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纳米药物递送系统以纳米尺度载体携带或包封活性药物成分，可改善难溶性或不稳定药物的体内处置，通过改变体内分布、促进胞内递送和维持联合用药暴露比例，提高疗效、降低毒性。与普通小分子药物不同，纳米药物进入体内后，活性药物成分会处于载体携带或包封、已释放、未结合及代谢物等不同形态，进而表现为总药物暴露升高、载体循环时间延长或病灶示踪信号增强，但这不直接等同于作用部位活性药物成分暴露增加。区分这些药物形态，并分析其与疗效、安全性的关系，是纳米药物临床转化和可比性评价中需要解决的问题。通过综述近年来纳米药物递送系统的人体药动学研究、体内释药测定方法、上市产品证据，并结合国内外监管要求，重点讨论多分析物药动学在解释体内过程、衔接质量评价与临床转化中的作用，为纳米药物研究设计、质量控制和监管评价提供参考。
Abstract：Nanomedicine delivery systems use nanoscale carriers to carry or encapsulate active pharmaceutical ingredients(APIs). The systems improve the in vivo disposition of poorly soluble or unstable drugs by altering in vivo drug distribution, promoting intracellular delivery, and maintaining exposure ratios in combination therapy. These alterations improve therapeutic efficacy and reduce toxicity. Unlike conventional small-molecule drugs, after administration, the APIs in nanomedicines may exist in different forms, including carrier-associated or encapsulated drug, released drug, unbound drug, and metabolites. Therefore, increased total drug exposure, prolonged carrier circulation time, or enhanced lesion tracer signals cannot be directly equated with increased exposure to active APIs at the site of action. Distinguishing these drug forms and analyzing their relationships with efficacy and safety are issues that need to be addressed in the clinical translation and comparability assessment of nanomedicines. This review summarizes recent human pharmacokinetic studies, in vivo drug release measurement methods, evidence from marketed products, and domestic and international regulatory requirements for nanomedicine delivery systems. Emphasis is placed on the role of multi-analyte pharmacokinetics in interpreting in vivo processes and linking quality assessment with clinical translation. The review is intended to provide a reference for study design, quality control, and regulatory evaluation of nanomedicines.
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基本信息:
DOI：10.19577/j.1007-4406.2026.09.001
中图分类号:R969.1
引用信息:
[1]邓智方,李杰琛,陈熙妮,等.纳米药物递送系统的药动学与临床转化研究进展[J].中国临床药学杂志,2026,35(09):769-777.DOI:10.19577/j.1007-4406.2026.09.001.
基金信息:
国家自然科学基金（编号82374296）; 上海市2024年度“科技创新行动计划”生物医药创新发展项目（编号24S11903000）
2026-09-25
2026-09-25