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具有葡聚糖/壳聚糖壳和 BSA/壳聚糖核的纳米粒子——阿霉素的负载和递送。

Nanoparticles with dextran/chitosan shell and BSA/chitosan core--doxorubicin loading and delivery.

机构信息

Key Laboratory of Molecular Engineering of Polymer and Department of Macromolecular Science, Fudan University, 220 Handan Road, Shanghai 200433, China.

出版信息

Int J Pharm. 2010 Jun 30;393(1-2):176-84. doi: 10.1016/j.ijpharm.2010.03.063. Epub 2010 Apr 8.

Abstract

Biocompatible bovine serum albumin (BSA)-dextran-chitosan nanoparticles were fabricated by heating the mixture of chitosan and BSA-dextran conjugates by virtue of the electrostatic attraction between BSA and chitosan as well as the gelation of BSA. The BSA-dextran conjugates were prepared by Maillard reaction. The nanoparticles were characterized by light scattering, zeta-potential, atomic force microscopy and pyrene fluorescence. The nanoparticles having a spherical shape and hydrodynamic diameters of 130-230 nm are stable in physiological condition. Doxorubicin can be effectively loaded into the nanoparticles after changing the pH of their mixture to 7.4 by virtue of the electrostatic and hydrophobic interactions between the nanoparticles and doxorubicin. The antitumor effects of doxorubicin loaded nanoparticles were investigated by the tumor inhibition and survivability of murine ascites hepatoma H22 tumor-bearing mice. The loaded nanoparticles can largely decrease the toxicity of doxorubicin and significantly increase the survivability of the tumor-bearing mice.

摘要

采用静电吸引和 BSA 的胶凝作用,通过加热壳聚糖和 BSA-葡聚糖缀合物的混合物,制备了生物相容性牛血清白蛋白(BSA)-葡聚糖-壳聚糖纳米粒子。BSA-葡聚糖缀合物通过美拉德反应制备。通过光散射、Zeta 电位、原子力显微镜和芘荧光对纳米粒子进行了表征。纳米粒子呈球形,水动力直径为 130-230nm,在生理条件下稳定。通过改变混合物的 pH 值至 7.4,利用纳米粒子与阿霉素之间的静电和疏水相互作用,可以有效地将阿霉素载入纳米粒子中。通过对荷瘤小鼠肿瘤抑制率和存活率的研究,考察了载药纳米粒子的抗肿瘤作用。负载的纳米粒子可以显著降低阿霉素的毒性,并显著提高荷瘤小鼠的存活率。

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