The preparation and properties of docetaxel-carrying lipid microbubble ultrasound contrast agent / 中华超声影像学杂志

ABSTRACT

Objective Self-made docetaxel-carrying microbubbles were developed and evaluated as a new ultrasound contrast agent for diagnosis and targeted-chemotherapeutic drug delivery.Methods Docetaxel was mixed with an aqueous suspension of phospholipids in vials,which were put into 40℃ water for 30 minutes,after cooling,gas in vials was replaced with perfluoropropane gas,then vials were agitated for 45 s on a shaking device.Properties were studied contained concentration,size,zeta potential,drug entrapment efficiency and drug-loading amount.Drug released with ultrasound and imaging for VX2 carcinoma in rabbits were observed.Results Docetaxel-carrying microbubbles had a concentration of approximately 2.2×109～3.2×109/ml,a mean size of 623.1 am and a zeta potential of -(3.1±0.9)mV.Size distribution was 473.4～706.6 nm.Drug entrapment efficiency was more than 70% and drug-loading amount was(17.5±0.8)%.Fixed amount of ultrasound energy ruptured microbubbles and released docetaxel.Liver imaging of rabbits could be enhanced obviously and persistently,"fast in and out"phenomena was typical of VX2 carcinoma.Conclusions Liposome microbubbles represent a new class of acoustically active drug delivery vehicles.Docetaxel-carrying microbubbles can promote the value of ultrasound in tumor diagnosis,and docetaxel-carrying microbubbles combined with ultrasound have a hope to establish a kind of real-time monitoring,targeted system for tumor therapy.