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Aggregation control of phthalocyanines via Tween 20 micelles for improved photodynamic cytotoxicity
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DOI：10.1016/j.rechem.2026.103254.png)
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Abstract
En 中文
Photodynamic therapy (PDT) is a promising modality for selective cancer treatment; however, aggregation of hydrophobic photosensitizers in aqueous environments often leads to fluorescence quenching, reduced reactive oxygen species (ROS) generation, and diminished photocytotoxicity. In this study, we designed a micellar delivery system based on Tween 20, a biocompatible nonionic surfactant composed of a polyoxyethylene hydrophilic chain and a sorbitan ester-derived hydrophobic moiety, to optimize the photochemical performance of phthalocyanine photosensitizers. The micellar hydrophobic core was intended to encapsulate the photo-sensitizer through hydrophobic interactions and pi-pi stacking, thereby suppressing aggregation, while the hydrated polyoxyethylene shell provided steric stabilization and minimized nonspecific biological interactions. This core-shell architecture was designed to maintain the photosensitizer in a monomeric or weakly associated state, enabling efficient photoactivation and singlet oxygen generation. Photocytotoxicity toward HeLa cells was evaluated using the MTT assay. Micellized ZnPc-OH exhibited significantly enhanced light-induced cytotoxicity at 0.08 and 0.16 mg mL-1 compared with non-irradiated controls, whereas micellized ZnBuPc-OH showed only concentration-dependent cytotoxicity without a clear light-dependent effect. These findings indicate that the optimized Tween 20 micellar environment facilitates efficient ROS generation, suitable micellar encapsulation, and favorable cellular uptake/localization for ZnPc-OH, thereby preserving photocytotoxic activity. Overall, this study demonstrates that rational micellar design can mitigate aggregation-induced deactivation of hydrophobic photosensitizers and represents a viable strategy for improving PDT efficacy.
Keywords:
DRUG-DELIVERY
PHOTOSENSITIZERS
PORPHYRIN
Journal
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4.2
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506
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