Faculty of Pharmacy and Alternative Medicine, the Islamia University of Bahawalpur, Punjab, Pakistan.
College of Pharmacy, University of Sargodha, University Road Sargodha City, Punjab, Pakistan.
Life Sci. 2021 Feb 15;267:118931. doi: 10.1016/j.lfs.2020.118931. Epub 2020 Dec 30.
Aim of the study was to enhance the solubility of Chlorthalidone by developing beta-cyclodextrin cross-linked hydrophilic nanomatrices.
Nine different formulations were fabricated by free radical polymerization technique. All formulations were characterized through different studies. FTIR spectroscopy of unloaded and loaded nanomatrices was processed to determine compatibility of constituents and that of the drug with the system. Surface morphology of the nanomatrices was studied by SEM. The size of the optimized formulation was determined by zeta sizer. Swelling, in-vitro release and solubility studies were carried out in different media and results of in-vitro release profiles of nanomatrices and commercially available tablet of Chlorthalidone were compared. For determination of biocompatibility, toxicity studies were proclaimed in rabbits.
Main peaks of corresponding functional groups of individual constituents and that of drug were depicted in FTIR spectra of unloaded and loaded nanomatrices. Porous and fluffy structure was visualized through SEM images. Particle size of the optimized formulation was in the range of 175 ± 5.27 nm. Percent loading of optimized formulation showed the best result. Comparing the in-vitro drug release profiles of nanomatrices and commercially available tablet, the results of the synthesized nanomatrices were quite satisfactory. Solubility profiles were also high as compared to the drug alone. Moreover, toxicity studies confirmed that nanomatrices were biocompatible and no sign of any toxic effect was found.
We concluded that our developed nanomatrices had successfully enhanced the solubility of Chlorthalidone and can also be used for other poorly aqueous soluble drugs.
本研究旨在通过开发β-环糊精交联亲水纳米基质来提高氯噻酮的溶解度。
采用自由基聚合技术制备了 9 种不同的配方。通过不同的研究对所有配方进行了表征。对未负载和负载的纳米基质进行傅里叶变换红外光谱分析，以确定成分的相容性以及药物与系统的相容性。通过扫描电子显微镜研究纳米基质的表面形态。通过zeta 粒径仪确定优化配方的粒径。在不同的介质中进行溶胀、体外释放和溶解度研究，并比较纳米基质和市售氯噻酮片剂的体外释放曲线的结果。为了确定生物相容性，在兔子中进行了毒性研究。
未负载和负载的纳米基质的傅里叶变换红外光谱中显示了各个成分的对应功能基团的主要峰和药物的主要峰。通过 SEM 图像可以观察到多孔和蓬松的结构。优化配方的粒径在 175±5.27nm 范围内。优化配方的载药量表现出最佳结果。比较纳米基质和市售片剂的体外药物释放曲线，合成的纳米基质的结果相当令人满意。与单独的药物相比，溶解度曲线也更高。此外，毒性研究证实纳米基质具有生物相容性，没有发现任何毒性作用的迹象。
我们得出结论，我们开发的纳米基质成功地提高了氯噻酮的溶解度，并且也可用于其他水溶性差的药物。
