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藻酸盐微球通过与白及多糖混合来改善黏膜黏附性,作为潜在的胃滞留型给药载体。

Mucoadhesive improvement of alginate microspheres as potential gastroretentive delivery carrier by blending with Bletilla striata polysaccharide.

机构信息

School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing City, Jiangsu Province 210023, PR China; Jiangsu Engineering Research Center for Efficient Delivery System of TCM, Nanjing City, Jiangsu Province 210023, PR China.

School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing City, Jiangsu Province 210023, PR China; Jiangsu Engineering Research Center for Efficient Delivery System of TCM, Nanjing City, Jiangsu Province 210023, PR China.

出版信息

Int J Biol Macromol. 2020 Aug 1;156:1191-1201. doi: 10.1016/j.ijbiomac.2019.11.156. Epub 2019 Nov 19.

DOI:10.1016/j.ijbiomac.2019.11.156
PMID:31756485
Abstract

As polysaccharide from Bletilla striata (BSP) was anticipated with mucoadhesive improvement in sodium alginate (SA) microspheres, BSP was mixed with SA to construct a composite microsphere to retain in the gastrointestinal tract for a long time. The morphological properties, particle size and thermodynamic properties of the microspheres in combination with comprehensive evaluations in the swelling properties, mucin adsorption, ex vivo and in vivo gastric retention were determined to characterize the mucoadhesion of SA-BSP blend microspheres. Results showed that the prepared microspheres were discrete and spherical. The addition of BSP increased flexibility and reduced rigidity of SA microsphere. Furthermore, the swelling property, mucin adsorption ability and the retention rate on the gastric mucosa of SA matrix were increased after blending with BSP. Mucoadhesion tests showed the SA-BSP microspheres stayed much longer in rats' stomach than the SA microsphere did. Above all, the SA-BSP microspheres with the enhanced mucoadhesion suggested being a potential drug carrier in developing the gastroretentive drug delivery system.

摘要

由于白芨多糖(BSP)有望改善海藻酸钠(SA)微球的粘膜粘附性,因此将 BSP 与 SA 混合构建复合微球,以使其在胃肠道中长时间保留。通过测定微球的形态特性、粒径和热力学性质,并结合对膨胀性能、粘蛋白吸附、离体和体内胃滞留的综合评价,来表征 SA-BSP 共混微球的粘膜粘附性。结果表明,所制备的微球是离散的和球形的。BSP 的添加增加了 SA 微球的柔韧性并降低了其刚性。此外,与 BSP 混合后,SA 基质的膨胀性能、粘蛋白吸附能力和对胃粘膜的滞留率均提高。粘膜粘附性测试表明,SA-BSP 微球在大鼠胃中的停留时间明显长于 SA 微球。总之,具有增强的粘膜粘附性的 SA-BSP 微球有望成为开发胃滞留药物传递系统的潜在药物载体。

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