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柚皮苷载药微乳的制备、优化及经皮给药考察。

Preparation, Optimization, and Investigation of Naringenin-Loaded Microemulsion for Topical Application.

机构信息

Nanotechnology Research Center, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran.

Department of Pharmaceutics, Faculty of Pharmacy, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran.

出版信息

Iran Biomed J. 2022 Nov 1;26(5):366-73. doi: 10.52547/ibj.3722.

DOI:10.52547/ibj.3722
PMID:36403103
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9763875/
Abstract

BACKGROUND

Flavonoids are a large group of phenolic compounds possessing anti-inflammatory and antioxidant effects. NAR is a flavonoid with various pharmacological properties. Using pharmaceutical compounds on skin is one of the routes of administration to achieve local and systemic effects. The aim of this study was to develop a topical formulation of NAR by the preparation of a NAR ME, which was further tested its skin permeability in rats.

METHODS

Eight 0.5% NAR MEs were prepared by mixing appropriate amounts of surfactant (Tween 80 and Labrasol), cosurfactant (Capryol 90) and the oil phase (oleic acid-Transcutol P in a ratio of 1:10). The drug was dissolved in the oil phase. The physicochemical properties of MEs such as droplet size, viscosity, release, and skin permeability were assessed using Franz Cells diffusion.

RESULTS

Based on the results, the droplet size of MEs ranged between 5.07 and 35.15 nm, and their viscosity was 164-291 cps. Independent factors exhibited a strong relationship with both permeability and drop size. The permeability findings revealed that the diffusion coefficient of NAR by the ME carrier increased compared to the drug saturation solution.

CONCLUSION

The most validated results were obtained for Jss and particle size. Optimal formulations containing MEs with Jss and particle sizes varying between minimum and maximum amounts are suitable for topical formulations of NAR.

摘要

背景

类黄酮是一大类具有抗炎和抗氧化作用的酚类化合物。NAR 是一种具有多种药理特性的类黄酮。将药物化合物应用于皮肤是实现局部和全身效果的一种给药途径。本研究的目的是通过制备 NAR ME 来开发 NAR 的局部制剂,并进一步测试其在大鼠皮肤中的渗透性。

方法

通过将适量的表面活性剂(吐温 80 和 Labrasol)、助表面活性剂(Capryol 90)和油相(油酸-Transcutol P 以 1:10 的比例混合)混合,制备了 8 种 0.5%的 NAR ME。药物溶解在油相中。使用 Franz 细胞扩散法评估 ME 的物理化学性质,如粒径、粘度、释放和皮肤渗透性。

结果

根据结果,ME 的粒径范围在 5.07 至 35.15nm 之间,其粘度为 164-291cps。独立因素与渗透性和粒径均有很强的关系。渗透性研究结果表明,与药物饱和溶液相比,NAR 通过 ME 载体的扩散系数增加。

结论

最有效的结果是 Jss 和粒径。含有 ME 的最佳配方,Jss 和粒径在最小和最大之间变化,适合 NAR 的局部制剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ddd0/9763875/d1aea1159cd2/ibj-26-366-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ddd0/9763875/7e67aa778aed/ibj-26-366-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ddd0/9763875/87bcf0cc5fd8/ibj-26-366-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ddd0/9763875/e28e48b14f0f/ibj-26-366-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ddd0/9763875/deed7f571048/ibj-26-366-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ddd0/9763875/ebef87f22fea/ibj-26-366-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ddd0/9763875/2a2d5a3d1ebf/ibj-26-366-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ddd0/9763875/d1aea1159cd2/ibj-26-366-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ddd0/9763875/7e67aa778aed/ibj-26-366-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ddd0/9763875/87bcf0cc5fd8/ibj-26-366-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ddd0/9763875/e28e48b14f0f/ibj-26-366-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ddd0/9763875/deed7f571048/ibj-26-366-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ddd0/9763875/ebef87f22fea/ibj-26-366-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ddd0/9763875/2a2d5a3d1ebf/ibj-26-366-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ddd0/9763875/d1aea1159cd2/ibj-26-366-g007.jpg

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