Development of a nystatin nanosuspension formulation using high pressure homogenisation

制霉菌素是目前治疗口咽念珠菌病（OPC）的首选，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。的 口服给药后活性成分的生物利用度是有限的， 粪便据报道，难溶性药物的纳米化是一种有吸引力的方法，以提高其疗效 口服后。先前的出版物表明，纳米尺寸提供了一种有前途的方法， 增加局部施用制霉菌素治疗OPC的功效。前述公式 使用三种不同的纳米研磨方法筛选制霉菌素显示高压均质化 技术提供了一个更好的研磨产率比湿磨，而90%的颗粒尺寸在所获得的 悬浮液小于1.9 µm。 本项目的目标是探索制霉菌素混悬液的新剂型，以获得更好的 使用高压均质器，在颗粒尺寸和物理稳定性方面产生结果。新 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。的 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 将在制霉菌素的有前途的制剂的长期稳定性研究期间评估聚集 纳米悬浮液

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.