We investigated the bio-distributions of [125 I]Spiro-I formulated in sterically stabilized liposomes （SSL） or targeted liposomes （SSTL） in mice,especially their brain uptake.The [125 I]Spiro-I liposomes were prep...We investigated the bio-distributions of [125 I]Spiro-I formulated in sterically stabilized liposomes （SSL） or targeted liposomes （SSTL） in mice,especially their brain uptake.The [125 I]Spiro-I liposomes were prepared by film-ultrasound dispersion method.Cereport （RMP-7） was covalently conjugated with DSPE-PEG,which was attached to the surface of SSL to form SSTL.The encapsulation efficiencies （ee%） of [125 I]Spiro-I-SSL and [125 I]Spiro-I-SSTL were 97.47%±4.01% and 93.02%±2.98%,respectively.The average particle sizes were （66.47±0.76） nm and （71.40±0.45） nm,respectively.After intravenous administration,[125 I]Spiro-I was quickly eliminated from blood.SSL could prolong the retention time of [125 I]Spiro-I in blood and SSTL improved its brain uptake.The AUC of [125 I]Spiro-I-SSTL in brain was increased by 1.52 times as compared to [125 I]Spiro-I,indicating that SSTL could be used for the formulation of [125 I]Spiro-I for the imaging of central nervous system （CNS）.展开更多
Novel spiro[dibenzo[a,i]xanthene-14,3＇-indoline]-2＇,8,13-triones were prepared by the three-component reaction ofβ-naphthol, isatins,and 2-hydroxy-1,4-naphoquinone in the presence of a catalytic amount of H_4SiW_...Novel spiro[dibenzo[a,i]xanthene-14,3＇-indoline]-2＇,8,13-triones were prepared by the three-component reaction ofβ-naphthol, isatins,and 2-hydroxy-1,4-naphoquinone in the presence of a catalytic amount of H_4SiW_（12）O_（40）.This protocol provides a simple one-step procedure with the advantages of easy work-up,mild reaction conditions and environmentally benign.展开更多
基金Research supported by the National Natural Science Foundation of China(2110406421172188)+1 种基金Research Grant from the Innovation Project for Undergraduate of Jiangsu Province(2012JSSPIT3190)Undergraduate of School of Chemistry & Chemical Engineering(HXKY2D201202)
基金National Basic Research Program of China (973 Program, Grant No. 2009CB930300)National Natural Science Foundation of China (Grant No.20501004 and 20871021)
文摘We investigated the bio-distributions of [125 I]Spiro-I formulated in sterically stabilized liposomes （SSL） or targeted liposomes （SSTL） in mice,especially their brain uptake.The [125 I]Spiro-I liposomes were prepared by film-ultrasound dispersion method.Cereport （RMP-7） was covalently conjugated with DSPE-PEG,which was attached to the surface of SSL to form SSTL.The encapsulation efficiencies （ee%） of [125 I]Spiro-I-SSL and [125 I]Spiro-I-SSTL were 97.47%±4.01% and 93.02%±2.98%,respectively.The average particle sizes were （66.47±0.76） nm and （71.40±0.45） nm,respectively.After intravenous administration,[125 I]Spiro-I was quickly eliminated from blood.SSL could prolong the retention time of [125 I]Spiro-I in blood and SSTL improved its brain uptake.The AUC of [125 I]Spiro-I-SSTL in brain was increased by 1.52 times as compared to [125 I]Spiro-I,indicating that SSTL could be used for the formulation of [125 I]Spiro-I for the imaging of central nervous system （CNS）.
基金the financial support from Xinxiang Medical University
文摘Novel spiro[dibenzo[a,i]xanthene-14,3＇-indoline]-2＇,8,13-triones were prepared by the three-component reaction ofβ-naphthol, isatins,and 2-hydroxy-1,4-naphoquinone in the presence of a catalytic amount of H_4SiW_（12）O_（40）.This protocol provides a simple one-step procedure with the advantages of easy work-up,mild reaction conditions and environmentally benign.
