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Synthesis and Photodynamic Efficacy of PAMAM-Photosensitiser Conjugates in Vitro

C.L. Peng, P.S. Lai, C.H. Chiu, C.C. Chang, T.-Y. Lai and M.J. Shieh
National Taiwan University, TW

Keywords:
photodynamic therapy, polymer-durg conjugate, polyamidoamine dendrimer

Abstract:
Starburst polyamidoamine (PAMAM) dendrimer is a new class of highly branched spherical polymer. Covalent attachment of porphyrin to PAMAM dendrimer may alter the pharmacokinetics, cell targeting, and photophysical properties of photosensitizer. We investigated the uptake, localization, and phototoxicity of PAMAM-porphyrin conjugate with different charges and hydrophobicity in Hela cell lines. The cellular uptake of PAMAM-porphyrin conjugate for HeLa cells was much higher than that of native porphyrin. PAMAM-porphyrin conjugate was accumulated in the endosomal/lysosomal compartments in HeLa cells, and with more effective photocytotoxity after irradiation. The hydrophobic porphyrin conjugated to PAMAM became less aggregation, more cellular uptake, and lysosomal targeting that could be applied on photosensitizer delivery system in clinical cancer therapy.

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