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用于递送紫糯玉米芯提取物中花色苷的丝胶蛋白水凝胶的研制及抗炎作用的体外评价

Development of a Sericin Hydrogel to Deliver Anthocyanins from Purple Waxy Corn Cob ( L.) Extract and In Vitro Evaluation of Anti-Inflammatory Effects.

作者信息

Kanpipit Nattawadee, Nualkaew Natsajee, Kiatponglarp Worawikunya, Priprem Aroonsri, Thapphasaraphong Suthasinee

机构信息

Biomedical Science Program, Graduate School, Khon Kaen University, Khon Kaen 40002, Thailand.

Department of Pharmacognosy and Toxicology, Faculty of Pharmaceutical Sciences, Khon Kaen University, Khon Kaen 40002, Thailand.

出版信息

Pharmaceutics. 2022 Mar 6;14(3):577. doi: 10.3390/pharmaceutics14030577.

Abstract

Sericin-alginate hydrogel formulations with purple waxy corn ( L.) cob extract (PWCC) for topical anti-inflammatory application are developed and evaluated. The physical properties such as viscosity, pH, and anthocyanin release are examined and in vitro anti-inflammatory activities, such as NO inhibition and IL-6, IL-1β, TNF-α, iNOS, and COX-2 expression, are evaluated in LPS-stimulated RAW 264.7 murine macrophages. The sericin-alginate hydrogel is prepared by physical crosslinking through the ionic interaction of the polymers combined with anthocyanin from PWCC at pH 6.5. The hydrogel formulation with 2.00% / sericin, 0.20% / alginate, and 0.15% / PWCC (SN6) shows a suitable viscosity for topical treatment, the highest nitric oxide inhibition (79.43%), no cytotoxicity, and reduced expression of IL-6, IL-1β, and TNF-α mediators. Moreover, the SN6 formulation displays a sustained anthocyanin release over 8-12 h, which correlates with the Korsmeyer-Peppas model. The FT-IR spectrum of SN6 confirmed interaction of the sericin polymer with anthocyanins from PWCC via H-bonding by the shifted peak of amide I and amide III. In addition, the anthocyanin is stable in sericin hydrogels under heating-cooling storage conditions. Therefore, we suggest that this hydrogel formulation has potential as an anti-inflammatory agent. The formulation will be further investigated for in vivo studies and clinical trials in the future.

摘要

开发并评估了含紫糯玉米(L.)穗轴提取物(PWCC)的丝胶蛋白-海藻酸盐水凝胶制剂用于局部抗炎应用。检测了其诸如粘度、pH值和花青素释放等物理性质,并在脂多糖刺激的RAW 264.7小鼠巨噬细胞中评估了体外抗炎活性,如一氧化氮抑制以及白细胞介素-6、白细胞介素-1β、肿瘤坏死因子-α、诱导型一氧化氮合酶和环氧化酶-2的表达。丝胶蛋白-海藻酸盐水凝胶通过聚合物在pH 6.5时的离子相互作用与来自PWCC的花青素进行物理交联制备。含2.00%/丝胶蛋白、0.20%/海藻酸盐和0.15%/PWCC的水凝胶制剂(SN6)显示出适合局部治疗的粘度、最高的一氧化氮抑制率(79.43%)、无细胞毒性以及白细胞介素-6、白细胞介素-1β和肿瘤坏死因子-α介质表达降低。此外,SN6制剂在8 - 12小时内显示出花青素的持续释放,这与Korsmeyer-Peppas模型相关。SN6的傅里叶变换红外光谱通过酰胺I和酰胺III的峰位移证实了丝胶蛋白聚合物与来自PWCC的花青素通过氢键相互作用。此外,花青素在加热-冷却储存条件下在丝胶水凝胶中稳定。因此,我们认为这种水凝胶制剂有作为抗炎剂的潜力。该制剂未来将进一步进行体内研究和临床试验。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce54/8951468/b7cb272c83c1/pharmaceutics-14-00577-g001.jpg

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