting effects were more obvious. The effective targeting properties have also been proved by fluorescence tests. In vivo pharmacokinetic studies indicated that FA-F127-PLGA nanoparticles prolong the circulation time of PTX in plasma, and delay the blood clearance of PTX. These results indicated that Folated FA-F127-PLGA could be a potential carrier in long-term targeted PTX delivery.