Microencapsulation and characterization of controlled-release intestinal drugs: a critical review

Weiguang SU; Dawei WANG; Siegfried YEBOAH; Jinshen WANG; Chonghai XU; Li WANG

doi:10.1631/jzus.B2400617

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Review | Updated：2026-04-23

Microencapsulation and characterization of controlled-release intestinal drugs: a critical review
Microencapsulation and characterization of controlled-release intestinal drugs: a critical review
肠道控释药物微胶囊的制备和表征研究综述
Journal of Zhejiang University-SCIENCE B Vol. 27, Issue 4, Pages: 321-342(2026)
Affiliations：

1.School of Mechanical Engineering, Qilu University of Technology (Shandong Academy of Sciences), Jinan 250353, China
2.Shandong Institute of Mechanical Design and Research, Jinan 250031, China
3.School of Engineering and Design, London South Bank University, London, SE1 0AA, UK
4.Department of Gastrointestinal Surgery, Shandong Provincial Hospital Affiliated to Shandong First Medical University, Jinan 250021, China
Funds：
DOI：10.1631/jzus.B2400617
CLC：
CSTR：
Received：08 December 2024，

Revised：2025-04-06，

Online First：13 March 2026，

Published：23 April 2026
Accepted：

苏伟光,王大伟,Siegfried YEBOAH等.肠道控释药物微胶囊的制备和表征研究综述[J].浙江大学学报（英文版）（B辑：生物医学和生物技术）,2026,27(04):321-342.

Weiguang SU, Dawei WANG, Siegfried YEBOAH, et al. Microencapsulation and characterization of controlled-release intestinal drugs: a critical review[J]. Journal of Zhejiang University-SCIENCE B, 2026, 27(4): 321-342.
苏伟光,王大伟,Siegfried YEBOAH等.肠道控释药物微胶囊的制备和表征研究综述[J].浙江大学学报（英文版）（B辑：生物医学和生物技术）,2026,27(04):321-342. DOI： 10.1631/jzus.B2400617.

Weiguang SU, Dawei WANG, Siegfried YEBOAH, et al. Microencapsulation and characterization of controlled-release intestinal drugs: a critical review[J]. Journal of Zhejiang University-SCIENCE B, 2026, 27(4): 321-342. DOI： 10.1631/jzus.B2400617.

摘要

口服给药具有较高的患者依从性，不仅是营养物质和肽类药物在主要吸收部位的给药途径，也是治疗肠道疾病的重要手段。然而，传统的口服肠道药物由于胃酸和消化酶的影响，尤其是蛋白质和肽类药物，易降解和失活，难以实现有效的靶向递送。为了应对这些挑战，肠道药物控释微胶囊（MeIDs）被开发出来，并因其在保护药物免受胃酸和消化酶降解方面的能力而备受关注。本研究系统性地梳理了来自Google Scholar、Web of Science和Science Direct等检索平台的162篇文献，对MeID的制备方法、释放机制和评价策略进行综述。结果发现，MeID的开发需综合考虑乳液制备、微胶囊化方法、包衣材料选择以及药物自身性质。此外，通过涂层技术、微/纳米载体以及吸收促进剂的联合使用，可显著提升微胶囊的性能。现有研究普遍采用细胞模型、动物实验及光谱分析等方法，系统评估其生物相容性、稳定性及药效。另有文献表明，优化制备工艺可有效调控药物的释放动力学。展望未来，我们建议研究方向可聚焦于低成本制备单分散微胶囊的方法，开发动态响应型壳材，以及应用器官芯片技术实现精确评价，从而为微胶囊药物和靶向药物递送系统的发展提供理论依据。

Abstract

Oral administration is associated with high patient adherence

as it is not only the route for primary site absorption of nutrients and peptide drugs but also is important for treating intestinal diseases. However

traditional oral intestinal drugs are limited by drug degradation and inactivation

particularly for proteins and peptides

due to gastric acid and digestive enzymes

making it difficult to effectively deliver drugs to target sites. To address these challenges

controlled-release microencapsulated intestinal drugs (MeIDs) have been developed and have attracted attention for their ability to protect drugs from degradation by gastric acid and digestive enzymes. In this study

we systematically reviewed research articles on the preparation methods

release mechanisms

and evaluation strategies of MeIDs using Google Scholar

Web of Science

and Science Direct databases. Our findings show that the preparation of emulsions

microencapsulation methods

shell material selection

and drug properties need to be considered comprehensively for MeID development. In addition

we found that coating

micro/nanocarriers

and absorption enhancers can be combined to enhance microcapsule performance. Beyond focusing on drug loading efficiency and microcapsule morphology

we also found that cell models

animal models

and spectroscopic analysis techniques can be used to evaluate drug biocompatibility

stability

and efficacy. Finally

the literature has shown that optimizing the preparation process can regulate drug release kinetics. For future research

we suggest that studies should focus on low-cost methods for producing monodisperse microcapsules

developing dynamic responsive shell materials

and using organ-on-a-chip technology for precise evaluation

as part of the theoretical support towards the development of microencapsulated drugs and targeted drug delivery.

关键词

Keywords

references

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