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.%Objective To prepare a 10-hydroxycamptothecin (10-HCPT) loaded folate-receptor targeted phase-change contrast agent (FR-HCPT-PNPCA),and to study the general characteristics including drug loading,phase changing and targeting capability in vitro.Methods Using a method of two-step emulsification,the phase-change nanoparticles loading anticancer drug (10-HCPT) with lipids shell and liquid pefluorocarbon core were prepared.The entrapment efficiency and the drug-loading amounts were studied by high performance liquid chromatography,and the phase transition of the nanoparticles after heating was observed.The targeting ability was evaluated on liver cancer cell line 7721 in vitro.Results The FR-HCPT-PNPCA,with a drug encapsulation rate of about 70.42 ％ and drug loading amounts of about 20.05 ％,was prepared successfully.When being heated to 70℃,obvious phase changing and microbubbles generating could be observed under microscope.In addition,a large amount of FR-HCPT-PNPCA particles could adhere specifically around the 7721 cells.Conclusion The prepared FR-HCPT-PNPCA,which has a stable characteristic and high performance of drug loading and tumor targeting,is expected to become a promising multifunctional molecular ultrasound probe for diagnosis and treatment of tumor.
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