Department of Pharmaceutics and Drug Delivery, School of Pharmacy, The University of Mississippi, University, Mississippi, 38677, USA.
Department of Pharmaceutics, College of Pharmacy, Northern Border University, 91431, Arar, Saudi Arabia.
AAPS PharmSciTech. 2024 Oct 8;25(7):236. doi: 10.1208/s12249-024-02965-w.
This review investigates the progression and effectiveness of colon-targeted drug delivery systems, offering a comprehensive understanding of the colon's anatomy and physiological environment. Recognizing the distinctive features of the colon is crucial for successfully formulating oral dosage forms that precisely target specific areas in the gastrointestinal tract (GIT) while minimizing side effects through mitigating off-target sites. This understanding forms the basis for designing effective targeted drug delivery systems. The article extensively examines diverse approaches to formulating drugs for colonic targeting, highlighting key polymers and excipients in their production. Special emphasis is given to innovative approaches such as hot-melt extrusion (HME) and three-dimensional printing (3D-P), renowned for their accuracy in drug release kinetics and intricate dosage form geometry. However, challenges arise regarding material standardization and the complex network of regulatory clearances required to confirm safety and effectiveness. The review provides insights into each application's advantages and potential challenges. Furthermore, it sheds light on the local diseases that necessitate colon targeting and the available marketed products, providing an overview of the current state of colon-targeted drug delivery systems. Additionally, the review emphasizes the importance of testing drugs in a controlled in vitro environment during the development phase. It also discusses the future directions for successful development in this field. By integrating knowledge across anatomy, formulation techniques, and assessment methodologies, this review is a valuable resource for researchers navigating the dynamic field of colonic drug delivery.
本文综述了结肠定位给药系统的研究进展和效果，全面了解了结肠的解剖结构和生理环境。认识到结肠的独特特征对于成功设计能够精确靶向胃肠道（GI）特定区域的口服剂型至关重要，同时通过减轻非靶部位的副作用来最小化不良反应。这种理解是设计有效靶向药物传递系统的基础。本文广泛探讨了用于结肠定位的药物制剂的多种方法，强调了在其生产过程中关键的聚合物和赋形剂。特别强调了热熔挤出（HME）和三维打印（3D-P）等创新方法，这些方法以其在药物释放动力学和复杂剂型几何形状方面的精确性而闻名。然而，在材料标准化和确认安全性和有效性所需的复杂监管审批网络方面，仍然存在挑战。本文综述了每种应用的优势和潜在挑战。此外，还介绍了需要结肠靶向的局部疾病和现有的市售产品，概述了结肠靶向药物传递系统的现状。此外，本文强调了在开发阶段在受控体外环境中测试药物的重要性。还讨论了该领域成功开发的未来方向。通过整合解剖学、制剂技术和评估方法学方面的知识，本文综述为研究人员在结肠药物传递领域提供了有价值的资源。
