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用于炎症性关节炎的纳米药物:含糖皮质激素的聚合物、胶束和脂质体的头对头比较。

Nanomedicines for inflammatory arthritis: head-to-head comparison of glucocorticoid-containing polymers, micelles, and liposomes.

机构信息

Department of Pharmaceutical Sciences, University of Nebraska Medical Center, Omaha, Nebraska 68198, (USA).

Department of Pharmaceutics, Utrecht Institute for Pharmaceutical Sciences, Utrecht University, Universiteitsweg 99, 3584 CG Utrecht, (The Netherlands).

出版信息

ACS Nano. 2014 Jan 28;8(1):458-466. doi: 10.1021/nn4048205. Epub 2013 Dec 27.

Abstract

As an emerging research direction, nanomedicine has been increasingly utilized to treat inflammatory diseases. In this head-to-head comparison study, four established nanomedicine formulations of dexamethasone, including liposomes (L-Dex), core-cross-linked micelles (M-Dex), slow releasing polymeric prodrugs (P-Dex-slow), and fast releasing polymeric prodrugs (P-Dex-fast), were evaluated in an adjuvant-induced arthritis rat model with an equivalent dose treatment design. It was found that after a single i.v. injection, the formulations with the slower drug release kinetics (i.e., M-Dex and P-Dex-slow) maintained longer duration of therapeutic activity than those with relatively faster drug release kinetics, resulting in better joint protection. This finding will be instructional in the future development and optimization of nanomedicines for the clinical management of rheumatoid arthritis. The outcome of this study also illustrates the value of such head-to-head comparison studies in translational nanomedicine research.

摘要

作为一个新兴的研究方向,纳米医学已被越来越多地用于治疗炎症性疾病。在这项头对头比较研究中,用等效剂量设计,在佐剂诱导关节炎大鼠模型中评估了四种已确立的地塞米松纳米药物制剂,包括脂质体(L-Dex)、核交联胶束(M-Dex)、缓慢释放聚合物前药(P-Dex-slow)和快速释放聚合物前药(P-Dex-fast)。结果发现,单次静脉注射后,药物释放动力学较慢的制剂(即 M-Dex 和 P-Dex-slow)比药物释放动力学较快的制剂具有更长的治疗活性持续时间,从而更好地保护关节。这一发现将对未来类风湿关节炎的临床治疗中纳米药物的开发和优化具有指导意义。本研究的结果还说明了这种头对头比较研究在转化纳米医学研究中的价值。

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