title: Nanoparticles generated by PEG-Chrysin conjugates for efficient anticancer drug delivery.
abstract: 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 methoxy 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 nm. 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.
authors.affiliation: National Engineering Research Center for Biomaterials, Sichuan University, Chengdu, China; School of Chemical Engineering, Sichuan University, Chengdu, China.
authors.forename: Hui
authors.initials: H
authors.lastname: Zheng
authors.affiliation: School of Chemical Engineering, Sichuan University, Chengdu, China. Electronic address: lisai@scu.edu.cn.
authors.forename: Sai
authors.initials: S
authors.lastname: Li
authors.affiliation: National Engineering Research Center for Biomaterials, Sichuan University, Chengdu, China.
authors.forename: Yuji
authors.initials: Y
authors.lastname: Pu
authors.affiliation: National Engineering Research Center for Biomaterials, Sichuan University, Chengdu, China.
authors.forename: Yusi
authors.initials: Y
authors.lastname: Lai
authors.affiliation: National Engineering Research Center for Biomaterials, Sichuan University, Chengdu, China. Electronic address: bhe@scu.edu.cn.
authors.forename: Bin
authors.initials: B
authors.lastname: He
authors.affiliation: National Engineering Research Center for Biomaterials, Sichuan University, Chengdu, China. Electronic address: zwgu@scu.edu.cn.
authors.forename: Zhongwei
authors.initials: Z
authors.lastname: Gu
mesh_terms: D016475:3T3 Cells; D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage*; D004317:Doxorubicin / Q000008:administration & dosage*; D004337:Drug Carriers / Q000008:administration & dosage; D016503:Drug Delivery Systems / Q000379:methods; D004705:Endocytosis / Q000187:drug effects; D005419:Flavonoids / Q000008:administration & dosage*; D056945:Hep G2 Cells; D006801:Humans; D051379:Mice; D053758:Nanoparticles / Q000008:administration & dosage*; D010316:Particle Size; D011092:Polyethylene Glycols / Q000008:administration & dosage*; D011108:Polymers / Q000008:administration & dosage
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D005419:Flavonoids; D011108:Polymers; C043561:chrysin; D011092:Polyethylene Glycols; D004317:Doxorubicin
keywords: Anticancer activity; Doxorubicin; Drug delivery; Nanoparticles; mPEG-Chrysin conjugate; π–π Stacking interaction