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Design and Evaluation of Eudragit RS-100 Based Itraconazole Nanosus-pension for Ophthalmic Application

机译:设计和评价Eudragit基于rs - 100的伊曲康唑Nanosus-pension眼科应用程序

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Background: Poor water soluble compounds are difficult to develop as drug products using conventional formulation techniques.Objective: In the present study, the potential of Eudragit RS-100 nanosuspension as a new vehicle for the improvement of the delivery of drugs to the intraocular level was investigated.Methods: Solvent evaporation technique has been employed for nanosuspension preparation. Surfactant concentration and drug to polymer ratio has been optimized using 32 factorial design to achieve desired particle size, entrapment efficiency and percent permeation responses as dependent variables. All the formulations were characterized for particle size, zeta potential, polydispersity index (PDI), Fourier Transform Infrared Spectroscopy (FTIR), Differential scanning calorimetery (D-SC), X-ray Diffraction (XRD) analysis, viscosity, antifungal study and Transmission Electron Microscopy (TEM). Secondly, itraconazole eye drop was prepared by using sulfobuty ether-P-cy-clodextrin and comparatively studying its antifungal efficacy.Results: The nanosuspension had a particle size range of 332.7-779.2nm, zeta potential +0.609-16.3, entrapment efficiency 61.32 ± 1.36%-76.34 ± 2.04%. Ex vitro corneal permeability study showed that optimized itraconazole nanosuspension produced higher permeation as compared to the market formulation and Itraconazole eye drop. Moreover, optimized nanosuspension was found as more active against Candida albicans & Aspergillus flavus compared to the market formulation and Itraconazole eye drop.Conclusion: The nanosuspension approach could be an ideal, promising approach to increase the solubility and dissolution of Itraconazole.
机译:背景:可怜的水溶性化合物难以开发药物产品使用传统配方技术。目前的研究中,Eudragit的潜力rs - 100 nanosuspension的新车提高药物的交付眼内水平调查。一直采用溶剂蒸发技术nanosuspension准备。浓度和药物聚合物比例优化使用32的阶乘设计实现所需的粒度、截留效率和渗透反应百分比依赖变量。粒度特征,电动电势,多分散性指数(PDI),傅里叶变换红外光谱(FTIR)、差扫描calorimetery (D-SC), x射线衍射(XRD)分析、粘度、抗真菌研究透射电子显微镜(TEM)。伊曲康唑滴眼剂是通过使用准备的sulfobuty ether-P-cy-clodextrin和相对研究其抗菌功效。nanosuspension的粒径范围332.7 - -779.2 nm,电动电势+ 0.609 - -16.3,截留效率61.32±-76.34±1.36%2.04%。,优化伊曲康唑nanosuspension产生更高的渗透比市场制定和伊曲康唑滴眼剂。此外,优化nanosuspension被发现对白色念珠菌和更活跃黄曲霉相比市场制定和伊曲康唑滴眼剂。nanosuspension方法可能是一个理想,有前途的方法来增加溶解度和伊曲康唑的解散。

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