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叶酸-PAMAM 缀合物的表征:药物载药效率和树枝状大分子形态。

Characterization of folic acid-PAMAM conjugates: drug loading efficacy and dendrimer morphology.

机构信息

a Department of Chemistry-Biochemistry and Physics , University of Québec at Trois-Rivières , C. P. 500, Trois-Rivières, Quebec G9A 5H7 , Canada.

出版信息

J Biomol Struct Dyn. 2018 May;36(7):1918-1924. doi: 10.1080/07391102.2017.1341339. Epub 2017 Jun 28.

Abstract

We report the loading efficacy of folic acid (FA) by polyamidoamine (PAMAM-G3 and PAMAM-G4) nanoparticles in aqueous solution at physiological pH. Thermodynamic parameters ΔH = -47.57 (kJ Mol), ΔS = -122.78 (J Mol, K) and ΔG = -10.96 (kJ Mol) showed FA-PAMAM bindings occur via H-bonding and van der Waals contacts. The stability of acid-PAMAM conjugate increased as polymer size increased. The acid loading efficacy was 40 to 50%. TEM images exhibited major polymer morphological changes upon acid encapsulation. PAMAM dendrimers are capable of FA delivery in vitro.

摘要

我们报告了在生理 pH 值下,多聚酰胺胺(PAMAM-G3 和 PAMAM-G4)纳米粒子在水溶液中对叶酸(FA)的负载效率。热力学参数ΔH=-47.57(kJ/mol)、ΔS=-122.78(J/mol,K)和ΔG=-10.96(kJ/mol)表明 FA-PAMAM 结合是通过氢键和范德华接触发生的。随着聚合物尺寸的增加,酸-PAMAM 结合物的稳定性增加。酸的负载效率为 40%至 50%。TEM 图像显示酸包封后主要的聚合物形态发生变化。PAMAM 树突状聚合物能够在体外递送 FA。

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