基于 Eudragit RS-100 的伊曲康唑纳米混悬剂的设计与评价。
Design and Evaluation of Eudragit RS-100 Based Itraconazole Nanosuspension for Ophthalmic Application.
机构信息
Department of Pharmaceutics, Annasaheb Dange College of B Pharmacy, Ashta, Tal-Walwa, Dist-Sangli, MS 415301, India.
Department of Pharmaceutics (PG), Gourishankar Institute of Pharmaceutical Education & Research, Limb, NH-4, Satara, MS 415015, India.
出版信息
Curr Drug Res Rev. 2021;13(1):36-48. doi: 10.2174/2589977512666200929111952.
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 (DSC), X-ray Diffraction (XRD) analysis, viscosity, antifungal study and Transmission Electron Microscopy (TEM). Secondly, itraconazole eye drop was prepared by using sulfobuty ether-β-cyclodextrin 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.
背景
水溶性差的化合物很难通过传统的制剂技术开发成药物产品。
目的
本研究旨在探讨 Eudragit RS-100 纳米混悬剂作为一种新的药物传递载体，以提高药物向眼内水平传递的潜力。
方法
采用溶剂蒸发技术制备纳米混悬剂。采用 32因子设计优化表面活性剂浓度和药物与聚合物的比例，以获得所需的粒径、包封效率和渗透百分率作为因变量。所有制剂均进行粒径、Zeta 电位、多分散指数（PDI）、傅里叶变换红外光谱（FTIR）、差示扫描量热法（DSC）、X 射线衍射（XRD）分析、粘度、抗真菌研究和透射电子显微镜（TEM）表征。其次，采用磺丁基醚-β-环糊精制备伊曲康唑滴眼液，并比较其抗真菌效果。
结果
纳米混悬剂的粒径范围为 332.7-779.2nm，Zeta 电位+0.609-16.3，包封效率 61.32±1.36%-76.34±2.04%。体外角膜渗透研究表明，与市售制剂和伊曲康唑滴眼液相比，优化的伊曲康唑纳米混悬剂具有更高的渗透性。此外，与市售制剂和伊曲康唑滴眼液相比，优化的纳米混悬剂对白色念珠菌和黄曲霉的活性更高。
结论
纳米混悬剂方法可能是提高伊曲康唑溶解度和溶解度的理想、有前途的方法。
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