title: Radiosynthesis, biodistribution and micro-SPECT imaging study of dendrimer-avidin conjugate.
abstract: Partially acetylated generation five polyamidoamine (PAMAM) dendrimer (G5-Ac) was reacted with biotin and 2-(p-isothiocyanatobenzyl)-6-methyl-diethylenetria minepentaacetic acid (1B4M-DTPA), respectively to form the complex Bt-G5-Ac-1B4M which was further conjugated with avidin to give the conjugate Av-G5-Ac-1B4M. Then both of the conjugates were radiolabeled with technetium-99m ((99m)Tc), respectively. Their in vitro cellular uptake study shows that the conjugate of Av-G5-Ac-1B4M-(99m)Tc exhibits much higher cellular uptake in HeLa cells than that of Bt-G5-Ac-1B4M-(99m)Tc. Accordingly the following evaluation such as in vitro/in vivo stability, biodistribution and micro-SPECT imaging was observed only for the conjugate of Av-G5-Ac-1B4M-(99m)Tc.
authors.affiliation: Shanghai Institute of Applied Physics, Chinese Academy of Sciences, Shanghai, China.
authors.forename: Xiaoping
authors.initials: X
authors.lastname: Xu
authors.forename: Yuanqing
authors.initials: Y
authors.lastname: Zhang
authors.forename: Xudong
authors.initials: X
authors.lastname: Wang
authors.forename: Xunxiang
authors.initials: X
authors.lastname: Guo
authors.forename: Xuezhu
authors.initials: X
authors.lastname: Zhang
authors.forename: Yujin
authors.initials: Y
authors.lastname: Qi
authors.forename: Yu-Mei
authors.initials: YM
authors.lastname: Shen
mesh_terms: D000818:Animals; D001360:Avidin / Q000138:chemical synthesis* / Q000737:chemistry; D002851:Chromatography, High Pressure Liquid; D050091:Dendrimers / Q000138:chemical synthesis* / Q000737:chemistry; D004355:Drug Stability; D006367:HeLa Cells; D006801:Humans; D051379:Mice; D015394:Molecular Structure; D004369:Pentetic Acid / Q000031:analogs & derivatives; D013667:Technetium; D014018:Tissue Distribution; D015899:Tomography, Emission-Computed, Single-Photon
chemical_list: D050091:Dendrimers; D001360:Avidin; C077295:2-(4-isothiocyanatobenzyl)-6-methyldiethylenetriaminepentaacetic acid; D013667:Technetium; D004369:Pentetic Acid