Abstract
Phytol is a diterpene alcohol and can be found as a product of the metabolism of chlorophyll in plants. This compound has been explored as a potential antimicrobial agent, but it is insoluble in water. In this study, we describe a novel approach for an interesting anticandidal drug delivery system containing phytol. Different formulations of phytol-loaded solid lipid nanoparticles (SLN) were designed and tested using a natural lipid, 1,3-distearyl-2-oleyl-glycerol (TG1). Different compositions were considered to obtain three formulations with 1:10, 1:5, and 1:3 w/w phytol/TG1 ratios. All the formulations were prepared by emulsification solvent evaporation method and had their physicochemical properties assessed. The biocompatibility assay was performed in the HEK-293 cell line and the antifungal efficacy was demonstrated in different strains of Candida ssp., including different clinical isolates. Spherical and uniform SLN (<300 nm, PdI < 0.2) with phytol-loading efficiency >65% were achieved. Phytol-loaded SLN showed a dose-dependent cytotoxic effect in the HEK-293 cell line. The three tested formulations of phytol-loaded SLN considerably enhanced the minimal inhibitory concentration of phytol against 15 strains of Candida spp. Considering the clinical isolates, the formulations containing the highest phytol/TG1 ratios showed MICs at 100%. Thus, the feasibility and potential of phytol-loaded SLN was demonstrated in vitro, being a promising nanocarrier for phytol delivery from an anticandidal approach.
Highlights
In the last few decades it is estimated that more than 150 million individuals develop severe fungal diseases every year, resulting in high rates of morbidity and mortality [1]
The increasing amount of phytol in the solid lipid nanoparticles (SLN) did not affect their mean diameter of approximately 300 nm, their particle size distribution (PdI < 0.2), or their negative zeta potential
Results from SLN tests with the Candida spp. reference strains showed that these nanoparticles were able to induce 100% growth inhibition
Summary
In the last few decades it is estimated that more than 150 million individuals develop severe fungal diseases every year, resulting in high rates of morbidity and mortality [1]. VVC has been considered a global public health problem, affecting millions of women of all social strata. It causes great discomfort, impairs sexual relationships, and damages work performance [7]. Invasive infections due to Candida spp. are widely recognized as a major cause of morbidity and mortality in the healthcare environment and it is estimated that over 750,000 cases of invasive candidiasis are reported per year. At least 15 distinct Candida species may cause human diseases, whereas more than 95% of invasive infections are caused by the 5 most common Candida spp.: Candida albicans, Candida glabrata, Candida tropicalis, Candida parapsilosis, and Candida krusei [11]
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