Study On The Preparation Of The Ptx-Loading Microbubbles Ultrasound Contrast Agent Targeted To Vcam-1and Related Applications

Objective:To investigate the preparation of ultrasound microbubbles (MBs) which can load Paclitaxel (PTX) and study their drug-loading capacity; controlled release characteristics; targeting ability and related application.Methods:MBs were fabricated by mechanical oscillation; PTX was embedded into the membrane of MBs which were connected with Bio-VCAM-1antibody by biotin-avidin linker system, Characterization of MBs were analyzed by particle size analyzer, and UV-visible spectrometer was identified their PTX-loading capacity, ultrasound image was performed with10MHz linear-array probe; to Evaluation their targeting ability in static and fluid state, the efficiency of releasing PTX were evaluated through ultrasound irradiation with different MI were triggered cavitation; the inhibition effect of ultrasound mediated PTX-loading targeted MBs destruction on mouse tumor.Result:Given that3mg of phospholipid, the maximum of PTX-loading MBs that the mean size was (1.45±0.27)μm encapsulation efficiency was (54.64±2.98)%; and can significantly enhanced ultrasound image; when MI=1.0was used to trigger loaded drug MBs, the efficiency of PTX releasing was35%and90%microbubbles were broken; MBs had displayed specific binding to activated endothelial cells under static conditions, as well as under simulated blood flow conditions, PTX-loaded MBs targeted to VCAM-1combined ultrasound irradiation can Significantly inhibited endothelial cell proliferation (54.43±1.51)%versus the normal group(38.53±0.63)%, Similarly, in vivo, also can effectively inhibit tumor growth and promote tumor cell apoptosis.Conclusion:PTX-loading MBs target to VCAM-1as drug carrier can targeting delivery of PTX, and combined with ultrasound can serve as a safe and effective targeted therapy approaches.