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载于桉叶油基纳米凝胶中的美洛昔康抗炎作用的研发、表征及优化

Development, Characterization and Optimization of the Anti-Inflammatory Influence of Meloxicam Loaded into a Eucalyptus Oil-Based Nanoemulgel.

作者信息

Shehata Tamer M, Elnahas Hanan M, Elsewedy Heba S

机构信息

Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Alhofuf 31982, Saudi Arabia.

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Zagazig University, Zagazig 44519, Egypt.

出版信息

Gels. 2022 Apr 22;8(5):262. doi: 10.3390/gels8050262.

Abstract

The purpose of the present study was to explore the influence of a certain natural essential oil, namely eucalyptus oil, as an anti-inflammatory agent in addition to its prospective role in enhancing the action of meloxicam in reducing inflammation. As far as we know, this has been the first integration of meloxicam and eucalyptus essential oil into a nanoemulgel formulation intended for topical use. Primarily, eucalyptus oil was utilized in developing a nanoemulsion formulation incorporating meloxicam. A 2 factorial design was constructed using two independent variables (oil concentration and surfactant concentration) with two responses (particle size and % of in vitro release). One optimized formula was selected depending on the desirability function and subjected to a stability study. The optimized nanoemulsion was mixed with HPMC as a gelling agent to produce a meloxicam-loaded nanoemulgel, which was examined for its properties, stability, in vitro release and ex vivo permeation. Eventually, the anti-inflammatory activity was evaluated and compared with a placebo and corresponding gel formulation. The developed nanoemulgel revealed acceptable physical characteristics to be applied topically. Studying of the in vitro release was conducted successfully for 6 h. The ex vivo permeation from the nanoemulgel formulations was prompted, showing an appropriate value of the steady-state transdermal flux (SSTF). As a final point, the anti-inflammatory activity of the developed nanoemulgel revealed a valued anti-inflammatory influence. Additionally, the concurrence of eucalyptus essential oil and meloxicam was assured, and their potential in combating and lowering inflammation was supported.

摘要

本研究的目的是探讨某种天然精油(即桉叶油)作为抗炎剂的作用,以及它在增强美洛昔康抗炎作用方面的潜在作用。据我们所知,这是首次将美洛昔康和桉叶精油整合到一种用于局部应用的纳米乳凝胶制剂中。首先,桉叶油被用于开发一种包含美洛昔康的纳米乳剂配方。使用两个自变量(油浓度和表面活性剂浓度)和两个响应变量(粒径和体外释放率)构建了一个二因素设计。根据可取性函数选择了一个优化配方,并进行了稳定性研究。将优化后的纳米乳剂与作为胶凝剂的羟丙基甲基纤维素混合,制成载有美洛昔康的纳米乳凝胶,并对其性质、稳定性、体外释放和离体渗透进行了研究。最后,评估了抗炎活性,并与安慰剂和相应的凝胶制剂进行了比较。所开发的纳米乳凝胶显示出可接受的物理特性,适用于局部应用。成功进行了6小时的体外释放研究。纳米乳凝胶制剂的离体渗透得到促进,显示出稳态透皮通量(SSTF)的适当值。最后,所开发的纳米乳凝胶的抗炎活性显示出有价值的抗炎作用。此外,确保了桉叶精油和美洛昔康的协同作用,并支持了它们在对抗和减轻炎症方面的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4033/9141593/e3d23c6fd010/gels-08-00262-g001.jpg

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