NOBIPOL, Department of Biotechnology and Food Science, Norwegian University of Science and Technology NTNU, 7491 Trondheim, Norway.
Adv Drug Deliv Rev. 2018 Jan 15;124:175-183. doi: 10.1016/j.addr.2018.01.001. Epub 2018 Jan 4.
Nanoparticulate drug delivery systems (nDDS) offer a variety of options when it comes to routes of administration. One possible path is crossing mucosal barriers, such as in the airways and in the GI tract, for systemic distribution or local treatment. The main challenge with this administration route is that the size and surface properties of the nanoparticles, as opposed to small molecular drugs, very often results in mucosal capture, immobilization and removal, which in turn results in a very low bioavailability. Strategies to overcome this challenge do exist, like surface 'stealth' modification with PEG. Here we review an alternative or supplemental strategy, co-association of mucus modulating agents with the nDDS to improve bioavailability, where the nDDS may be surface modified or unmodified. This contribution presents some examples on how possible co-association systems may be achieved, using currently marketed mucolytic drugs, alternative formulations or novel agents.
纳米药物递送系统 (nDDS) 在给药途径方面提供了多种选择。一种可能的途径是穿过黏膜屏障,例如在呼吸道和胃肠道中,以实现全身分布或局部治疗。这种给药途径的主要挑战是,与小分子药物相比,纳米颗粒的大小和表面特性常常导致黏膜捕获、固定和清除,从而导致生物利用度非常低。确实存在克服这一挑战的策略,例如用 PEG 进行表面“隐形”修饰。在这里,我们回顾了一种替代或补充策略,即将黏液调节剂与 nDDS 共同关联以提高生物利用度,其中 nDDS 可以进行表面修饰或未修饰。本贡献介绍了如何使用当前市售的黏液溶解药物、替代制剂或新型制剂来实现可能的共同关联系统的一些示例。