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丝胶稳定原花青素协同缓解溃疡性结肠炎。

Silk sericin stabilized proanthocyanidins for synergetic alleviation of ulcerative colitis.

机构信息

Department of Pharmacy, College of Chemical Engineering, Qingdao University of Science and Technology, Qingdao 266042, China.

School of Agricultural Engineering and Food Science, Shandong University of Technology, Zibo 255000, China.

出版信息

Int J Biol Macromol. 2022 Nov 1;220:1021-1030. doi: 10.1016/j.ijbiomac.2022.08.134. Epub 2022 Aug 23.

DOI:10.1016/j.ijbiomac.2022.08.134
PMID:36007701
Abstract

Silk sericin (SS) has become a noticeable drug nanocarrier due to its excellent biocompatibility and bioactivity. To further extend the application of SS, a facile one-step process was constructed to fabricate SS-stabilized-drug composites. Various insoluble drugs can be encapsulated into SS with high loading amount, and showed good dispersity in aqueous solution. For example, proanthocyanidins (PAC), a natural polyphenol with initial antioxidant and anti-inflammatory effects, can be loaded on SS to form SS/PAC composites. The SS/PAC can disperse uniformly in aqueous solution with an average particle diameter of ~136 nm, and showed high drug loading amount of 1767 mg/g. The SS/PAC exhibited high antioxidant efficiency and excellent biocompatibility (non-irritant, non-hemolysis, and non-cytotoxicity), could remarkably alleviate the symptoms of dextran sulfate sodium-induced ulcerative colitis by decreasing the disease activity index scores, inhibiting the shortening of colon length, regulating oxidative stress, suppressing inflammation, and reversing the histopathological injuries. This work provides a simple method to fabricate SS-stabilized-drug composites, promises high potential in therapeutic and pharmaceutical applications.

摘要

丝胶(SS)由于其优异的生物相容性和生物活性,已成为一种引人注目的药物纳米载体。为了进一步扩展 SS 的应用,构建了一种简便的一步法来制备 SS 稳定药物复合材料。各种不溶性药物可以被包裹在 SS 中,具有较高的载药量,并在水溶液中表现出良好的分散性。例如,原花青素(PAC)是一种具有初始抗氧化和抗炎作用的天然多酚,可以负载在 SS 上形成 SS/PAC 复合材料。SS/PAC 在水溶液中均匀分散,平均粒径约为 136nm,载药量高达 1767mg/g。SS/PAC 具有较高的抗氧化效率和良好的生物相容性(无刺激性、无溶血、无细胞毒性),可以通过降低疾病活动指数评分、抑制结肠长度缩短、调节氧化应激、抑制炎症和逆转组织病理学损伤,显著缓解葡聚糖硫酸钠诱导的溃疡性结肠炎的症状。这项工作提供了一种制备 SS 稳定药物复合材料的简单方法,有望在治疗和药物应用方面具有很高的潜力。

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