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KMID : 0369820100400010039
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Jorunal of Korean Pharmaceutical Sciences
2010 Volume.40 No. 1 p.39 ~ p.43
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Preparation and Evaluation of Freeze-dried Solid Lipid Nanoparticles with Various Cryoprotectants
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Ri Hua Li
Seo Seung-Yong
Eun Jae-Soon
Lee Mi-Kyung
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Abstract
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Solid lipid nanoparticles (SLNs) were freeze-dried to obtain a stable solid dosage form with the aid of various cryoprotectants such as trehalose, sucrose, glucose, fructose, and glycerol. Tricaprin(TC) and trilaurin(TL) were used as lipid matrices for SLNs and stabilizers were egg phosphatidylcholine and pegylated phospholipid. All cryoprotectants tested did not cause changes in mean particle size of SLNs when mixed with SLNs before freeze-drying. However, the mean particle sizes of reconstituted SLNs after freeze-drying were significantly different from those of the un-lyophilized original SLN dispersions depending on the types and concentration of cryoprotectants. Although the freeze-dried SLNs without any cryoprotectants were easily reconstituted by hand-shaking, the mean particle size drastically increased (> for TC SLNs and around for TL SLNs) compared to that of un-lyophilized original dispersion (97 nm for TC SLNs and 164 nm for TL SLNs). Trehalose and sucrose were the most effective additives to protect the SLNs during lyophilization. The reconstituted SLNs were physically stable for 24 hours when lyophilized with 12.5% trehalose, sucrose, glucose, fructose or glycerol.
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KEYWORD
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solid lipid nanoparticles, tricarprin, trilaurin, freeze-drying, cryoprotectants
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