Development of a nystatin nanosuspension formulation using high pressure homogenisation

使用高压均质化开发制霉菌素纳米混悬剂制剂

• 批准号: 486974-2015
• 负责人: Leclair, Grégoire
• 金额: $ 0.91万
• 依托单位: Université de Montréal
• 依托单位国家: 加拿大
• 项目类别: Engage Plus Grants Program
• 财政年份: 2015
• 资助国家: 加拿大
• 起止时间: 2015-01-01 至 2016-12-31
• 项目状态: 已结题
• 来源: https://www.nserc-crsng.gc.ca/ase-oro/Details-Detailles_eng.asp?id=585870
• 关键词: Development; nystatin; nanosuspension; formulation; using

Nystatin is the current treatment of choice for Oropharyngeal candidiasis (OPC), a common fungal infection of the oral cavity. Poorly soluble nystatin is formulated as a suspension intended for local application. The bioavailability of the active ingredient after oral administration is limited and principally eliminated in the faeces. Nanosizing of poorly soluble drugs has been reported as an attractive approach to improve their efficacy after oral administration. A previous publication showed that nanosizing provides a promising approach to increasing the efficacy of topically administered nystatin in the treatment of OPC. A foregoing formulation screening of nystatin using three different nanomilling processes showed that high pressure homogenisation technique offered a better milling yield than the wet milling while the size of 90% of particles in the obtained suspension were smaller than 1.9 µm. The goal of the present project is to explore new formulations of nystatin suspension in order to obtain better results in terms of particle size and physical stability, using the high pressure homogeniser. The new formulations will be compared with the commercial nystatin suspension milled in the same conditions. The chemical stability, the physicochemical stability, the presence of residual contamination and the nanoparticle aggregation will be assessed during the long-term stability study of the promising formulation of nystatin nanosuspension.

制霉菌素是目前治疗口咽部念珠菌病 (OPC) 的首选治疗方法，OPC 是一种常见的真菌感染 口腔。难溶性制霉菌素被配制成用于局部应用的悬浮液。这 口服给药后活性成分的生物利用度有限，并且基本上在体内消除 粪便。据报道，难溶性药物的纳米化是提高其疗效的一种有吸引力的方法 口服给药后。先前的出版物表明，纳米尺寸提供了一种有前途的方法 提高局部施用制霉菌素治疗 OPC 的疗效。上述配方 使用三种不同的纳米研磨工艺筛选制霉菌素表明，高压均质化 技术提供了比湿磨更好的研磨产率，同时获得的颗粒中 90% 的尺寸 悬浮液小于 1.9 µm。 本项目的目标是探索制霉菌素混悬剂的新剂型，以获得更好的效果。 使用高压均质器获得粒径和物理稳定性方面的结果。新的 将制剂与在相同条件下研磨的商业制霉菌素悬浮液进行比较。这 化学稳定性、物理化学稳定性、残留污染物的存在和纳米颗粒 将在有前景的制霉菌素制剂的长期稳定性研究过程中评估聚集情况 纳米悬浮液。