摘要
目的制备槲皮素纳米脂质体(Quercetin nano-liposomes,Que-LPs),并对其理化性质进行考察。方法采用乳化溶剂挥发法制备Que-LPs,Box-Behnken效应面法筛选最优处方。并对Que-LPs形态、Zeta电位、粒径及粒度分布、包封率、载药量进行研究。透析法测定制剂体外释药行为。结果制备的Que-LPs多呈类球形、大小比较均匀、表面圆整,粒径均在109.4 nm左右,粒度分布呈单峰,Zeta电位(-40.6±0.11)m V,其包封率为(87.93±1.03)%,载药量为(6.40±0.08)%,体外释放48 h时药物累积释放56.93%,且呈缓释现象,符合双相动力学方程。结论乳化溶剂挥发法适用于制备Que-LPs,纳米粒在溶液中分散均匀且稳定性良好。制备工艺安全可靠、稳定可行。体外释放呈现前期快速释药,后期缓慢释药的特征,与原料药相比有明显缓释作用。
Objective To prepare quercetin nano-liposomes（Que-LPs）, and detect their physicochemical properties. Method Que-LPs were prepared by emulsification solvent volatilization, and the optimum prescription was screened out by Box-Behnken Design. The morphology, zeta potential, particle size and particle size distribution, entrapment efficiency and drug loading of Que-LPs were characterized. Dialysis method was adopted to detect drug release in vitro of preparations. Result Que-LPs prepared under optimum conditions was mostly spherical, with the average size of 109.4 nm, which were distributed evenly, and zeta potential was （-40.6 ± 0.11 ）inV. The encapsulation rate of Que-LPs was （87.93 ± 1.03）%, and the drug-loading rate was （6.40± 0.08）%. The drug release in vitro was 56.93 % in 48 h, with sustained release phenomenon, which was followed by the biphase kinetic equation. Conclusion The emulsification solvent volatilization is applicable for preparing Que-LPs, and the nanoparticles are dispersed unitbrmly in solution and have good stability. The preparation process is safe, reliable and feasible. Drug release in vitro show a rapid release of the early release and a sustained release of the lately release. There is a significant sustained release effect, compared with the original drug.
作者
赵文琦
郭宇
于莲
Zhao Wenqi Guo Yu Yu Lian(College of Pharmacy, Jiamusi University, Jiamusi 154007, China)
出处
《广东化工》
CAS
2017年第20期13-14,共2页
Guangdong Chemical Industry
基金
国家自然科学基金项目(81274101)
关键词
槲皮素
纳米脂质体
乳化溶剂挥发法
缓释
quercetin
nano-liposomes： emulsification solvent volatilization
sustained-release
作者简介
赵文琦（1992-），女，河南新乡人，硕士研究生，主要研究方向为靶向、缓释给药系统研究。
为通讯作者：于莲，女，教授，硕士生导师，主要从事靶向、缓释给药系统研究，微生态调节剂。
