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载有越桔提取物的纳米结构醇质体凝胶;作为一种用于皮肤年轻化的化妆品的体外/体内评估。

Nanostructured Ethosomal Gel Loaded with Arctostaphylosuva-Ursi Extract; In-Vitro/In-Vivo Evaluation as a Cosmeceutical Product for Skin Rejuvenation.

机构信息

Department of Pharmacy, The Islamia University of Bahawalpur, Bahawalpur 63100, Punjab, Pakistan.

School of Pharmacy and Pharmaceutical Sciences, Trinity College Dublin, The University of Dublin, Dublin 2, Ireland.

出版信息

Curr Drug Deliv. 2022;19(6):706-720. doi: 10.2174/1567201818666210729111026.

DOI:10.2174/1567201818666210729111026
PMID:34325633
Abstract

BACKGROUND

Arctostaphylosuva-ursi(AUU) being rich in polyphenols and arbutin is known to have promising biological activities and can be a potential candidate as a cosmaceutical. Ethosomes encourage the formation of lamellar-shaped vesicles with improved solubility and entrapment of many drugs including plant extracts.

OBJECTIVE

The objective of this work was to develop an optimized nanostructured ethosomal gel formulation loaded with AUU extract and evaluated for skin rejuvenation and depigmentation.

METHODS

AUU extract was tested for phenolic and flavonoid content, radical scavenging potential, reducing power activity, and in-vitro SPF (sun protection factor) estimation. AUU loaded 12 formulations were prepared and characterized by SEM (Scanning Electron Microscopy), vesicular size, zeta potential, and Entrapment Efficiency (%EE). The optimized formulation was subjected to noninvasive in-vivo investigations after incorporating it into the gel system and ensuring its stability and skin permeation.

RESULTS

Ethosomal vesicles were spherical in shape and Zeta size, zeta potential, PDI (Polydispersity Index), percentages of EE and in-vitro skin permeation of optimized formulation (F3) were found to be 114.7nm, -18.9mV, 0.492, 97.51±0.023%, and 79.88±0.013% respectively. AUU loaded ethosomal gel formulation was stable physicochemically and exhibited non-Newtonian behavior rheologically. Moreover, it significantly reduced skin erythema, melanin as well as sebum level and improved skin hydration and elasticity.

CONCLUSION

A stable AUU based ethosomal gel formulation could be a better vehicle for phytoextracts than conventional formulations for cosmeceutical applications such as for skin rejuvenation and depigmentation.

摘要

背景

熊果酸含有丰富的多酚和熊果苷,具有有前景的生物活性,因此可以成为一种潜在的化妆品候选物。醇质体能够促进形成具有改善的溶解度和包封许多药物(包括植物提取物)的层状囊泡。

目的

本工作的目的是开发一种载有熊果酸提取物的优化纳米结构醇质体凝胶制剂,并对其进行皮肤年轻化和脱色评估。

方法

测试了熊果酸提取物的酚类和类黄酮含量、自由基清除能力、还原能力活性以及体外 SPF(防晒因子)评估。制备了 12 种载有 AUU 的制剂,并通过 SEM(扫描电子显微镜)、囊泡大小、Zeta 电位和包封效率(%EE)进行了表征。将优化的制剂纳入凝胶系统后,进行了非侵入性的体内研究,以确保其稳定性和皮肤渗透。

结果

醇质体囊泡呈球形,Zeta 大小、Zeta 电位、PDI(多分散指数)、优化制剂(F3)的 EE 百分比和体外皮肤渗透分别为 114.7nm、-18.9mV、0.492、97.51±0.023%和 79.88±0.013%。AUU 载醇质体凝胶制剂在物理化学上是稳定的,表现出非牛顿流变行为。此外,它显著减少了皮肤红斑、黑色素和皮脂水平,并改善了皮肤水合作用和弹性。

结论

与传统制剂相比,基于熊果酸的稳定醇质体凝胶制剂可能是植物提取物的更好载体,可用于化妆品应用,如皮肤年轻化和脱色。

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