百里醌负载纳米乳凝胶促进伤口愈合和抗炎功效的比较皮肤动力学评价

IF 4 3区 化学 Q2 POLYMER SCIENCE
Mariam K. Alamoudi, Niyaz Ahmad, Khalid Ansari, Rana M. Aldossari, Mohammed Saifuddin Khalid, Zabih Ullah, Hanan Mesfer Alyami, Ali Jaber Alqahtani, Ahmed Merghani, Sarfaraz Ahmad, Anzarul Haque
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引用次数: 0

摘要

目的设计、制备并评价一种负载百里醌(TQN)的纳米乳液,并将其转化为纳米乳液,以提高其溶解度,改善皮肤渗透和皮肤动力学特性,并优化其在伤口愈合和抗炎治疗中的外用效果。由于TQN的水溶性有限或较差,直接影响其治疗效果。因此,开发TQN-NE凝胶对于增强透皮给药至关重要。方法采用微水滴定法制备负载tqn纳米乳(TQN-NE),以Labrafil®M2125为原料,Tween 80为表面活性剂,plurol oleique为助表面活性剂。为了提高局部使用的保留时间,纳米乳液与卡波波尔934凝胶结合,形成纳米乳液。通过热力学稳定性、粒径、物理性质、pH值、zeta电位、多分散性指数(PDI)、药物含量、流变性能、皮肤渗透性、体外药物释放、粘度、展布性、剪切应力、生物黏附强度、溶胀指数和粘附力等参数对纳米乳和纳米凝胶进行了分析。结果制备的TQN-NE6纳米乳透明、稳定,粒径为151.7±5.93 nm, ZP为−18.10±2.61 mV,多分散性指数为0.197±0.061。百里醌纳米乳凝胶(TQN-NE-Gel)的平均粒径为172.32±6.94 nm, PDI为0.126±0.123,ZP为- 23.30±0.45 mV, pH为6.66±0.08。在100 rpm下,它的粘度为5424 cP,涂覆系数为0.129±0.09 cm2/g,同时通过TEM分析证实,它具有增强的粘接强度和光滑的球形。优化后的TQN- ne - gel配方显著改善了皮肤渗透,皮肤动力学分析显示,与传统的TQN凝胶相比,处理后皮肤的Cmax和AUC0-8 h显着(p < 0.001)增强。此外,优化后的TQN-NE-Gel在局部应用时表现出优异的伤口愈合效果。治疗后未观察到炎症细胞浸润的迹象,证实了该配方的安全性和无毒性。结论研制出一种新型的tqn - ne -凝胶,具有提高百里醌溶解度和改善皮肤渗透的作用。当局部应用时,该配方在促进伤口愈合和提供抗炎作用方面表现出优越的功效。TQN-NE-Gel作为百里醌的有效载体,有助于改善透皮给药和未来的治疗潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

A comparative dermatokinetic evaluation of thymoquinone-loaded nanoemulsion gel for enhanced wound healing and anti-inflammatory efficacy

A comparative dermatokinetic evaluation of thymoquinone-loaded nanoemulsion gel for enhanced wound healing and anti-inflammatory efficacy

Purpose

This study aims to design, formulate, and assess a Thymoquinone (TQN)-loaded nanoemulsion, which is further transformed into a nanoemulgel to enhance solubility, improve skin penetration with dermatokinetic properties, and optimize its topical application for wound healing and anti-inflammatory treatment. Since TQN has limited or poor water solubility, its therapeutic efficacy is directly impacted. Therefore, developing a TQN-NE gel is essential to enhance transdermal delivery.

Methods

The TQN-loaded nanoemulsion (TQN-NE) was formulated using the aqueous microtitration method, incorporating Labrafil®M2125, i.e., oil, Tween 80, i.e., surfactant, and plurol oleique i.e., co-surfactant. To improve retention time for topical use, the nanoemulsion was combined with a carbopol 934-based gel, resulting in a nanoemulgel. Both nanoemulsion and nanoemulgel were analyzed by various parameters, including thermodynamic-stability, globule–size, physical–properties, pH, zeta potential, polydispersity index (PDI), drug content, rheological properties, permeation via skin, in vitro drug release, viscosity, -spreadability, shear stress, -bioadhesive strength, -swelling index, and adhesive force.

Results

The TQN-NE6 formulation resulted in a transparent, stable, and well-defined nanoemulsion with an average droplet/globule size of 151.7 ± 5.93 nm, a ZP of − 18.10 ± 2.61 mV, and a polydispersity index of 0.197 ± 0.061. The Thymoquinone nanoemulsion gel (TQN-NE-Gel) exhibited a mean droplet size of 172.32 ± 6.94 nm, a PDI of 0.126 ± 0.123, a ZP of − 23.30 ± 0.45 mV, and a pH of 6.66 ± 0.08. It also demonstrated a viscosity of 5424 cP at 100 rpm and a spreadability factor of 0.129 ± 0.09 cm2/g, along with enhanced mucoadhesive strength and a smooth, spherical shape confirmed by TEM analysis. The optimized TQN-NE-Gel formulation significantly improved skin permeation, with dermatokinetic analysis showing a notable (p < 0.001) enhance in Cmax and AUC0–8 h in treated skin compared to conventional TQN gel. Additionally, the optimized TQN-NE-Gel demonstrated superior wound healing efficacy upon topical application. No signs of inflammatory cell infiltration were observed post-treatment, confirming the formulation’s safety and non-toxic nature.

Conclusion

A novel TQN-NE-Gel was successfully developed, demonstrating enhanced solubility and improved skin permeation of Thymoquinone. The formulation exhibited superior efficacy in promoting wound healing and providing anti-inflammatory effects when applied topically. TQN-NE-Gel serves as an effective carrier for the Thymoquinone, facilitating improved transdermal delivery and therapeutic potential in future.

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来源期刊
Polymer Bulletin
Polymer Bulletin 化学-高分子科学
CiteScore
6.00
自引率
6.20%
发文量
0
审稿时长
5.5 months
期刊介绍: "Polymer Bulletin" is a comprehensive academic journal on polymer science founded in 1988. It was founded under the initiative of the late Mr. Wang Baoren, a famous Chinese chemist and educator. This journal is co-sponsored by the Chinese Chemical Society, the Institute of Chemistry, and the Chinese Academy of Sciences and is supervised by the China Association for Science and Technology. It is a core journal and is publicly distributed at home and abroad. "Polymer Bulletin" is a monthly magazine with multiple columns, including a project application guide, outlook, review, research papers, highlight reviews, polymer education and teaching, information sharing, interviews, polymer science popularization, etc. The journal is included in the CSCD Chinese Science Citation Database. It serves as the source journal for Chinese scientific and technological paper statistics and the source journal of Peking University's "Overview of Chinese Core Journals."
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