一种基于聚乙烯醇/丙烯酸的水凝胶用于双氯芬酸钠控释的新方法。
A Novel Approach of Polyvinyl Alcohol/Acrylic Acid Based Hydrogels for Controlled Delivery of Diclofenac Sodium.
作者信息
Suhail Muhammad, Badshah Syed Faisal, Chiu I-Hui, Ullah Arif, Khan Arshad, Ullah Hamid, Al-Sowayan Noorah Saleh, Tsai Ming-Jun, Wu Pao-Chu
机构信息
School of Pharmacy, Kaohsiung Medical University, Kaohsiung, 80708, Taiwan.
Institute of Biomedical Materials, School of Materials Science and Engineering, Zhejiang Sci-Tech University, Hangzhou, 310018, China.
出版信息
Curr Pharm Biotechnol. 2025;26(4):477-489. doi: 10.2174/0113892010296120240327055943.
AIM AND OBJECTIVE
The aim of this study was to prepare polyvinyl alcohol/acrylic acid (PVA/AA) hydrogels for the controlled release of diclofenac sodium as controlled release carriers to overcome not only the side effects of diclofenac sodium but also sustain its release for an extended period.
BACKGROUND
Diclofenac sodium is employed for relieving pain and fever. The half-life of diclofenac sodium is very short (1-2 h). Hence, multiple intakes of diclofenac sodium are required to maintain a constant pharmacological action. Multiple GI adverse effects are produced as a result of diclofenac sodium intake.
METHODS
A free radical polymerization technique was used for crosslinking PVA with AA in the presence of APS. EGDMA was used as a cross-linker. FTIR and XRD confirmed the preparation and loading of the drug by prepared hydrogels. An increase in the thermal stability of PVA was shown by TGA and DSC analysis. Surface morphology was investigated by SEM. Similarly, water penetration and drug loading were demonstrated by porosity and drug loading studies. The pH-sensitive nature of PVA/AA hydrogels was investigated at different pH values by swelling and drug release studies.
RESULTS
The development and drug loading of PVA/AA hydrogels were confirmed by FTIR and XRD analysis. TGA and DSC indicated high thermal stability of prepared hydrogels as compared to unreacted PVA. SEM indicated a hard and compact network of developed hydrogels. The swelling and drug release studies indicated maximum swelling and drug release at high pH as compared to low pH values, indicating the pH-sensitive nature of prepared hydrogels. Moreover, we demonstrated that drug release was sustained for a prolonged time in a controlled pattern by prepared hydrogels by comparing the drug release of the developed hydrogels with the commercial product Cataflam.
CONCLUSION
The results indicated that prepared PVA/AA hydrogels can be used as an alternative approach for the controlled delivery of diclofenac sodium.
目的
本研究的目的是制备聚乙烯醇/丙烯酸（PVA/AA）水凝胶，用于双氯芬酸钠的控释，作为控释载体，不仅要克服双氯芬酸钠的副作用，还要使其长时间持续释放。
背景
双氯芬酸钠用于缓解疼痛和发热。双氯芬酸钠的半衰期很短（1 - 2小时）。因此，需要多次服用双氯芬酸钠以维持恒定的药理作用。服用双氯芬酸钠会产生多种胃肠道不良反应。
方法
采用自由基聚合技术，在过硫酸铵存在下使PVA与AA交联。乙二醇二甲基丙烯酸酯用作交联剂。傅里叶变换红外光谱（FTIR）和X射线衍射（XRD）证实了所制备水凝胶对药物的制备和负载。热重分析（TGA）和差示扫描量热法（DSC）分析表明PVA的热稳定性有所提高。通过扫描电子显微镜（SEM）研究表面形态。同样，通过孔隙率和载药研究证明了水渗透和载药情况。通过溶胀和药物释放研究，在不同pH值下研究了PVA/AA水凝胶的pH敏感性。
结果
FTIR和XRD分析证实了PVA/AA水凝胶的形成和载药情况。TGA和DSC表明，与未反应的PVA相比，所制备的水凝胶具有较高的热稳定性。SEM表明所制备的水凝胶形成了坚硬而致密的网络。溶胀和药物释放研究表明，与低pH值相比，在高pH值下溶胀和药物释放最大，表明所制备的水凝胶具有pH敏感性。此外，通过将所制备水凝胶的药物释放与市售产品扶他林进行比较，我们证明所制备的水凝胶以可控方式使药物长时间持续释放。
结论
结果表明，所制备的PVA/AA水凝胶可作为双氯芬酸钠控释的替代方法。
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