Department of Pharmaceutical Technology, Faculty of Pharmacy of the University of Coimbra, University of Coimbra, Coimbra, Portugal; REQUIMTE/LAQV, Group of Pharmaceutical Technology, Faculty of Pharmacy of the University of Coimbra, University of Coimbra, Coimbra, Portugal.
Department of Pharmaceutical Technology, Faculty of Pharmacy of the University of Coimbra, University of Coimbra, Coimbra, Portugal.
Eur J Pharm Biopharm. 2022 Sep;178:35-52. doi: 10.1016/j.ejpb.2022.07.007. Epub 2022 Jul 19.
Parenteral formulations are indispensable in clinical practice and often are the only option to administer drugs that cannot be administrated through other routes, such as proteins and certain anticancer drugs - which are indispensable to treat some of the most prevailing chronic diseases worldwide (like diabetes and cancer). Additionally, parenteral formulations play a relevant role in emergency care since they are the only ones that provide an immediate action of the drug after its administration. However, the development of parenteral formulations is a complex task owing to the specific quality and safety requirements set for these preparations and the intrinsic properties of the drugs. Amongst all the strategies that can be useful in the development of parenteral formulations, the formation of water-soluble host-guest inclusion complexes with cyclodextrins (CDs) has proven to be one of the most advantageous. CDs are multifunctional pharmaceutical excipients able to form water-soluble host-guest inclusion complexes with a wide variety of molecules, particularly drugs, and thus improve their apparent water-solubility, chemical stability, and bioavailability, to make them suitable for parenteral administration. Besides, CDs can be employed as building blocks of more complex injectable drug delivery systems with enhanced characteristics, such as nanoparticles and supramolecular hydrogels, that has been found particularly beneficial for the delivery of anticancer drugs. However, only a few CDs are considered safe when parenterally administered, and some of these types are already approved to be used in parenteral dosage forms. Therefore, the application of CDs in the development of parenteral formulations has been a more common practice in the last few years, due to their significant worldwide acceptance by the health authorities, promoting the development of safer and more efficient injectable drug delivery systems.
肠外制剂在临床实践中不可或缺，通常是唯一选择用于管理无法通过其他途径给药的药物，如蛋白质和某些抗癌药物 - 这些药物对于治疗世界上一些最流行的慢性疾病（如糖尿病和癌症）是不可或缺的。此外，肠外制剂在急救护理中也发挥着重要作用，因为它们是给药后药物能立即起效的唯一制剂。然而，由于这些制剂的特殊质量和安全要求以及药物的固有特性，开发肠外制剂是一项复杂的任务。在开发肠外制剂的所有策略中，用环糊精（CDs）形成水溶性主客体包合络合物已被证明是最有利的策略之一。CDs 是多功能药物辅料，能够与多种分子（特别是药物）形成水溶性主客体包合络合物，从而提高其表观水溶性、化学稳定性和生物利用度，使其适合肠外给药。此外，CDs 可以作为构建更复杂的注射给药系统的构建块，这些系统具有增强的特性，如纳米粒子和超分子水凝胶，这对于抗癌药物的递送特别有益。然而，只有少数 CD 被认为在肠外给药时是安全的，其中一些类型已经被批准用于肠外剂型。因此，由于它们在全球范围内得到了卫生当局的广泛认可，CD 在开发肠外制剂中的应用在过去几年中变得更加普遍，促进了更安全、更有效的注射给药系统的发展。
