伏立康唑负载固体脂质纳米颗粒眼科应用的设计与评价。

Journal of drug delivery Pub Date : 2016-01-01 Epub Date: 2016-05-12 DOI:10.1155/2016/6590361
Anubha Khare, Inderbir Singh, Pravin Pawar, Kanchan Grover
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引用次数: 51

摘要

伏立康唑是第二代抗真菌药物,具有良好的广谱抗真菌活性,可用于口服和静脉注射。全身给药伏立康唑有副作用,包括视觉和肝脏异常。本研究以硬脂酸为脂质材料,tween 80为稳定剂,Carbopol 934为控释剂,评估了固体脂质纳米颗粒用于voriconazole眼部给药的可行性,并增加了voriconazole在眼内角膜前停留时间。采用超声法和微乳液法制备了两种不同的体系。结果表明:微乳法制备的SLN粒径(308±3.52 nm ~ 343±3.51 nm)比超声法制备的SLN粒径(234±3.52 nm ~ 288±4.58 nm)大;两种方法制备的多分散性指数均小于0.3,zeta电位变化范围为-22.71±0.63 mV ~ -28.86±0.58 mV。粉末x射线衍射和差示扫描量热法显示药物结晶度降低。体外释放研究和超声法制备的SLN制剂均显示缓释达12小时。本研究表明,超声法制备SLN比微乳液法制备SLN更合适,且对角膜水化水平无明显影响。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Design and Evaluation of Voriconazole Loaded Solid Lipid Nanoparticles for Ophthalmic Application.

Design and Evaluation of Voriconazole Loaded Solid Lipid Nanoparticles for Ophthalmic Application.

Design and Evaluation of Voriconazole Loaded Solid Lipid Nanoparticles for Ophthalmic Application.

Design and Evaluation of Voriconazole Loaded Solid Lipid Nanoparticles for Ophthalmic Application.

Voriconazole is a second-generation antifungal agent with excellent broad spectrum of antifungal activity commercially available for oral and intravenous administration. Systemic administration of voriconazole is associated with side effects including visual and hepatic abnormalities. This study assessed the feasibility of using solid lipid nanoparticles for ocular delivery of voriconazole adopting stearic acid as lipidic material, tween 80 as a stabilizer, and Carbopol 934 as controlled release agent and for increasing the precorneal residence time in eye. The systems were prepared using two different methods, that is, ultrasonication method and microemulsion technique. The results indicated that the larger particle size of SLNs was found with microemulsion technique (308 ± 3.52 nm to 343 ± 3.51) compared to SLN prepared with ultrasonication method (234 ± 3.52 nm to 288 ± 4.58 nm). The polydispersity index values were less than 0.3 for all formulations and zeta potential of the prepared formulations by these two methods varied from -22.71 ± 0.63 mV to -28.86 ± 0.58 mV. Powder X-ray diffraction and differential scanning calorimetry indicated decrease in crystallinity of drug. The in vitro release study and the SLN formulations prepared with ultrasonication method demonstrated sustained release up to 12 hours. This study demonstrated that SLN prepared by ultrasonication method is more suitable than microemulsion technique without causing any significant effect on corneal hydration level.

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来源期刊
Journal of drug delivery
Journal of drug delivery PHARMACOLOGY & PHARMACY-
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