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制备包埋黄芩苷的结冷胶-胆固醇纳米水凝胶及其创伤愈合活性评价。

Preparation of gellan-cholesterol nanohydrogels embedding baicalin and evaluation of their wound healing activity.

机构信息

Dept. of Scienze della Vita e dell'Ambiente, University of Cagliari, Cagliari, Italy.

Dept. of Scienze della Vita e dell'Ambiente, University of Cagliari, Cagliari, Italy.

出版信息

Eur J Pharm Biopharm. 2018 Jun;127:244-249. doi: 10.1016/j.ejpb.2018.02.015. Epub 2018 Feb 27.

DOI:10.1016/j.ejpb.2018.02.015
PMID:29499300
Abstract

In the present work, the preparation, characterization and therapeutic potential of baicalin-loaded nanohydrogels are reported. The nanohydrogels were prepared by sonicating (S nanohydrogel) or autoclaving (A nanohydrogel) a dispersion of cholesterol-derivatized gellan in phosphate buffer. The nanohydrogel obtained by autoclave treatment showed the most promising results: smaller particles (∼362 nm vs. ∼530 nm), higher homogeneity (polydispersity index = ∼0.24 vs. ∼0.47), and lower viscosity than those obtained by sonication. In vitro studies demonstrated the ability of the nanohydrogels to favour the deposition of baicalin in the epidermis. A high biocompatibility was found for baicalin-loaded nanohydrogels, along with a great ability to counteract the toxic effect induced by hydrogen peroxide in cells, as the nanohydrogels re-established the normal conditions (∼100% viability). Further, the potential of baicalin-loaded nanohydrogels in skin wound healing was demonstrated in vivo in mice by complete skin restoration and inhibition of specific inflammatory markers (i.e., myeloperoxidase, tumor necrosis factor-α, and oedema).

摘要

本工作报道了黄芩苷载纳米水凝胶的制备、表征和治疗潜力。纳米水凝胶通过超声(S 纳米水凝胶)或高压釜处理(A 纳米水凝胶)胆固醇衍生的凝胶在磷酸盐缓冲液中的分散体制备。通过高压釜处理获得的纳米水凝胶表现出最有希望的结果:更小的颗粒(362nm 与530nm 相比)、更高的均匀性(多分散指数=0.24 与0.47 相比)和更低的粘度比超声处理获得的纳米水凝胶。体外研究表明,纳米水凝胶有利于黄芩苷在表皮中的沉积。发现黄芩苷载纳米水凝胶具有高生物相容性,并且能够很好地对抗细胞中过氧化氢诱导的毒性作用,因为纳米水凝胶重新建立了正常条件(~100%活力)。此外,通过完整皮肤恢复和抑制特定炎症标志物(即髓过氧化物酶、肿瘤坏死因子-α和水肿),在体内用小鼠证明了黄芩苷载纳米水凝胶在皮肤伤口愈合中的潜力。

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