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《Journal of Peking University(Health Sciences)》 2010-05
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Synthesis of G3.5 dendrimer-2-aminoethylβ-D-galactopyranoside conjugates and its specificity on hepatocyte targeting in vitro

ZHANG Miao1,3,WANG Jian2,3,LI Yong-ji2,WANG Xiang-tao3,HU Xin1 (1.Department of Pharmacy,Peking University School of Pharmaceutical Sciences,Beijing 100191,China;2.Heilongjiang University of Chinese Medicine;3.The Institute of Medicinal Plant Development)  
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 β-D-galactopyranoside (Dgal) in different molar ratios (1:5,1:10,1:15,1:20) to obtain Dgaln-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 diffe-rent 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.Conclusion:Dgal20-G3.5 PAMAM-FITC can be used for liver-targeting drug delivery system.
【Fund】: 国家自然科学基金(30FF2059);; 国家重点基础研究发展计划(973计划 009CB930300)项目资助~~
【CateGory Index】: R944.9
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1 SHI Jing~1, QI Xian-rong~1*, YANG Li~1, FEI Ran~2 , WEI Lai~2(1. Department of Pharmaceutics, School of Pharmaceutical Science, Peking University, Beijing 100083, China; 2. Institute of Hepatology, People’s Hospital, Peking University, Beijing 100044, China);Liver targeting of cationic liposomes modified with soybean-derived sterylglucoside in vitro[J];Acta Pharmaceutica Sinica;2006-01
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