期刊
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
卷 26, 期 5, 页码 438-445出版社
ELSEVIER
DOI: 10.1016/j.ejps.2005.08.001
关键词
nano-emulsions; surfactants; low-energy emulsification methods; drug solubilisation
The formation of O/W nano-emulsions suitable for pharmaceutical application and the solubilisation of a practically non-water-soluble drug, lidocaine, have been studied in water/non-ionic surfactant/oil systems. Nano-emulsions were prepared by using low-energy emulsification methods, changing the composition at constant temperature. Kinetic stability was assessed by measuring droplet diameter as a function of time. Lidocaine solubilisation was studied in nano-emulsions with high water content. In the water/Cremophor EL/Miglyol 812 system the lowest droplet sizes, from 14 to 39 nm at 10/90 and 40/60 oil/surfactant ratios, respectively, and 90% of water content, were obtained with an emulsification method consisting of stepwise addition of water to oil/surfactant mixtures at 70 degrees C. Nano-emulsions of this system showed high kinetic stability. Droplet diameters did not exceed 67 nm after a period of at least 7 months. The maximum lidocaine concentration solubilised in nano-emulsions of the water/Cremophor EL/Miglyol 812 system with 90 and 95% of water content was 3.5 and 2.1%, respectively. These values are within the therapeutic range of lidocaine. (c) 2005 Elsevier B.V. All rights reserved.
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