Division of Gastroenterology, Massachusetts General Hospital, Harvard Medical School, Boston, MA, USA.
Massachusetts Institute of Technology, Cambridge, MA, USA.
Nat Rev Gastroenterol Hepatol. 2022 Apr;19(4):219-238. doi: 10.1038/s41575-021-00539-w. Epub 2021 Nov 16.
Gastrointestinal-based drug delivery is considered the preferred mode of drug administration owing to its convenience for patients, which improves adherence. However, unique characteristics of the gastrointestinal tract (such as the digestive environment and constraints on transport across the gastrointestinal mucosa) limit the absorption of drugs. As a result, many medications, in particular biologics, still exist only or predominantly in injectable form. In this Review, we examine the fundamentals of gastrointestinal drug delivery to inform clinicians and pharmaceutical scientists. We discuss general principles, including the challenges that need to be overcome for successful drug formulation, and describe the unique features to consider for each gastrointestinal compartment when designing drug formulations for topical and systemic applications. We then discuss emerging technologies that seek to address remaining obstacles to successful gastrointestinal-based drug delivery.
胃肠道给药被认为是首选的给药方式,因为它方便患者,提高了顺应性。然而,胃肠道的独特特性(如消化环境和对跨胃肠道黏膜运输的限制)限制了药物的吸收。因此,许多药物,特别是生物制剂,仍然仅以注射剂形式存在或主要以注射剂形式存在。在这篇综述中,我们考察了胃肠道药物传递的基础原理,以为临床医生和药物科学家提供信息。我们讨论了一般原则,包括成功药物制剂所需克服的挑战,并描述了在设计用于局部和全身应用的药物制剂时,每个胃肠道隔室需要考虑的独特特征。然后,我们讨论了寻求解决胃肠道给药成功的剩余障碍的新兴技术。