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用于芥子酸的自纳米乳化药物递送系统的开发与评价，其对严重急性呼吸综合征冠状病毒2（SARS-CoV-2）具有增强的抗病毒功效

Development and Evaluation of a Self-Nanoemulsifying Drug Delivery System for Sinapic Acid with Improved Antiviral Efficacy against SARS-CoV-2.

作者信息

Alhadrami Hani A, El-Din Ahmed S G Srag, Hassan Hossam M, Sayed Ahmed M, Alhadrami Albaraa H, Rateb Mostafa E, Naguib Demiana M

机构信息

Faculty of Applied Medical Sciences, Department of Medical Laboratory Technology, King Abdulaziz University, P.O. Box 80402, Jeddah 21589, Saudi Arabia.

King Fahd Medical Research Centre, King Abdulaziz University, P.O. Box 80402, Jeddah 21589, Saudi Arabia.

出版信息

Pharmaceutics. 2023 Oct 25;15(11):2531. doi: 10.3390/pharmaceutics15112531.

DOI:10.3390/pharmaceutics15112531
PMID:38004511
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10674535/
Abstract

This study aimed to develop a self-nanoemulsifying drug delivery system (SNE) for sinapic acid (SA) to improve its solubility and antiviral activity. Optimal components for the SA-SNE formulation were selected, including Labrafil as the oil, Cremophor EL as the surfactant, and Transcutol as the co-surfactant. The formulation was optimized using surface response design, and the optimized SA-SNE formulation exhibited a small globule size of 83.6 nm, high solubility up to 127.1 ± 3.3, and a 100% transmittance. In vitro release studies demonstrated rapid and high SA release from the formulation. Pharmacokinetic analysis showed improved bioavailability by 2.43 times, and the optimized SA-SNE formulation exhibited potent antiviral activity against SARS-CoV-2. The developed SA-SNE formulation can enhance SA's therapeutic efficacy by improving its solubility, bioavailability, and antiviral activity. Further in silico, modeling, and Gaussian accelerated molecular dynamics (aMD)-based studies revealed that SA could interact with and inhibit the viral main protease (M). This research contributes to developing effective drug delivery systems for poorly soluble drugs like SA, opening new possibilities for their application via nebulization in SARS-CoV-2 therapy.

摘要

本研究旨在开发一种用于芥子酸（SA）的自纳米乳化药物递送系统（SNE），以提高其溶解度和抗病毒活性。选择了SA - SNE制剂的最佳成分，包括Labrafil作为油相、聚氧乙烯蓖麻油（Cremophor EL）作为表面活性剂以及二乙二醇单乙醚（Transcutol）作为助表面活性剂。使用表面响应设计对制剂进行优化，优化后的SA - SNE制剂呈现出83.6 nm的小球径、高达127.1±3.3的高溶解度以及100%的透光率。体外释放研究表明制剂中SA释放迅速且量大。药代动力学分析显示生物利用度提高了2.43倍，并且优化后的SA - SNE制剂对严重急性呼吸综合征冠状病毒2（SARS-CoV-2）表现出强效抗病毒活性。所开发的SA - SNE制剂可通过提高SA的溶解度、生物利用度和抗病毒活性来增强其治疗效果。进一步的计算机模拟、建模以及基于高斯加速分子动力学（aMD）的研究表明，SA可与病毒主要蛋白酶（M）相互作用并抑制该酶。本研究有助于为SA等难溶性药物开发有效的药物递送系统，为其在SARS-CoV-2治疗中通过雾化给药的应用开辟新的可能性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/67db/10674535/4760b85726b9/pharmaceutics-15-02531-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/67db/10674535/d49f1b1cc53f/pharmaceutics-15-02531-g001.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/67db/10674535/ddad85245926/pharmaceutics-15-02531-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/67db/10674535/631a51a96924/pharmaceutics-15-02531-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/67db/10674535/0ce3a8eb8e47/pharmaceutics-15-02531-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/67db/10674535/d2461b5bd2d6/pharmaceutics-15-02531-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/67db/10674535/2ff0ed643da1/pharmaceutics-15-02531-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/67db/10674535/51bd035e4d90/pharmaceutics-15-02531-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/67db/10674535/1e79fe176075/pharmaceutics-15-02531-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/67db/10674535/d62d68e7d086/pharmaceutics-15-02531-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/67db/10674535/4760b85726b9/pharmaceutics-15-02531-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/67db/10674535/d49f1b1cc53f/pharmaceutics-15-02531-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/67db/10674535/bf7f7c3a5f5f/pharmaceutics-15-02531-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/67db/10674535/ddad85245926/pharmaceutics-15-02531-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/67db/10674535/631a51a96924/pharmaceutics-15-02531-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/67db/10674535/0ce3a8eb8e47/pharmaceutics-15-02531-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/67db/10674535/d2461b5bd2d6/pharmaceutics-15-02531-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/67db/10674535/2ff0ed643da1/pharmaceutics-15-02531-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/67db/10674535/51bd035e4d90/pharmaceutics-15-02531-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/67db/10674535/1e79fe176075/pharmaceutics-15-02531-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/67db/10674535/d62d68e7d086/pharmaceutics-15-02531-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/67db/10674535/4760b85726b9/pharmaceutics-15-02531-g011.jpg

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