Ashraf Muhammad Umer, Iqbal Muhammad Awais, Barkat Kashif, Anjum Irfan, Mushtaq Muhammad Naveed, Gul Rabia, Aamir Muhammad, Ibenmoussa Samir, Salamatullah Ahmad Mohammad, Bourhia Mohammed, Shazly Gamal A, Wondmie Gezahign Fentahun
Faculty of Pharmacy, The University of Lahore, Lahore, Pakistan.
Faculty of Sciences, Equator University of Science and Technology, Masaka, Uganda.
Naunyn Schmiedebergs Arch Pharmacol. 2025 May;398(5):5579-5592. doi: 10.1007/s00210-024-03590-x. Epub 2024 Nov 23.
The development of drug delivery systems that allow precise control over drug release pattern has fetched significant attention in the pharmaceutical field. This research work investigates the potential of a pH-sensitive interpenetrating network (IPN) composed of tragacanth and pectin as a carrier for the controlled release of levosulpiride. To enhance the solubility of poorly soluble drug levosulpiride, inclusion complexes were formed with beta cyclodextrin (βCD). The IPN was prepared by cross-linking tragacanth with pectin by adopting a green chemistry approach. The resulting cross-linked polymeric network was subjected to repetitive freeze-drying cycles for preparation of spongy mass. The physicochemical properties of the resultant product were thoroughly characterized using a range of analytical techniques, including Fourier-transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), thermal analyses (DSC/TGA), and X-ray diffraction (XRD). The physical parameters like sol-gel fraction (%), drug loading (%), swelling behavior, electrolyte responsiveness, and in vitro drug release profile of the developed sponge were systematically evaluated under varying pH conditions. Results of FTIR demonstrated the formation of cross-linked network, ruling out drug-excipient interaction. SEM analysis unveiled porous and rough geometry. Thermal analyses proved the hydrogel network thermally stable whereas, PXRD demonstrated the overall amorphous nature of the hydrogel sponge. The outcomes of physical parameters demonstrated an incremental trend in gel fraction from 63 to 85% on raising the molar concentration of cross-linker from TP1 to TP3. However, increasing tragacanth content escalation in gel fraction from 75 to 79% was noticed. While gel fraction was augmented from 79 to 83% with increasing pectin contents. The maximum drug loading formulation TP3 was computed to be 89%. Hydrogel sponges also demonstrated electrolyte responsiveness. The release profile indicated a pH-responsive behavior, with sustained release up to 10 h observed in a buffer solution of pH 6.8 and 7.4. In an acidic medium, a minor amount of drug was released during 10 h dissolution. Drug release kinetics was observed to be in zero order. The findings of this study highlight the promising potential of the tragacanth/pectin hydrogel sponge as a pH-sensitive dais for the controlled delivery of levosulpiride, emphasizing its potential application in personalized drug therapy and the treatment of gastrointestinal disorders.
能够精确控制药物释放模式的药物递送系统的开发在制药领域引起了广泛关注。本研究工作考察了由黄芪胶和果胶组成的pH敏感互穿网络(IPN)作为左舒必利控释载体的潜力。为提高难溶性药物左舒必利的溶解度,将其与β-环糊精(βCD)形成包合物。采用绿色化学方法,通过将黄芪胶与果胶交联制备IPN。将所得的交联聚合物网络进行反复冷冻干燥循环以制备海绵状物质。使用一系列分析技术,包括傅里叶变换红外光谱(FTIR)、扫描电子显微镜(SEM)、热分析(DSC/TGA)和X射线衍射(XRD),对所得产品的物理化学性质进行了全面表征。在不同pH条件下,系统地评估了所制备海绵的物理参数,如溶胶-凝胶分数(%)、载药量(%)、溶胀行为、电解质响应性和体外药物释放曲线。FTIR结果表明形成了交联网络,排除了药物-辅料相互作用。SEM分析揭示了多孔且粗糙的几何形状。热分析证明水凝胶网络具有热稳定性,而PXRD表明水凝胶海绵整体为无定形性质。物理参数结果表明,将交联剂的摩尔浓度从TP1提高到TP3时,凝胶分数从63%增加到85%呈递增趋势。然而,随着黄芪胶含量增加,凝胶分数从75%增加到79%。随着果胶含量增加,凝胶分数从79%增加到83%。计算得出最大载药配方TP3为89%。水凝胶海绵也表现出电解质响应性。释放曲线表明具有pH响应行为,在pH 6.8和7.4的缓冲溶液中观察到长达10小时的持续释放。在酸性介质中,10小时溶解过程中释放少量药物。观察到药物释放动力学为零级。本研究结果突出了黄芪胶/果胶水凝胶海绵作为左舒必利控释的pH敏感平台的潜在前景,强调了其在个性化药物治疗和胃肠道疾病治疗中的潜在应用。