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羧甲基魔芋葡甘聚糖对多层乳液的包被用于提高姜黄素的生物利用度和靶向递送。

Carboxymethyl konjac glucomannan coating on multilayered emulsions for improved bioavailability and targeted delivery of curcumin.

机构信息

College of Food Science and Engineering, Qingdao Agricultural University, Qingdao 266109, PR China.

出版信息

Food Funct. 2021 Jun 21;12(12):5429-5439. doi: 10.1039/d0fo03390a. Epub 2021 May 14.

Abstract

Curcumin was entrapped in multilayered emulsions to increase its stability and bioavailability. Curcumin emulsion stabilized by whey protein isolate (WPI) was coated with chitosan (CHI) or carboxymethyl konjac glucomannan (CMKGM) alone to form secondary emulsions and their combination in sequence to form the tertiary emulsion, in which, the polyelectrolyte concentrations were 1.0% WPI for the primary emulsion, 0.4% CMKGM for the secondary emulsion -CMKGM, 0.2% CHI for the secondary emulsion -CHI, and 0.1% CMKGM for the tertiary emulsion. The characteristics of the emulsions, including their particle size, ζ potential, microstructure, creaming stability, and biopolymer distribution, were investigated and their colon-targeted delivery potential was evaluated through both in vitro and in vivo studies as well. The curcumin-loaded secondary and tertiary emulsions were stable with a narrow size distribution and were generated by layer-by-layer assembly according to confocal laser scanning microscope observation. When CMKGM was located at the outermost layer, the corresponding secondary and tertiary emulsions showed a greatly reduced release of curcumin in the simulated gastric fluid, but exhibited increased release in the β-mannanase-containing simulated colonic fluid. In vivo evaluation in mice demonstrated that the bioavailability of curcumin in the CMKGM-coated secondary and tertiary emulsions was increased by about 4 folds compared with that of free curcumin and curcumin could be released in a sustainable manner. These results demonstrated that multilayered emulsions coated with CMKGM could promote curcumin absorption in the gastrointestinal tract and hence is a promising colon-targeted delivery system for curcumin.

摘要

姜黄素被包埋在多层乳液中以提高其稳定性和生物利用度。用乳清蛋白分离物(WPI)稳定的姜黄素乳液单独用壳聚糖(CHI)或羧甲基魔芋葡甘露聚糖(CMKGM)进行涂层,以形成二次乳液,并将它们组合形成三级乳液,其中,聚电解质浓度为 1.0% WPI 用于初级乳液,0.4% CMKGM 用于二级乳液-CMKGM,0.2% CHI 用于二级乳液-CHI,0.1% CMKGM 用于三级乳液。研究了乳液的特性,包括其粒径、ζ电位、微观结构、乳状液稳定性和生物聚合物分布,并通过体外和体内研究评估了其结肠靶向递送的潜力。载姜黄素的二级和三级乳液具有窄的粒径分布,并且通过层层组装产生,根据共焦激光扫描显微镜观察。当 CMKGM 位于最外层时,相应的二级和三级乳液在模拟胃液中的姜黄素释放明显减少,但在含有β-甘露聚糖酶的模拟结肠液中的释放增加。在小鼠体内评价中,与游离姜黄素相比,CMKGM 涂层的二级和三级乳液中的姜黄素生物利用度提高了约 4 倍,并且可以以可持续的方式释放姜黄素。这些结果表明,用 CMKGM 涂层的多层乳液可以促进姜黄素在胃肠道中的吸收,因此是一种有前途的姜黄素结肠靶向递送系统。

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