RESUMEN
Aims: Develop and analyze triple-negative breast cancer targeted nanoparticles loaded with the demethylating agent decitabine. Materials & methods: The polymers were synthesized by ring-opening polymerization of D,L-lactide and formulated into nanoparticles via emulsion-evaporation method. The nanoparticles were characterized by physicochemical analysis as well as in vitro using breast cancer cell lineages. Results & conclusion: The targeted nanoparticles exhibited a hydrodynamic diameter of 75 ± 12 nm, zeta potential -6.3 ± 0.2 mV and spherical morphology, and displayed greater in vitro accumulation into MDA-MB-231 (triple-negative breast cancer cell-line) compared with MCF7 and HB4A cell lineages as verified by fluorescence confocal microscopy and significant demethylating effects via ADAM33 screening by PCR.
Asunto(s)
Neoplasias de la Mama , Nanopartículas , Neoplasias de la Mama Triple Negativas , Humanos , Femenino , Neoplasias de la Mama Triple Negativas/tratamiento farmacológico , Neoplasias de la Mama Triple Negativas/genética , Epigénesis Genética , Ligandos , Línea Celular Tumoral , Nanopartículas/química , Proteínas ADAMRESUMEN
Sixteen porphyrins, including neutral, anionic and cationic meso-(aryl)porphyrins and meso-(1-methyl-4-pyridinium)porphyrins were herein evaluated in terms of their photosensitizing properties against HaCaT keratinocytes. After an initial screening, the cationic porphyrins were studied in more details, by both determining their log POW and performing PDT assays in lower porphyrin concentrations. Porphyrins presenting two or more adjacent positively charged groups, directly linked to the macrocycle meso positions, appeared to be the most effective photosensitizers. The present study also included the dicationic 5,10-diphenyl-15,20-di(1-methylpyridinium-4-yl)porphyrin (14b), which has previously shown promising results on a psoriasis-like in vivo model. Overall results indicated that the beneficial effect related to porphyrins on psoriasis can be related to the decreasing of keratinocyte viability. Furthermore, some of the cationic porphyrins studied appeared as candidates to be utilized as photosensitizers for psoriasis treatment.