Encapsulation of Hydrophobic Porphyrins into Biocompatible Nanoparticles: An Easy Way to Benefit of Their Two-Photon Phototherapeutic Effect without Hydrophilic Functionalization

Simple Summary Efficient photosensitizers for photodyanmic therapy (PDT) need to be soluble in physiologic media. This requirement often complicates significantly the chemical access to such compounds, resulting in lower availability and higher production costs for the best representatives. Given that their screening and selection is often initially conducted in organic media from series of hydrophobic model compounds, the possibility to use directly such hydrophobic photosensitizers in real PDT studies was highly desirable to speed up their definitive identification but also to alleviate their cost. In this respect, PMLABe polymeric nanoparticles (NPs) were presently probed as nanocarriers to water-solubilize hydophobic star-shaped porphyrin-based which turned out to be promising oxygen photosensitizers for theranostic approaches. We show here that PDT conducted using such NPs loaded with these compounds is as efficient than when functional hydrosoluble analogues of these photosensitiers are tested alone and that tracking of the photosensitizer by fluorescence imaging is even easier. Star-shaped hydrophobic porphyrins, acting as powerful fluorescent two-photon photosensitizers for oxygen in organic solvents, can easily be loaded into PMLABe polymeric nanoparticles at various concentrations. In this contribution, the performance of these porphyrin-containing nanoparticles in terms of photodynamic therapy (PDT) is compared to those of the corresponding water-soluble porphyrin analogues when irradiated in MCF-7 cancer cells. While quite promising results are obtained for performing PDT with these nanoparticles, validating this approach as a mean for using more easily accessible and less expensive photosensitizers, from a synthetic perspective, we also show that their luminescence can still be used for bioimaging purposes in spite of their confinement in the nanoparticles, validating also the use of these nano-objects for theranostic purposes.

Automated summary

In this study, we successfully transformed hydrophobic star-shaped porphyrin-based photosensitizers into water-soluble ones by loading them into PMLABe polymeric nanoparticles. The nanoparticles loaded with these photosensitizers showed equivalent efficiency in photodynamic therapy as the water-soluble analogues, and the fluorescence imaging for tracking the photosensitizers was even easier.