A novel 2-taurine substituted hypocrellin B (THB) was designed and synthesized in this work. Both the light absorbance in the phototherapeutic window (600–900 nm) and the amphiphilicity (a compromise between the lipophilicity and hydrophilicity) were greatly improved. The semiquinone anion radical (THB˙−), superoxide anion (O2˙−), hydroxyl radical (˙OH) (Type I mechanism) and singlet oxygen (1O2) (Type II mechanism) could be generated via the photosensitization of THB, confirming its photosensitization activity. In this work, it was also found that the cytochrome c reduction method is not the exclusive one for detecting O2˙− in photosensitization systems.

This paper presents a strategy for the biofunctionalization of novel photosensitizer carriers, mesoporous silica nanoparticles (MSNs). After being calcined and absorbed with photosensitizers (hypocrellin B, HB), MSNs can be coated with a lipid layer. Transmission electron microscopy (TEM) and confocal laser scanning microscopy (CLSM) results proved that HB molecules can be loaded into MSN porous and lipid can coated on the surface of the nanoparticles. When co-cultured with cancer cells (MCF-7), MSNs can transport HB molecules into cells and present low cytotoxicity. With the introduction of a lipid layer, the efficiency of MSN uptake by cells can be improved. These intracellular HB-loaded MSN materials also present cytotoxicity to MCF-7 cells after light irradiation which indicates the materials can be used as good photosensitizer carriers in photodynamic therapy.

This paper presents a strategy for the biofunctionalization of novel photosensitizer carriers, mesoporous silica nanoparticles (MSNs). After being calcined and absorbed with photosensitizers (hypocrellin B, HB), MSNs can be coated with a lipid layer. Transmission electron microscopy (TEM) and confocal laser scanning microscopy (CLSM) results proved that HB molecules can be loaded into MSN porous and lipid can coated on the surface of the nanoparticles. When co-cultured with cancer cells (MCF-7), MSNs can transport HB molecules into cells and present low cytotoxicity. With the introduction of a lipid layer, the efficiency of MSN uptake by cells can be improved. These intracellular HB-loaded MSN materials also present cytotoxicity to MCF-7 cells after light irradiation which indicates the materials can be used as good photosensitizer carriers in photodynamic therapy.

To optimize synergistic cancer therapy, we rationally assemble an inorganic–organic nanocomplex using a folate-modified lipid bilayer spread on photosensitizer-entrapped mesoporous silica nanoparticle (MSN) coated gold nanorods (AuNRs). In this hybrid bioconjugate, the large specific surface area and pore size of AuNR@MSN guarantee a high loading capacity of small photosensitive molecules. The modification with selective mixed liposomes on the surface of AuNR@MSN enables faster cellular internalization and enhancement of endocytosis. Under one-time NIR two-photon illumination, AuNR-mediated hyperthermia can kill cancer cells directly. Meanwhile, the loaded photosensitizer, hypocrellin B, generates two kinds of reactive oxygen species (ROS) to induce cell apoptosis. Remarkably, hyperthermia can improve the yield of ROS. After intravenous injection of this bioconjugate into female BALB/c nude mice followed by laser irradiation (808 nm, 1.3 W cm−2, 6 min), the tumor growth is suppressed completely. The tumors are not recurrent within the observation time (19 days), and the normal or main organs are not obviously pathological. Thus, such a simplified and selective cancer treatment, combining photothermal and photodynamic therapy in a synergistic manner, provides outstanding efficiency in vivo. This nanocomplex with well-defined core@shell nanostructures integrated with a two-photon technique holds great promise to improve cancer phototherapy with a high efficiency in the clinic.