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KMID : 1146920180480050595
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Journal of Pharmaceutical Investigation
2018 Volume.48 No. 5 p.595 ~ p.601
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Improvement of cellular uptake of hydrophilic molecule, calcein, formulated by liposome
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Han Su-Min
Na Young-Guk
Lee Han-Sol
Son Gi-Ho
Jeon Seong-Hoon
Bang Ki-Hyun
Kim Sung-Jin
Lee Hye-Jin
Cho Cheong-Weon
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Abstract
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The aim of this study was to prepare the liposome with 1,2-distearoyl-sn-glycero-3-phosphocholine, 1.2 dioleoyl-sn-glycero-3-phosphoethanolamine, cholesteyl hemisuccinate, calcein as a drug model and evaluate physicochemical characteristics such as particle size, polydispersity index (PDI), encapsulation efficiency (EE). Also, the morphology of the blank liposome (without calcein) and the calcein-loaded liposome was observed by a transmission electron microscope (TEM). The particle size and PDI of the blank liposome and the calcein-loaded liposome without tween 80 were 139.8?±?4.497, 0.31?±?0.03 and 150.8?±?8.45, 0.29?±?0.03 nm, respectively. In addition, it was confirmed that the particle size of the calcein-loaded liposome increased from 294. 6?±?17.8 to 466.4?±?78.4 nm when tween 80 was used from 1 to 6%. EE of the calcein-loaded liposome was 66.0?±?0.58%, independent of the concentration of tween 80. TEM images showed that the shape of the blank liposome and the calcein-loaded liposome was round. In vitro drug release test, calcein from the liposome released approximately 20?25 and 40?50% in pH 7.4 and 4.0, respectively, with a sustained release pattern. The cellular uptake of calcein from the calcein-loaded liposome was about 1.08-fold than that from the calcein solution at 10 μM for a 2 h incubation time. These results suggest that the calcein-loaded liposome was successfully prepared, and could be an application for a hydrophilic drug in further study.
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KEYWORD
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Liposome, Tween 80, Cellular uptake, Calcein, In vitro release
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