Preparation of paclitaxel-loaded polymeric nanoparticles and evaluation on their anti-tumor activities

The aim of the research was to prepare paclitaxel-loaded low molecular weight heparin-all-trans-retinoid acid conjugate grafted with c(RGDyK)(PTX-LHRyK)nanoparticles, and to study the in vivo and in vitro anti-tumor effect of the PTX-LHRyK nanoparticles. The PTX-LHRyK nanoparticles were prepared by dialysis and characterized in terms of size, Zeta potential, and drug entrapment efficiency. The effect of PTX-LHRyK nanoparticles on PTX-induced cytotoxicity was investigated in B16F10 cell lines by MTT assay. The in vivo anti-tumor effect(in terms of tumor growth)and tumor inhibition rate were also evaluated. The PTX-LHRyK nanoparticles were generally spherical with a mean diameter of(131. 7±2. 3)nm, a negative surface charge, and encapsulation efficiency of(84. 84±2. 63)%. The tumor inhibition rate of the PTX-LHRyK nanoparticles was up to 75. 28%, which is 1. 46-fold higher than the combined injection. It was shown in the in vitro anti-tumor activity study that the PTX-LHRyK nanoparticles displayed slightly higher in vitro cytotoxicity as compared to the combined injection as the increase of the incubate time, but LHRyK conjugate at the studied concentration range did not show significant influence on the cell viability of the B16F10 cells。The in vivo anti-tumor effect of the PTX was significantly improved using the LHRyK conjugate as a carrier, with more powerful anti-tumor activity than PTX-ATRA-INJ as well as lower side-effects.