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.

Conclusion: Dgal(20)-G3.5 PAMAM-FITC can be used for liver-targeting drug delivery system.

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