Department of Chemistry, Florence University, via Schiff 6, Sesto Fiorentino, Florence, Italy.
Int J Pharm. 2020 Apr 15;579:119181. doi: 10.1016/j.ijpharm.2020.119181. Epub 2020 Feb 26.
Complexation with cyclodextrins (CDs) has been widely and successfully used in pharmaceutical field, mainly for enhancing solubility, stability and bioavailability of a variety of drugs. However, some important drawbacks, including rapid removal from the bloodstream after in vivo administration, or possible replacement, in biological media, of the entrapped drug moieties by other molecules with higher affinity for the CD cavity, can limit the CDs effectiveness as drug carriers. This review is focused on combined strategies simultaneously exploiting CD complexation, and loading of the complexed drug into various colloidal carriers (liposomes, niosomes, polymeric nanoparticles, lipid nanoparticles, nanoemulsions, micelles) which have been investigated as a possible means for circumventing the problems associated with both such carriers, when used separately, and join their relative benefits in a unique delivery system. Several examples of applications have been reported, to illustrate the possible advantages achievable by such a dual strategy, depending on the CD-nanocarrier combination, and mainly resulting in enhanced performance of the delivery system and improved biopharmaceutical properties and therapeutic efficacy of drugs. The major problems and/or drawbacks found in the development of such systems, as well as the (rare) case of failures in achieving the expected improvements have also been highlighted.
环糊精（CDs）的络合作用已被广泛且成功地应用于制药领域，主要用于提高各种药物的溶解度、稳定性和生物利用度。然而，一些重要的缺点，包括在体内给药后从血液中迅速清除，或者在生物介质中，被 CD 腔中具有更高亲和力的其他分子取代被包封的药物部分，可能会限制 CD 作为药物载体的有效性。本综述重点介绍了同时利用 CD 络合作用和将络合药物装载到各种胶体载体（脂质体、非离子囊泡、聚合物纳米粒、脂质纳米粒、纳米乳液、胶束）的联合策略，这些胶体载体已被研究为规避单独使用这两种载体时相关问题的一种可能方法，并将它们的相对优势结合到一个独特的给药系统中。已经报道了几个应用实例，说明了这种双重策略可能实现的优势，这取决于 CD-纳米载体的组合，主要导致给药系统的性能得到提高，以及药物的生物制药特性和治疗效果得到改善。还强调了开发此类系统时发现的主要问题和/或缺点，以及（罕见）未能实现预期改进的情况。
