Article ID Journal Published Year Pages File Type
5550810 International Journal of Pharmaceutics 2017 14 Pages PDF
Abstract

Cutaneous melanoma is the most aggressive skin cancer and is particularly resistant to current therapeutic approaches. Photodynamic therapy (PDT) is a well-established photoprocess that is employed to treat some cancers, including non-melanoma skin cancer. Aluminum chloride phthalocyanine (ClAlPc) is used as a photosensitizer in PDT; however, its high hydrophobicity hampers its photodynamic activity under physiological conditions. The aim of this study was to produce solid lipid nanoparticles (SLN) containing ClAlPc using the direct emulsification method. ClAlPc-loaded SLNs (ClAlPc/SLNs) were characterized according to their particle size and distribution, zeta potential, morphology, encapsulation efficiency, stability, and phototoxic action in vitro in B16-F10 melanoma cells. ClAlPc/SLN had a mean diameter between 100 and 200 nm, homogeneous size distribution (polydispersity index <0.3), negative zeta potential, and spherical morphology. The encapsulation efficiency was approximately 100%. The lipid crystallinity was investigated using X-ray diffraction and differential scanning calorimetry and indicated that ClAlPc was integrated into the SLN matrix. The ClAlPc/SLN formulations maintained their physicochemical stability without expelling the drug over a 24-month period. Compared to free ClAlPc, ClAlPc/SLN exerted outstanding phototoxicity effects in vitro against melanoma cells. Therefore, our results demonstrated that the ClAlPc/SLN described in the current study has the potential for use in further preclinical and clinical trials in PDT for melanoma treatment.

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