Department of Drug Form Technology, Wroclaw Medical University, Borowska 211 A, 50-556 Wroclaw, Poland.
Department of Pharmaceutical Microbiology and Parasitology, Wroclaw Medical University, Borowska 211 A, 50-556 Wroclaw, Poland.
Mar Drugs. 2020 Nov 26;18(12):591. doi: 10.3390/md18120591.
Chitosans represent a group of multifunctional drug excipients. Here, we aimed to estimate the impact of high-molecular weight chitosan on the physicochemical properties of clotrimazole-chitosan solid mixtures (CL-CH), prepared by grinding and kneading methods. We characterised these formulas by infrared spectroscopy, differential scanning calorimetry, and powder X-ray diffractometry, and performed in vitro clotrimazole dissolution tests. Additionally, we examined the antifungal activity of clotrimazole-chitosan mixtures against clinical isolates under neutral and acid conditions. The synergistic effect of clotrimazole and chitosan S combinations was observed in tests carried out at pH 4 on strains. The inhibition of growth reached at least 90%, regardless of the drug/excipient weight ratio, and even at half of the minimal inhibitory concentrations of clotrimazole. Our results demonstrate that clotrimazole and high-molecular weight chitosan could be an effective combination in a topical antifungal formulation, as chitosan acts synergistically with clotrimazole against non-albicans candida strains.
壳聚糖是一类多功能的药物辅料。在这里，我们旨在评估高分子量壳聚糖对克霉唑-壳聚糖固体混合物（CL-CH）理化性质的影响，这些混合物是通过研磨和捏合方法制备的。我们通过红外光谱、差示扫描量热法和粉末 X 射线衍射法对这些配方进行了表征，并进行了克霉唑体外溶出度试验。此外，我们还在中性和酸性条件下，研究了克霉唑-壳聚糖混合物对临床分离株的抗真菌活性。在 pH 值为 4 的条件下进行的试验中，观察到克霉唑和壳聚糖 S 组合的协同作用。无论药物/赋形剂重量比如何，甚至达到克霉唑最小抑菌浓度的一半，对 的生长抑制均达到至少 90%。我们的研究结果表明，克霉唑和高分子量壳聚糖可作为一种有效的组合，应用于局部抗真菌制剂中，因为壳聚糖与克霉唑对非白色念珠菌具有协同作用。
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