论文部分内容阅读
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 carrier (GEN-NLC) for characterization, stability and release in vitro. Methods: GEN-NLC was prepared by solvent dispersion method. The particle size, Zeta potential and entrapment efficiency were used as indexes to investigate the effects of the ratio of solid / liquid lipid, drug-lipid ratio, surfactant type and concentration The morphology was observed by transmission electron microscopy, and the stability and in vitro release were investigated. Results: The best prescription for the selection of 0.1% poloxamer 188 as surfactant, drug-lipid ratio of 1:10, the proportion of liquid lipids 10%. The encapsulation efficiency of GEN-NLC (38.19 ± 1.61)%, drug loading (3.47 ± 0.08)%, particle size of 129.9 ± 3.07 nm, PDI of 0.264 ± 0.01 and Zeta potential of -22.5 ± 0.42 mV . GEN-NLC is a spherical particle with a monodisperse distribution, uniform in appearance and uniform in size. After being stored at 4 ° C for 30 days, the encapsulation efficiency, particle size and Zeta potential of GEN-NLC showed no obvious change, and only 39.65% At 36 h, the cumulative release reached 79.86%. Conclusion: GEN-NLC prepared by solvent dispersion method has good physico-chemical properties and stability, and has certain sustained-release long-term effect.