Abstract
BODIPY dyes have recently attracted attention as potential photosensitizers. In this work, commercial and novel photosensitizers (PSs) based on BODIPY chromophores (haloBODIPYs and orthogonal dimers strategically designed with intense bands in the blue, green or red region of the visible spectra and high singlet oxygen production) were covalently linked to mesoporous silica nanoparticles (MSNs) further functionalized with PEG and folic acid (FA). MSNs approximately 50 nm in size with different functional groups were synthesized to allow multiple alternatives of PS-PEG-FA decoration of their external surface. Different combinations varying the type of PS (commercial Rose Bengal, Thionine and Chlorine e6 or custom-made BODIPY-based), the linkage design, and the length of PEG are detailed. All the nanosystems were physicochemically characterized (morphology, diameter, size distribution and PS loaded amount) and photophysically studied (absorption capacity, fluorescence efficiency, and singlet oxygen production) in suspension. For the most promising PS-PEG-FA silica nanoplatforms, the biocompatibility in dark conditions and the phototoxicity under suitable irradiation wavelengths (blue, green, or red) at regulated light doses (10–15 J/cm2) were compared with PSs free in solution in HeLa cells in vitro.
Highlights
Several alternatives are used to treat cancer, including surgery and chemo, radio- or immune-therapy, depending on the type of cancer an effective method has not been found yet
Mesoporous silica nanoparticles with a suitable size for medical applications and for Photodynamic Therapy (PDT) [98,106] were synthesized by the modified Stöber method [107] as described elsewhere [105]
The latter type was obtained after conversion of CN-mesoporous silica nanoparticles (MSNs) in acidic conditions, according to the synthesis route described in Materials and methods section and Supporting Material
Summary
Several alternatives are used to treat cancer, including surgery and chemo, radio- or immune-therapy, depending on the type of cancer an effective method has not been found yet. In this regard, Photodynamic Therapy (PDT) is a complementary treatment that can be applied as a combined therapy to enhance anticancer efficiency by a synergic or additive effect with conventional methods. PDT is considered a less invasive and more precise treatment (locally controlled by the light irradiation of malignant tissue), without inducing long-term side effects, and it has a lower cost with respect to other treatments. Despite there being several PSs approved by the FDA, most of them are hydrophobic and/or tend to have poor selectivity to malignant tissues [6,7,8,9]
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