Uekama K, Otagiri M
Crit Rev Ther Drug Carrier Syst. 1987;3(1):1-40.
One of the important characteristics of cyclodextrins is the formation of an inclusion complex with a variety of drug molecules in solution and in the solid state. As a consequence of intensive basic research, exhaustive toxic studies, and realization of industrial production during the past decade, there seem to be no more barriers for the practical application of natural cyclodextrins in the biomedical field. Recently, a number of cyclodextrin derivatives and cyclodextrin polymers have been prepared to obtain better inclusion abilities than parent cyclodextrins. The natural cyclodextrins and their synthetic derivatives have been successfully utilized to improve various drug properties, such as solubility, dissolution and release rates, stability, or bioavailability. In addition, the enhancement of drug activity, selective transfer, or the reduction of side effects has been achieved by means of inclusion complexation. The drug-cyclodextrin complex is generally formed outside of the body and, after administration, it dissociates, releasing the drug into the organism in a fast and nearly uniform manner. In the biomedical application of cyclodextrins, therefore, particular attention should be directed to the magnitude of the stability constant of the inclusion complex. In the case of parenteral application, a rather limited amount of work has been done because the cyclodextrins in the drug carrier systems have to be more effectively designed to compete with various biological components in the circulatory system. However, the works published thus far apparently indicate that the inclusion phenomena of cyclodextrin analogs may allow the rational design of drug formulation and that the combination of molecular encapsulation with other carrier systems will become a very effective and valuable method for the development of a new drug delivery system in the near future.
环糊精的重要特性之一是在溶液和固态中与多种药物分子形成包合物。由于过去十年深入的基础研究、详尽的毒性研究以及工业化生产的实现，天然环糊精在生物医学领域的实际应用似乎不再存在障碍。最近，人们制备了许多环糊精衍生物和环糊精聚合物，以获得比母体环糊精更好的包合能力。天然环糊精及其合成衍生物已成功用于改善各种药物性质，如溶解度、溶解和释放速率、稳定性或生物利用度。此外，通过包合络合实现了药物活性的增强、选择性转运或副作用的减少。药物 - 环糊精络合物通常在体外形成，给药后解离，以快速且几乎均匀的方式将药物释放到生物体中。因此，在环糊精的生物医学应用中，应特别关注包合物稳定常数的大小。在肠胃外给药的情况下，由于药物载体系统中的环糊精必须更有效地设计以与循环系统中的各种生物成分竞争，所以开展的工作相当有限。然而，迄今为止发表的研究显然表明，环糊精类似物的包合现象可能有助于合理设计药物剂型，并且分子包封与其他载体系统的结合在不久的将来将成为开发新型药物递送系统的一种非常有效且有价值的方法。
