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INNOSC Theranostics and
Pharmacological Sciences The biochemical and biophysical guide for photodynamic therapy

promoting the degradation of the nanopreparations. This Zinc(III)-dipicolylamine di-iodo-BODIPY is a
degradation facilitates the release of DOX into the cell chemical complex that has attracted significant interest
nucleus, thereby enabling the combined action of PDT and due to its unique properties and potential applications in
chemotherapy. In conclusion, these micelles can serve as various scientific and technological fields. This compound,
nanocarriers for chemotherapeutic drugs such as DOX, which consists of a zinc atom, dipicolylamine, and
thus enabling a dual treatment approach of photodynamic di-iodine BODIPY, represents an innovative combination
and chemotherapeutic anticancer treatment. The in coordination chemistry.
synthesized water-soluble BODIPY dyes, designated 24 These properties make zinc(III)-dipicolylamine
and 25, modified with PEG, showed improved solubility di-iodo-BODIPY highly useful in nanotechnology, where
and fluorescence quantum yield in water while minimizing it can be employed to construct nanomaterials with
the tendency to aggregate. 37 specific properties. Moreover, the compound’s fluorescent

BODIPY conjugates 24 and 25 demonstrated no toxicity capabilities open up applications in biochemistry, enabling
to MCF-7 cells at low concentrations for 24 h. These the tracking of cells and chemicals in living organisms.
dyes were permeable to MCF-7 cells and accumulated In medical diagnostics, this complex can be utilized
in the cytoplasm, as confirmed by confocal microscopy. for tissue imaging, contributing to the advancement of
These findings highlight the promising potential of these modern diagnostic techniques. Its unique properties make
conjugates for use in fluorescence bioimaging. 38 it valuable across emerging fields of science, advancing
progress in optical materials, nanotechnology, cell biology,
By combining the modified BODIPY with hydrophilic
PEG, the amphipathic polymer PEG-BODIPY 26 was and medical diagnostics. Furthermore, its ability to
interact with metal ions allows for use in ion recognition
synthesized, exhibiting effective PDT capabilities with and separation processes, which are applied in various
“favorable” phototoxicity against HepG2 and 4T1 cell branches of chemistry. Its fluorescence also enables
lines. Amphiphilic macromolecules 26 can self-assemble precise tracking of biological processes at the cellular
into micelles of appropriate size, allowing for long-term level, which is critical for analyzing disease mechanisms
circulation in the body and targeted accumulation in tumor and molecular interactions. The compound’s ability to
sites. Polymer PEG-BODIPY 26 functions both as a PS and enhance contrast can help identify pathological changes
as a fluorescent probe, presenting excellent therapeutic and at early stages, a crucial factor for effective diagnosis
imaging properties in vitro and in vivo. and treatment. Moreover, this compound has potential
Aza-BODIPYs are structural analogs of organic applications in optical sensors, where its responsiveness
dyes from the group of 4,4-difluoro-4-bora-3a,4a- to specific chemicals or ions can facilitate the detection
diaza-s-indacenes (i.e., BODIPY), known for their high and monitoring of various chemical processes. Recent
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fluorescence quantum yield, photostability, and absorption advancements in PDT utilizing nanotechnology, including
and emission properties. These compounds exhibit the use of quantum dots as innovative PSs or energy donors,
absorption and emission across the visible light to near- along with the combination of PDT with radiotherapy
infrared spectrum. Some aza-BODIPY derivatives also and immunotherapy, represent promising future
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contain photosensitizing groups. Photosensitization is a approaches for cancer treatment. The incorporation of
process in which a PS absorbs light and transfers energy PSs into conjugated polymer NPs has proven beneficial
1
to another substance, inducing a chemical or physical by improving O formation through effective energy
2
reaction. These derivatives are employed in PDT for transfer. The evolution of nanotechnology has emerged
cancer treatment, using their ability to generate reactive as a promising avenue for enhancing the performance
oxygen species under light exposure. In medicine, of existing PSs and overcoming significant challenges in
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photosensitization is most commonly associated with PDT. cancer PDT. In addition, silicon phthalocyanines are
Tetraaryl aza-BODIPY, a derivative that serves as the basis recognized as suitable PSs for PDT due to their ability to
1
for constructing a PS, exhibits absorption properties within generate O with a long triplet lifetime. 43
2
the therapeutic window, ensuring effective treatment while
minimizing toxicity and side effects. Due to the presence of 10. Future clinical prospects of PDT
a heavy atom, this compound can efficiently generate O . Convincing clinicians and experienced doctors to adopt
1
2
Another effective PS used in PDT is the biotin-conjugated PDT in clinical practice remains challenging due to
aza-BODIPY derivative, obtained through Sonogashira the ongoing development of this treatment in cancer
coupling. This modification increases the compound’s therapy. Treatment regimens still require optimization
affinity for cancer cells, making it more effective compared and standardization to ensure improved therapeutic
to other PSs. 39 efficacy. Moreover, unfavorable side effects have been

Volume 8 Issue 2 (2025) 27 doi: 10.36922/itps.4559