基于海藻酸钠的快速溶胀纳米凝胶用于提高氯酞酮的溶解度;合成、表征和生物安全性评价。

Syed Faisal Badshah, Orva Abdullah, Kifayat Ullah Khan, Abid Hussain, Muhammad Mukhtiar, Kashif Barkat, Nasrullah Jan, Samiullah Khan, Muhammad Aamir, Huma Liaqat, Yasir Mehmood, Abdul Jabbar, Maham Waqar, Tehreem Khanum
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引用次数: 0

摘要

氯塞酮是一种溶解性很差的利尿剂,过去半个世纪以来一直被用于降低高血压。约 90% 的候选药物都面临溶解性问题。氯塞酮是 BCS IV 类药物,其溶解性较差,需要加以改进,以优化其疗效。利用自由基聚合技术,配制了海藻酸钠基纳米凝胶,以提高氯塞酮的溶解度。通过结构表征、药物负载、溶胀、溶胶-凝胶转变、体外释放、溶解度和毒性测试,对纳米凝胶的各种特性进行了评估。傅立叶变换红外光谱(FT-IR)显示了主要原材料和聚合物纳米凝胶的特征峰。氯塞酮负载纳米凝胶的傅立叶变换红外光谱显示出离散的药物峰,证实了药物负载的成功。粉末 X 射线衍射仪和热分析表明了该系统的无定形性质和热稳定性。扫描电子显微镜显示了清晰的多孔结构。纳米凝胶的粒度通过 zeta 粒度分析测定为 189 ±18.35 n.m。所制备的生物相容性纳米凝胶可用于提高疏水性药物的溶解度。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Sodium alginate based fast swelling nanogels for solubility enhancement of chlorthalidone; synthesis, characterization and biosafety evaluation.

Purpose of the study was to enhance the solubility of Chlorthalidone, poorly soluble diuretic that has been the used for lowering high blood pressure for the past half-century. Solubility is a challenge for approximately 90 % of drug candidates. Chlorthalidone is BCS Class IV drug whose poor solubility needs to be improved in order to optimize its efficacy. Using a free radical polymerization technique, sodium alginate-based nanogels were formulated for enhancing solubility of Chlorthalidone. The evaluation of various characteristics of nanogels was done by structural characterization, drug loading, swelling, sol-gel transition, in-vitro release, solubility, and toxicity tests. Fourier transform infrared spectroscopy (FT-IR) revealed characteristic peaks of the primary raw materials and polymeric nanogels. The FT-IR spectra of the Chlorthalidone-loaded nanogels suggested discrete drug peaks confirming successful drug loading. The system's amorphous nature and thermal stability were indicated by powder X-ray diffractometry and thermal analysis. The scanning electron microscopy indicated a well-defined porous structure. The size of the nanogels was determined by zeta size analysis to be 189 ±18.35 n.m. The solubility enhancement factor demonstrated the potential for improved solubility of the poorly soluble drug. The resulting biocompatible nanogels could be used to improve the solubility of hydrophobic drugs.

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