Department of Food Science and Nutrition, National Engineering Laboratory of Intelligent Food Technology and Equipment, Zhejiang Key Laboratory for Agro-Food Processing, Zhejiang University, Hangzhou 310058, China.
Department of Food Science and Nutrition, National Engineering Laboratory of Intelligent Food Technology and Equipment, Zhejiang Key Laboratory for Agro-Food Processing, Zhejiang University, Hangzhou 310058, China; Ningbo Research Institute, Zhejiang University, Ningbo 315100, China.
Int J Biol Macromol. 2020 Sep 15;159:341-355. doi: 10.1016/j.ijbiomac.2020.05.076. Epub 2020 May 15.
Colon-targeted delivery is an active area of research as it can improve drug stability, bioactivity, and lessen the systematic toxicity. In this study, the colon-specific delivery of pelargonidin-3-O-glucoside (P3G) was investigated using pectin (P)/chitosan (CH)-functionalized nanoliposome (NL). The food simulant stability, transport mechanism, and bioactivity retention potential of carrier systems were studied. Results showed that polymer-coated nanoliposomes (P-CH-NL and CH-NL) improved the thermal and food simulant stability as well as enhanced the P3G retention during the in vitro digestion. The maximum P3G retention after enzymatic and non-enzymatic digestion was observed by P-CH-NL and the values were 47.5% and 57.5%, respectively. However, all nanoliposomal carriers followed Fickian diffusion mechanism both in in vitro food simulants and in vitro digestion models. Digested functionalized nanoliposomes revealed higher antioxidant properties after gastric digestion. Following by simulated intestinal fluid digestion, ABTS antioxidant activity of P-CH-P3G-NL was 12.52% and 6.31% higher than that of P3G-NL and CH-P3G-NL, respectively, while DPPH scavenging capacity of P-CH-P3G-NL was 5.57% and 1.86% greater than that of P3G-NL and CH-P3G-NL, respectively. Therefore, the developed functionalized nanoliposome can be useful for colon-targeted delivery and applicable in functional foods and/or beverages.
靶向结肠给药是一个活跃的研究领域,因为它可以提高药物的稳定性、生物活性,并降低系统性毒性。在这项研究中,使用果胶(P)/壳聚糖(CH)-功能化纳米脂质体(NL)研究了矢车菊素-3-O-葡萄糖苷(P3G)的结肠特异性递送。研究了载体系统的食品模拟稳定性、传输机制和生物活性保留潜力。结果表明,聚合物包被的纳米脂质体(P-CH-NL 和 CH-NL)提高了热稳定性和食品模拟物稳定性,并增强了体外消化过程中 P3G 的保留。在酶和非酶消化后,P-CH-NL 观察到最大的 P3G 保留率,分别为 47.5%和 57.5%。然而,所有纳米脂质体载体在体外食品模拟物和体外消化模型中均遵循菲克扩散机制。经胃消化后,消化后的功能化纳米脂质体显示出更高的抗氧化性能。在模拟肠液消化后,P-CH-P3G-NL 的 ABTS 抗氧化活性分别比 P3G-NL 和 CH-P3G-NL 高 12.52%和 6.31%,而 P-CH-P3G-NL 的 DPPH 清除能力分别比 P3G-NL 和 CH-P3G-NL 高 5.57%和 1.86%。因此,开发的功能化纳米脂质体可用于结肠靶向给药,并适用于功能性食品和/或饮料。