龙胆苦苷纳米脂质载体的制备和性质表征

Preparation and Characterization of Gentiopicroside Nano-lipid Carriers

目的:制备龙胆苦苷纳米脂质载体(GEN-NLC),进行性质表征及稳定性、体外释放情况考察。方法:采用溶剂分散法制备GEN-NLC,以粒径、Zeta电位及包封率为指标,考察固/液脂质的比例、药脂比、表面活性剂种类及浓度等对GEN-NLC制备工艺的影响,通过透射电镜观察其形态,并进行稳定性、体外释药考察。结果:最佳处方为选用0.1%泊洛沙姆188为表面活性剂,药脂比1∶10,液态脂质的比例10%。制备的GEN-NLC包封率(38.19±1.61)%,载药量(3.47±0.08)%,粒径(129.9±3.07)nm,PDI(0.264±0.01),Zeta电位(-22.5±0.42)mV。GEN-NLC为球形粒子且呈单分散分布,外观圆整,大小均一,于4℃下放置30 d,包封率、粒径和Zeta电位均无明显变化,在4 h时仅释放39.65%,36 h时累积释放量达79.86%。结论:溶剂分散法制备的GEN-NLC具有较好的理化性质和稳定性,且具备一定的缓释长效作用。

Objective： To prepare gentiopicroside nano-lipid carriers （GEN-NLC） and investigate its stability, in vitro release and properties. Method： Solvent dispersion method was used to prepare GEN-NLC. With＇ particle size, Zeta potential and encapsulation efficiency as indexes, effects of proportion of solid-liquid lipid, drug-lipid ratio and the type and concentration of surfactant on preparation technology were investigated, morphology of prepared GEN-NLC was observed by transmission electron microscopy, its characteristics and stability was investigated. Result： Optimal prescription was as following： 0. 1% poloxamer 188 as surfactant, drug-lipid ratio 1 ： 10, liquid lipid ratio 10%. Encapsulation efficiency of prepared GEN-NLC was （38.19 ±1.61）% drug loading was （3.47 ±0.08）%, particle size was （129.9 ±3.07） nm, PDI was （0.264 ±0.01）, Zeta potential was （ - 22.5 ± 0.42） mV. GEN-NLC was spherical particles and showed monodisperse distribution, rounded appearance and uniform size. After stored at 4 ℃ for 30 d, indicators were not changed significantly, release of gentiopicroside 39.65% in 4 h, cumulative release amounted to 79.86% at 36 h. Conclusion： It showed that there were good physicochemical properties and stability of GEN-NLC prepared by solvent dispersion method, and had a certain degree of sustained-release long-lasting effect.