College of Chemistry, Jilin University, Changchun, 130012, China.
College of Resources and Environment, Jilin Agricultural University, Changchun, 130118, PR China.
Mater Sci Eng C Mater Biol Appl. 2020 Jan;106:110251. doi: 10.1016/j.msec.2019.110251. Epub 2019 Oct 10.
In this work, a versatile folic acid (FA) decorated reductive-responsive ε-poly-l-Lysine (ε-PL)-based microcapsules (FA-ε-PLMCs) were designed and facilely assembled by using sonochemical technique. Cellular uptake experiment of FA-ε-PLMCs loaded with Coumarin 6 (C6) as a model of hydrophobic drugs implied that hydrophobic drugs encapsulated inside FA-ε-PLMCs could be delivered selectively into Hela cells via folate-receptor (FR)-mediated endocytosis due to FA decorated on microcapsules. Furthermore, the shells of FA-ε-PLMCs cross-linked by disulfide bonds were derived from sulfhydryl groups (-SH) under ultrasonication. Under reductive environment, the hydrophobic drugs loaded in FA-ε-PLMCs would be easily released due to the cleavage of disulfide bonds. Benefiting from their suitable particle size, good loading capacity for hydrophobic drugs, remarkable targetability and reductive-triggered release, the obtained FA-ε-PLMCs could be a promising hydrophobic drugs carrier for the cancer treatment.
在这项工作中，设计了一种多功能叶酸（FA）修饰的还原响应性 ε-聚-L-赖氨酸（ε-PL）基微胶囊（FA-ε-PLMCs），并通过超声化学技术简便地组装。作为疏水性药物模型的负载香豆素 6（C6）的 FA-ε-PLMCs 的细胞摄取实验表明，由于微胶囊上修饰的 FA，包封在 FA-ε-PLMCs 内的疏水性药物可以通过叶酸受体（FR）介导的内吞作用选择性递送至 Hela 细胞。此外，由巯基（-SH）在超声下交联的 FA-ε-PLMCs 的壳来源于二硫键。在还原环境下，由于二硫键的断裂，负载在 FA-ε-PLMCs 中的疏水性药物很容易释放。由于其合适的粒径、对疏水性药物的良好负载能力、显著的靶向性和还原触发释放，所得到的 FA-ε-PLMCs 可能成为治疗癌症的有前途的疏水性药物载体。
