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基于废弃蜂胶改性的纳米脂质体系统用于伤口愈合:设计、体外与体内评价。

Nanostructured lipid systems modified with waste material of propolis for wound healing: Design, in vitro and in vivo evaluation.

机构信息

Postgraduate Program in Pharmaceutical Sciences, Laboratory of Research and Development of Drug Delivery Systems, Department of Pharmacy, State University of Maringa, Maringa, Parana, Brazil.

Department of Life Sciences and Biotechnology, University of Ferrara, Ferrara, Italy.

出版信息

Colloids Surf B Biointerfaces. 2017 Oct 1;158:441-452. doi: 10.1016/j.colsurfb.2017.07.029. Epub 2017 Jul 10.

Abstract

Propolis, a natural compound that can accelerate the wound healing process, is mainly used as ethanolic extract. The extractive solution may also be obtained from the propolis by-product (BP), transforming this waste material into a pharmaceutical active ingredient. Even if propolis does not show toxicity, when used as an extract over harmed skin or mucosa, the present ethanol content may be harmful to the tissue recovering, besides hindering the drug release. This study describes the development of solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) as topical propolis delivery systems and the investigation of their in vitro and in vivo activities. The extracts were evaluated to guarantee their quality, and the lipid dispersions were characterized with respect to morphology (cryo-TEM), size and diffractometry (X-ray) properties. The occlusive capacity of formulations was also evaluated by an in vitro technique, which determines the occlusion factor. The drug entrapment efficiency (EE), as well as the in vitro drug release profile from the nanoparticulate systems was investigated as well. The size analysis performed through 90days was favorable to a topical administration and the polydispersity index, though not ideal in all cases due to the high content of resins and gums from the extracts, were relatively stable for the SLN. The propolis extract contributes to the occlusive potential of the formulations. The human immortalized keratinocytes presented good cell viability when tested with both extracts (propolis and BP) freely or entrapped in the systems. SLN modified with propolis material provided an acceleration of the in vivo wound healing process.

摘要

蜂胶是一种天然化合物,可以加速伤口愈合过程,主要用作乙醇提取物。提取物也可以从蜂胶副产物 (BP) 中获得,将这种废物转化为药物活性成分。即使蜂胶没有显示出毒性,当用作受损皮肤或粘膜上的提取物时,目前的乙醇含量可能对组织恢复有害,并且会阻碍药物释放。本研究描述了固体脂质纳米粒 (SLN) 和纳米结构脂质载体 (NLC) 的开发,作为局部蜂胶传递系统,并研究了它们的体外和体内活性。对提取物进行了评估,以保证其质量,并且对脂质分散体的形态(冷冻 TEM)、大小和衍射(X 射线)特性进行了表征。还通过体外技术评估了制剂的封闭能力,该技术确定了封闭因子。还研究了纳米颗粒系统的药物包封效率 (EE) 以及体外药物释放特性。通过 90 天进行的尺寸分析有利于局部给药,尽管由于提取物中的树脂和树胶含量高,多分散指数在所有情况下都不理想,但对于 SLN 来说,它相对稳定。蜂胶提取物有助于制剂的封闭潜力。用人永生化角质形成细胞进行测试时,两种提取物(蜂胶和 BP)自由或包封在系统中时,细胞均具有良好的细胞活力。用蜂胶材料修饰的 SLN 加速了体内伤口愈合过程。

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