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载有辣木叶提取物的聚合物微球的制备及表征及其在透皮伤口治疗中的应用。

Preparation and characterization of polymeric microparticles loaded with Moringa oleifera leaf extract for exuding wound treatment.

机构信息

Department of Pharmaceutical Sciences, University of Perugia, via del Liceo 1, 06123 Perugia, Italy.

Department of Pharmaceutical Sciences, University of Perugia, via del Liceo 1, 06123 Perugia, Italy.

出版信息

Int J Pharm. 2020 Sep 25;587:119700. doi: 10.1016/j.ijpharm.2020.119700. Epub 2020 Jul 29.

Abstract

The aim of this study was to develop an innovative formulation, particularly useful for the treatment of exuding wounds. An extract from Moringa oleifera leaves (MOE), prepared by an eco-friendly method, was used as active ingredient. Its preliminary characterization showed that MOE is rich in quercetin-O-glucoside and quercetin-O-malonyl glucoside, responsible for the antioxidant, radical scavenging and antibacterial activities (toward Staphylococcus aureus, S. epidermidis, S. faecalis and S. pyogenes). Moreover, MOE showed the ability to stimulate keratinocytes growth. Thus, bioadhesive biocompatible polymeric microparticles loaded with such extract were developed and prepared in order to treat exuding wounds. The microparticles, obtained by spray drying, using chitosan as polymer, showed good swelling ability. This is useful to obtain the transition from microparticles to a continuous gel covering the wound, after deposition on it. This has the double function to protect the damage area and to promote the healing. The in vitro release study showed that the formed gel is able to release immediately MOE, in the first minutes after application, and to promote a sustained release within 24 h reaching an efficacious concentration against the most sensitive bacterial strains. These findings suggest that the developed microparticles represent an interesting tool for exuding wounds treatment.

摘要

本研究旨在开发一种创新制剂,特别适用于治疗渗出性伤口。使用一种环保方法制备的辣木叶(MOE)提取物作为活性成分。其初步特性表明,MOE 富含槲皮素-O-葡萄糖苷和槲皮素-O-丙二酰葡萄糖苷,具有抗氧化、清除自由基和抗菌活性(针对金黄色葡萄球菌、表皮葡萄球菌、粪肠球菌和化脓性链球菌)。此外,MOE 显示出刺激角质细胞生长的能力。因此,开发并制备了负载这种提取物的生物粘附性生物相容性聚合物微球,以治疗渗出性伤口。通过喷雾干燥获得的微球,使用壳聚糖作为聚合物,显示出良好的溶胀能力。这对于在伤口上沉积后,从微球过渡到覆盖伤口的连续凝胶非常有用。这具有双重功能,既能保护损伤区域,又能促进愈合。体外释放研究表明,形成的凝胶能够在涂抹后的最初几分钟内立即释放 MOE,并在 24 小时内促进持续释放,达到对最敏感的细菌菌株有效的浓度。这些发现表明,开发的微球为治疗渗出性伤口提供了一种有前途的工具。

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