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首页> 外文期刊>Bioorganic and medicinal chemistry >Liposomes modified with double-branched biotin: A novel and effective way to promote breast cancer targeting
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Liposomes modified with double-branched biotin: A novel and effective way to promote breast cancer targeting

机译：双支化生物素修饰脂质体：一种促进乳腺癌靶向的新颖有效方法

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Although active targeting liposomes with cancer-specific ligands can bind and internalize into cancer cells, only a few high-efficiency liposomes have been developed so far because traditional single branched ligand modified liposomes generally failed to deliver adequate therapeutic payload. In this paper, we broke the traditional design concept and synthesized the double branched biotin modified cholesterol (Bio(2)-Chol) for the first time. On this basis, different biotin density modified liposomes ((Bio-Chol) Lip, (Bio-Chol)(2)Lip and (Bio(2)-Chol) Lip) were successfully prepared and used as active targeting drug delivery systems for the treatment of breast cancer. The in vitro and in vivo breast cancer-targeting ability of these liposomes were systemically studied using paclitaxel (PTX) as the model drug. And the uptake mechanism of (Bio(2)-Chol) Lip was investigated. The results showed that (Bio(2)-Chol) Lip had the best breast cancer-targeting ability compared with naked paclitaxel, unmodified Lip, (Bio-Chol) Lip and (Bio-Chol)(2)Lip. In particular, the relative uptake efficiency (RE) and concentration efficiency (CE) of (Bio(2)-Chol) Lip were respectively enhanced by 5.61- and 5.06-fold compared to that of naked paclitaxel. Both distribution data and pharmacokinetic parameters suggested that the double branched biotin modified liposome ((Bio(2)-Chol) Lip) is a very promising drug delivery carrier for breast cancer.
机译：尽管具有癌症特异性配体的活性靶向脂质体可以结合并内化到癌细胞中，但到目前为止，只有少数高效脂质体被开发出来，因为传统的单支链配体修饰脂质体通常无法提供足够的治疗有效载荷。本文打破了传统的设计理念，首次合成了双支链生物素修饰胆固醇（Bio（2）-Chol）。在此基础上，成功制备了不同生物素密度修饰的脂质体（（Bio-Chol） Lip、（Bio-Chol）（2）Lip和（Bio（2）-Chol） Lip），并作为治疗乳腺癌的活性靶向药物递送系统。以紫杉醇（PTX）为模型药物，系统研究了这些脂质体的体外和体内乳腺癌靶向能力。并研究了（Bio（2）-Chol）Lip的摄取机制。结果表明，与裸紫杉醇、未修饰的Lip、（Bio-Chol）Lip和（Bio-Chol）（2）Lip相比，（Bio（2）-Chol）Lip具有最佳的乳腺癌靶向能力。特别是，与裸紫杉醇相比，（Bio（2）-Chol）唇的相对吸收效率（RE）和浓缩效率（CE）分别提高了5.61倍和5.06倍。分布数据和药代动力学参数都表明，双支化生物素修饰脂质体（（Bio（2）-Chol） Lip）是一种非常有前途的乳腺癌药物递送载体。

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