ULTRASOUND-TRIGGERED DRUG RELEASE AND ENHANCED ANTICANCER EFFECT OF DOXORUBICIN-LOADED POLY(D,L-LACTIDE-CO-GLYCOLIDE)-METHOXY-POLY(ETHYLENE GLYCOL) NANODROPLETS
ULTRASOUND-TRIGGERED DRUG RELEASE AND ENHANCED ANTICANCER EFFECT OF DOXORUBICIN-LOADED POLY(D,L-LACTIDE-CO-GLYCOLIDE)-METHOXY-POLY(ETHYLENE GLYCOL) NANODROPLETS
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DOI：
10.1016/j.ultrasmedbio.2011.05.012
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发表时间：
2011-08-01
影响因子：
2.9
通讯作者：
Zhao, Jingyu
中科院分区：
文献类型：
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作者：
Du, Lina;Jin, Yiguang;Zhao, Jingyu
本研究制备了一种新型超声响应的阿霉素（DOX）纳米微粒系统。首先使用聚（D，L-丙交酯-共-乙交酯）-甲氧基-聚（乙二醇）（PLGA-mPEG）制备了载DOX的聚合物胶束，具有89.2%的高包封率。在用全氟戊烷（沸点29摄氏度）填充后，胶束转化成由于PEG壳而稳定的纳米液滴。纳米液滴在37摄氏度下转化为纳米气泡，如果不施加超声波，几乎没有药物释放。显示了具有pH依赖性的超声触发的药物释放。在37 ℃超声处理0.5min后，在pH 6.5时DOX释放百分比为9.59%（也出现在肿瘤中），而在pH 7.4时仅为2.22%。第三组（载阿霉素纳米液滴联合超声）的抑瘤率为84.3%，高于第二组（载阿霉素纳米液滴）的60.4%。此外，纳米液滴显示出比游离药物低得多的毒性。这种新型的纳米液滴有望成为一种很有前途的抗癌药物传递系统。（电子邮件：jinyg@bmi.ac.cn）（C）2011年世界医学和生物学超声联合会。
A novel ultrasound-responsive doxorubicin (DOX)-loaded nanoparticulate system was prepared in this study. The DOX-loaded polymeric micelles were first prepared using poly(D, L-lactide-co-glycolide)-methoxy-poly(ethylene glycol) (PLGA-mPEG) with a high encapsulation efficiency of 89.2%. After filling with perfluoropentane (boiling point 29 degrees C), the micelles were transformed into nanodroplets that were stable as a result of the PEG shell. The nanodroplets were transformed into nanobubbles at 37 degrees C, and little drug was released if no ultrasound was exerted. Ultrasound-triggered drug release, with pH dependency, was shown. The DOX release percentage was 9.59% at pH 6.5 (also appeared in tumor) and only 2.22% at pH 7.4 after sonicating for 0.5 min at 37 degrees C. The tumor inhibitory rate of Group III (DOX-loaded nanodroplets combined with ultrasound) was 84.3%, more than that of Group II (DOX-loaded nanodroplets), which was 60.4%. Moreover, the nanodroplets showed much lower toxicity than free drugs. The novel nanodroplets could be a promising anticancer drug delivery system. (E-mail: jinyg@bmi.ac.cn) (C) 2011 World Federation for Ultrasound in Medicine & Biology.