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壳聚糖-海藻酸钠纳米胶囊的研制及其用于糖尿病患者口服 delivery 的利拉鲁肽。

Development of chitosan coated calcium-alginate nanocapsules for oral delivery of liraglutide to diabetic patients.

机构信息

Department of Nanobiotechnology, Faculty of Biological Sciences, Tarbiat Modares University, Tehran, Iran.

Department of Nanobiotechnology, Faculty of Biological Sciences, Tarbiat Modares University, Tehran, Iran; Department of Biochemistry, Faculty of Biological Sciences, Tarbiat Modares University, Tehran, Iran.

出版信息

Int J Biol Macromol. 2018 Dec;120(Pt A):460-467. doi: 10.1016/j.ijbiomac.2018.08.078. Epub 2018 Aug 17.

Abstract

Chitosan coated calcium-alginate nanocapsules were developed for oral sustained delivery of liraglutide. The effect of coating components including sodium alginate, calcium chloride, and chitosan concentrations on the particle size was studied based on response surface methodology. The beads were characterized by dynamic light scattering, scanning and transmission electron microscopy as well as Fourier transform infrared spectroscopy. It was shown that the diameter of the formed beads was most dependent on the encapsulation technique and alginate concentration. SEM revealed spherical and smooth particles of up to 100 nm diameter for the optimum composition of alginate 0.5%, chitosan 0.5% and calcium chloride 0.5% in the volume ratio of 3:1:1. The resulting bead formulation had a loading efficiency of 92.5% and loading capacity of 54.16%. The nanocapsules exhibited stability of 92.4% and 72.3% over freeze drying and subsequent 60 days storage at 4 °C, respectively. In-vitro release studies in simulated gastrointestinal conditions were carried out in a sequential technique and the amount of drug release was found to be 59.1% after 6 h. The results of this study demonstrated that chitosan coated calcium-alginate nanocapsules hold promise as a potential natural biodegradable polymer-based oral carrier of liraglutide for better management of diabetes.

摘要

壳聚糖包被的海藻酸钙纳米胶囊被开发用于利拉鲁肽的口服缓释。基于响应面法研究了包衣成分(包括海藻酸钠、氯化钙和壳聚糖浓度)对粒径的影响。采用动态光散射、扫描和透射电子显微镜以及傅里叶变换红外光谱对微球进行了表征。结果表明,形成的微球的直径最依赖于包封技术和海藻酸钠浓度。SEM 显示,对于海藻酸钠 0.5%、壳聚糖 0.5%和氯化钙 0.5%的最佳组成,在体积比为 3:1:1 时,可得到直径高达 100nm 的球形光滑颗粒。所得微球制剂的载药效率为 92.5%,载药量为 54.16%。冷冻干燥和随后在 4°C 下储存 60 天的稳定性分别为 92.4%和 72.3%。在模拟胃肠道条件下进行了顺序技术的体外释放研究,发现 6 小时后药物释放量为 59.1%。这项研究的结果表明,壳聚糖包被的海藻酸钙纳米胶囊有望成为一种潜在的天然可生物降解聚合物口服载体制剂,用于更好地管理糖尿病。

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