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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 35, Number 11
BKCSDE 35(11)
November 20, 2014 

Fabrication of Compound K-loaded Polymeric Micelle System and its Characterization in vitro and Oral Absorption Enhancement in vivo
Sun-Mi Hong, Sang-ok Jeon, Jo-Eun Seo, Kyeung-Hwa Chun, Dong-Ho Oh, Young Wook Choi, Do Ik Lee, Seong Hoon Jeong, Jae Seon Kang, Sangkil Lee*
Absorption enhancement, Compound K, Ginseng saponins, Pharmacokinetics, Polymeric micelle
Compound K (CK) was formulated as polymeric micelles (PM) using Pluronic® F-127 to enhance the oral absorption of CK, an intestinal bacterial metabolite of ginseng protopanaxadiol saponin. The physicochemical properties of Ck-loaded PM were characterized and an in vitro transport study using the Caco-2 cell system as well as an in vivo pharmacokinetic study using SD rats was carried out. The hydrodynamic mean particle size of CK-loaded PM (CK-PM) was 254 ± 23.45 nm after rehydration and the drug loading efficiency was ca. 99.9%. The FT-IR spectroscopy, X-ray diffraction, differential scanning calorimetry and scanning electron microscopy data supported the presence of a new solid phase in the PM. The Papp value of in vitro Caco-2 cell permeation of CK- PM and the oral absorption of CK was enhanced about 1.2-fold and 2.6-fold compared to CK suspension, respectively, showing that the present PM formulation enabled an enhancement of oral CK absorption.
3188 - 3194
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