透明质酸自组装聚合物胶束的制备及表征

发布时间：2018-11-11 18:01

【摘要】：为了增强抗肿瘤药物的靶向性与抗肿瘤活性,本文制备了透明质酸-十八烷聚合物,用其对阿霉素进行包载,考察其理化性质及体外细胞毒性。合成两亲性透明质酸-十八烷聚合物,利用核磁对其结构进行确证。选择超声法制备载阿霉素的聚合物胶束,考察胶束的粒径、电位、包封率、载药量以及体外释放行为。选择乳腺癌细胞MCF-7为肿瘤细胞模型,考察载药胶束的体外抗肿瘤活性。成功合成了透明质酸-十八烷聚合物。制备的空白胶束和载药的胶束的粒径分别为(180.7±1.25)nm和(178.3±2.24)nm,Zeta电位分别为(-21.3±0.25)mV和(-18.1±0.31)mV。载阿霉素聚合物胶束的包封率为(96.1%±0.72%),载药量为16.1%±1.18%,体外释放行为表明在72h的累计药物释放率仅为40%左右,具有明显的缓释行为。体外细胞毒性结果表明,空白聚合物胶束对肿瘤细胞几乎没有毒性,而载阿霉素的聚合物胶束具有较好的抗肿瘤活性。结论:透明质酸-十八烷聚合物胶束可以有效地包载抗肿瘤药物阿霉素,具有良好的缓释特性和抗肿瘤活性。
[Abstract]:In order to enhance the targeting and antitumor activity of antitumor drugs, hyaluronic acid-octadecane polymer was prepared and encapsulated with adriamycin to investigate its physicochemical properties and cytotoxicity in vitro. Amphiphilic hyaluronic acid-octadecane polymer was synthesized and its structure was confirmed by NMR. The polymer micelles loaded with adriamycin were prepared by ultrasonic method. The particle size, potential, encapsulation efficiency, drug loading and release behavior of the micelles were investigated. Breast cancer cell line MCF-7 was selected as tumor cell model to investigate the antitumor activity of drug loaded micelles in vitro. Hyaluronic acid-octadecane polymer was successfully synthesized. The particle sizes of blank micelles and drug-loaded micelles were (180.7 卤1.25) nm and (178.3 卤2.24) nm,Zeta potentials of (-21.3 卤0.25) mV and (-18.1 卤0.31) mV., respectively. The encapsulation efficiency of the polymer micelles loaded with doxorubicin was (96.1% 卤0.72%) and the drug loading capacity was 16.1% 卤1.18.The release behavior in vitro indicated that the cumulative drug release rate was only about 40% at 72 h. The results of cytotoxicity in vitro showed that the blank polymer micelles had almost no toxicity to tumor cells, while the adriamycin loaded polymer micelles had good antitumor activity. Conclusion: hyaluronic acid-octadecane polymer micelles can effectively encapsulate adriamycin and have good sustained release properties and anti-tumor activity.
【作者单位】：江南大学药学院;
【基金】：教育部博士点基金博导类项目(20110093110008)
【分类号】：R943

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