(Im)](NAMI-A)的PLGA载药纳米微球制备与表征.docVIP

抗肿瘤药物[ImH][RuCl4(DMSO)(Im)]（NAMI-A）的PLGA载药纳米微球制备与表征 张璇 刘杰* 中山大学化学与化学工程学院 广州 510275 摘要 大量研究表明，钌的一系列配合物具有一定的抗肿瘤活性，其中最受人们关注的是[ImH][RuCl4(DMSO)(Im)]（NAMI-A）。与现今广泛使用的广谱抗癌药物顺铂相比，NAMI-A具有更高的生物活性及更低的毒性。在本实验中，我们用RuCl3与HCl和DMSO反应，生成前体[trans-RuCl4(Me2SO)2][(Me2SO)2H]，并用其与咪唑反应，生成[ImH][RuCl4(DMSO)(Im)]（NAMI-A）。我们利用紫外—可见光分光光度计、红外光谱等表征方法，对NAMI-A进行了表征，得到了一系列的性质。由于NAMI-A容易水解，无法长期保存，我们采用双乳化法，用聚合物poly(Lactide-co-glycolide)(PLGA)为载体，胆酸钠为乳化剂，将药物NAMI-A包裹起来，制成水包油包水体系的纳米微球;并运用冷冻干燥等技术，使得载药纳米微球能够在一定的温度及湿度下长期保存。此外，我们运用紫外－可见分光光度计、红外光谱、粒径分析仪等方法，对载药纳米微球的形态、药物包埋等方面的性质进行了表征。 关键词 NAMI-A；载药纳米微球；抗肿瘤活性 Synthesis and characterization of PLGA nanoparticles of antitumour drug [ImH][RuCl4(DMSO)(Im)](NAMI-A) Liu Jie * Zhang Xuan School of Chemistry and Chemistry Engineering, Sun Yat-sen University，Guangzhou 510275 Abstract Ruthenium complexes have attracted large attention as potential antitumour agents. Among all ruthenium-based antitumour agents, NAMI-A gained the largest attention. Differently from the most useful anticancer drug cisplatin and platinum related compounds, ruthenium complexes have better selectivity for solid tumor metastases and low host toxicity. RuCl3, HCl, DMSO and imidazole(Im) were used to synthesize NAMI-A. UV-vis, IR, MS and 1HNMR were used to characterize it. NAMI-A in aqueous solution was not stable enough to allow sterilization by moist heat, and none of them provided sufficient stability to allow long-term storage of an aqueous solution. We used lyophilization to gain drug that can be long-term stored. In recently study, nanoparticles have delivered selectively and controlled release. In our work, we prepared PLGA nanoparticles of NAMI-A by a double emulsion method, and characterized with UV-vis, IR, Particle Size Analyzer and dialysis research. Keyword NAMI-A, nanoparticles, antitumour activity 前言 恶性肿瘤具有极高的致死率，是目前危害人类健康最主要的疾病之一。1969年，Rosenber等人发现顺铂具有抗肿瘤活性，激发了许多科学家对顺铂的研究，并合成出大量顺铂的类似物[1]。现今，顺铂(cisplatin)是临床上最常用的抗癌药物，对睾丸癌、卵巢癌、头颈肿瘤和膀胱癌等多种癌症都具有显著的药效[2]，其药效随着给药量的增加而增强