Organic small-molecule
photosensitizers are well-characterized
and known for the light-responsive treatment modality including photodynamic
therapy. Compared with ultraviolet–visible (UV–vis)
light used in conventional photodynamic therapy with organic photosensitizers,
near-infrared (NIR) light from 700 to 900 nm is less absorbed and
scattered by biological tissue such as hemoglobin, lipids, and water,
and thus, the use of NIR excitation can greatly increase the penetration
depth and emission. Additionally, NIR light has lower energy than
UV–vis that can be beneficial due to less activation of fluorophores
present in tissues upon NIR irradiation. However, the low water stability,
nonspecific distribution, and short circulation half-life of the organic
photosensitizers limit its broad biological application. NIR responsive
small-molecule fluorescent agents are the focus of extensive research
for combined molecular imaging and hyperthermia. Recently a new class
of NIR dye, IR-820 with excitation and emission wavelengths of 710
and 820 nm, has been developed and explored as an alternative platform
to overcome some of the limitations of the most commonly used gold
nanoparticles for photothermal therapy of cancer. Herein, we synthesized
a core–shell biocompatible nanocarrier envelope made up of
a phospholipid conjugated with poly(ethylene glycol) as a shell, while
poly(lactic glycolic acid) (PLGA) was used as a core to encapsulate
IR-820 dye. The IR-820-loaded nanoparticles were prepared by nanoprecipitation
and characterized for their physicochemical properties and photothermal
efficiency. These nanoparticles were monodispersed and highly stable
in physiological pH with the hydrodynamic size of 103 ± 8 nm
and polydispersity index of 0.163 ± 0.031. The IR-820-loaded
nanocarrier showed excellent biocompatibility in the dark, whereas
remarkable phototoxicity was observed with breast cancer cells (MCF-7)
upon NIR laser excitation. Therefore, the IR-820-loaded phospholipid
mimicking biodegradable lipid-polymer composite nanoparticles could
have great potential for cancer theranostics.