药物的生物利用度是表示药物分子以各种途径或形式进入机体后，经口腔、胃、肠等消化吸收后进入体循环的比例参数。生物利用度是反映药物在生物体内吸收、分布、代谢和排泄情况的重要依据。在医药等领域，纳米药物递送体系是提高活性分子生物利用度非常有效的手段，药物发挥药效时需要从载体中释放才能被充分吸收。在生物活性分子的研发过程中，可通过体外模型和动物体内模型来模拟药物在机体的作用过程，以此推测药物的生物利用度。目前，广泛应用的生物利用度模型主要包括体外模拟释药模型、体外模拟消化模型、细胞模型、体内药代动力学模型等。该研究主要对常见的生物利用度研究模型构建和应用等进行总结，以期为今后纳米药物递送体系的生物利用度模型研究和拓新提供参考。

Drug bioavailability refers to the fraction of administered drug that reaches systemic circulation after ingestion by mouth and absorption in the gastrointestinal tract. Bioavailability is influenced by various routes or dosage forms. Bioavailability is impacted by absorption, distribution, metabolism, and excretion of drugs by an organism. In medicine and other fields, nanoscale drug delivery systems offer effective methods for improving the bioavailability of bioactives. Pharmaceuticals need to be released from these carriers to be fully absorbed and exert their therapeutic effects. In bioactive molecule research and development, in vitro models and in vivo animal models can be used to simulate delivery of drugs into the body and assess parameters that allow prediction of their bioavailability. To date, common bioavailability models include in vitro simulated drug release models, in vitro simulated digestion models, cellular models, and in vivo pharmacokinetic models. This paper summarizes the establishment and application of representative bioavailability models to provide a reference for future research and development of in vitro and in vivo bioavailability models for nanoscale drug delivery systems.

国家自然科学基金青年科学基金项目（31901677）；国家留学基金委公派访学项目（202008410088）；河南工业大学青年骨干教师培育计划（21420167）；河南工业大学高层次人才科研启动基金项目（2019BS021）；河南工业大学创新基金支持计划专项（2020ZKCJ23）