Fabrication of Compound K-loaded Polymeric Micelle System and its Characterization in vitro and Oral Absorption Enhancement in vivo

Bulletin of the Korean chemical society

Sangkil Lee¹  Jae Seon Kang¹  Sang-ok Jeon¹  Sun-Mi Hong¹  Kyeung-Hwa Chun¹  Seong Hoon Jeong¹  Dong-Ho Oh¹  Jo-Eun Seo¹  Do Ik Lee¹  Young Wook Choi¹ 

关键词: Absorption enhancement;    Compound K;    Ginseng saponins;    Pharmacokinetics;    Polymeric micelle;   

DOI  :  

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

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.

【 授权许可】

Unknown