title: Application of aluminum chloride phthalocyanine-loaded solid lipid nanoparticles for photodynamic inactivation of melanoma cells.
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 200nm, 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.
authors.affiliation: Universidade de São Paulo, Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Departamento de Ciências Farmacêuticas, Avenida do Café, s/n°, Ribeirão Preto, SP, 14040-903, Brazil.
authors.forename: Patrícia L
authors.initials: PL
authors.lastname: Goto
authors.affiliation: Universidade Federal do Vale do São Francisco, Colegiado Acadêmico de Ciências Farmacêuticas, Avenida José de Sá Maniçoba, s/n°, Centro, Petrolina, PE, 56304-205, Brazil.
authors.forename: Marigilson P
authors.initials: MP
authors.lastname: Siqueira-Moura
authors.affiliation: Universidade de São Paulo, Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Departamento de Ciências Farmacêuticas, Avenida do Café, s/n°, Ribeirão Preto, SP, 14040-903, Brazil; Universidade de São Paulo, Faculdade de Filosofia Ciências e Letras de Ribeirão Preto, Departamento de Química, Avenida Bandeirantes, 3900, Ribeirão Preto, SP, 14040-901, Brazil. Electronic address: atedesco@usp.br.
authors.forename: Antonio C
authors.initials: AC
authors.lastname: Tedesco
mesh_terms: D000077410:Aluminum Chloride; D000818:Animals; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D007211:Indoles / Q000008:administration & dosage / Q000737:chemistry; D008055:Lipids / Q000008:administration & dosage / Q000737:chemistry; D008546:Melanoma, Experimental; D051379:Mice; D041681:NIH 3T3 Cells; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry; D009942:Organometallic Compounds / Q000008:administration & dosage / Q000737:chemistry; D010778:Photochemotherapy; D017319:Photosensitizing Agents / Q000008:administration & dosage / Q000737:chemistry; D012878:Skin Neoplasms
chemical_list: D007211:Indoles; D008055:Lipids; D009942:Organometallic Compounds; D017319:Photosensitizing Agents; C000608700:aluminum chloride phthalocyanine; D000077410:Aluminum Chloride
keywords: Aluminum chloride phthalocyanine; Direct emulsification; Glyceryl behenate; Melanoma; Photodynamic therapy; Solid lipid nanoparticles