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盐酸青藤碱热敏脂质体联合微波热疗治疗类风湿关节炎。

Sinomenine hydrochloride loaded thermosensitive liposomes combined with microwave hyperthermia for the treatment of rheumatoid arthritis.

机构信息

College of Medicine, Hangzhou Normal University, Hangzhou, China; College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China.

College of Medicine, Hangzhou Normal University, Hangzhou, China.

出版信息

Int J Pharm. 2020 Feb 25;576:119001. doi: 10.1016/j.ijpharm.2019.119001. Epub 2019 Dec 29.

Abstract

The conventional medications are still facing a huge challenge for the treatment of rheumatoid arthritis (RA). Thus, looking for an effective therapy of RA has became an urgent issue nowadays. In this study, a novel thermosensitive liposome loaded with sinomenine hydrochloride (SIN-TSL) was developed by a pH gradient method. The SIN-TSL had a mean particle size of around 100 nm, and an high entrapment efficiency and drug loading capacity. The results also suggested that SIN-TSL had a thermosensitive drug release behaviour, with the drug release rate at 43 °C was much faster than the one at 37 °C. The SIN-TSL could be effectively taken up by lipopolysaccharide-activated HUVECs, without any cytotoxicity was observed. In addition, both in vitro and in vivo studies indicated that the SIN-TSL combined with microwave hyperthermia exhibited superior anti-rheumatoid arthritis effect. Overall, these results suggest that SIN-loaded thermosensitive liposomes combined with microwave hyperthermia could provide an optional strategy for alleviating the clinical symptoms of RA.

摘要

常规药物在治疗类风湿关节炎 (RA) 方面仍然面临巨大挑战。因此,寻找有效的 RA 治疗方法已成为当今的当务之急。在这项研究中,采用 pH 梯度法制备了一种载盐酸青藤碱的新型温敏脂质体(SIN-TSL)。SIN-TSL 的平均粒径约为 100nm,具有较高的包封率和载药量。结果还表明,SIN-TSL 具有温敏药物释放行为,在 43°C 时的药物释放率明显快于 37°C 时的药物释放率。SIN-TSL 可以被脂多糖激活的 HUVECs 有效摄取,且没有观察到细胞毒性。此外,体外和体内研究均表明,SIN-TSL 联合微波热疗具有优异的抗类风湿关节炎作用。总的来说,这些结果表明,载盐酸青藤碱的温敏脂质体联合微波热疗可能为缓解 RA 的临床症状提供一种可选策略。

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