荷载β-胡萝卜素OS-葡聚糖酯胶束结肠靶向递送特性的研究

Study on Colon-specific Delivery of β-carotene with Oat β-glucan Octenylsuccinate Micelles

聚合物胶束因其增溶、靶向递送亲脂性活性成分的特性,使得其在医药、营养、食品加工等领域具有广阔的应用前景。本文以辛烯基琥珀酸燕麦β-葡聚糖酯(oatβ-glucan octenylsuccinate,OS-glucan)胶束为研究对象,初步探讨其对β-胡萝卜素的结肠靶向递送特性。研究结果表明:OS-葡聚糖酯胶束在模拟胃液环境条件下,其粒度和多分散性指数(polydispersity index,PDI)的变化较小,荷载的β-胡萝卜素的保留率有所下降;在模拟肠液环境条件下,OS-葡聚糖酯胶束结构部分被破坏,导致一定程度降解,胶束中β-胡萝卜素的含量有所减少、胶束的粒度显著增大、PDI也显著性增大。在体外结肠发酵试验中,OS-葡聚糖酯胶束发生快速解体,7 h内β-胡萝卜素被迅速释放。因此,OS-葡聚糖酯胶束可作为β-胡萝卜素的载体,有效调控其在模拟胃肠液中的释放行为,并在一定程度上实现其向结肠部位的递送。

Polymeric micelles have broad potential applications in the fields of medicine, nutrition, food processing, and others owing to their capabilities to specifically deliver lipophilic active ingredients and enhancc their solubility. In this paper, oat β-glucan octenylsuccinate（OS-glucan） micelles were studied, and the colon-specific delivery of β-carotene using OS-glucan was preliminarily discussed. The study showed that in simulated gastrointestinal fluid, OS-glucan exhibited relatively small changes in particle size and polydispersity index（PDI）, and the retention rate of loaded β-carotene was decreased. In simulated intestinal fluid, the partial structure of OS-glucan micelles was damaged, leading to some degradation. The content of β-carotene in the micelles was decreased, the particle size of micelles was significantly increased, and the PDI was also pronouncedly increased. During the in vitro colonic fermentation experiment, OS-glucan micelles disintegrated rapidly, and β-carotene was quickly released in seven hours. Therefore, OS-glucan micelles can be used as a carrier of β-carotene to effectively regulate the releasing behavior in simulated gastrointestinal fluid, and the colon-specific delivery of β-carotene can somewhat be achieved.