Optimization of Conditions for Cyanidin-3-OGlucoside (C3G) Nanoliposome Production by Response Surface Methodology and Cellular Uptake Studies in Caco-2 Cells.

Optimization of Conditions for Cyanidin-3-OGlucoside (C3G) Nanoliposome Production by Response Surface Methodology and Cellular Uptake Studies in Caco-2 Cells.
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通过响应面方法优化花青素-3-O-葡萄糖苷 (C3G) 纳米脂质体生产条件和 Caco-2 细胞的细胞摄取研究

DOI:
10.3390/molecules22030457
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发表时间:
2017-03-13
期刊:
Molecules (Basel, Switzerland)
影响因子:
--
通讯作者:
Liu M
Liu M
中科院分区:
其他
文献类型:
--
作者:
Liang T;Guan R;Shen H;Xia Q;Liu M

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我们的目标是用响应面法优化C3G纳米脂质体的处方。此外,我们还考察了C3G纳米脂质体在不同温度、不同储存时间以及在模拟胃肠液(SGF)和模拟肠液中的稳定性、颗粒变化和包封率。用透射电子显微镜观察了C3G纳米脂质体的形态。以Caco-2细胞为模型,研究了C3G纳米脂质体对癌细胞形态的影响和对癌细胞增殖的抑制作用。反相蒸发法是一种简单有效的脂质体制备方法。该方法的最佳制备条件为:C3G浓度为0.17 mg/mL,磷脂酰胆碱/胆固醇比为2.87,旋转蒸发温度为41.41℃,在此条件下制备的C3G纳米脂质体的粒径为165.78±4.3 nm,EE为70.43%±1.95%。C3G纳米脂质体在37℃、4h的SGF中表现出较好的稳定性,但在长时间储存和高温下不稳定。此外,我们的结果表明,不同浓度的C3G纳米脂质体影响Caco-2细胞的形态并抑制其增殖。
We aimed to optimize the formulation of C3G nanoliposomes using response surface methodology. Additionally, we evaluated the stability, particle change, and encapsulation efficiency (EE) of C3G nanoliposomes under different temperatures and storage durations, as well as in simulated gastrointestinal juice (SGF) and simulated intestinal fluid. The morphology of C3G nanoliposomes was observed by transmission electron microscope. The ability of C3G nanoliposomes to affect cancer cell morphology and inhibit cancer cell proliferation was studied with Caco-2 cells. Reverse-phase evaporation method is a simple and efficient method for liposome preparation. The optimal preparation conditions for this method were as follows: C3G concentration of 0.17 mg/mL, phosphatidylcholine/cholesterol ratio of 2.87, and rotary evaporation temperature of 41.41 °C. At optimal conditions, the particle size and EE of the C3G nanoliposomes were 165.78 ± 4.3 nm and 70.43% ± 1.95%, respectively. The C3G nanoliposomes showed an acceptable stability in SGF at 37 °C for 4 h, but were unstable under extended storage durations and high temperatures. Moreover, our results showed that different concentrations of C3G nanoliposomes affected the morphology and inhibited the proliferation of Caco-2 cells.
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