Abstract
Polymeric nanoparticle-based carriers are promising agents to deliver drugs to cells. Vitis vinifera phenolic compounds are known for their antifungal activity against Candida albicans. The aim of the present study was to investigate the antifungal activity of pterostilbene or crude extracts from non-fermented grape pomace, entrapped in poly(lactic-co-glycolic) acid nanoparticles (NPs), with diameters of 50 and 150 nm, on Candida biofilm. The fluorescent probe coumarin 6 was used to study the uptake of poly(lactic-co-glycolic)acid (PLGA) NPs in planktonic cells and biofilm. The green fluorescent signal of coumarin 6 was observed in Candida biofilm after 24 and 48 hours. Both pterostilbene and crude pomace extract entrapped in NPs exerted a significantly higher anti-biofilm activity compared to their free forms. The entrapment efficiency of both pterostilbene and crude pomace extract in PLGA NPs was ~90%. At 16 µg/mL, pterostilbene loaded in PLGA NPs reduced biofilm formation of 63% and reduced mature biofilm of 50%. Moreover, at 50 µg/mL, the pomace extract loaded in NPs reduced mature biofilm of 37%. These results strongly suggest that PLGA NPs are promising nanodevices for the delivery of antifungal drugs as the crude grape pomace extract, a by-product of white wine making.
Highlights
Candida albicans is an opportunistic pathogen, part of the normal microbiota of the human oral cavity, gastrointestinal tract and female genital tract
Since few molecules are reported in the literature to inhibit or prevent the formation of C. albicans biofilms, the development of new anti-biofilm agents represents an important field of investigation
The results showed a higher activity of PTB-loaded PLGA NPs than free PTB against C. albicans biofilm formation (p < 0.05) in two C. albicans strains (Figure 3)
Summary
Candida albicans is an opportunistic pathogen, part of the normal microbiota of the human oral cavity, gastrointestinal tract and female genital tract. The medical impact of C. albicans is typically due to its ability to form biofilms which are closely packed communities of cells adhering to surfaces and embedded in a protective polymeric extracellular matrix. Treatment of C. albicans biofilms with drugs currently on the market represents a significant clinical problem due to the intrinsic tolerance of fungal biofilms to many anti-fungal. Molecules 2019, 24, 2070 agents [3]. To fight Candida biofilms, high doses and frequent administrations of antifungal drugs are required, causing adverse side effects or in some cases toxicity [4]. Since few molecules are reported in the literature to inhibit or prevent the formation of C. albicans biofilms, the development of new anti-biofilm agents represents an important field of investigation
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