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用从鼠尾藻中纯化得到的海藻酸钠制备微球及其pH响应行为和药物释放的研究

Preparation of microspheres by alginate purified from Sargassum horneri and study of pH-responsive behavior and drug release.

作者信息

Fernando Ilekuttige Priyan Shanura, Kirindage Kirinde Gedara Isuru Sandanuwan, Jeon Hyeong Nam, Han Eui Jeong, Jayasinghe Arachchige Maheshika Kumari, Ahn Ginnae

机构信息

Department of Marine Bio-Food Sciences, Chonnam National University, Yeosu 59626, Republic of Korea.

Department of Food Technology and Nutrition, Chonnam National University, Yeosu 59626, Republic of Korea.

出版信息

Int J Biol Macromol. 2022 Mar 31;202:681-690. doi: 10.1016/j.ijbiomac.2022.01.171. Epub 2022 Feb 2.

Abstract

Alginate is a biopolymer used in numerous biomedical applications. The current work describes the purification of alginate from Sargassum horneri and method optimization for formulating drug-loaded microparticles by water-in-oil emulsification/internal gelation. Molecular weights of S. horneri alginate were ranging 50-70 kDa. Among 16 method optimizations, the F4 method was selected for further studies based on shape descriptor parameters which indicated, 0.24 ± 0.01 circularity, 0.80 ± 0.11 roundness, 1.27 ± 0.20 aspect ratio between long and short axis, and less aggregation in PBS. Processing parameters of the F4 method were; CaCO/alginate ratio of 20/1 (w/w), 5% span 80 in oil (v/v), water/oil phase ratio of 1/20 (v/v), and 1000 rpm emulsification speed. Hollow pores were visible on the surface of dehydrated F4 microparticles. F4 microparticles indicated 41.84 ± 2.93 and 45.86 ± 1.65% encapsulation efficiencies for phloroglucinol (F4P) and indomethacin (F4I) with 32.69 ± 1.35 and 31.69 ± 1.98% loading capacities. These microparticles were found to be desirable for extending drug release over short periods (0-3 days) under pH 2.0-7.4. F4P and F4I were effective in suppressing intracellular reactive oxygen species in FD exposed HaCaT cells while increasing cell viability over 24 - 48 h duration.

摘要

藻酸盐是一种用于众多生物医学应用的生物聚合物。当前的工作描述了从鼠尾藻中纯化藻酸盐以及通过油包水乳化/内部凝胶化制备载药微粒的方法优化。鼠尾藻藻酸盐的分子量范围为50-70 kDa。在16种方法优化中,基于形状描述符参数选择了F4方法进行进一步研究,这些参数表明,圆形度为0.24±0.01,圆度为0.80±0.11,长轴与短轴的纵横比为1.27±0.20,并且在磷酸盐缓冲盐溶液(PBS)中的聚集较少。F4方法的工艺参数为:碳酸钙/藻酸盐比例为20/1(w/w),油相中5%的司盘80(v/v),水/油相比为1/20(v/v),乳化速度为1000 rpm。在脱水的F4微粒表面可见中空孔隙。F4微粒对间苯三酚(F4P)和吲哚美辛(F4I)的包封率分别为41.84±2.93%和45.86±1.65%,载药量分别为32.69±1.35%和31.69±1.98%。发现这些微粒有利于在pH 2.0-7.4条件下在短时间(0-3天)内延长药物释放。F4P和F4I在暴露于氟脱氧葡萄糖(FD)的人永生化角质形成细胞(HaCaT细胞)中有效抑制细胞内活性氧,同时在24-48小时内提高细胞活力。

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