Zhengqi Zha,Yinghua Miao,Huiling Tang,Daniela D. Herrera-Balandrano,Hongping Yin,Su-Yan Wang
Zinc(II) phthalocyanine (ZnPc) is a promising photosensitizer in photodynamic therapy (PDT) for melanoma treatment. However, the poor solubility of ZnPc limits its application. To overcome this limitation, heparosan (HP)-based nanoparticles were prepared by anchoring the l -lysine-linked α-linolenic acid branch to the carboxylic acid group to produce amphiphilic conjugates named heparosan with an l -lysine-linked α-linolenic acid branch (HLA). HLA conjugates could self-assemble into spherical nanoparticles in aqueous media and encapsulate ZnPc to form HLA-ZnPc nanoparticles. The cellular uptake of ZnPc could be improved by HLA carriers. These nanoparticles presented excellent photodynamic-mediated toxicity against mouse melanoma cells (B16) by markedly upregulating the intracellular reactive oxygen species (ROS) levels while showing no cytotoxicity to either B16 or normal cells (L02 and HK-2 cells) in the dark. Furthermore, HLA-ZnPc displayed excellent stability in both powder and Roswell Park Memorial Institute (RPMI) 1640 medium, indicating its promise for application in drug delivery and PDT. These results revealed a strategy for HP-based enhancement of ZnPc in PDT efficacy.
Phthalocyanines are potentially promising photosensitizers (PSs) for photodynamic therapy (PDT), but the inherent defects such as aggregation-caused quenching effects and non-specific toxicity severely hinder their further application in PDT. Herein, we synthesized two zinc(II) phthalocyanines (PcSA and PcOA) monosubstituted with a sulphonate group in the alpha position with “O bridge” and “S bridge” as bonds and prepared a liposomal nanophotosensitizer ([email protected]) by thin-film hydration method to regulate the aggregation of PcSA in the aqueous solution and enhance its tumor targeting ability.[email protected]exhibited highly efficient production of superoxide radical (O2∙−) and singlet oxygen (1O2) in water under light irradiation, which were 2.6-fold and 15.4-fold higher than those of free PcSA, respectively. Furthermore,[email protected]was able to accumulate selectively in tumors after intravenous injection with the fluorescence intensity ratio of tumors to livers was 4.1:1. The significant tumor inhibition effects resulted in a 98% tumor inhibition rate after[email protected]was injected intravenously at an ultra-low[email protected]dose (0.8 nmol g−1PcSA) and light dose (30 J cm−2). Therefore, the liposomal[email protected]is a prospective nanophotosensitizer possessing hybrid type I and type II photoreactions with efficient photodynamic anticancer effects.Keywords:photodynamic therapy;phthalocyanine;liposome;fluorescence imaging;anticancer
Min He,Yidong Bin,Lixian Huang,Caiying Li,Yuzhen Ma,Yan-Ni Luo,Shulin Zhao,Jinzhe Liang
In this work, novel zinc(II) phthalocyanine nanoparticles (ZnPcNPs) have been developed and verified to be a promising PTT agent in NIR-I range. Owing to the superior photostability, ZnPcNPs possess a high PCE of 30.01% under 660 nm NIR-I laser exposure. ZnPcNPs with strong adsorption in NIR-I biowindow, photothermal-enhanced cell death and single oxygen formation ability can function as an efficient diagnosis-treatment nanoprobe, thus accelerating the malignant breast cancer cell death. In vitro and in vivo findings verify that ZnPcNPs endow with suitable biosafety, superior photothermal therapeutic efficacy, and outstanding PA imaging performance. Taken together, ZnPcNP-mediated photothermal-enhanced PDT can be used for synergistic bimodal theranostics in future biomedical uses.
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