Chen Xuejun, Li Ziqing, Yang Chunrong, Yang Degong
Department of Pharmacy, Shantou University Medical College, Shantou 515041, China.
Guangdong Provincial Key Laboratory of Infectious Diseases and Molecular Immunopathology, Shantou University Medical College, Shantou 515041, China.
Asian J Pharm Sci. 2024 Apr;19(2):100900. doi: 10.1016/j.ajps.2024.100900. Epub 2024 Mar 6.
Ionic liquids (ILs) have been proven to be an effective technology for enhancing drug transdermal absorption. However, due to the unique structural components of ILs, the design of efficient ILs and elucidation of action mechanisms remain to be explored. In this review, basic design principles of ideal ILs for transdermal drug delivery system (TDDS) are discussed considering melting point, skin permeability, and toxicity, which depend on the molar ratios, types, functional groups of ions and inter-ionic interactions. Secondly, the contributions of ILs to the development of TDDS through different roles are described: as novel skin penetration enhancers for enhancing transdermal absorption of drugs; as novel solvents for improving the solubility of drugs in carriers; as novel active pharmaceutical ingredients (API-ILs) for regulating skin permeability, solubility, release, and pharmacokinetic behaviors of drugs; and as novel polymers for the development of smart medical materials. Moreover, diverse action mechanisms, mainly including the interactions among ILs, drugs, polymers, and skin components, are summarized. Finally, future challenges related to ILs are discussed, including underlying quantitative structure-activity relationships, complex interaction forces between anions, drugs, polymers and skin microenvironment, long-term stability, and safety issues. In summary, this article will promote the development of TDDS based on ILs.
离子液体（ILs）已被证明是一种增强药物经皮吸收的有效技术。然而，由于离子液体独特的结构组成，高效离子液体的设计及其作用机制的阐明仍有待探索。在这篇综述中，考虑到熔点、皮肤渗透性和毒性，讨论了用于透皮给药系统（TDDS）的理想离子液体的基本设计原则，这些特性取决于离子的摩尔比、类型、官能团以及离子间相互作用。其次，描述了离子液体通过不同作用对透皮给药系统发展的贡献：作为新型皮肤渗透促进剂增强药物的经皮吸收；作为新型溶剂提高药物在载体中的溶解度；作为新型活性药物成分（API - ILs）调节药物的皮肤渗透性、溶解度、释放和药代动力学行为；以及作为新型聚合物用于开发智能医疗材料。此外，总结了多种作用机制，主要包括离子液体、药物、聚合物和皮肤成分之间的相互作用。最后，讨论了与离子液体相关的未来挑战，包括潜在的定量构效关系、阴离子、药物、聚合物和皮肤微环境之间复杂的相互作用力、长期稳定性和安全性问题。总之，本文将推动基于离子液体的透皮给药系统的发展。
