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KMID : 0369820060360060355
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Jorunal of Korean Pharmaceutical Sciences
2006 Volume.36 No. 6 p.355 ~ p.361
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Preparation of Dexamethasone-21-palmitate Incorporated Lipid Nanosphere : Physical Properties by Varying Components 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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Intraarticular corticisteroid injections for therapy of rheumatic arthritis are administred with the aim of optimal local anti-inflammatory effect at the injection site. Since the side effects of cirticosteroidal drug, dexamethasone (DEX), administered at high dose limited the therapeutic eficacy, there was a need to design a new drug delivery system for controlled release of dexamethasone. as a prodrug for continuous therapeutic efficacy, dexamethasone-21-palmitate (DEX-PAL) was prepared via esterification of palmitoyl chloride and dexabethasone. DEX-PAL was identified by NMR and MASS analysis. DEX-PAL or DEX was entrapped in lipid nanosphere which could be prepared by using a self emulsification-solvent evaporation method. Physicochemical characteristics such as mean particle diameter, zeta potential and drug loading efficiency of the lipid nanosphere had a mean diameter 83~95 nm and DEX-PAL loading efficiency of up to 95%. The drug loading efficiency increased with the increase of alophatic chain length attached to the phospholipid. The incorporation of cationic lipid was very efficient for both reducing particle size of lipid nanospheres and enhancing drug loading efficiency. The lipid nanosphere containing DEX-PAL may be a promising novel drug carrier for the comtrolled release of the poorly water-soluble drugs.
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KEYWORD
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Dexamethasone-21-palmitate(DEX-PAL), Lipid Nanosphere, Controlled release formulation
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