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布洛芬与牛血清白蛋白-葡聚糖缀合物的自组装实现药物的有效负载。

Self-assembly of ibuprofen and bovine serum albumin-dextran conjugates leading to effective loading of the drug.

作者信息

Li Juan, Yao Ping

机构信息

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

出版信息

Langmuir. 2009 Jun 2;25(11):6385-91. doi: 10.1021/la804288u.

Abstract

A simple and green process of simultaneous formation of albumin nanoparticles and encapsulation of hydrophobic drugs in aqueous solution was developed. Bovine serum albumin (BSA)-dextran conjugates were prepared through the Maillard reaction. Ibuprofen was used as a drug model. The solubility of protonated ibuprofen decreases, and then precipitation occurs when the pH of saturated ibuprofen solution is changed from alkali to acidic value. In the presence of the conjugates, a binding of ibuprofen with BSA through hydrophobic and electrostatic interactions can suppress the precipitation of ibuprofen. After a heat treatment, the gelation of BSA results in the formation of nanoparticles and fixing of the ibuprofen in the core. The nanoparticles were characterized with dynamic and static light scattering, zeta-potential, and transmission electron microscopy. The nanoparticles are of spherical shape having a hydrodynamic diameter of about 70 nm. As much as 0.7 unit weight of ibuprofen can be loaded into one unit weight of the conjugates. The dextran conjugated to BSA stabilizes the nanoparticles in aqueous solution.

摘要

开发了一种在水溶液中同时形成白蛋白纳米颗粒并包封疏水药物的简单绿色方法。通过美拉德反应制备牛血清白蛋白(BSA)-葡聚糖缀合物。以布洛芬作为药物模型。当饱和布洛芬溶液的pH值从碱性变为酸性时,质子化布洛芬的溶解度降低,随后发生沉淀。在缀合物存在下,布洛芬通过疏水和静电相互作用与BSA结合可抑制布洛芬沉淀。经过热处理后,BSA凝胶化导致纳米颗粒形成并将布洛芬固定在核心中。用动态和静态光散射、zeta电位和透射电子显微镜对纳米颗粒进行了表征。纳米颗粒呈球形,流体动力学直径约为70 nm。每单位重量的缀合物可负载多达0.7单位重量的布洛芬。与BSA缀合的葡聚糖可使纳米颗粒在水溶液中稳定。

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