聚乙二醇6000和蜂蜡制备氯霉唑微粒

Kobra Najafzadeh Mahvizani, Marjan Daeihamed, Gita Alkan Saberi, Z. Hesari
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引用次数: 0

摘要

微颗粒是一种用于药物长时间缓释和控制释放的药物传递系统。克霉唑是一种广谱抗真菌药物,通常用于治疗白色念珠菌和其他真菌感染。目的采用蜂蜡(亲脂涂层)和聚乙二醇(亲水涂层)制备氯霉唑微粒。方法采用喷雾干燥技术,以聚乙二醇(PEG 6000)和蜂蜡为原料制备氯霉唑微粒。使用光学显微镜和扫描电镜对微颗粒的形态和大小进行了评估。采用Zetasizer技术进行粒度分析。紫外-可见光谱法测定药物释放率。利用傅里叶变换红外光谱(FTIR)研究微粒子与载体之间的相互作用。结果微颗粒粒径均在1000µm以下。由蜂蜡和peg6000制备的微粒子分别具有准晶和结晶形态。F3(蜂蜡制备的微颗粒)和F6 (PEG 6000制备的微颗粒)在6 h内的最大药物释放率分别为80.53%和79.29。FTIR结果显示,氯霉唑微粒可能与蜂蜡发生相互作用。结论蜂蜡与peg6000聚合物的释药速率相近;然而,由于蜂蜡与氯霉唑有相互作用,PEG 600配方似乎更适合于制造氯霉唑微粒。
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Fabrication of Clotrimazole Microparticles Using Polyethylene Glycol 6000 and Beeswax
Background Microparticles are one of drug delivery systems designed for sustained and controlled release of drugs for a long period of time. Clotrimazole is a broad-spectrum antifungal agent, which is generally used for treatment of Candida albicans and others fungal infections. Objective The present study aims to fabricate Clotrimazole microparticles using beeswax (lipophilic coating) and polyethylene glycol (hydrophilic coating). Methods In this study, Clotrimazole microparticles by polyethylene glycol (PEG 6000) and beeswax were prepared using spray drying technique. Morphology and size of the microparticles were assessed using optical microscopy and scanning electron microscopy. Particle size analyses were performed using Zetasizer technique. The drug release rate was measured using ultraviolet-visible spectroscopy. To study the interactions between microparticles and carriers, Fourier transform infrared spectroscopy (FTIR) was used. Results Size of the microparticles was below 1000 µm. The microparticles prepared from beeswax and PEG 6000 had quasicrystalline and crystalline morphologies, respectively. The maximum drug release rate in 6 hours was 80.53% in formulation F3 (microparticles prepared by beeswax) and 79.29 in formulation F6 (microparticles prepared by PEG 6000). The FTIR results showed probable interactions between clotrimazole microparticles and beeswax. Conclusion Both beeswax and PEG 6000 polymers result in similar rate of drug release; however, since beeswax has interactions with clotrimazole, PEG 600 formulation seems to be more appropriate for fabrication of clotrimazole microparticles.
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