纳米结构树枝状聚合物可提高卡维地洛、呋塞米和尼莫地平的溶解度

Jigar V. Patel, V. Patel, Pravinkumar M. Patel
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引用次数: 0

摘要

使用利尿剂和β-受体阻滞剂治疗原发性高血压已有 30 多年的历史。在治疗心力衰竭方面,目前使用的β-受体阻滞剂有三代。卡维地洛(Carvedilol)是第三代受体阻滞剂。尼莫地平是一种常见的 L 型钙通道阻滞剂。高血压药物呋塞米是一种襻利尿剂。这类药物在水中的低溶解度已成为制药业寻求更好治疗方法的严重障碍。最近,一类名为树枝状聚合物的新型聚合物因其令人印象深刻的增溶特性而备受关注。本文展示的新型纳米结构树枝状聚合物的溶血研究和细胞毒性测试结果表明,与市售的 PAMAM 树枝状聚合物相比,合成树枝状大分子的性能更优越。树枝状聚合物用于提高尼莫地平、呋塞米和卡维地洛的溶解度,使其分别达到 38.08µg/ml、70.999µg/ml 和 147.065µg/ml。树枝状聚合物介导溶解度的提高主要取决于树枝状聚合物的浓度和生成大小等因素。含有树枝状聚合物的药物可使用傅立叶变换红外光谱进行研究。根据这项研究的结果,纳米结构树枝状聚合物技术可能有助于疏水性药物的分散。
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Nanostructured dendrimer improves the solubility of carvedilol, furosemide and nimodipine
Essential hypertension has been treated for over 30 years using both diuretics and beta-blockers. When it comes to treating heart failure, there are three different generations of beta-blockers that are now in use. Carvedilol is a blocker from the third generation. Nimodipine is a common L-type calcium channel blocker. The hypertension medication furosemide is a loop diuretic. This class of medications' low solubility in water has emerged as a serious obstacle in the pharmaceutical industry's pursuit of better treatments. A novel class of polymers called dendrimers has recently gained a lot of interest due to its impressive solubility-enhancing characteristics. Results from hemolysis studies and cytotoxicity tests using the novel nanostructure dendrimer shown here demonstrate superior performance of synthetic dendritic macromolecules compared to commercially available PAMAM dendrimer. Dendrimers are used to enhance the solubility of nimodipine, furosemide, and carvedilol up to 38.08µg/ml, 70.999µg/ml and 147.065µg/ml respectively. The enhancement of dendrimer-mediated solubility is primarily determined by factors such as dendrimer concentration and generation size. Drugs containing dendrimers may be studied using Fourier-transform infrared spectroscopy. Based on the results of this investigation, nanostructured dendrimer technology may help with hydrophobic medication dispersion.
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