writer：Yan Zhang, Jiashi Li, Meidong Lang*, Xiaolin Tang, Lei Li, Xizhong Shen
keywords：poly(ε-caprolactone-co-4-maleate-ε-caprolactone)-folate, nanoparticles, 5-Fluorouracil, targeted delivery, drug controlled delivery, Anti-tumor effect
source：期刊
Issue time：2011年
In this paper, the vitamin folic acid (FA) was covalently linked to the main chain of the maleate-functionalized polymer, poly(ε-caprolactone-co-4-maleate-ε-caprolactone) (P(CL-co-MCL)) to produce folate conjugated poly(ε-caprolactone-co-4-maleate-ε- caprolactone) (P(CL-co-MCL)-folate) via an amide bond by a carbodiimide coupling reaction. The targeted drug delivery nanoparticles of P(CL-co-MCL)-folate for 5-Fluorouracil (5-FU) were achieved by solvent evaporationmethod, and characterized for particle size by dynamic light scattering (DLS), surface morphology by scan electron microscopy (SEM) and entrapment and release behavior by UV spectroscopy. DLS and SEM showed the nanoparticles were being in spherical shape and uniform size distribution. UV spectroscopy showed that the release behavior of 5-FU could be made well-controlled and the release half-life period could reach 16.86 h, which was 26.4 times of that of pure 5-FU. The in vitro targeting test of the drug loaded nanoparticles displayed that the 5-FU loaded nanoparticles exhibited enhanced cell inhibition because folate targeting increased the cytotoxicity of drug-loaded nanoparticles against folate receptor expressing tumor cells. Meanwhile, the tumor inhibition of folate linked nanoparticles was much higher than that of 5-FU alone and that of 5-FU loaded P(CL-co-MCL) nanoparticles. Therefore, P(CL-co-MCL)-folate nanoparticles wouldprovide increased benefits in biomedical and pharmaceutical applications.