Experimental study on preparation and targeting ability in vitro of HCC-targeted lipid microbubble containing 10-HCPT / 中国医学影像技术

ABSTRACT

Objective To prepare HCC-targeted lipid ultrasound microbubble containing 10-hydroxycamptothecin (10-HCPT), and to assess its targeting function in vitro. Methods After the biotinylated monoclonal antibody Hab18 was prepared, the biotinylated degree was determined. Microbubbles containing 10-HCPT were prepared by mechanical vibration. Then the biotinylated antibody was attached to the surface of the microbubbles by avidin-biotin interaction. The physical property, entrapment efficiency and the drug-loading amounts of 10-HCPT lipid microbubbles were determined. The combination of biotinylated Hab18 with microbubbles containing 10-HCPT was proved by immunofluorescent assay, and the targeting function of the targeted microbubbles containing 10-HCPT was observed with light microscope, served non-targeted microbubbles as control group. Results About 13 biotin molecules were coupled to each antibody in average. The disposition of the prepared microbubbles was steady and the mean diameter was 1.52 μm. The drug entrapment efficiency was 76.32% and the drug-loading amounts was 21.81%. Red fluorescence was observed at the edge of the microbubbles in immunofluorescent assay, and the conjugation of the targeted microbubbles containing 10-HCPT with 7721 cells was tight while control group was negative. Conclusion HCC-targeted lipid ultrasound microbubbles containing 10-HPTC can be prepared successfully, with higher entrapment efficiency and drug-loading amounts and strong targeting function in vitro.