双氯芬酸二乙胺深层共晶体系在人体皮肤上的开发、表征和体内渗透评估

IF 2.7 4区 医学 Q2 PHARMACOLOGY & PHARMACY
Layaly Al-Mawla, Faisal Al-Akayleh, Saifeddin Daadoue, Waseem Mahyoob, Badralbdoor Al-Tameemi, Mayyas Al-Remawi, Samer Adwan, Ahmed S. A. Ali Agha
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引用次数: 0

摘要

目的 本研究的主要目的是介绍治疗性深共晶系统(THEDES),将其作为一种新型、绿色和生物相容性溶剂系统,用于非甾体消炎药双氯芬酸二乙胺(DDEA)的给药。研究问题的重点是,与传统溶剂相比,THEDES 能否显著提高 DDEA 的溶解度和释放动力学。方法 THEDES 配方由不同比例的癸酸、薄荷醇和 Gelucire® 33/01 组成。采用傅立叶变换红外光谱法(FTIR)、差示扫描量热法(DSC)、流变学测量和接触角测试等技术来表征和研究药物增溶过程。结果所开发的 THEDES 表现出独特的分子相互作用和界面特性,其玻璃化转变温度低于 - 50 °C,并具有广泛的内热熔点,表明其具有出色的相稳定性。DDEA 在 THEDES 中的溶解度约为 101 mg/ml,与二甲亚砜和乙醇等溶剂相比,分别提高了 10 倍和 3 倍。与商用制剂 Voltaren® Emulgel 相比,药物释放动力学得到了改善。组织病理学评估表明,该制剂未出现皮肤红斑、炎症或侵蚀迹象,证实了其生物相容性。它具有卓越的增溶能力和良好的释放动力学,同时具有很高的生物相容性,与传统的给药溶剂系统相比具有显著的优势。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Development, Characterization, and Ex Vivo Permeation Assessment of Diclofenac Diethylamine Deep Eutectic Systems Across Human Skin

Development, Characterization, and Ex Vivo Permeation Assessment of Diclofenac Diethylamine Deep Eutectic Systems Across Human Skin

Purpose

The primary aim of this study is to introduce Therapeutic Deep Eutectic Systems (THEDES) as a novel, green, and biocompatible solvent system for the delivery of diclofenac diethylamine (DDEA), a non-steroidal anti-inflammatory drug. The research question focuses on whether THEDES could significantly enhance the solubility and release kinetics of DDEA compared to conventional solvents.

Methods

The THEDES formulation comprises capric acid, menthol, and Gelucire® 33/01 in varying ratios. Techniques such as Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), rheology measurement, and contact angle tests were employed to characterize and investigate the drug solubilization process. Ex vivo permeation studies using Franz diffusion cells and human skin were conducted to assess drug release kinetics.

Results

The developed THEDES demonstrated unique molecular interactions and interfacial properties, with glass transition temperatures below − 50 °C and a broad spectrum of endothermic melting points, indicating excellent phase stability. The solubility of DDEA in THEDES was approximately 101 mg/ml, which is a tenfold and threefold increase compared to solvents like dimethyl sulfoxide and ethanol, respectively. Enhanced drug release kinetics were observed when compared with Voltaren® Emulgel, a commercial formulation. Histopathological evaluations indicated no signs of skin erythema, inflammation, or erosion, confirming the biocompatibility of the formulation.

Conclusion

THEDES emerges as a potent, green, biocompatible solvent system for efficiently delivering DDEA. It exhibits superior solubilization capacities and favorable release kinetics, coupled with high biocompatibility, offering significant advantages over traditional solvent systems for drug delivery applications.

Graphical Abstract

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来源期刊
Journal of Pharmaceutical Innovation
Journal of Pharmaceutical Innovation PHARMACOLOGY & PHARMACY-
CiteScore
3.70
自引率
3.80%
发文量
90
审稿时长
>12 weeks
期刊介绍: The Journal of Pharmaceutical Innovation (JPI), is an international, multidisciplinary peer-reviewed scientific journal dedicated to publishing high quality papers emphasizing innovative research and applied technologies within the pharmaceutical and biotechnology industries. JPI''s goal is to be the premier communication vehicle for the critical body of knowledge that is needed for scientific evolution and technical innovation, from R&D to market. Topics will fall under the following categories: Materials science, Product design, Process design, optimization, automation and control, Facilities; Information management, Regulatory policy and strategy, Supply chain developments , Education and professional development, Journal of Pharmaceutical Innovation publishes four issues a year.
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