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Permeation of albumin through the skin depending on its concentration and the substrate used in simulated conditions in vivo
Biomedicine & Pharmacotherapy ( IF 7.5 ) Pub Date : 2022-09-21 , DOI: 10.1016/j.biopha.2022.113722
Wioletta Siemiradzka 1 , Lucyna Bułaś 1 , Barbara Dolińska 1
Affiliation  

Objective

Many drugs applied to the skin with a systemic effect do not have a therapeutic effect, due to the barrier posed by the complex structure of the skin. To counteract this, absorption promoters are often added to the drug formulation. The use of albumin as an effective drug carrier is increasingly being addressed. Albumin, a natural, non-toxic polymer, can target drugs to specific cells and extend their biological half-life. This study was designed to trace the permeation of albumin after topical administration to the skin as a potential carrier of therapeutic substances.

Materials and methods

Four dermal formulations based on different polymers were prepared: methyl cellulose, sodium alginate, hypromellose and chitosan with methyl cellulose, obtaining final concentrations of albumin of 2%, 1.5% and 1%. The permeation of albumin through the skin was examined under simulated in vivo conditions.

Results

Most albumin permeated from the methylcellulose-based hydrogel. Depending on the concentration of albumin, permeation profiles were plotted and permeation rate constant and AUC(0–24 h) were calculated.

Conclusion

Methylcellulose was the optimal polymer for albumin release, whereas hypromellose was the least favorable. The concentration of albumin influences the amount and rate of permeation of this protein. The optimal concentration was 10 mg/g, from which the most albumin penetrated and the fastest. Human skin appeared to be more permeable to albumin than pig skin. However, the similar permeation profile through both membranes successfully allows the use of pig skin to track and evaluate the permeation of therapeutic substances with systemic effects.



中文翻译:

白蛋白通过皮肤的渗透取决于其浓度和在体内模拟条件下使用的底物

客观的

由于皮肤的复杂结构造成的屏障,许多具有全身作用的皮肤药物不具有治疗作用。为了抵消这一点,吸收促进剂通常被添加到药物制剂中。越来越多地使用白蛋白作为有效的药物载体。白蛋白是一种天然的无毒聚合物,可以将药物靶向特定细胞并延长其生物半衰期。该研究旨在追踪作为治疗物质的潜在载体局部给药后白蛋白对皮肤的渗透。

材料和方法

制备了四种基于不同聚合物的皮肤制剂:甲基纤维素、海藻酸钠、羟丙甲纤维素和含有甲基纤维素的壳聚糖,最终白蛋白浓度分别为 2%、1.5% 和 1%。在模拟的体内条件下检查白蛋白通过皮肤的渗透。

结果

大多数白蛋白从基于甲基纤维素的水凝胶中渗透出来。根据白蛋白的浓度,绘制渗透曲线并计算渗透速率常数和 AUC (0-24 小时)

结论

甲基纤维素是白蛋白释放的最佳聚合物,而羟丙甲纤维素是最不利的。白蛋白的浓度影响这种蛋白质的渗透量和速率。最佳浓度为 10 mg/g,其中白蛋白渗透最多且速度最快。人皮肤似乎比猪皮肤更容易渗透白蛋白。然而,通过两种膜的相似渗透曲线成功地允许使用猪皮肤来跟踪和评估具有全身作用的治疗物质的渗透。

更新日期:2022-09-22
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