Size-Shifting Micelle Nanoclusters Based on a Cross-Linked and pH-Sensitive Framework for Enhanced Tumor Targeting and Deep Penetration Features
Size-Shifting Micelle Nanoclusters Based on a Cross-Linked and pH-Sensitive Framework for Enhanced Tumor Targeting and Deep Penetration Features
复制标题
基于交联和 pH 敏感框架的尺寸转移胶束纳米团簇，可增强肿瘤靶向和深度渗透功能。
DOI：
10.1021/acsami.6b00668
复制
发表时间：
2016-04-27
影响因子：
9.5
通讯作者：
Sha, Xianyi
中科院分区：
文献类型：
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作者：
Liang, Huihui;Ren, Xiaoqing;Sha, Xianyi
载有化疗药物的胶束的抗肿瘤作用主要取决于两个方面：在肿瘤区域的积累和向肿瘤内部的渗透。这两种工艺对粒度的要求不同。通常认为增强渗透性和保留性 (EPR) 的最佳颗粒尺寸约为 100 rim，而为了更深入地渗透到肿瘤内部，需要更小的颗粒尺寸。为了满足这两个不同的要求，我们构建了基于散布胶束的交联框架的尺寸变化胶束纳米团簇（MNC）。胶束的粒径为14.6 +/- 0.8 rim，在MNC形成后增加到104.2 +/- 8.1 nm，从而有效利用EPR效应。 MNC在溶酶体中转变为独立的胶束，从而可以实现更有利的渗透粒径。体内抗肿瘤生长的结果表明，尺寸移动的MNC比胶束更有利于肿瘤治疗。
The antitumor effect of chemotherapeutics loaded micelles mainly depends on two aspects: the accumulation in the tumor region and the penetration into the tumor interior. These two processes have different demands on particle size. The optimal particle size for enhanced permeability and retention (EPR) is commonly believed to be around 100 rim, while much smaller size is desired for deeper penetration into the tumor interior. To address these two different requirements, we constructed size shifting micelle nanoclusters (MNC) based on a cross-linked framework interspersed with micelles. The particle size of the micelles was 14.6 +/- 0.8 rim and increased to 104.2 +/- 8.1 nm after the MNC were formed, leading to an effective utilization of the EPR effect. MNC were shifted to independent micelles in lysosomes, so that a more favorable particle size for penetration could be realized. The results of antitumor growth in vivo demonstrated that size-shifting MNC were more beneficial for tumor therapy than micelles.