Morici Luca, Jordan Olivier, Allémann Eric, Rodríguez-Nogales Carlos
School of Pharmaceutical Sciences, University of Geneva, Geneva, Switzerland.
Institute of Pharmaceutical Sciences of Western Switzerland, Geneva, Switzerland.
Expert Opin Drug Deliv. 2025 Jul;22(7):1031-1042. doi: 10.1080/17425247.2025.2505758. Epub 2025 May 31.
More than 500 million people worldwide suffer from arthritis, experiencing daily pain and inflammation. Current treatments for osteoarthritis (OA) and rheumatoid arthritis (RA) are palliative, offering only symptom relief. No disease-modifying OA drugs (DMOADs) capable of restoring joint functionality and regenerating the cartilage matrix have yet been approved by the FDA or EMA.
This review highlights recent advances in nanocrystals (NCs) for arthritis drug delivery, including conventional nanosuspensions and novel transdermal microneedles. Special attention is given to intra-articular DMOADs formulated as NC-in-microparticles, designed to extend drug release over months. Papers and reviews with the mentioned contents and published over the last 5 years were included in the review process.
New DMOADs and disease-modifying antirheumatic drugs (DMARDs) are often poorly water-soluble, limiting their clinical progress. The versatility of NCs and nanosuspensions offers a potential advantage over other types of nanoparticles, as they can be adapted to various delivery systems, administration routes, and types of arthritis. Due to the avascular nature of cartilage, exploring the intra-articular route for OA management is essential. Implementing cartilage-targeted strategies or using stimuli-responsive hydrogels can further enhance their therapeutic potential.
全球超过5亿人患有关节炎,每天都遭受疼痛和炎症的折磨。目前用于骨关节炎(OA)和类风湿性关节炎(RA)的治疗方法是姑息性的,只能缓解症状。尚无能够恢复关节功能和再生软骨基质的疾病修饰性骨关节炎药物(DMOADs)获得美国食品药品监督管理局(FDA)或欧洲药品管理局(EMA)的批准。
本综述重点介绍了用于关节炎药物递送的纳米晶体(NCs)的最新进展,包括传统的纳米混悬液和新型透皮微针。特别关注了配制成微粒内纳米晶体的关节内DMOADs,其设计目的是将药物释放延长数月。过去5年内发表的包含上述内容的论文和综述被纳入了综述过程。
新型DMOADs和疾病修饰性抗风湿药物(DMARDs)通常水溶性较差,限制了它们的临床进展。NCs和纳米混悬液的多功能性相对于其他类型的纳米颗粒具有潜在优势,因为它们可以适用于各种递送系统、给药途径和关节炎类型。由于软骨的无血管性质,探索关节内途径用于OA治疗至关重要。实施软骨靶向策略或使用刺激响应水凝胶可以进一步提高它们的治疗潜力。