title: Brain-targeted delivery of trans-activating transcriptor-conjugated magnetic PLGA/lipid nanoparticles.
abstract: Magnetic poly (D,L-lactide-co-glycolide) (PLGA)/lipid nanoparticles (MPLs) were fabricated from PLGA, L-α-phosphatidylethanolamine (DOPE), 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-amino (polyethylene glycol) (DSPE-PEG-NH2), and magnetic nanoparticles (NPs), and then conjugated to trans-activating transcriptor (TAT) peptide. The TAT-MPLs were designed to target the brain by magnetic guidance and TAT conjugation. The drugs hesperidin (HES), naringin (NAR), and glutathione (GSH) were encapsulated in MPLs with drug loading capacity (>10%) and drug encapsulation efficiency (>90%). The therapeutic efficacy of the drug-loaded TAT-MPLs in bEnd.3 cells was compared with that of drug-loaded MPLs. The cells accumulated higher levels of TAT-MPLs than MPLs. In addition, the accumulation of QD-loaded fluorescein isothiocyanate (FITC)-labeled TAT-MPLs in bEnd.3 cells was dose and time dependent. Our results show that TAT-conjugated MPLs may function as an effective drug delivery system that crosses the blood brain barrier to the brain.
authors.affiliation: Jiangsu Key Laboratory of Brain Disease Bioinformation, Xuzhou Medical College, Xuzhou, Jiangsu Province, China; School of Basic Education Sciences, Xuzhou Medical College, Xuzhou, Jiangsu Province, China.
authors.forename: Xiangru
authors.initials: X
authors.lastname: Wen
authors.affiliation: College of Animal Science and Technology, Yunnan Agricultural University, Yunnan, Kunming Province, China.
authors.forename: Kai
authors.initials: K
authors.lastname: Wang
authors.affiliation: School of Pharmacy, Xuzhou Medical College, Xuzhou, Jiangsu Province, China.
authors.forename: Ziming
authors.initials: Z
authors.lastname: Zhao
authors.affiliation: College of Animal Science and Technology, Yunnan Agricultural University, Yunnan, Kunming Province, China.
authors.forename: Yifang
authors.initials: Y
authors.lastname: Zhang
authors.affiliation: College of Animal Science and Technology, Yunnan Agricultural University, Yunnan, Kunming Province, China.
authors.forename: Tingting
authors.initials: T
authors.lastname: Sun
authors.affiliation: Research Center for Neurobiology and Department of Neurobiology, Xuzhou Medical College, Xuzhou, Jiangsu Province, China.
authors.forename: Fang
authors.initials: F
authors.lastname: Zhang
authors.affiliation: Research Center for Neurobiology and Department of Neurobiology, Xuzhou Medical College, Xuzhou, Jiangsu Province, China.
authors.forename: Jian
authors.initials: J
authors.lastname: Wu
authors.affiliation: Research Center for Neurobiology and Department of Neurobiology, Xuzhou Medical College, Xuzhou, Jiangsu Province, China.
authors.forename: Yanyan
authors.initials: Y
authors.lastname: Fu
authors.affiliation: Research Center for Neurobiology and Department of Neurobiology, Xuzhou Medical College, Xuzhou, Jiangsu Province, China.
authors.forename: Yang
authors.initials: Y
authors.lastname: Du
authors.affiliation: Department of Neurology, Affiliated Hospital of Xuzhou Medical College, Xuzhou, Jiangsu Province, China.
authors.forename: Lei
authors.initials: L
authors.lastname: Zhang
authors.affiliation: Department of Neurology, Affiliated Hospital of Xuzhou Medical College, Xuzhou, Jiangsu Province, China.
authors.forename: Ying
authors.initials: Y
authors.lastname: Sun
authors.affiliation: Department of Neurology, Affiliated Hospital of Xuzhou Medical College, Xuzhou, Jiangsu Province, China.
authors.forename: YongHai
authors.initials: Y
authors.lastname: Liu
authors.affiliation: School of Basic Education Sciences, Xuzhou Medical College, Xuzhou, Jiangsu Province, China; Department of Medical Information, Xuzhou Medical College, Xuzhou, Jiangsu Province, China.
authors.forename: Kai
authors.initials: K
authors.lastname: Ma
authors.affiliation: Research Center for Neurobiology and Department of Neurobiology, Xuzhou Medical College, Xuzhou, Jiangsu Province, China.
authors.forename: Hongzhi
authors.initials: H
authors.lastname: Liu
authors.affiliation: Jiangsu Key Laboratory of Brain Disease Bioinformation, Xuzhou Medical College, Xuzhou, Jiangsu Province, China; Research Center for Neurobiology and Department of Neurobiology, Xuzhou Medical College, Xuzhou, Jiangsu Province, China.
authors.forename: Yuanjian
authors.initials: Y
authors.lastname: Song
mesh_terms: D000818:Animals; D001921:Brain / Q000378:metabolism*; D016503:Drug Delivery Systems / Q000379:methods; D044950:Flavanones / Q000737:chemistry; D005978:Glutathione / Q000737:chemistry; D006569:Hesperidin / Q000737:chemistry; D006801:Humans; D019344:Lactic Acid / Q000737:chemistry*; D053758:Nanoparticles / Q000737:chemistry*; D010714:Phosphatidylethanolamines / Q000737:chemistry; D011092:Polyethylene Glycols / Q000737:chemistry; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer
chemical_list: D044950:Flavanones; D010714:Phosphatidylethanolamines; C107570:polyethylene glycol-distearoylphosphatidylethanolamine; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D011092:Polyethylene Glycols; D006569:Hesperidin; D005978:Glutathione; C005274:naringin