Rhein is a potential anti-inflammatory agent, but its poor water solubility significantly restricts its clinical application. In this study, rhein micelles (RMs) with improved water solubility were fabricated on Pluronic F127 (F-127). Transmission electron microscopy showed that the as-prepared RMs displayed a mean diameter of approximately 20 nm and a spherical morphology. The encapsulation efficiency of the micelles towards drugs varied from 81.38 ± 4.35% to 24.87 ± 4.32%. The RMs exhibited a burst release during the first 6 h and a following sustained release up to 96 h with a biphasic drug release pattern as suggested by the drug release assay. Cytotoxicity assessment showed that the RMs caused no change in cell viability at drug concentrations below 40 μM after 24 and 48 h of incubation. In RAW264.7 macrophages, the RMs inhibited the lipopolysaccharide-induced activation of p65/NF-κB, which in turn suppressed the transcription of its downstream inducible nitric oxide synthase, and cytokine genes such as interleukin-1β and tumor necrosis factor-α . Simultaneously, the RMs led to reduced cytokine secretions, including cyclooxygenase-2, prostaglandin E2, nitric oxide, and interleukin-6 in a dose-dependent manner. The RMs reported herein may be a promising candidate for developing anti-inflammatory therapeutic formulations.

中文翻译：

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制成的大黄酸胶束的抗炎功效。

大黄酸是一种潜在的抗炎药，但水溶性差，严重限制了其临床应用。在这项研究中，在Pluronic F127（F-127）上制备了具有改善的水溶性的大黄酸胶束（RM）。透射电子显微镜显示，所制备的RM显示出约20nm的平均直径和球形形态。胶束对药物的包封效率为81.38±4.35％至24.87±4.32％。RMs在最初的6小时内表现出爆发性释放，随后持续释放直至96 h，具有药物释放测定所建议的双相药物释放模式。细胞毒性评估显示，在孵育24和48小时后，当药物浓度低于40μM时，RM不会引起细胞活力的变化。在RAW264.7巨噬细胞中 RMs抑制了脂多糖诱导的p65 /NF-κB的激活，进而抑制了其下游诱导型一氧化氮合酶以及白细胞介素-1β和肿瘤坏死因子-α等细胞因子基因的转录。同时，RM以剂量依赖性方式导致细胞因子分泌减少，包括环加氧酶2，前列腺素E2，一氧化氮和白介素6。本文报道的RM可能是开发抗炎治疗制剂的有前途的候选者。和白介素6呈剂量依赖性。本文报道的RM可能是开发抗炎治疗制剂的有前途的候选者。和白介素6呈剂量依赖性。本文报道的RM可能是开发抗炎治疗制剂的有前途的候选者。