title: Preparation of folate-modified pullulan acetate nanoparticles for tumor-targeted drug delivery.
abstract: The purpose of this work was to develop a novel nano-carrier with targeting property to tumor. In this study, pullulan acetate (PA) was synthesized by the acetylation of pullulan to simplify the preparation technique of nanoparticles. Folic acid (FA) was conjugated to PA in order to improve the cancer-targeting activity. The products were characterized by proton nuclear magnetic resonance (¹H NMR) spectroscopy. Epirubicin-loaded nanoparticles were prepared by a solvent diffusion method. The loading efficiencies and EPI content increased with the amount of triethylamine (TEA) increasing in some degree. FPA nanoparticles could incorporate more epirubicin than PA nanoparticles. The folate-modified PA nanoparticles (FPA/EPI NPs) exhibited faster drug release than PA nanoparticles (PA/EPI NPs) in vitro. Confocal image analysis and flow cytometry test revealed that FPA/EPI NPs exhibited a greater extent of cellular uptake than PA/EPI NPs against KB cells over-expressing folate receptors on the surface. FPA/EPI NPs also showed higher cytotoxicity than PA/EPI NPs. The cytotoxic effect of FPA/EPI NPs to KB cells was inhibited by an excess amount of folic acid, suggesting that the binding and/or uptake were mediated by the folate receptor.
authors: Institute of Biomedical Engineering, Chinese Academy of Medical Science, Peking Union Medical College, The Key Laboratory of Biomedical Material of Tianjin, PO Box 25-204, Tianjin 300192, PR China.
authors: Hui-zhu
authors: HZ
authors: Zhang
authors: Xue-min
authors: XM
authors: Li
authors: Fu-ping
authors: FP
authors: Gao
authors: Ling-rong
authors: LR
authors: Liu
authors: Zhi-min
authors: ZM
authors: Zhou
authors: Qi-qing
authors: QQ
authors: Zhang
mesh_terms: D000107:Acetylation; D000903:Antibiotics, Antineoplastic / Q000008:administration & dosage* / Q000494:pharmacology; D018929:Cell Culture Techniques; D002470:Cell Survival / Q000187:drug effects; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding; D004705:Endocytosis; D015251:Epirubicin / Q000008:administration & dosage* / Q000494:pharmacology; D005434:Flow Cytometry; D005492:Folic Acid / Q000737:chemistry*; D005936:Glucans / Q000737:chemistry*; D006801:Humans; D007624:KB Cells; D018613:Microscopy, Confocal; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D012995:Solubility; D013499:Surface Properties
chemical_list: D000903:Antibiotics, Antineoplastic; D004337:Drug Carriers; D005936:Glucans; D015251:Epirubicin; C009109:pullulan; D005492:Folic Acid