Protoporphyrin IX (PpIX) loaded PLGA nanoparticles for topical Photodynamic Therapy of melanoma cells

Nanoparticles (Np) can increase drug efficacy and overcome problems associated with solubility and aggregation in a solution of PpIX.

Evaluate if Np interferes in the photophysical and photobiological capacity of the PpIX comparing with free PpIX intended for topical PDT of melanoma.

In vitro photophysical evaluation of Np-PpIX was carried out through singlet oxygen (₁O²) quantum yield. In vitro cytotoxicity and phototoxicity assays have used murine melanoma cell culture.

The quantum yield of singlet oxygen has shown that Np did not influence the formation capacity of this reactive species. In the dark, all PpIX-Nps concentrations were less cytotoxic compared to free drugs. At a higher light dose (1500 mJ.cm²) 3.91 μg / mL PpIX had similar % viable cells for free and Np (∼34 %) meaning Nps did not interfere in the photodynamic effect of PpIX. However, at 7.91 μg / mL the phototoxicity increased for both (5.8 % viable cells for free versus 21.7 % for Nps). Despite the higher phototoxicity of free PpIX at this concentration, greater cytotoxicity in the dark was obtained (∼49 % viable cells for free versus ∼90.6 % Np) which means Nps protect the tumor tissue from the photodynamic action of PpIX.

Np is a potential delivery system for melanoma skin cancer, since it maintained the photophysical properties of PpIX and excellent in vitro phototoxicity effect against melanoma cells, reducing cell viability ∼80 % (7.91 μg / mL PpIX in Nps) and provides safe PDT (due to lower cytotoxicity in the dark).