title: Folate-functionalized nanoparticles for controlled ergosta-4,6,8(14),22-tetraen-3-one delivery.
abstract: To improve the therapeutic effect of ergosta-4,6,8(14),22-tetraen-3-one (ergone), a folate-decorated ergone-bovine serum albumin nanoparticles (abbreviated FA-ergone-BSANPs) was prepared. The properties were extensively studied by Zetasizer Nano Particle Size Analyzer and TEM, which indicated the prepared nanoparticles were spherical in shape and uniform in size with a zeta potential of -23.8 mV. The drug-loading capacity also has been determined with drug loading content of 2.73% and encapsulation efficiency of 61.8%. In vitro release studies proved the much slow drug release from the nanoparticles during circulating in the blood stream and the increase of drug release at the target sites. The FA-ergone-BSANPs showed enhanced cellular uptake, increased targeting capacity, and increased cytotoxicity against KB cells over-expressing folate receptor (FR), which indicated that its potent cell-killing activity is specific for cells that express the FR. In vivo experiment also confirmed that FA-ergone-BSANPs represent a FR-targeted chemotherapeutic that can produce potent activity against FR-positive tumors. In conclusion, this report has a great significance in pharmacology and clinical medicine as well as methodology. Further detailed dose-optimization studies will be required for better understanding in vivo pharmacokinetic and bio-distribution behaviors.
authors.affiliation: School of Chemical Engineering, Northwest University, No. 229 Taibai North Road, Xi'an, Shaanxi 710069, China.
authors.forename: Xuhua
authors.initials: X
authors.lastname: Liang
authors.forename: Yang
authors.initials: Y
authors.lastname: Sun
authors.forename: Lusha
authors.initials: L
authors.lastname: Liu
authors.forename: Xuan
authors.initials: X
authors.lastname: Ma
authors.forename: Xiaoyun
authors.initials: X
authors.lastname: Hu
authors.forename: Jun
authors.initials: J
authors.lastname: Fan
authors.forename: Yingyong
authors.initials: Y
authors.lastname: Zhao
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D002783:Cholestenones / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D003692:Delayed-Action Preparations; D016503:Drug Delivery Systems; D005260:Female; D058973:Folate Receptors, GPI-Anchored / Q000378:metabolism; D006801:Humans; D007624:KB Cells; D051379:Mice; D008807:Mice, Inbred BALB C; D053758:Nanoparticles; D010316:Particle Size; D012710:Serum Albumin, Bovine / Q000737:chemistry; D014018:Tissue Distribution
chemical_list: D000970:Antineoplastic Agents; D002783:Cholestenones; D003692:Delayed-Action Preparations; D058973:Folate Receptors, GPI-Anchored; D012710:Serum Albumin, Bovine; C015860:ergosta-4,6,8(14),22-tetraen-3-one