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抗氧化化合物水溶性改善的当前技术及其与活性的相关性：分子药剂学

Current Techniques of Water Solubility Improvement for Antioxidant Compounds and Their Correlation with Its Activity: Molecular Pharmaceutics.

作者信息

Budiman Arif, Rusdin Agus, Aulifa Diah Lia

机构信息

Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Universitas Padjadjaran, Bandung 45363, Indonesia.

Department of Pharmaceutical Analysis and Medicinal Chemistry, Faculty of Pharmacy, Universitas Padjadjaran, Bandung 45363, Indonesia.

出版信息

Antioxidants (Basel). 2023 Feb 4;12(2):378. doi: 10.3390/antiox12020378.

DOI:10.3390/antiox12020378
PMID:36829937
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9952677/
Abstract

The aqueous solubility of a drug is important in the oral formulation because the drug can be absorbed from intestinal sites after being dissolved in the gastrointestinal fluid, leading to its bioavailability. Almost 80% of active pharmaceutical ingredients are poorly water-soluble, including antioxidant compounds. This makes antioxidant activity inefficient in preventing disease, particularly for orally administered formulations. Although several investigations have been carried out to improve the solubility of antioxidant compounds, there is still limited research fully discussing the subject. Therefore, this study aimed to provide an overview and discussion of the issues related to the methods that have been used to improve the solubility and activity of antioxidant compounds. Articles were found using the keywords "antioxidant" and "water solubility improvement" in the Scopus, PubMed, and Google Scholar databases. The selected articles were published within the last five years to ensure all information was up-to-date with the same objectives. The most popular methods of the strategies employed were solid dispersion, co-amorphous, and nanoparticle drug delivery systems, which were used to enhance the solubility of antioxidant compounds. These investigations produced impressive results, with a detailed discussion of the mechanism of improvement in the solubility and antioxidant activity of the compounds developed. This review shows that the strategies used to increase the solubility of antioxidant compounds successfully improved their antioxidant activity with enhanced free radical scavenging abilities.

摘要

药物的水溶性在口服制剂中很重要，因为药物溶解于胃肠液后可从肠道部位吸收，从而影响其生物利用度。几乎80%的活性药物成分水溶性较差，包括抗氧化化合物。这使得抗氧化活性在预防疾病方面效率低下，尤其是对于口服制剂而言。尽管已经进行了多项研究来提高抗氧化化合物的溶解度，但全面讨论该主题的研究仍然有限。因此，本研究旨在概述和讨论与用于提高抗氧化化合物溶解度和活性的方法相关的问题。在Scopus、PubMed和谷歌学术数据库中使用关键词“抗氧化剂”和“提高水溶性”搜索文章。所选文章发表于过去五年内，以确保所有信息都与相同目标相关且最新。所采用策略中最常用的方法是固体分散体、共无定形和纳米颗粒药物递送系统，它们被用于提高抗氧化化合物的溶解度。这些研究取得了令人瞩目的成果，并对所开发化合物溶解度和抗氧化活性的改善机制进行了详细讨论。本综述表明，用于提高抗氧化化合物溶解度的策略成功提高了它们的抗氧化活性，并增强了自由基清除能力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2947/9952677/9815535a4470/antioxidants-12-00378-g011.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2947/9952677/fe77bb2409ec/antioxidants-12-00378-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2947/9952677/72e0a6dfbccf/antioxidants-12-00378-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2947/9952677/9815535a4470/antioxidants-12-00378-g011.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2947/9952677/1a6a4782011b/antioxidants-12-00378-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2947/9952677/2fc0f6fddf00/antioxidants-12-00378-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2947/9952677/d48d4672fa62/antioxidants-12-00378-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2947/9952677/0d4cc1e4def3/antioxidants-12-00378-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2947/9952677/fe77bb2409ec/antioxidants-12-00378-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2947/9952677/72e0a6dfbccf/antioxidants-12-00378-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2947/9952677/9815535a4470/antioxidants-12-00378-g011.jpg

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