Department of Orthopaedics, Dongguk University Ilsan Hospital, Goyang, Republic of Korea.
Biomaterials. 2013 Jul;34(21):5359-68. doi: 10.1016/j.biomaterials.2013.03.066. Epub 2013 Apr 16.
Sulforaphane (SFN) is a member of the isothiocyanate family that has anti-inflammatory action as well as anti-carcinogenic properties. The authors have devised an intra-articular injectable SFN-PLGA microsphere system that can be used for treating osteoarthritis (OA). The purpose of this study was to evaluate the in vitro and in vivo efficacy of the SFN-PLGA microsphere system. Articular chondrocytes were obtained from knee OA patients and were cultured in monolayers. The optimal concentration of SFN was obtained and the dose of SFN-PLGA microspheres was determined based on the concentration. The in vitro anti-inflammatory effect on markers such as cyclooxygenase (COX)-2, a disintegrin and metalloproteinase with thrombospondin motifs (ADAMTS)-5, and matrix metalloproteinase (MMP)-2 was assessed by real-time PCR and Western blotting. The in vivo therapeutic effect of SFN-PLGA microspheres was investigated using surgically-induced rat OA model. Treatment with SFN-PLGA microspheres inhibited the mRNA and protein expression of COX-2, ADAMTS-5 and MMP-2 induced by LPS in articular chondrocytes. Intraarticular SFN-PLGA microspheres delayed the progression of surgically-induced osteoarthritis in rats. In conclusion, SFN-PLGA microspheres can be a useful injectable delivery system for treating osteoarthritis.
萝卜硫素（SFN）是异硫氰酸酯家族的一员，具有抗炎作用和抗癌特性。作者设计了一种关节内注射 SFN-PLGA 微球系统，可用于治疗骨关节炎（OA）。本研究的目的是评估 SFN-PLGA 微球系统的体外和体内疗效。从膝骨关节炎患者的膝关节中获取关节软骨细胞，并在单层培养物中培养。获得 SFN 的最佳浓度，并根据浓度确定 SFN-PLGA 微球的剂量。通过实时 PCR 和 Western blot 评估 SFN 对细胞因子如环氧化酶（COX）-2、解整合素和金属蛋白酶与凝血酶敏感蛋白 5（ADAMTS）-5 和基质金属蛋白酶（MMP）-2 等标志物的体外抗炎作用。使用手术诱导的大鼠 OA 模型研究 SFN-PLGA 微球的体内治疗效果。SFN-PLGA 微球治疗抑制了 LPS 诱导的关节软骨细胞中 COX-2、ADAMTS-5 和 MMP-2 的 mRNA 和蛋白表达。关节内 SFN-PLGA 微球延缓了手术诱导的大鼠骨关节炎的进展。总之，SFN-PLGA 微球可以成为治疗骨关节炎的一种有用的可注射给药系统。
