通过原子转移自由基聚合（ATRP）方法合成的胃肠道黏液与口服两亲嵌段共聚物相互作用的机理研究。

INTRODUCTION: Nanoparticles are increasingly used as drug carriers for oral administration. The delivery of drug molecules is largely dependent on the interaction of nanocarriers and gastrointestinal (GI) mucus, a critical barrier that regulates drug absorption. It is therefore important to understand the effects of physical and chemical properties of nanocarriers on the interaction with GI mucus. Unfortunately, most of the nanoparticles are unable to be prepared with satisfactory structural monodispersity to comprehensively investigate the interaction. With controlled size, shape, and surface chemistry, copolymers are ideal candidates for such purpose. MATERIALS AND METHODS: We synthesized a series of diblock copolymers via the atom transfer radical polymerization method and investigated the GI mucus permeability in vitro and in vivo. RESULTS: Our results indicated that uncharged and hydrophobic copolymers exhibited enhanced GI absorption. CONCLUSION: These results provide insights into developing optimal nanocarriers for oral administration.

简介：纳米颗粒越来越多地被用作口服给药的药物载体。药物分子的输送在很大程度上取决于纳米载体与胃肠道（GI）粘液的相互作用，GI 粘液是调节药物吸收的关键屏障。因此，了解纳米载体的物理和化学性质对与 GI 粘液相互作用的影响非常重要。不幸的是，大多数纳米颗粒无法制备出具有令人满意的结构单分散性来全面研究相互作用。具有受控尺寸、形状和表面化学性质的嵌段共聚物是实现这一目的的理想候选物。

材料和方法：我们通过原子转移自由基聚合方法合成了一系列嵌段共聚物，并在体外和体内研究了 GI 粘液的通透性。

结果：我们的结果表明，不带电荷和疏水性的共聚物表现出增强的 GI 吸收。

结论：这些结果为开发用于口服给药的最佳纳米载体提供了思路。