Application of aluminum chloride phthalocyanine-loaded solid lipid nanoparticles for photodynamic inactivation of melanoma cells

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• 作者：Patrí ; cia L. Goto^a ; Marigilson P. Siqueira-Moura^b ; Antonio C. Tedesco^a ; ^c ; ^{atedesco@usp.br}
• 关键词：PDT ; photodynamic therapy ; ClAlPc ; aluminum chloride phthalocyanine ; SLN ; solid lipid nanoparticles ; ClAlPc/SLN ; ClAlPc-loaded SLN ; ROS ; reactive oxygen species ; HLB ; hydrophilic lipophilic balance ; PCS ; photon correlation spectroscopy ; PdI ; polydispersity index ; PS ; photosensitizer drug ; EE ; encapsulation efficiency ; TEM ; transmission electron microscopy ; AFM ; atomic force microscopy ; ANOVA ; analysis of variance ; CD ; crystallinity degree ; DMEM ; Dulbecco Eagle&rsquo ; s minimum essential medium ; D
• 刊名：International Journal of Pharmaceutics
• 出版年：2017
• 出版时间：25 February 2017
• 年：2017
• 卷：518
• 期：1-2
• 页码：228-241
• 全文大小：4182 K
• 卷排序：518

文摘

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.