天冬氨酸-谷氨酸共聚物的合成、表征及性质研究

Preparation, Characterization and Characteristics of Copolypeptide Consisting of L-aspartic acid and L-glutamic acid

制备了 L-天冬氨酸 - L-谷氨酸共聚物 (摩尔比为 8:2 ) ,将 3-氨基丙醇接入材料母体 ,制得聚 - (3-羟丙基 ) - L-天冬氨酸 -谷氨酸材料 (PHPAG)。对材料用核磁共振、X- ray衍射、DSC差热分析及元素分析等作了表征 ,以葡聚糖标准品为相对分子量 ,用凝胶色谱法测定材料的分子量。材料注入小鼠体内后进行了急性毒性、血液参数、微核等生物相容性检测 ,结果表明材料为无毒材料。用不同水解酶对材料作了体外酶解实验 ,实验显示酶对共聚材料有一定程度的酶解。对材料在不同 p H值、光照、湿度等条件下进行了稳定性实验 。

For the purpose of increasing the hydrophilicity of poly-aspartic acid, a copolypeptide consisting of L-aspartic acid and L-glutamic acid (82 2 mol/mol) was prepared. The copolymer was characterized by 1H NMR, 13C NMR, differential scanning calorimetry, X-ray and element analysis. 3-hydroxyamino, as a side chain, was linked to the polymer, and poly-(3-hydroxypropyl)-L-aspartamide-L-glutamide (PHPAG) was obtained. The molecular weight of PHPAG was determined by GPC. Tests of the PHPAG on laboratory animals corrobrated its potential use as a drug carrier. Acute toxicity studies revealed no death in animals treated, other studies recorded no notable difference between treated and control animals either in terms of principal haematological parameters or in micronucleus test. In vitro enzymatic hydrolysis for the co-polymer was performed using chymotrypsin, fungi protease and trypsin. It showed that these proteins could degrade the copolymer to some degree. The effects of pH, light and humidity on PHPAG were also investigated. The results indicated that it was stable under the experiment conditions.