Boczar Dariusz, Michalska Katarzyna
Department of Synthetic Drugs, National Medicines Institute, Chełmska 30/34, 00-725 Warsaw, Poland.
Pharmaceutics. 2022 Jun 30;14(7):1389. doi: 10.3390/pharmaceutics14071389.
Cyclodextrins (CDs) are a family of cyclic oligosaccharides, consisting of a macrocyclic ring of glucose subunits linked by α-1,4 glycosidic bonds. The shape of CD molecules is similar to a truncated cone with a hydrophobic inner cavity and a hydrophilic surface, which allows the formation of inclusion complexes with various molecules. This review article summarises over 200 reports published by the end of 2021 that discuss the complexation of CDs with antibiotics and antibacterial agents, including beta-lactams, tetracyclines, quinolones, macrolides, aminoglycosides, glycopeptides, polypeptides, nitroimidazoles, and oxazolidinones. The review focuses on drug-delivery applications such as improving solubility, modifying the drug-release profile, slowing down the degradation of the drug, improving biological membrane permeability, and enhancing antimicrobial activity. In addition to simple drug/CD combinations, ternary systems with additional auxiliary substances have been described, as well as more sophisticated drug-delivery systems including nanosponges, nanofibres, nanoparticles, microparticles, liposomes, hydrogels, and macromolecules. Depending on the desired properties of the drug product, an accelerated or prolonged dissolution profile can be achieved when combining CD with antibiotics or antimicrobial agents.
环糊精（CDs）是一类环状寡糖，由通过α-1,4糖苷键连接的葡萄糖亚基大环组成。CD分子的形状类似于截顶圆锥，具有疏水的内腔和亲水的表面，这使得它能够与各种分子形成包合物。这篇综述文章总结了截至2021年底发表的200多篇报告，这些报告讨论了CDs与抗生素和抗菌剂的络合作用，包括β-内酰胺类、四环素类、喹诺酮类、大环内酯类、氨基糖苷类、糖肽类、多肽类、硝基咪唑类和恶唑烷酮类。该综述重点关注药物递送应用，如提高溶解度、改变药物释放曲线、减缓药物降解、提高生物膜通透性以及增强抗菌活性。除了简单的药物/CD组合外，还描述了含有额外辅助物质的三元体系，以及更复杂的药物递送系统，包括纳米海绵、纳米纤维、纳米颗粒、微粒、脂质体、水凝胶和大分子。根据药物产品的预期性质，将CD与抗生素或抗菌剂组合时，可以实现加速或延长的溶解曲线。
