Objective To prepare a kind of paclitaxel loaded PLGA-COOH-targeted Ultrasound Contrast Agent,and to explore its effect of enhancing ultrasound imaging in vitro. Methods The paclitaxe loaded high molecular polymer PLGA-COOH ultrasound contrast agents were produced by the double emulsion technique. Herceptin was covalently linked to the paclitaxel loaded PLGA-COOH nanoparticle surface by carbodiimide technique. The physical property, entrapment efficiency and the drug-loading amounts of paclitaxel were determined. The paclitaxel loaded PLGA-COOH-targeted nanoparticle targeting specifity to breast cancer cells was observed with confocal microscope, and to explore its effect of enhancing ultrasound imaging in vitro. Results The average diameter of paclitaxel loaded PLGA-COOH-targeted nanoparticle was (733.4 ± 30. 7) nm. The drug entrapment efficiency was (65.08 ±2. 31 ) ％ and the drug-loading amounts was (6. 51±0. 23)％. The conjugation of paclitaxel loaded PLGA-COOH-targeted nanoparticle with MCF-7 cells was tight while the control group was negative. In vitro experiment showed that they can enhance the ultrasound imaging greatly. Conclusions The paclitaxel loaded PLGA-COOH-targeted nanoparticle with higher entrapment efficiency can bind to breast cancer effectively in vitro,and can also enhance the ultrasound imaging greatly.%目的 制备一种携Herceptin包裹紫杉醇的高分子造影剂,并进行体外显影实验.方法 通过双乳化法制备出包裹紫杉醇的高分子PLGA-COOH造影刺,然后通过碳二亚胺化学连接法将制备出的载药造影剂与Herceptin连接,检测其一般性质及其包封率与载药量,观察所制备的载药靶向高分子造影剂与乳腺癌细胞的结合能力,并进行体外显影实验.结果 载药靶向高分子造影剂的平均粒径大小为(733.4±30.7)nm,包封率为(65.08±2.31)%,载药量为(6.51±0.23)%,体外寻靶能力实验可观察到载药靶向高分子造影剂与乳腺癌细胞有较强的结合能力,体外显影实验显示载药靶向造影剂显影效果好.结论 成功制备出的携Herceptin包裹紫杉醇的高分子造影剂具有较高的包封率和与乳腺癌细胞结合的能力,在体外显影实验中显影效果好.
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