Galactosylated fluorescent labeled micelles as a liver targeting drug carrier.
Galactosylated and fluorescein isothiocyanate (FITC) labeled polycaprolactone-g-dextran (Gal-PCL-g-Dex-FITC) polymers were synthesized. The grafted polymers can self-assemble into stable micelles in aqueous medium and in serum. Transmission electron microscopy (TEM) images showed that the self-assembled micelles were regularly spherical in shape. Micelle size determined by size analysis was around 120 nm. The anti-inflammation drug prednisone acetate as a model drug was loaded in the polymeric micelles, and the in vitro drug release was investigated. The galactosylated micelles could be selectively recognized by HepG2 cells and subsequently accumulate in HepG2 cells. The in vivo study demonstrated the relative uptake of the micelles by liver is much higher than the other tissues, indicating that the galactosylated micelles have great potential as a liver targeting drug carrier.
Wu
De-Qun
DQ
Key Laboratory of Biomedical Polymers of Ministry of Education, Department of Chemistry, Wuhan University, Wuhan 430072, China.
Lu
Bo
B
Chang
Cong
C
Chen
Chang-Sheng
CS
Wang
Tao
T
Zhang
Yuan-Yuan
YY
Cheng
Si-Xue
SX
Jiang
Xue-Jun
XJ
Zhang
Xian-Zheng
XZ
Zhuo
Ren-Xi
RX
D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000378:metabolism; D001672:Biocompatible Materials / Q000737:chemistry / Q000378:metabolism; D002460:Cell Line; D003911:Dextrans / Q000737:chemistry; D004187:Disaccharides / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry / Q000378:metabolism; D016503:Drug Delivery Systems; D005029:Ethylenediamines / Q000737:chemistry; D016650:Fluorescein-5-isothiocyanate / Q000031:analogs & derivatives / Q000737:chemistry; D005456:Fluorescent Dyes / Q000737:chemistry / Q000378:metabolism; D005690:Galactose / Q000737:chemistry*; D006801:Humans; D008099:Liver / Q000378:metabolism* / Q000648:ultrastructure; D008422:Materials Testing; D008823:Micelles; D015394:Molecular Structure; D010316:Particle Size; D011108:Polymers / Q000737:chemistry*; D011241:Prednisone / Q000737:chemistry / Q000378:metabolism; D014018:Tissue Distribution
D000893:Anti-Inflammatory Agents; D001672:Biocompatible Materials; D003911:Dextrans; D004187:Disaccharides; D004337:Drug Carriers; D005029:Ethylenediamines; D005456:Fluorescent Dyes; D008823:Micelles; D011108:Polymers; C015219:fluorescein isothiocyanate dextran; C031234:ethylenediamine; C005608:lactobionic acid; D016650:Fluorescein-5-isothiocyanate; D011241:Prednisone; D005690:Galactose