他克莫司类脂囊泡的构建及表征
发布时间：2019-03-18 10:02
【摘要】：目的:制备他克莫司类脂囊泡(Tac-NS)并进行体外表征。方法:采用薄膜水化-超声法制备Tac-NS。以包封率(EE%)、载药量、平均粒径及粒径分布(PDI)的综合评分为指标,设计正交试验对硬脂山梨坦(Span-60)浓度、Span-60与胆固醇的摩尔比、Span-60与脱氧胆酸钠(SDC)的摩尔比进行优化。考察所制Tac-NS的外观形态、平均粒径、PDI、Zeta电位及EE%,并通过体外经皮渗透试验比较Tac-NS与Tac和NS物理混合物的累积经皮渗透量(Q)、累积皮肤滞留量(Qs)。结果:最优处方为Span-60 0.025mol/L,Span-60与胆固醇的摩尔比10∶1,Span-60与SDC的摩尔比15∶1,药载比5%。所制Tac-NS形态圆整、分散均匀、很少有聚集,平均粒径为(233.0±6.48)nm,PDI为0.266±0.021,Zeta电位为(-41.7±0.32)m V,EE%为(76.83±4.61)%。经皮渗透试验表明,24 h后Tac-NS的Qs值约为物理混合物的2.4倍,而二者Q值相当。结论:成功制得EE%高、粒径小、分布均匀、透皮效果较为理想的Tac-NS。
[Abstract]:Objective: to prepare tacrolimus-like vesicles (Tac-NS) and characterize them in vitro. Methods: Tac-NS. was prepared by thin film hydration-ultrasound method. Taking EE%, drug loading, average particle size and size distribution of (PDI) as indexes, the orthogonal test was designed to determine the concentration of stearosortan (Span-60), the molar ratio of Span-60 to cholesterol, and the concentration of stearic sorbitan (Span-60) and the molar ratio of Span-60 to cholesterol. The molar ratio of Span-60 to sodium deoxycholate (SDC) was optimized. The appearance, average diameter, PDI,Zeta potential and EE%, of the prepared Tac-NS were investigated. The cumulative transdermal permeation of Tac-NS, Tac and NS was compared by in vitro transdermal permeation test. The cumulative skin retention of (Q), was compared with that of the physical mixture of Tac-NS and Tac and NS. Results: the optimal formulation was Span-60 0.025 mol / L, the molar ratio of Span 60 to cholesterol was 10 渭 1, the molar ratio of Spana 60 to SDC was 15 mol / L, and the drug loading ratio was 5%. The morphology of the prepared Tac-NS was round and uniform, with little aggregation. The average particle size was (233.0 卤6.48) nm,PDI, the mean diameter was 0.266 卤0.021, the Zeta potential was (- 41.7 卤0.32) MV, and the EE% was (76.83 卤4.61)%. The results of percutaneous permeation test showed that the Qs value of Tac-NS was about 2.4 times higher than that of physical mixture after 24 h, and the Q value of them was the same as that of physical mixture. Conclusion: the Tac-NS. with high EE%, small particle size, uniform distribution and better transdermal effect has been successfully prepared.
【作者单位】： 深圳市福田区第二人民医院药剂科;广东医学院附属福田医院药剂科;
【分类号】：R943
[Abstract]:Objective: to prepare tacrolimus-like vesicles (Tac-NS) and characterize them in vitro. Methods: Tac-NS. was prepared by thin film hydration-ultrasound method. Taking EE%, drug loading, average particle size and size distribution of (PDI) as indexes, the orthogonal test was designed to determine the concentration of stearosortan (Span-60), the molar ratio of Span-60 to cholesterol, and the concentration of stearic sorbitan (Span-60) and the molar ratio of Span-60 to cholesterol. The molar ratio of Span-60 to sodium deoxycholate (SDC) was optimized. The appearance, average diameter, PDI,Zeta potential and EE%, of the prepared Tac-NS were investigated. The cumulative transdermal permeation of Tac-NS, Tac and NS was compared by in vitro transdermal permeation test. The cumulative skin retention of (Q), was compared with that of the physical mixture of Tac-NS and Tac and NS. Results: the optimal formulation was Span-60 0.025 mol / L, the molar ratio of Span 60 to cholesterol was 10 渭 1, the molar ratio of Spana 60 to SDC was 15 mol / L, and the drug loading ratio was 5%. The morphology of the prepared Tac-NS was round and uniform, with little aggregation. The average particle size was (233.0 卤6.48) nm,PDI, the mean diameter was 0.266 卤0.021, the Zeta potential was (- 41.7 卤0.32) MV, and the EE% was (76.83 卤4.61)%. The results of percutaneous permeation test showed that the Qs value of Tac-NS was about 2.4 times higher than that of physical mixture after 24 h, and the Q value of them was the same as that of physical mixture. Conclusion: the Tac-NS. with high EE%, small particle size, uniform distribution and better transdermal effect has been successfully prepared.
【作者单位】： 深圳市福田区第二人民医院药剂科;广东医学院附属福田医院药剂科;
【分类号】：R943
【参考文献】
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1 周彦彬;何花;赵欢U，
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