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.

以胃肠道为基础的给药方式因其对患者的便利性而被认为是首选的给药方式，从而提高了患者的依从性。然而，胃肠道的独特特性（如消化环境和跨胃肠道粘膜运输的限制）限制了药物的吸收。因此，许多药物，特别是生物制剂，仍然仅或主要以注射形式存在。在这篇综述中，我们研究了胃肠道药物输送的基本原理，以告知临床医生和药物科学家。我们讨论了一般原则，包括成功药物制剂需要克服的挑战，并描述了在设计局部和全身应用药物制剂时要考虑的每个胃肠道隔室的独特特征。