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纳米脂质体介导长春西汀经皮给药用于治疗阿尔茨海默病

Nanoethosomes mediated transdermal delivery of vinpocetine for management of Alzheimer's disease.

作者信息

Moghaddam Atefeh Afshar, Aqil Mohd, Ahmad Farhan J, Ali Mushir M, Sultana Yasmin, Ali Asgar

机构信息

a Department of Pharmaceutics, Faculty of Pharmacy , Hamdard University , New Delhi , India.

出版信息

Drug Deliv. 2015 Dec;22(8):1018-1026. doi: 10.3109/10717544.2013.846433. Epub 2014 Apr 10.

DOI:10.3109/10717544.2013.846433
PMID:24717007
Abstract

AIM

To develop and statistically optimize nanoethosomal formulation for transdermal delivery of vinpocetine as an anti-Alzheimer's drug.

MATERIALS AND METHODS

Box-Behnken experimental design was applied for optimization of nanoethosomes. The independent variables were phospholipid (X), Tween 80 (X) and Ethanol (X) while entrapment efficiency (Y), particle sizes (Y), elasticity (Y) and flux (Y) were the dependent variables.

RESULTS AND CONCLUSION

Optimized nanoethosomal vinpocetine formulation with mean particle size 50.57 ± 26.11 nm showed 97.51 ± 0.86% entrapment efficiency, achieved mean transdermal flux 925.60 ± 39.80 µg/cm/h and elasticity of 86.61 ± 2.88. Ex-vivo study of nanoethosomal formulation showed a significant increase flux and entrapment efficiency compared with control vinpocetine solution. Our results suggest that nanoethosome is an efficient carrier for transdermal delivery of vinpocetine as compared to its oral form.

摘要

目的

开发并通过统计学方法优化用于长春西汀经皮给药的纳米脂质体配方,长春西汀作为一种抗阿尔茨海默病药物。

材料与方法

采用Box-Behnken实验设计对纳米脂质体进行优化。自变量为磷脂(X₁)、吐温80(X₂)和乙醇(X₃),而包封率(Y₁)、粒径(Y₂)、弹性(Y₃)和通量(Y₄)为因变量。

结果与结论

优化后的长春西汀纳米脂质体配方平均粒径为50.57 ± 26.11 nm,包封率为97.51 ± 0.86%,平均经皮通量为925.60 ± 39.80 μg/cm²/h,弹性为86.61 ± 2.88。纳米脂质体配方的体外研究表明,与长春西汀对照溶液相比,通量和包封率显著增加。我们的结果表明,与口服形式相比,纳米脂质体是长春西汀经皮给药的有效载体。

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