探索对 pH 值敏感的水凝胶海绵的潜力:用于左旋舒必利控制给药的刺参和果胶互穿网络。

IF 3.1 4区 医学 Q2 PHARMACOLOGY & PHARMACY Naunyn-Schmiedeberg's archives of pharmacology Pub Date : 2024-11-23 DOI:10.1007/s00210-024-03590-x
Muhammad Umer Ashraf, Muhammad Awais Iqbal, Kashif Barkat, Irfan Anjum, Muhammad Naveed Mushtaq, Rabia Gul, Muhammad Aamir, Samir Ibenmoussa, Ahmad Mohammad Salamatullah, Mohammed Bourhia, Gamal A Shazly, Gezahign Fentahun Wondmie
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引用次数: 0

摘要

开发能够精确控制药物释放模式的给药系统在制药领域备受关注。本研究工作探讨了一种由刺蒺藜和果胶组成的 pH 敏感互穿网络(IPN)作为载体控制左旋舒必利释放的潜力。为了提高溶解性较差的药物左旋舒必利的溶解度,β-环糊精(βCD)形成了包合物。这种 IPN 是通过绿色化学方法将水黄皮与果胶交联制备的。得到的交联聚合物网络经过重复冷冻干燥循环制备海绵状物质。利用一系列分析技术,包括傅立叶变换红外光谱(FTIR)、扫描电子显微镜(SEM)、热分析(DSC/TGA)和 X 射线衍射(XRD),对所得产品的理化性质进行了全面鉴定。在不同的 pH 值条件下,系统地评估了所开发海绵的物理参数,如溶胶-凝胶成分(%)、药物负载(%)、膨胀行为、电解质响应性和体外药物释放曲线。傅立叶变换红外光谱(FTIR)结果表明形成了交联网络,排除了药物与敷料相互作用的可能性。扫描电镜分析揭示了多孔和粗糙的几何形状。热分析证明水凝胶网络具有热稳定性,而 PXRD 则表明水凝胶海绵总体上是无定形的。物理参数结果表明,当交联剂摩尔浓度从 TP1 增加到 TP3 时,凝胶部分从 63% 增加到 85%。然而,随着角苋菜含量的增加,凝胶分数从 75%上升到 79%。而随着果胶含量的增加,凝胶部分从 79% 增加到 83%。经计算,TP3 配方的最大药物负荷为 89%。水凝胶海绵还具有电解质响应性。释放曲线显示了对 pH 值的响应行为,在 pH 值为 6.8 和 7.4 的缓冲溶液中观察到了长达 10 小时的持续释放。在酸性介质中,10 小时的溶解过程中释放了少量药物。药物释放动力学呈零序。这项研究的结果突显了角叉菜/pectin 水凝胶海绵作为一种对 pH 值敏感的载体来控制左旋舒必利给药的巨大潜力,强调了它在个性化药物治疗和胃肠道疾病治疗中的潜在应用。
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Exploring the potential of a pH-sensitive hydrogel sponge: interpenetrating network of tragacanth and pectin for controlled delivery of levosulpiride.

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.

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来源期刊
CiteScore
6.20
自引率
5.60%
发文量
142
审稿时长
4-8 weeks
期刊介绍: Naunyn-Schmiedeberg''s Archives of Pharmacology was founded in 1873 by B. Naunyn, O. Schmiedeberg and E. Klebs as Archiv für experimentelle Pathologie und Pharmakologie, is the offical journal of the German Society of Experimental and Clinical Pharmacology and Toxicology (Deutsche Gesellschaft für experimentelle und klinische Pharmakologie und Toxikologie, DGPT) and the Sphingolipid Club. The journal publishes invited reviews, original articles, short communications and meeting reports and appears monthly. Naunyn-Schmiedeberg''s Archives of Pharmacology welcomes manuscripts for consideration of publication that report new and significant information on drug action and toxicity of chemical compounds. Thus, its scope covers all fields of experimental and clinical pharmacology as well as toxicology and includes studies in the fields of neuropharmacology and cardiovascular pharmacology as well as those describing drug actions at the cellular, biochemical and molecular levels. Moreover, submission of clinical trials with healthy volunteers or patients is encouraged. Short communications provide a means for rapid publication of significant findings of current interest that represent a conceptual advance in the field.
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