Currently, sorafenib is the only systemic therapy capable of increasing overall survival of hepatocellular carcinoma patients. Unfortunately, its side effects, particularly its overall toxicity, limit the therapeutic ...Currently, sorafenib is the only systemic therapy capable of increasing overall survival of hepatocellular carcinoma patients. Unfortunately, its side effects, particularly its overall toxicity, limit the therapeutic response that can be achieved. Superparamagnetic iron oxide nanoparticles （SPIONs） are very attractive for drug delivery because they can be targeted to specific sites in the body through application of a magnetic field, thus improving intratumoral accumulation and reducing adverse effects. Here, nanoformulations based on polyethylene glycol modified phospholipid micelles, loaded with both SPIONs and sorafenib, were successfully prepared and thoroughly investigated by complementary techniques. This nanovector system provided effective drug delivery, had an average hydrodynamic diameter of about 125 nm, had good stability in aqueous medium, and allowed controlled drug loading. Magnetic analysis allowed accurate determination of the amount of SPIONs embedded in each micelle. An in vitro system was designed to test whether the SPION micelles can be efficiently held using a magnetic field under typical flow conditions found in the human liver. Human hepatocellular carcinoma （HepG2） cells were selected as an in vitro system to evaluate tumor cell targeting efficacy of the superparamagnetic micelles loaded with sorafenib. These experiments demonstrated that this delivery platform is able to enhance sorafenib＇s antitumor effectiveness by magnetic targeting. The magnetic nanovectors described here represent promising candidates for targeting specific hepatic tumor sites, where selective release of sorafenib can improve its efficacy and safety profile.展开更多
目的制备PEG修饰的葛根素纳米脂质体,建立快速检测其包封率与体外释放的方法。方法采用薄膜分散法制备PEG修饰的葛根素纳米脂质体,用透射电子显微镜观察并拍照,激光粒度仪测定脂质体的粒径和Zeta电位;采用多功能酶标仪,结合葛根素荧光...目的制备PEG修饰的葛根素纳米脂质体,建立快速检测其包封率与体外释放的方法。方法采用薄膜分散法制备PEG修饰的葛根素纳米脂质体,用透射电子显微镜观察并拍照,激光粒度仪测定脂质体的粒径和Zeta电位;采用多功能酶标仪,结合葛根素荧光光谱性质,建立葛根素含量的快速分析方法,超滤离心法分离未包封的葛根素,并对包封率进行测定,透析法考察其体外释放行为。结果所制备的PEG修饰的葛根素纳米脂质体轮廓清晰,呈圆形或类圆形,粒径为230.8 nm,多分散指数(PDI)为0.094,Zeta电位为-3.38 m V,葛根素在0.01~1.0μg·m L-1浓度范围内与RFU呈良好的线性关系,R2=0.9991;PEG修饰的葛根素纳米脂质体具有一定程度的缓释作用。结论多功能酶标仪结合葛根素荧光光谱性质能快速、准确测定葛根素含量。展开更多
文摘Currently, sorafenib is the only systemic therapy capable of increasing overall survival of hepatocellular carcinoma patients. Unfortunately, its side effects, particularly its overall toxicity, limit the therapeutic response that can be achieved. Superparamagnetic iron oxide nanoparticles （SPIONs） are very attractive for drug delivery because they can be targeted to specific sites in the body through application of a magnetic field, thus improving intratumoral accumulation and reducing adverse effects. Here, nanoformulations based on polyethylene glycol modified phospholipid micelles, loaded with both SPIONs and sorafenib, were successfully prepared and thoroughly investigated by complementary techniques. This nanovector system provided effective drug delivery, had an average hydrodynamic diameter of about 125 nm, had good stability in aqueous medium, and allowed controlled drug loading. Magnetic analysis allowed accurate determination of the amount of SPIONs embedded in each micelle. An in vitro system was designed to test whether the SPION micelles can be efficiently held using a magnetic field under typical flow conditions found in the human liver. Human hepatocellular carcinoma （HepG2） cells were selected as an in vitro system to evaluate tumor cell targeting efficacy of the superparamagnetic micelles loaded with sorafenib. These experiments demonstrated that this delivery platform is able to enhance sorafenib＇s antitumor effectiveness by magnetic targeting. The magnetic nanovectors described here represent promising candidates for targeting specific hepatic tumor sites, where selective release of sorafenib can improve its efficacy and safety profile.
文摘目的制备PEG修饰的葛根素纳米脂质体,建立快速检测其包封率与体外释放的方法。方法采用薄膜分散法制备PEG修饰的葛根素纳米脂质体,用透射电子显微镜观察并拍照,激光粒度仪测定脂质体的粒径和Zeta电位;采用多功能酶标仪,结合葛根素荧光光谱性质,建立葛根素含量的快速分析方法,超滤离心法分离未包封的葛根素,并对包封率进行测定,透析法考察其体外释放行为。结果所制备的PEG修饰的葛根素纳米脂质体轮廓清晰,呈圆形或类圆形,粒径为230.8 nm,多分散指数(PDI)为0.094,Zeta电位为-3.38 m V,葛根素在0.01~1.0μg·m L-1浓度范围内与RFU呈良好的线性关系,R2=0.9991;PEG修饰的葛根素纳米脂质体具有一定程度的缓释作用。结论多功能酶标仪结合葛根素荧光光谱性质能快速、准确测定葛根素含量。
