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KMID : 0369820120420020057
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Jorunal of Korean Pharmaceutical Sciences
2012 Volume.42 No. 2 p.57 ~ p.63
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Enhanced transdermal delivery and optimization of nano-liposome preparation using hydrophilic drug
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Park Jun-Bom
Noh Hyung-Gon
Jung Jae-Hyuk
Kim Jung-Mi
Kang Chin-Yang
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Abstract
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The aim of this study is the appropriate manufacture of nano-liposome and evaluation of transdermal drug delivery after drug was loaded in liposome for topical site especially nose. To make small, stable, uniform and highly encapsulated nano-liposome, many factors including solvent, stabilizer, pH balance, homogenization speed, sonication time and filtration are critical. Especially, stearate series surfactants have positive effects on liposome size and long-term stability. In this experiment, unsaturated lecithin and Pseudoephedrine HCl (PSE) were selected for the surfactant and model drug, respectively. The unsaturated lecithin, one of the surfactants used to make the liposome, has excellent skin affinity and penetration. Tween 20 and Tween 80, support emulsifying agents, propylene glycol, a lecithin solvent and triethanolamine as stabilizer were also used as materials for liposome. Nano-liposome was made with a high shear homogenizer and pulverized by ultrasonicator to reduce the size and increase uniformity. After that, a transdermal experiment was conducted with Franz-cells on hairless mouse skin and PSE was determined by HPLC. Based on the results of the experiments, when the appropriate concentrations of support emulsifying agent and stabilizer were added, the average size of the liposome was about 300 nm and the encapsulation rate was close up to 40%. Moreover, with faster mixing speed and longer sonication time, more uniform and smaller particles tended to be manufactured. In the skin permeation test, PSE entrapped in liposome had 20 times higher permeability than PSE raw material.
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KEYWORD
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Nano-liposome, Lecithin, PSE HCl, Encapsulation rate, Transdermal test
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