| 周柳莎,胡香莲,俞瑜媛,徐海星,施永清.荞麦糖肽脂质体的制备及其稳定性和缓释研究[J].中国粮油学报,2024,39(4):119-130 |
| 荞麦糖肽脂质体的制备及其稳定性和缓释研究 |
| Research on the Preparation, Stability and Sustained Release of Buckwheat Glycopeptide Liposomes |
| 投稿时间：2023-03-14 修订日期：2023-06-04 |
| DOI： |
| 中文关键词: 荞麦糖肽 脂质体 稳定性 体外缓释 生物活性 |
| 英文关键词:buckwheat glycopeptide stability liposomes in vitro sustained release bioactivity |
| 基金项目: |
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| 中文摘要: |
| 为提高荞麦糖肽(buckwheat glycopeptide,BG)的生物利用率,本研究首先对制备所得的BG进行稳定性分析,随后利用反向蒸发法制备荞麦糖肽脂质体(buckwheat glycopeptide liposomes,BGL),经响应面试验对包埋工艺进行优化,并探究其稳定性、体外缓释特性、α-葡萄糖苷酶(α-glucosidase,AGase)抑制活性和抗氧化活性。结果表明：温度(20~80 ℃)对BG的活性影响较小,碱性条件下BG极易失活。从五种磷脂中筛选出蛋黄卵磷脂制备BGL,响应面优化工艺条件为磷脂与胆固醇质量比为4.2:1,脂药比为7.5:1,水相体积为1 mL,此条件下,BGL包埋率为72.64%。BGL对高温(100 ℃)环境不耐受,在短时间(1 h)内具有广谱pH(2~10)稳定性,反复冻融5次对其渗漏率无显著影响(P＞0.05)。BGL在体外模拟胃、肠体系中表现出良好的缓释特性,24 h累计释放速率分别为（84.50±2.30）%和（60.17±1.42）%。脂质体包埋体系的建立有利于提高BG的稳定性,并对其AGase抑制和抗氧化活性表现出良好的保护作用,为荞麦糖肽脂质体开发应用提供理论依据。 |
| 英文摘要: |
| To improve the bioavailability of buckwheat glycopeptide (BG), the stability of the prepared BG was firstly analyzed in this study, and reverse evaporation was used to prepared buckwheat glycopeptide liposomes (BGL), whose encapsulation process was optimized by response surface experiment. Subsequently, the stability, in vitro sustained release properties and biological activity of BGL were further investigated. The results showed that temperature (20~80 ℃) had little effect on the activity of BG, but it declined rapidly in alkaline environment. Egg yolk lecithin was selected from five phospholipids to prepare BGL, and the optimum embedding conditions determined by the response surface experiment were as follows: the phospholipid to cholesterol mass ratio 4.2:1, lipid to drug ratio 7.5:1 and aqueous phase volume 1 mL. Experiments carried out under these conditions led to the encapsulation rate of 72.64% for BGL. In vitro stability results indicated that the structural integrity of the BGL was easily destroyed under high temperatures (100 ℃). Conversely, BGL showed a broad-spectrum pH (2~10) activity when the treatment time was 1 h and there was no significant effect (P＞0.05) on leakage rate of BGL after repeated freezing and thawing five times. BGL had sustained-release characteristics in the simulated gastric and intestinal systems in vitro, and the cumulative release rate of 24 h was （84.50±2.30）% and （60.17±1.42）%, respectively. The establishment of the liposome embedding system was beneficial to improve the stability of BG, and showed a good protective effect on its AGase inhibition and antioxidant activity, which provides a theoretical basis for the development and application of buckwheat glycopeptide liposomes. |
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