负载疏水药物的两亲性聚（丙氨酸）-b-聚（肌氨酸）微球

Amphiphilic poly(Ala)-b-poly(Sar) microspheres loaded with hydrophobic drug.

作者信息

Kidchob T, Kimura S, Imanishi Y

机构信息

Department of Material Chemistry, Kyoto University, Japan.

出版信息

J Control Release. 1998 Feb 12;51(2-3):241-8. doi: 10.1016/s0168-3659(97)00176-4.

DOI:10.1016/s0168-3659(97)00176-4

PMID:9685922

Abstract

Amphiphilic block polypeptides, (Ala)m(Sar)n, were synthesized. Transmission electron microscopy showed that three kinds of block polypeptides, (Ala)42(Sar)21, (Ala)34(Sar)22, and (Ala)34(Sar)27, formed spherical aggregates in water. Dynamic light scattering measurement revealed that the average diameters of (Ala)42(Sar)21 and (Ala)34(Sar)22 aggregates were in the range of 80-90 nm, whilst that of (Ala)34(Sar)27 was about 30 nm. The polypeptides in aqueous solution took a beta-sheet structure, while they took an alpha-helical conformation in trifluoroethanol. These polypeptide aggregates took up 8-anilinonaphthalene-1-sulfonate (ANS), and the capacity of the aggregates for ANS decreased in the order of (Ala)42(Sar)21 > (Ala)34(Sar)22 > (Ala)34(Sar)27. Sumithion, which is a commercial agricultural insecticide, was also taken up by the polypeptide aggregates. When increasing amounts of Sumithion were introduced, (Ala)42(Sar)21 aggregates kept their shape, but (Ala)34(Sar)27 aggregate increased in size. These different behaviors of the polypeptide aggregates were discussed in terms of different structure of aggregates.

摘要

合成了两亲性嵌段多肽（Ala）m（Sar）n。透射电子显微镜显示，三种嵌段多肽（Ala）42（Sar）21、（Ala）34（Sar）22和（Ala）34（Sar）27在水中形成球形聚集体。动态光散射测量表明，（Ala）42（Sar）21和（Ala）34（Sar）22聚集体的平均直径在80 - 90 nm范围内，而（Ala）34（Sar）27的平均直径约为30 nm。水溶液中的多肽呈β-折叠结构，而在三氟乙醇中呈α-螺旋构象。这些多肽聚集体摄取了8-苯胺基萘-1-磺酸盐（ANS），聚集体对ANS的摄取能力按（Ala）42（Sar）21 > （Ala）34（Sar）22 > （Ala）34（Sar）27的顺序降低。杀螟松是一种商业农用杀虫剂，也被多肽聚集体摄取。当引入越来越多的杀螟松时，（Ala）42（Sar）21聚集体保持其形状，但（Ala）34（Sar）27聚集体尺寸增大。根据聚集体的不同结构对多肽聚集体的这些不同行为进行了讨论。