International Journal of Pharmaceutics ( IF 5.3 ) Pub Date : 2023-08-10 , DOI: 10.1016/j.ijpharm.2023.123305 Aysha Aslam 1 , Muhammad Umer Ashraf 2 , Kashif Barkat 2 , Asif Mahmood 3 , Rai Muhammad Sarfraz 4 , Rania T Malatani 5 , Heba A Gad 6
The present study aims to utilize green synthesis to fabricate stimuli-responsive, smart, quince/pectin cross-linked hydrogel sponges for the pH-regulated conveyance of domperidone. The designed hydrogel sponges were evaluated for a sol–gel fraction (%), swelling studies and kinetics, drug loading (%), electrolyte-responsive character, scanning electron microscopy (SEM), thermal analysis, drug-excipient compatibility studies (FTIR), X-ray diffraction (XRD) analysis, mechanical testing, in-vitro drug release studies, and acute oral toxicity studies. The drug loading (%) ranged from 67 to 85%. Hydrogel sponges displayed pH-responsive swelling potential, with optimum swelling in a phosphate buffer (pH 7.4) and insignificant swelling in an acidic buffer of pH 1.2. The prepared hydrogel sponges displayed second-order swelling dynamics. The FTIR data revealed the successful fabrication of the hydrogel sponges with the primary drug peaks remaining unchanged, demonstrating excipients-drug compatibility. SEM confirmed the rough, porous surface of hydrogel sponges with numerous cracks. XRD measurements revealed the transformation of the crystalline nature of domperidone into an amorphous one within the developed hydrogel sponges. Dissolution studies revealed little domperidone release in an acidic environment. However, hydrogel sponges exhibited release up to 10 h in phosphate buffer. The sponge's non-toxic or biocompatible character was confirmed through toxicological studies. Thus, the finding indicates that quince/pectin cross-linked hydrogel sponges are durable enough to deliver the domperidone to the gut for a longer time.
中文翻译:
绿色合成柑橘/果胶交联超孔水凝胶海绵用于 pH 调节持续多潘立酮递送
本研究旨在利用绿色合成来制造刺激响应、智能、柑橘/果胶交联水凝胶海绵,用于调节 pH 值的多潘立酮输送。对设计的水凝胶海绵进行了溶胶-凝胶分数 (%)、溶胀研究和动力学、载药量 (%)、电解质响应特性、扫描电子显微镜 (SEM)、热分析、药物辅料相容性研究 (FTIR) 的评估、X 射线衍射 (XRD) 分析、机械测试、体外药物释放研究和急性口服毒性研究。载药量(%)范围为67%至85%。水凝胶海绵表现出 pH 响应性膨胀潜力,在磷酸盐缓冲液 (pH 7.4) 中膨胀最佳,在 pH 1.2 酸性缓冲液中膨胀不显着。制备的水凝胶海绵表现出二级溶胀动力学。FTIR 数据显示水凝胶海绵的成功制造,其主要药物峰保持不变,证明了赋形剂与药物的相容性。SEM 证实水凝胶海绵的表面粗糙、多孔,有许多裂纹。XRD 测量揭示了所开发的水凝胶海绵中多潘立酮的晶体性质转变为无定形晶体。溶出度研究表明,在酸性环境中多潘立酮释放很少。然而,水凝胶海绵在磷酸盐缓冲液中的释放时间长达 10 小时。 毒理学研究证实了海绵的无毒或生物相容性。因此,该发现表明柑橘/果胶交联水凝胶海绵足够耐用,可以将多潘立酮更长时间地输送到肠道。