Moussa Aalaa K, Abd El-Rahman Heba A, Mohamed Riham R, Hanna Demiana H
Chemistry Department, Faculty of Science, Cairo University, Giza 12613, Egypt.
Zoology Department, Faculty of Science, Cairo University, Giza 12613, Egypt.
Biomacromolecules. 2025 Jan 13;26(1):341-362. doi: 10.1021/acs.biomac.4c01189. Epub 2024 Dec 25.
Acyclovir (ACV) is a potentially effective antiviral medication; however, it has a serious drawback, which is its poor solubility, bioavailability, and short half-life. The goal of this study is to improve its drawbacks through the synthesis of nanogels. In this study, the cross-linked hyaluronic acid-grafted poly(acrylamide--itaconic acid) nanogel is synthesized successfully through free radical polymerization and used as a safe pH-responsive carrier for ACV. The nanogels showed pH response in vitro and in vivo. The prepared nanogel C5 (1:1 ratio of acrylamide: itaconic), which had the highest grafting efficiency, showed maximum swelling, drug loading, and release in pH 7.4, higher than pH 1.2. Also, nanogel C5, which had a large surface area, showed good stability, and its matrices shrank in acidic medium and protected the drug, while in basic medium, it expanded and released ACV in a sustained manner and improved the bioavailability and half-life of ACV in vivo.
阿昔洛韦（ACV）是一种具有潜在疗效的抗病毒药物；然而，它有一个严重的缺点，即其溶解性差、生物利用度低且半衰期短。本研究的目的是通过合成纳米凝胶来改善其缺点。在本研究中，通过自由基聚合成功合成了交联透明质酸接枝聚（丙烯酰胺-衣康酸）纳米凝胶，并将其用作ACV的安全pH响应载体。纳米凝胶在体外和体内均表现出pH响应。制备的纳米凝胶C5（丙烯酰胺：衣康酸比例为1:1）具有最高的接枝效率，在pH 7.4时表现出最大的溶胀、载药量和释放量，高于pH 1.2时。此外，具有大表面积的纳米凝胶C5表现出良好的稳定性，其基质在酸性介质中收缩并保护药物，而在碱性介质中，它膨胀并持续释放ACV，提高了ACV在体内的生物利用度和半衰期。
