载10-羟基喜树碱的叶酸受体靶向相变超声造影剂的制备及一般特性

发布时间：2018-03-14 08:11

  本文选题：-羟基喜树碱　切入点：叶酸　出处：《中国介入影像与治疗学》2017年03期 　论文类型：期刊论文

【摘要】：目的制备一种载10-羟基喜树碱(10-HCPT)的叶酸受体靶向相变纳米粒超声造影剂(FR-HCPT-PNPCA),评价其载药及在体外的相变能力、对肿瘤细胞的靶向能力等一般特性。方法通过双步乳化法制备以脂质为壳膜材料、液态氟碳为内核,且包裹抗癌药物10-HCPT的纳米粒,采用高效液相色谱研究其药物包封率和载药量,在体外通过加热法研究其相变产生微泡的能力,并在肝癌细胞株7721细胞上研究其体外寻靶能力。结果成功制备出载10-HCPT的靶向相变纳米粒FR-HCPT-PNPCA,其药物包封率为70.42%,载药量为20.05%。当加热至70℃时,显微镜下可以观察到明显的相变并产生微气泡,且大量纳米粒可特异性地黏附于肝癌细胞周围。结论 FR-HCPT-PNPCA载药率高,性质稳定,靶向肿瘤能力强,有望成为一种集肿瘤诊治于一体的多功能超声分子探针,具有良好的应用前景。
[Abstract]:Objective to prepare FR-HCPT-PNPCAA, a kind of folic acid receptor targeting phase change nano-particle ultrasound contrast agent (FR-HCPT-PNPCAA) loaded with 10-hydroxycamptothecin (10-HCPTT), and to evaluate its drug loading and phase transformation ability in vitro. Methods the nanoparticles with lipids as shell material and liquid fluorocarbon as core and encapsulated with anticancer drug 10-HCPT were prepared by two-step emulsification. High performance liquid chromatography (HPLC) was used to study the encapsulation efficiency and drug loading, and the ability of phase change to produce microbubbles was studied by heating method in vitro. The target finding ability of FR-HCPT-PNPCAA was studied on the hepatoma cell line 7721 in vitro. Results the target phase change nanoparticles FR-HCPT-PNPCAA carrying 10-HCPT were successfully prepared. The encapsulation efficiency of FR-HCPT-PNPCAA was 70.42 and the drug loading capacity was 20.05.When heated to 70 鈩，

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