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开发稳定的生育酚琥珀酸酯负载醇质体以增强透皮渗透:体外和体内特性研究。

Development of stable tocopherol succinate-loaded ethosomes to enhance transdermal permeation: In vitro and in vivo characterizations.

机构信息

Department of Pharmacy, The Islamia University of Bahawalpur, Bahawalpur, Pakistan.

出版信息

J Cosmet Dermatol. 2022 Oct;21(10):4942-4955. doi: 10.1111/jocd.14907. Epub 2022 Mar 21.

DOI:10.1111/jocd.14907
PMID:35274433
Abstract

BACKGROUND

Tocopherol succinate (TS) represents synthetic derivative of α-tocopherol (vitamin E), it act as anti-aging, moisturizing, and antioxidant. Ultraviolet (UV) photo stability of TS is low, and it cause skin irritation.

AIM

To develop tocopherol succinate loaded ethosomal gel for topical TS delivery and to evaluate its moisturizing and anti-aging effects.

METHOD

Cold method technique was used to produce ethosomal formulations (N = 9) by varying ethanol and lipid concentrations (F1-F9). The most optimized formulation (F5) was selected for further study on the basis of characterization. F5 Formulation was incorporated into gel. Ex vivo permeation study was done by using Franz diffusion cell. Non-invasive in vivo study was performed using corneometer for the evaluation of skin moisture content and skin mechanical properties by using cutometer, for 12 weeks on human subjects (N = 13).

RESULTS

Particle size (PS), zeta potential (ZP) and polydispersity index (PDI), Entrapment efficiency were found to be 179.1 nm, -13.7 mV and 0.345, and 99.71%, respectively. Transmission electron microscopy (TEM) depicted spherical ethosomal particles. Ethosomal gel and control gel were evaluated for conductivity and pH. Rheological analysis revealed a non-Newtonian flow. The release profile showed initial burst and then, sustained release, release data followed Korsmeyer-Peppas model. TS-loaded ethosomal gel appeared physically stable and showed significant results in terms of skin capacitance and mechanical properties.

CONCLUSION

The prepared ethosomal gel formulation containing TS is more stable with enhanced antioxidant, moisturizing properties, and increased TS deposition into the skin layer.

摘要

背景

琥珀酸生育酚酯(TS)是 α-生育酚(维生素 E)的合成衍生物,具有抗衰老、保湿和抗氧化作用。琥珀酸生育酚酯的紫外线(UV)光稳定性低,会引起皮肤刺激。

目的

开发用于局部 TS 递送的琥珀酸生育酚酯负载醇质体凝胶,并评价其保湿和抗衰老作用。

方法

采用冷法技术,通过改变乙醇和脂质浓度(F1-F9)制备醇质体配方(N=9)。基于特性,选择最优化的配方(F5)进行进一步研究。将 F5 制剂掺入凝胶中。通过 Franz 扩散池进行离体渗透研究。通过使用皮肤水分计对人体受试者(N=13)进行 12 周的非侵入性体内研究,使用皮肤弹性计评估皮肤水分含量和皮肤机械性能,使用皮肤弹性计评估皮肤机械性能。

结果

粒径(PS)、Zeta 电位(ZP)和多分散指数(PDI)、包封效率分别为 179.1nm、-13.7mV 和 0.345、99.71%。透射电子显微镜(TEM)显示出球形醇质体颗粒。醇质体凝胶和对照凝胶的电导率和 pH 值进行了评估。流变分析显示出非牛顿流动。释放曲线显示出初始突释,然后是持续释放,释放数据符合 Korsmeyer-Peppas 模型。载有 TS 的醇质体凝胶外观稳定,在皮肤电容和机械性能方面表现出显著的效果。

结论

含有 TS 的制备醇质体凝胶配方更稳定,具有增强的抗氧化、保湿性能,并且 TS 沉积到皮肤层中增加。

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