Mura Paola
Department of Chemistry, School of Human Health Sciences, University of Florence, Via Schiff 6, Sesto Fiorentino I-50019, Florence, Italy.
J Pharm Biomed Anal. 2014 Dec;101:238-50. doi: 10.1016/j.jpba.2014.02.022. Epub 2014 Mar 12.
Cyclodextrins are cyclic oligosaccharides endowed with a hydrophilic outer surface and a hydrophobic inner cavity, able to form inclusion complexes with a wide variety of guest molecules, positively affecting their physicochemical properties. In particular, in the pharmaceutical field, cyclodextrin complexation is mainly used to increase the aqueous solubility and dissolution rate of poorly soluble drugs, and to enhance their bioavailability and stability. Analytical characterization of host-guest interactions is of fundamental importance for fully exploiting the potential benefits of complexation, helping in selection of the most appropriate cyclodextrin. The assessment of the actual formation of a drug-cyclodextrin inclusion complex and its full characterization is not a simple task and often requires the use of different analytical methods, whose results have to be combined and examined together. The purpose of the present review is to give, as much as possible, a general overview of the main analytical tools which can be employed for the characterization of drug-cyclodextrin inclusion complexes in solution, with emphasis on their respective potential merits, disadvantages and limits. Further, the applicability of each examined technique is illustrated and discussed by specific examples from literature.
环糊精是一种环状寡糖，其外表面亲水，内腔疏水，能够与多种客体分子形成包合物，对其物理化学性质产生积极影响。特别是在制药领域，环糊精络合主要用于提高难溶性药物的水溶性和溶解速率，并增强其生物利用度和稳定性。主客体相互作用的分析表征对于充分利用络合的潜在益处至关重要，有助于选择最合适的环糊精。评估药物 - 环糊精包合物的实际形成及其全面表征并非易事，通常需要使用不同的分析方法，其结果必须综合起来进行考察。本综述的目的是尽可能全面地概述可用于表征溶液中药物 - 环糊精包合物的主要分析工具，重点介绍它们各自的潜在优点、缺点和局限性。此外，通过文献中的具体实例对每种研究技术的适用性进行了说明和讨论。
