Department of Chemical Engineering and David H. Koch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, MA, USA.
Department of Mechanical Engineering, Massachusetts Institute of Technology, Cambridge, MA, USA.
J Nanobiotechnology. 2022 Aug 6;20(1):362. doi: 10.1186/s12951-022-01539-x.
Oral delivery of therapeutics is the preferred route of administration due to ease of administration which is associated with greater patient medication adherence. One major barrier to oral delivery and intestinal absorption is rapid clearance of the drug and the drug delivery system from the gastrointestinal (GI) tract. To address this issue, researchers have investigated using GI mucus to help maximize the pharmacokinetics of the therapeutic; while mucus can act as a barrier to effective oral delivery, it can also be used as an anchoring mechanism to improve intestinal residence. Nano-drug delivery systems that use materials which can interact with the mucus layers in the GI tract can enable longer residence time, improving the efficacy of oral drug delivery. This review examines the properties and function of mucus in the GI tract, as well as diseases that alter mucus. Three broad classes of mucus-interacting systems are discussed: mucoadhesive, mucus-penetrating, and mucolytic drug delivery systems. For each class of system, the basis for mucus interaction is presented, and examples of materials that inform the development of these systems are discussed and reviewed. Finally, a list of FDA-approved mucoadhesive, mucus-penetrating, and mucolytic drug delivery systems is reviewed. In summary, this review highlights the progress made in developing mucus-interacting systems, both at a research-scale and commercial-scale level, and describes the theoretical basis for each type of system.
口服给药是首选的给药途径，因为给药方便，与患者更高的药物依从性相关。药物和药物递送系统从胃肠道（GI）快速清除是口服递送和肠道吸收的主要障碍。为了解决这个问题，研究人员研究了利用胃肠道粘液来帮助最大限度地提高治疗药物的药代动力学；虽然粘液可以作为有效口服递送的屏障，但它也可以用作锚定机制来改善肠道停留时间。利用可以与 GI 道粘液层相互作用的材料的纳米药物递送系统可以实现更长的停留时间，从而提高口服药物递送的疗效。本综述检查了 GI 道中粘液的性质和功能，以及改变粘液的疾病。讨论了三类广泛的与粘液相互作用的系统：粘膜粘附、粘液穿透和粘液溶解药物递送系统。对于每类系统，都介绍了粘液相互作用的基础，并讨论和回顾了告知这些系统开发的材料实例。最后，审查了 FDA 批准的粘膜粘附、粘液穿透和粘液溶解药物递送系统的列表。总之，本综述强调了在开发粘液相互作用系统方面取得的进展，包括在研究规模和商业规模水平上，并描述了每种系统的理论基础。
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