LIBRO-Laboratório de Investigação em Biofilmes Rosário Oliveira, CEB-Centre of Biological Engineering, University of Minho, 4710-057 Braga, Portugal.
IPC-Institute for Polymers and Composites, Department of Polymers Engineering, University of Minho, 4800-056 Guimarães, Portugal.
ACS Appl Bio Mater. 2021 May 17;4(5):4607-4617. doi: 10.1021/acsabm.1c00334. Epub 2021 Apr 30.
Anti- 2'-MethylRNA is an antisense oligonucleotide (ASO) that has the ability to recognize and block the gene and to control filamentation. However, it is important to protect the anti- 2'-MethylRNA ASO from the environmental human body conditions and to ensure that they will be delivered to their site of action, and polyplex microparticles (MPs) represent a class of vehicles to ASO cargo with these functionalities. Thus, the goal of this work was to develop polyplexes based on porous poly(γ-butyrolactam) (PA4) or poly(ε-caprolactam) (PA6) MPs for the anti- 2'-MethylRNA ASO cargo and delivery. Two types of polyplexes were prepared with payloads of anti- 2'-MethylRNA molecules, either entrapped or immobilized on prefabricated polyamide MPs. Our data confirm that PA4 and PA6 polyplex MPs can be feasible carriers for anti- 2'-MethylRNA ASO molecules, using either the entrapment or immobilization strategies, whereby the released ASO maintains its activity against cells.
抗 2'-甲基 RNA 是一种反义寡核苷酸 (ASO)，具有识别和阻断 基因并控制丝状化的能力。然而，保护抗 2'-甲基 RNA ASO 免受环境和人体条件的影响，并确保它们能够被递送到作用部位是很重要的，而多聚物微粒 (MPs) 则代表了一类具有这些功能的 ASO 载体。因此，本工作的目的是开发基于多孔聚(γ-丁内酯) (PA4) 或聚(ε-己内酯) (PA6) MPs 的多聚物复合物，用于负载抗 2'-甲基 RNA ASO。用负载有抗 2'-甲基 RNA 分子的两种类型的多聚物复合物进行制备，将负载物包封或固定在预制的聚酰胺 MPs 上。我们的数据证实，PA4 和 PA6 多聚物 MPs 可以作为抗 2'-甲基 RNA ASO 分子的可行载体，无论是采用包封还是固定化策略，释放的 ASO 都能保持对 细胞的活性。
