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Cyclodextrin-Based Supramolecular Ternary Complexes: Emerging Role of Ternary Agents on Drug Solubility, Stability, and Bioavailability
Critical Reviews in Therapeutic Drug Carrier Systems ( IF 3.0 ) Pub Date : 2022-01-01 , DOI: 10.1615/critrevtherdrugcarriersyst.2022038870
Pooja Suvarna 1 , Pinal Chaudhari 1 , Shaila A Lewis 1
Affiliation  

The aqueous solubility of active drug moiety plays a crucial role in the development of an efficacious formulation. The poor aqueous solubility of BCS class II and IV drugs is manifested as poor bioavailability. Preparation of cyclodextrin inclusion complex to improve the solubility, stability, and bioavailability is a well-established technique. The latest trend in cyclodextrin research is focused on ternary complexes wherein an auxiliary agent such as water-soluble polymers, organic ions, metals, or amino acids is incorporated in the inclusion complex. The cyclodextrin-based supramolecular ternary complex offers significant advantages over binary complex specifically for oral drug delivery. Compared with the binary complex, the ternary complex exhibits better complexation efficiency and stability constant. Moreover, the ternary complex has a major advantage of reducing the concentration of cyclodextrin required to achieve maximum solubility and stability. Lately, in silico molecular modeling has gained tremendous attention as a preliminary tool to evaluate the cyclodextrin-based ternary or binary complex which has been discussed. This review gives an insight into various ternary agents explored worldwide, significant observations, safety, and clinical studies carried out on ternary cyclodextrin complexes.

中文翻译:

基于环糊精的超分子三元配合物:三元药剂对药物溶解度、稳定性和生物利用度的新兴作用

活性药物部分的水溶性在开发有效制剂中起着至关重要的作用。BCS II类和IV类药物水溶性差,表现为生物利用度差。制备环糊精包合物以提高溶解度、稳定性和生物利用度是一项成熟的技术。环糊精研究的最新趋势集中在三元配合物上,其中将水溶性聚合物、有机离子、金属或氨基酸等助剂掺入包合配合物中。基于环糊精的超分子三元配合物比专门用于口服药物递送的二元配合物具有显着优势。与二元配合物相比,三元配合物具有更好的络合效率和稳定性常数。而且,三元络合物的主要优点是降低了达到最大溶解度和稳定性所需的环糊精浓度。最近,作为评估已讨论的基于环糊精的三元或二元配合物的初步工具,计算机分子建模已获得极大关注这篇综述对世界范围内探索的各种三元药剂、重要观察结果、安全性和对三元环糊精复合物进行的临床研究进行了深入了解。
更新日期:2022-01-01
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