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基于环糊精的黏膜给药制剂中水溶性聚合物的最新进展。

A recent update of water-soluble polymers in cyclodextrin-based formulations for mucosal drug delivery.

作者信息

Hnin Hay Marn, Tun Theingi, Loftsson Thorsteinn, Jansook Phatsawee

机构信息

Faculty of Pharmaceutical Sciences, Chulalongkorn University, 254 Phyathai Road, Pathumwan, Bangkok 10330, Thailand.

Faculty of Pharmaceutical Sciences, University of Iceland, Hofsvallagata 53, IS-107 Reykjavik, Iceland.

出版信息

Carbohydr Polym. 2025 Jun 15;358:123539. doi: 10.1016/j.carbpol.2025.123539. Epub 2025 Mar 26.

DOI:10.1016/j.carbpol.2025.123539
PMID:40383595
Abstract

Cyclodextrins (CDs) play a crucial role in pharmaceutical formulations due to their unique ability to form inclusion complexes with a wide range of lipophilic drugs. Ternary complexes comprising CD, water-soluble polymer, and drug molecule have emerged as promising multicomponent to the challenges associated with poorly water-soluble drugs. The addition of water-soluble polymer as a ternary component often reduces the amount of CD required to form an inclusion complex thereby decreasing formulation bulk and toxicity. This review outlines the physicochemical properties of CDs and the formation of their inclusion complexes, as well as methods to enhance the complexation efficiency of drug/CD complexes. Additionally, it explores the classification and mucoadhesive properties of water-soluble polymers, and their mechanisms of mucoadhesion on mucosal membranes. The presence of small amounts of water-soluble polymers has been demonstrated to synergistically improve the complexation efficiency of drug/CD complexes. Recent advancements in modified CD-polymer conjugates and the use of water-soluble polymers in CD-based formulations, and their applications across various routes of administration are discussed, highlighting the potential of these ternary complexes as innovative platforms for drug delivery and therapeutic applications.

摘要

环糊精(CDs)在药物制剂中发挥着关键作用,因为它们具有与多种亲脂性药物形成包合物的独特能力。由CD、水溶性聚合物和药物分子组成的三元复合物已成为应对水溶性差的药物相关挑战的有前景的多组分体系。作为三元组分添加水溶性聚合物通常会减少形成包合物所需的CD量,从而降低制剂的体积和毒性。本综述概述了CDs的物理化学性质及其包合物的形成,以及提高药物/CD复合物络合效率的方法。此外,还探讨了水溶性聚合物的分类和粘膜粘附特性,以及它们在粘膜上的粘膜粘附机制。已证明少量水溶性聚合物的存在可协同提高药物/CD复合物的络合效率。讨论了修饰的CD-聚合物共轭物的最新进展以及水溶性聚合物在基于CD的制剂中的应用,及其在各种给药途径中的应用,突出了这些三元复合物作为药物递送和治疗应用创新平台的潜力。

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A recent update of water-soluble polymers in cyclodextrin-based formulations for mucosal drug delivery.基于环糊精的黏膜给药制剂中水溶性聚合物的最新进展。
Carbohydr Polym. 2025 Jun 15;358:123539. doi: 10.1016/j.carbpol.2025.123539. Epub 2025 Mar 26.
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