Liang Tisong, Guan Rongfa, Shen Haitao, Xia Qile, Liu Mingqi
Zhejiang Proceincial Key Laboratory of Biometrology and Inspection and Quarantine, China Jiliang University, Hangzhou 310018, China.
Zhejiang Provincial Center for Disease Control and Prevention, 3399 Binsheng Road, Hangzhou 310051, China.
Molecules. 2017 Mar 13;22(3):457. doi: 10.3390/molecules22030457.
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.
我们旨在采用响应面法优化C3G纳米脂质体的配方。此外,我们评估了C3G纳米脂质体在不同温度和储存时间下,以及在模拟胃液(SGF)和模拟肠液中的稳定性、粒径变化和包封率(EE)。通过透射电子显微镜观察C3G纳米脂质体的形态。用Caco-2细胞研究了C3G纳米脂质体影响癌细胞形态和抑制癌细胞增殖的能力。逆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如下: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℃。在最佳条件下,C3G纳米脂质体的粒径和包封率分别为165.78±4.3 nm和70.43%±1.95%。C3G纳米脂质体在37℃的SGF中4小时表现出可接受的稳定性,但在延长的储存时间和高温下不稳定。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。