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Methoxypolyethylene Glycol-Substituted Zinc Phthalocyanines for Multiple Tumor-Selective Fluorescence Imaging and
Wenzhi Wang1, Jiawen Wang1, Ge Hong1
1Tianjin Key Laboratory of Biomedical Materials, Institute of Biomedical Engineering, Chinese Academy of Medical Sciences & Peking Union Medical College, Tianjin 300192, China.
Abstract:
Highly tumor-tissue-selective drugs are a prerequisite for accurate diagnosis and efficient photodynamic therapy (PDT) of tumors, but the currently used fluorescent dyes and photosensitizers generally lack the ability for high accumulation and precise localization in tumor tissues. Here we report that monomethoxy polyethylene glycol (MPEG)-modified zinc phthalocyanine (ZnPc) can be selectively accumulated in multiple tumor tissues, and that the selectivity is controlled by the chain length of MPEG. MPEG-monosubstituted ZnPcs with different chain lengths were synthesized, among which the shorter chain (mw < 2k)-modified ZnPc did not show tumor tissue selectivity, while MPEG2k-5k-substituted ZnPc could be rapidly and selectively accumulated in H22 tumor tissues in mice after intravenous injection. Especially, MPEG4k-Pc showed the best tumor tissue selectivity with a tumor/liver (T/L) ratio of 1.7-2.2 in HepG2, MDA-MB231, AGS, and HT-29 tumor-bearing mice. It also exhibited potent photodynamic therapy effects after one PDT treatment, and tumor growth was significantly inhibited in H22-bearing mice with an inhibition rate over 98% and no obvious toxicity. Consequently, MPEG-modified ZnPc could serve as a potential platform for selective fluorescence imaging and photodynamic therapy of multiple tumors.
Insights
Monomethoxy polyethylene glycol (MPEG)-modified zinc phthalocyanine (ZnPc) shows selective tumor accumulation, controlled by MPEG chain length. This offers a promising platform for tumor imaging and photodynamic therapy (PDT) with minimal toxicity.
Area of Science:
- Materials Science
- Biomedical Engineering
- Organic Chemistry
Background:
- Accurate tumor diagnosis and effective photodynamic therapy (PDT) require drugs with high tumor-tissue selectivity.
- Current fluorescent dyes and photosensitizers often lack sufficient accumulation and precise localization in tumor tissues.
Purpose of the Study:
- To develop and evaluate monomethoxy polyethylene glycol (MPEG)-modified zinc phthalocyanine (ZnPc) for selective tumor accumulation and photodynamic therapy.
- To investigate the influence of MPEG chain length on the tumor selectivity of ZnPc derivatives.
Main Methods:
- Synthesis of MPEG-monosubstituted ZnPcs with varying chain lengths.
- Evaluation of tumor tissue selectivity in multiple tumor-bearing mouse models (HepG2, MDA-MB231, AGS, HT-29, H22) after intravenous injection.
- Assessment of photodynamic therapy efficacy and toxicity in H22 tumor-bearing mice.
Main Results:
- MPEG chain length critically controlled ZnPc tumor selectivity; shorter chains (<2k) showed no selectivity.
- MPEG2k-5k substituted ZnPc demonstrated rapid and selective accumulation in H22 tumors.
- MPEG4k-Pc exhibited the highest tumor/liver (T/L) selectivity (1.7-2.2) across multiple tumor types.
- A single PDT treatment with MPEG4k-Pc resulted in >98% tumor growth inhibition in H22 mice with no apparent toxicity.
Conclusions:
- MPEG-modified ZnPc, particularly MPEG4k-Pc, is a promising candidate for selective tumor accumulation.
- This platform enables effective photodynamic therapy and fluorescence imaging for various tumors.
- The findings highlight the potential of tailored MPEG chain length for optimizing ZnPc-based cancer treatments.
