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新型冻干桑叶提取物传递体凝胶的研制

Development of a Novel Freeze-dried Mulberry Leaf Extract-based Transfersome Gel.

作者信息

Nangare Sopan, Bhatane Dhananjay, Mali Rushikesh, Shitole Mayuri

机构信息

H.R. Patel Institute of Pharmaceutical Education and Research, Department of Pharmaceutical Chemistry, Dhule, India.

Bharati Vidyapeeth College of Pharmacy, Department of Pharmaceutics, Maharashtra, India.

出版信息

Turk J Pharm Sci. 2021 Feb 25;18(1):44-55. doi: 10.4274/tjps.galenos.2019.98624.

Abstract

OBJECTIVES

Nowadays, antioxidants are important for health-related concerns related to acne vulgaris. Acne vulgaris is interrelated with the development of free radicals that interact with cells. Mulberry leaves contain phenolic compounds, including antioxidants such as quercetin. An antioxidant is a scavenger of free radicals. The current study addresses the development of a mulberry leaf extract-based transfersome gel containing quercetin by a thin-layer hydration method for topical antioxidant delivery. The process was optimized by encapsulating the drug in a variety of transfersome formulations.

MATERIALS AND METHODS

Batch optimization was carried out by particle size and zeta analysis, entrapment efficiency (%), polydispersity index, drug release, and drug content analysis.

RESULTS

The optimized batch MF5 provided 86.23% entrapment efficiency of quercetin in the vesicles and 95.79% drug release. It furnished a spherical shaped vesicle with an average diameter of 118.7 nm and zeta potential of -45.11 mV. The MG1 formulation provided superior antioxidant activity, drug content, and entrapment efficiency, drug release, spreadability, homogeneity, and stability to MG2. The presence of quercetin in the extract and gel formulation was confirmed by using high performance thin layer chromatography.

CONCLUSION

It is evident from this study that a mulberry leaf extract-based transfersome gel is a promising prolonged delivery system for quercetin and has reasonably good stability characteristics. This research recommends that mulberry leaf extract-based transfersome gel can potentially be used in the treatment of acne vulgaris through a transdermal drug delivery system.

摘要

目的

如今,抗氧化剂对于与寻常痤疮相关的健康问题很重要。寻常痤疮与自由基的产生相关,自由基会与细胞相互作用。桑叶含有酚类化合物,包括抗氧化剂如槲皮素。抗氧化剂是自由基的清除剂。本研究旨在通过薄层水化法开发一种含槲皮素的桑叶提取物传递体凝胶,用于局部抗氧化剂递送。通过将药物包裹在多种传递体制剂中来优化该过程。

材料与方法

通过粒径和zeta分析、包封率(%)、多分散指数、药物释放和药物含量分析进行批次优化。

结果

优化后的批次MF5在囊泡中槲皮素的包封率为86.23%,药物释放率为95.79%。它提供了一种平均直径为118.7 nm、zeta电位为 -45.11 mV的球形囊泡。MG1制剂在抗氧化活性、药物含量、包封率、药物释放、铺展性、均匀性和稳定性方面优于MG2。通过高效薄层色谱法确认了提取物和凝胶制剂中槲皮素的存在。

结论

从本研究中可以明显看出,基于桑叶提取物的传递体凝胶是一种有前景的槲皮素长效递送系统,具有相当好的稳定性特征。本研究建议基于桑叶提取物的传递体凝胶有可能通过透皮给药系统用于寻常痤疮的治疗。

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