Department of Chemistry "Ugo Schiff", University of Florence, via Schiff 6, Sesto Fiorentino, Florence, Italy.
Department of Chemistry "Ugo Schiff", University of Florence, via Schiff 6, Sesto Fiorentino, Florence, Italy.
Int J Pharm. 2021 Apr 1;598:120375. doi: 10.1016/j.ijpharm.2021.120375. Epub 2021 Feb 10.
Metronidazole is the drug of choice in the treatment of bacterial vaginosis, but the oral therapy can induce several collateral effects. Aim of this work was the development of a vaginal multiparticulate system, loaded with metronidazole, able to improve its residence time allowing a complete drug release. Several kinds of MS were prepared using chitosan dissolved in different organic acids or alginate coated with chitosan. FTIR and DSC analyses were performed to study the interactions between the drug and the polymers, while MS morphology was investigated with optical and electron microscopy. All the formulations were characterized in terms of drug entrapment efficiency, mucoadhesion, swelling capacity and drug release behavior, demonstrating the best results for alginate MS coated with chitosan. The formulations evidenced a complete and rapid release of drug, compared with the commercial form: Zidoval®.The best formulations assayed for antibacterial activity confirmed the suitability of this new formulation for the vaginal treatment of local diseases.
甲硝唑是治疗细菌性阴道病的首选药物，但口服治疗会引起多种副作用。本工作的目的是开发一种载有甲硝唑的阴道多颗粒系统，能够延长其驻留时间，实现完全药物释放。使用溶解在不同有机酸中的壳聚糖或用壳聚糖包被的藻酸盐制备了几种 MS。进行了傅里叶变换红外光谱（FTIR）和差示扫描量热法（DSC）分析，以研究药物与聚合物之间的相互作用，而 MS 形态则使用光学显微镜和电子显微镜进行了研究。所有配方均根据药物包封效率、粘膜粘附性、溶胀能力和药物释放行为进行了表征，结果表明壳聚糖包被的藻酸盐 MS 的效果最佳。与商业形式 Zidoval®相比，这些配方表现出完全快速的药物释放。对最佳配方进行的抗菌活性测试证实了这种新配方适用于阴道局部疾病的治疗。
