Hypericin (Hyp) is considered a promising photosensitizer for Photodynamic Therapy (PDT), due to its high hydrophobicity, affinity for cell membranes, low toxicity and high photooxidation activity. In this study, Hyp photophysical properties and photodynamic activity against melanoma B16-F10 cells were optimized using DPPC liposomes (1,2-dipalmitoyl-sn-glycero-3-phosphocholine) as a drug delivery system. This nanoparticle is used as a cell membrane biomimetic model and solubilizes hydrophobic drugs. Hyp oxygen singlet lifetime (τ) in DPPC was approximately two-fold larger than that in P-123 micelles (Pluronic™ surfactants), reflecting a more hydrophobic environment provided by the DPPC liposome. On the other hand, singlet oxygen quantum yield values (Φ_Δ ¹O₂) in DPPC and P-123 were similar; Hyp molecules were preserved as monomers. The Hyp/DPPC liposome aqueous dispersion was stable during fluorescence emission and the liposome diameter remained stable for at least five days at 30 °C. However, the liposomes collapsed after the lyophilization/rehydration process, which was resolved by adding the lyoprotectant Trehalose to the liposome dispersion before lyophilization. Cell viability of the Hyp/DPPC formulation was assessed against healthy HaCat cells and high-metastatic melanoma B16-F10 cells. Hyp incorporated into the DPPC carrier presented a higher selectivity index than the Hyp sample previously solubilized in ethanol under the illumination effect. Moreover, the IC₅₀ was lower for Hyp in DPPC than for Hyp pre-solubilized in ethanol. These results indicate the potential of the formulation of Hyp/DPPC for future biomedical applications in PDT treatment.

Chagas is a parasitic endemic disease caused by the protozoan Trypanosoma cruzi. It represents a strong threat to public health due to its strong resistance against commonly available drugs. We studied the in vitro ability to inactivate the trypomastigote form of this parasite using photodynamic inactivation of microorganisms (or antimicrobial Photodynamic Therapy, aPDT). For this, we chose to use the photosensitizer hypericin (Hyp) formulated in ethanol/water (1% v/v) and Hyp loaded in the dispersion of different aqueous nanocarrier systems. These included polymeric micelles of F-127 and P-123 (both Pluronic™ surfactants), and liposomal vesicles of phospholipid 2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC). These systems with Hyp had their activity compared against trypomastigote forms under light and in the dark. Hyp revealed a high level of effectiveness to eradicate protozoa in vitro. Samples at concentrations higher than 0.8 μmol L⁻¹ of Hyp in Pluronic micelles showed efficacy even in the dark, with the EC₅₀ around (6–8) μmol L⁻¹. Therefore, Hyp/Pluronics can be used also as a chemotherapeutic agent. The best result for EC₅₀ is at approximately 0.31 μmol L⁻¹ for illuminated systems of Hyp in F-127 micelles. For Hyp in P-123 micelles under light, the results also led to a low EC₅₀ value of 0.36 μmol L⁻¹. The highest value of EC₅₀ was 2.22 μmol L⁻¹, which was found for Hyp/DPPC liposomes under light. For the Hyp-free (ethanol/water, 1% v/v)/illuminated group, the EC₅₀ value was 0.37 μmol L⁻¹, which also is a value that shows effectiveness. However, in free-form, Hyp is not protected against blood components, unlike when Hyp is loaded into the nanocarriers.