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采用新型喷雾干燥工艺对水不溶性药物进行纳米和微粒工程处理。

Nano and microparticle engineering of water insoluble drugs using a novel spray-drying process.

机构信息

BÜCHI Labortechnik AG, Meierseggstrasse 40, 9230 Flawil, Switzerland.

出版信息

Colloids Surf B Biointerfaces. 2012 Feb 1;90:8-15. doi: 10.1016/j.colsurfb.2011.09.038. Epub 2011 Oct 4.

Abstract

In the current study nano and microparticle engineering of water insoluble drugs was conducted using a novel piezoelectric spray-drying approach. Cyclosporin A (CyA) and dexamethasone (DEX) were encapsulated in biodegradable poly(D,L-lactide-co-glycolide) (PLGA) grades of different molecular weights. Spray-drying studies carried out with the Nano Spray Dryer B-90 employed with piezoelectric driven actuator. The processing parameters including inlet temperature, spray mesh diameter, sample flow rate, spray rate, applied pressure and sample concentration were examined in order to optimize the particle size and the obtained yield. The process parameters and the solute concentration showed a profound effect on the particle engineering and the obtained product yield. The produced powder presented consistent and reproducible spherical particles with narrow particle size distribution. Cyclosporin was found to be molecularly dispersed while dexamethasone was in crystalline state within the PLGA nanoparticles. Further evaluation revealed excellent drug loading, encapsulation efficiency and production yield. In vitro studies demonstrated sustained release patterns for the active substances. This novel spray-drying process proved to be efficient for nano and microparticle engineering of water insoluble active substances.

摘要

在当前的研究中,使用新型压电喷雾干燥方法对水不溶性药物的纳米和微粒工程进行了研究。环孢素 A(CyA)和地塞米松(DEX)被包封在可生物降解的聚(D,L-丙交酯-共-乙交酯)(PLGA)不同分子量的等级中。使用压电驱动执行器的 Nano Spray Dryer B-90 进行喷雾干燥研究。为了优化粒径和获得的产率,考察了包括入口温度、喷雾网孔直径、样品流速、喷雾速率、施加压力和样品浓度在内的加工参数。加工参数和溶质浓度对颗粒工程和获得的产品产率有深远的影响。所生产的粉末呈现出一致且可重复的球形颗粒,具有较窄的粒径分布。环孢素以分子形式分散,而地塞米松则以结晶状态存在于 PLGA 纳米颗粒中。进一步的评估显示出优异的药物负载、包封效率和生产产率。体外研究表明活性物质具有持续释放的模式。这种新型喷雾干燥工艺被证明对水不溶性活性物质的纳米和微粒工程有效。

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