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Fabrication of dendrimer-releasing lipidic nanoassembly for cancer drug delivery

机译:树枝状聚合物释放脂质纳米组件的制备,用于癌症药物的递送

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An inherent dilemma in the use of nanomedicines for cancer drug delivery is their limited penetration into tumors due to their large size. We have demonstrated that dendrimer/lipid nanoassemblies can solve this problem by means of tumor-triggered disassembly and the release of small (several nanometers) dendrimers to facilitate tumor penetration. Herein, we report a general strategy for the fabrication of nanoassemblies from hydrophobic and hydrophilic dendrimers with phospholipids. Hydrophobic dendrimers could assemble with lipids via hydrophobic interactions, whereas hydrophilic dendrimers could only assemble with lipids in the presence of anionic surfactants via both electrostatic and hydrophobic interactions. The nanoassemblies of hydrophobic dendrimers/lipids were found to be capable of stripping off their lipid layers via fusion with the cell membrane and then intracellular or extracellular release of dendrimers, whereas the nanoassemblies of hydrophilic dendrimers/lipids were internalized via endocytosis and then released their dendrimers inside the cells. Therefore, these dendrimer/lipid nanoassemblies could be used for the delivery of different cancer drugs.
机译:在纳米药物用于癌症药物递送中使用的固有难题是由于其大尺寸而限制了其渗透到肿瘤中。我们已经证明,树枝状大分子/脂质纳米组装体可以通过肿瘤触发的拆卸和释放小(几个纳米)树枝状大分子来促进肿瘤渗透来解决该问题。在本文中,我们报告了由疏水性和亲水性树状大分子与磷脂制造纳米组件的一般策略。疏水树状聚合物可通过疏水相互作用与脂质组装,而亲水树状聚合物仅可在阴离子表面活性剂存在下通过静电和疏水相互作用与脂质组装。发现疏水树状分子/脂质的纳米组件能够通过与细胞膜融合,然后通过树突聚合物在细胞内或细胞外释放来剥离脂质层,而亲水树状分子/脂质的纳米组件通过内吞作用被内在化,然后释放其树状聚合物。里面的细胞。因此,这些树状聚合物/脂质纳米组件可用于递送不同的癌症药物。

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