Dataset Information

Self-Amplified Photodynamic Therapy through the ¹ O₂ -Mediated Internalization of Photosensitizers from a Ppa-Bearing Block Copolymer.

ABSTRACT: Nanocarriers are employed to deliver photosensitizers for photodynamic therapy (PDT) through the enhanced penetration and retention effect, but disadvantages including the premature leakage and non-selective release of photosensitizers still exist. Herein, we report a ¹ O₂ -responsive block copolymer (POEGMA-b-P(MAA-co-VSPpaMA) to enhance PDT via the controllable release of photosensitizers. Once nanoparticles formed by the block copolymer have accumulated in a tumor and have been taken up by cancer cells, pyropheophorbide?a (Ppa) could be controllably released by singlet oxygen (¹ O₂ ) generated by light irradiation, enhancing the photosensitization. This was demonstrated by confocal laser scanning microscopy and in?vivo fluorescence imaging. The ¹ O₂ -responsiveness of POEGMA-b-P(MAA-co-VSPpaMA) block copolymer enabled the realization of self-amplified photodynamic therapy by the regulation of Ppa release using NIR illumination. This may provide a new insight into the design of precise PDT.

SUBMITTER: Liu Z

PROVIDER: S-EPMC7028480 | biostudies-literature | 2020 Feb

REPOSITORIES: biostudies-literature

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Publications

Self-Amplified Photodynamic Therapy through the 1 O2 -Mediated Internalization of Photosensitizers from a Ppa-Bearing Block Copolymer.

Liu Zhiyong Z Cao Tianye T Xue Yudong Y Li Mengting M Wu Mengsi M Engle Jonathan W JW He Qianjun Q Cai Weibo W Lan Minbo M Zhang Weian W

Angewandte Chemie (International ed. in English) 20200130 9

Nanocarriers are employed to deliver photosensitizers for photodynamic therapy (PDT) through the enhanced penetration and retention effect, but disadvantages including the premature leakage and non-selective release of photosensitizers still exist. Herein, we report a 1 O2 -responsive block copolymer (POEGMA-b-P(MAA-co-VSPpaMA) to enhance PDT via the controllable release of photosensitizers. Once nanoparticles formed by the block copolymer have accumulated in a tumor and ha ...[more]

PMID: 31808983

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Project description:There are a number of lipophilic cations that can be chosen; the triphenylphosphonium (TPP) ion is particularly unique for mitochondrion targeting, mainly due to its simplicity in structure and ease to be linked to the target molecules. In this work, mitochondrion-targeted AB3-type novel phthalocyanine and porphyrin photosensitizers (PSs) were synthesized and their photophysical photochemical properties were defined. Fluorescence quantum yields (ΦF) are 0.009, 0.14, 0.13, and 0.13, and the singlet-oxygen quantum yields (ΦΔ) are 0.27, 0.75, 0.57, and 0.58 for LuPcPox(OAc), AB 3 TPP-Pc, AB 3 TPP-Por-C4, and AB 3 TPP-Por-C6, respectively. To evaluate the photodynamic efficacy of the TPP-conjugated PS cell viabilities of A549 and BEAS-2B lung cells were comparatively measured and IC-50 values were determined. AB 3 TPP-Por-C4, AB 3 TPP-Por-C6, and AB 3 TPP-Pc compounds compared to the reference molecules ZnPc and H 2 TPP were found to be highly cytotoxic (sub-micromolar concentration) under the light. LuPcPox(OAc) is the most effective molecule regarding cell killing (the activity). The cell killing of the TPP-conjugated porphyrin derivatives exhibits a similar response compared to LuPcPox(OAc) when the light absorbing factor of the PS is normalized at 660 nm: TPP-conjugated porphyrins absorb less light (lower extinction coefficient) but produce more radical species (higher singlet-oxygen quantum yield) and therefore effectively kill the cells. The singlet oxygen-producing capacity of AB 3 TPP-Pc is almost 3 times higher compared to LuPcPox(OAc) and 50% more efficient with respect to ZnPc, suggesting that TPP-conjugated phthalocyanine may serve as a good photosensitizer for photodynamic therapy (PDT). The high singlet oxygen generation capacity of these novel TPP-conjugated porphyrin and phthalocyanine PS suggests that they might be useful for PDT requiring lower photosensitizer concentration and reduced energy deposited through less light exposure.

Dataset Information

Self-Amplified Photodynamic Therapy through the ¹ O₂ -Mediated Internalization of Photosensitizers from a Ppa-Bearing Block Copolymer.

Publications

Self-Amplified Photodynamic Therapy through the <sup>1</sup> O<sub>2</sub> -Mediated Internalization of Photosensitizers from a Ppa-Bearing Block Copolymer.

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