writer：Hui Zheng, Sai Li*, Yuji Pu, Yusi Lai, Bin He*, Zhongwei Gu*
keywords：PEG-Chrysin Conjugates, Drug Delivery
source：期刊
specific source：Europe Journal of Pharmaceutics and Biopharmaceutics, DOI: 10.1016/j.ejpb.2014.03.011
Issue time：2014年
Nanoparticle-based drug delivery systems promise the safety and efficacy of anticancer drugs. Herein, we presented a facile approach to fabricate novel nanoparticles generated by PEG-Chrysin conjugates for the delivery of anticancer drug doxorubicin. Chrysin was immobilized on the terminal group of methoxyl poly(ethylene glycol) (mPEG) to form mPEG-Chrysin conjugate. The conjugates were self-assembled into nanoparticles. Doxorubicin (DOX) was loaded in the nanoparticles. The self-assembly, drug release profiles, interactions between nanoparticle and drug, cellular uptake and in vitro anticancer activity of the DOX loaded nanoparticles were investigated. The results showed that the mean diameters of drug loaded nanoparticles were below 200 nanometers. Strong π-π stacking interaction was tested within the drug loaded nanoparticles. The drug release rate was closely related to the chain length of PEG, shorter PEG chain resulted faster release. The mPEG-Chrysin conjugate was non-toxic to both 3T3 fibroblasts and HepG2 cancer cells. The cellular uptake measurements demonstrated that the mPEG₁₀₀₀-Chrysin nanoparticles exhibited higher capability in endocytosis. The IC₅₀ of drug loaded mPEG₁₀₀₀-Chrysin nanoparticles was 4.4 μg/mL, which was much lower than that of drug loaded mPEG₂₀₀₀-Chrysin nanoparticles (6.8 μg/mL). These nanoparticles provided a new strategy for fabricating antitumor drug delivery systems.