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Current Cancer Drug Targets

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ISSN (Print): 1568-0096
ISSN (Online): 1873-5576

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Research Article

Conjugation of Phthalocyanine Photosensitizer with Poly(amidoamine) Dendrimer: Improved Solubility, Disaggregation and Photoactivity Against HepG2 Cells

Author(s): Zhou Jiang, Jiqing Ye, Jingyi Yang, Jian Wang*, Lee Jia* and Rodney JY Ho

Volume 19, Issue 4, 2019

Page: [312 - 320] Pages: 9

DOI: 10.2174/1568009618666180706164046

Price: $65

Abstract

Objective: To improve solubility and to reduce aggregation, ZnPcC4 was conjugated to a third-generation poly-amidoamine dendrimer with amino end group (G3-PAMAM-NH2), which acts as a novel photodynamic therapy (PDT) drug carrier system.

Methods: The phthalocyanines were synthesized by construction reaction. The nano drug was obtained from the conjugation of ZnPcC4 to G3-PAMAM-NH2, using EDC and NHS as coupling agents. The ZnPcC4@G3-PAMAM-NH2 conjugation was characterized by UV-Vis and MS. The 1O2 quantum yield of ZnPcC4@G3-PAMAM-NH2 in water was measured by the chemiluminescence method. The in vitro PDT responses of the studied photosensitizers were studied in hepatocellular carcinoma cell line HepG2 by MTT assay.

Results: At ZnPcC4/G3-PAMAM-NH2 raw ratio of 100/1, the ZnPcC4 conjugate had improved solubility and reduced aggregation tendency in aqueous solution. At this optimum molar ratio, ZnPcC4- G3-PAMAM-NH2 inhibited HepG2 cells, with a half-maximal inhibitory concentration of 1.67 µg/mL upon infrared light exposure. The controls, including dark conditions, or media as well as G3-PAMAM-NH2 exposure, exhibited no inhibitory response.

Conclusion: The conjugation of phthalocyanine photosensitizer ZnPcC4 to poly-amidoamine dendrimer G3-PAMAM-NH2 improved the PDT outcomes, in which the optimized binding ratio of ZnPcC4 to G3-PAMAM-NH2 was 6:1.

Keywords: Poly(amidoamine) dendrimer, tetra-carboxyl phthalocyaninato zinc, HepG2 cells, photodynamic therapy, reactive oxygen species, hepatocellular carcinoma.

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