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KMID : 1059520060500060464
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Journal of the Korean Chemical Society
2006 Volume.50 No. 6 p.464 ~ p.470
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Preparation of the Dexamethasone-incorporated Lipid Nanosphere: Characteristics of Lipid Nanosphere by Varying Species and Ratio of Lipid
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Jung Suk-Hyun
Lee Jung-Eun
Seong Ha-soo
Shin Byung-Cheol
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Abstract
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Though the coricosteroid drug dexamethasone is an efficacious antiinflammatory drug, it is difficult to formulate in an injectable formulation due to its poor aqueous solubility. A lipid-based nanosphere formulation containing dexamethasone was designed for solubilization of the drug in aqueous solution and sustained release of the drug from the nanosphere. The lipid nanospheres, composed of phospholipid, cholesterol and cationic lipid, were prepared by self emulsification-solvent diffusion method followed by diafiltration. Physicochemical characteristics such as mean particle diameter, zeta potential and drug loading efficiency of the lipid nanospheres were investigated according to the variation of either the kind of lipid or the lipid composition. The lipid nanospheres had a mean diameter 80-120 nm and dexamethasone loading efficiency of greater than 80%. The drug loading efficiency increased with the increase of the length of aliphatic chain attached to the phospholipid. However, the drug loading efficiency was inversely proportional to the increase of cholesterol content in the lipid composition. The lipid nanosphere could not be prepared without the use of cationic lipid and the drug loading efficiency was proportional to the increase of cationic lipid content. The lipid nanospheres containing dexamethasone are a promising novel drug carrier for an injectable formulation of the poorly water-soluble drugs.
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KEYWORD
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Lipid Nanosphere, Spontaneous Emulsification-solvent Diffusion, Poorly Water-soluble Drug, Dexamethasone
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