[Synthesis of G3.5 dendrimer-2-aminoethyl ß-D-galactopyranoside conjugates and its specificity on hepatocyte targeting in vitro].
OBJECTIVE
To prepare a valuable nanodevice targeting for hepatic parenchymal cells to improve the effects of drugs for treatment of hepatitis B and liver cancer.


METHODS
Generation 3.5 dendrimer (G3.5 PAMAM) was conjugated with fluoresceine isothiocyanate (FITC) to obtain G3.5 PAMAM-FITC, which was then conjugated with 2-aminoethyl ß-D-galactopyranoside (Dgal) in different molar ratios (1:5, 1:10, 1:15, 1:20) to obtain Dgal(n)-PAMAM-FITC. Flow cytometry was applied to examine which of the molar ratios was the best.


RESULTS
Through active ester method, we got conjugates in different molar ratios of G3.5 PAMAM-FITC to Dgal (1:5, 1:10, 1:15, 1:20). Cellular entry of FITC-labeled PAMAM conjugated with different numbers of Dgal was evaluated in vitro by using rat hepatocytes with flow cytometry, and it was found that one molecule of PAMAM conjugated with 20 molecules of Dgal was the best ratio.


CONCLUSIONS
Dgal(20)-G3.5 PAMAM-FITC can be used for liver-targeting drug delivery system.
Department of Pharmacy, Peking University School of Pharmaceutical Sciences, Beijing 100191, China.
Miao
M
Zhang
Jian
J
Wang
Yong-ji
YJ
Li
Xiang-tao
XT
Wang
Xin
X
Hu
D000606:Amino Sugars / Q000737:chemistry*; D000818:Animals; D050091:Dendrimers / Q000737:chemistry*; D004337:Drug Carriers / Q000138:chemical synthesis / Q000737:chemistry; D016503:Drug Delivery Systems; D015195:Drug Design; D005434:Flow Cytometry; D022781:Hepatocytes / Q000378:metabolism*; D051381:Rats
C435776:2-aminoethyl-galactopyranosyl-(1-3')-lactoside; D000606:Amino Sugars; D050091:Dendrimers; D004337:Drug Carriers; C522260:PAMAM G3.5 dendrimer