Guan Yong-Mei, Liu Jia, Zhang Jian-Lin, Chen Li-Hua, Zhu Wei-Feng, Zang Zhen-Zhong, Jin Chen, Wu Lu
Key Laboratory of Modern Preparation of Traditional Chinese Medicine, Ministry of Education, Jiangxi University of Traditional Chinese Medicine Nanchang 330004, China.
Zhongguo Zhong Yao Za Zhi. 2019 Apr;44(7):1363-1370. doi: 10.19540/j.cnki.cjcmm.20190115.007.
In order to increase the stability and solubility of essential oil in Jieyu Anshen Formula, this study was to prepare the essential oil into liposomes. In this experiment, the method for the determination of encapsulation efficiency of liposomes was established by ultraviolet spectrophotometer and dextran gel column. The encapsulation efficiency and particle size of liposomes were used as evaluation indexes for single factor investigation and Box-Behnken design-response surface method was used to optimize the design. Then the optimal formulation of volatile oil liposome was characterized using methyleugenol, elemin, β-asarone and α-asarone as index components. Finally, the in vitro transdermal properties of liposomes were studied by modified Franz diffusion cell. The results showed that the concentration of lecithin, the mass ratio of lecithin to volatile oil, and the stirring speed were the three most significant factors affecting the liposome preparation. The optimum formulation of volatile oil liposome was as follows: the concentration of lecithin was 7 g·L(-1); mass ratio of lecithin to volatile oil was 5∶1; and the stirring speed was 330 r·min(-1). Under such conditions, the prepared liposomes had blue emulsion light, good fluidity, half translucent, with particle size of(102.6±0.35) nm, Zeta potential of(-17.8±0.306) mV, permeability of(1.67±1.01)%, and stable property if liposome was stored at 4 ℃. 24 h after percutaneous administration, the cumulative osmotic capacity per unit time was(30.485 2±1.238 9),(34.794 8±0.928 3),(26.677 1±1.171 7),(3.066 2±0.175 3) μg·cm~(-2)respectively for methyleugenol, elemin, β-asarone and α-asarone. In vitro transdermal behaviors of methyleugenol, elemin, β-asarone and α-asarone in liposomes were all consistent with Higuchi equation. The prepared volatile oil liposomes met the relevant quality requirements, providing a reference for further research on preparation of multi-component Chinese medicine essential oil liposomes.
为提高解郁安神方中挥发油的稳定性和溶解性,本研究将挥发油制备成脂质体。本实验采用紫外分光光度计和葡聚糖凝胶柱法建立脂质体包封率的测定方法。以脂质体的包封率和粒径为评价指标进行单因素考察,并采用Box-Behnken设计-响应面法进行优化设计。然后以甲基丁香酚、榄香烯、β-细辛醚和α-细辛醚为指标成分对挥发油脂质体的最佳处方进行表征。最后采用改良的Franz扩散池研究脂质体的体外透皮性能。结果表明,卵磷脂浓度、卵磷脂与挥发油的质量比以及搅拌速度是影响脂质体制备的三个最显著因素。挥发油脂质体的最佳处方为:卵磷脂浓度为7 g·L⁻¹;卵磷脂与挥发油的质量比为5∶1;搅拌速度为330 r·min⁻¹。在此条件下,制备的脂质体呈蓝色乳光,流动性好,半透明,粒径为(102.6±0.35) nm,Zeta电位为(-17.8±0.306) mV,渗透率为(1.67±1.01)%,4℃保存时性质稳定。经皮给药24 h后,甲基丁香酚、榄香烯、β-细辛醚和α-细辛醚的单位时间累积渗透量分别为(30.485 2±1.238 9)、(34.794 8±0.928 3)、(26.677 1±1.171 7)、(3.066 2±0.175 3) μg·cm⁻²。甲基丁香酚、榄香烯、β-细辛醚和α-细辛醚在脂质体中的体外透皮行为均符合Higuchi方程。所制备的挥发油脂质体符合相关质量要求,为多组分中药挥发油脂质体制备的进一步研究提供参考。