聚（L-谷氨酸苄酯）的诊断和治疗潜力

Diagnostic and therapeutic potential of poly(benzyl L-glutamate).

作者信息

Yang D J, Li C, Nikiforow S, Gretzer M B, Kuang L R, Lopez M S, Vargas K, Wallace S

机构信息

Division of Diagnostic Imaging, University of Texas M.D. Anderson Cancer Center, Houston 77030.

出版信息

J Pharm Sci. 1994 Mar;83(3):328-31. doi: 10.1002/jps.2600830312.

DOI:10.1002/jps.2600830312

PMID:7515964

Abstract

Poly(benzyl L-glutamate) (PBLG) microcapsules, prepared by a solvent evaporation technique for intravenous injection, are evaluated for their potential use in diagnostic computed tomographic enhancement of liver images. The smaller microcapsules, < 3 microns, loaded with a radiopaque contrast material, ethyl iopanoate (IOPAE), produced prolonged opacification of the liver when delivered intravenously. In vivo tissue distribution studies of PBLG-131I-IOPAE (5 microCi/rat, iv) showed that liver had the highest uptake (percent of injected dose/g of tissue) among other organs 24 h postinjection. An in vitro estrogen receptor assay in pig uteri indicated that PBLG conjugated with estrone did not interfere with estrogen receptor affinity, suggesting the estrogen therapy potential of PBLG-estrone.

摘要

通过溶剂蒸发技术制备的用于静脉注射的聚（L-谷氨酸苄酯）（PBLG）微胶囊，被评估其在肝脏图像诊断性计算机断层扫描增强中的潜在用途。装载不透射线造影剂碘番酸乙酯（IOPAE）的小于3微米的较小微胶囊静脉给药后可使肝脏的显影时间延长。PBLG-131I-IOPAE（5微居里/大鼠，静脉注射）的体内组织分布研究表明，注射后24小时肝脏在其他器官中摄取量最高（每克组织中注射剂量的百分比）。猪子宫的体外雌激素受体测定表明，与雌酮结合的PBLG不干扰雌激素受体亲和力，提示PBLG-雌酮具有雌激素治疗潜力。