Abstract
Background and Purpose:Encapsulation can lead to improved efficacy and safety of antifungal compounds. The attention of scientists has recently turned to biocompatible lipids as the carriers for the delivery of antifungal drugs, such as fluconazole. Although several research reports have already been published on fluconazole loaded solid lipid nanoparticles (FLZ-SLNs) and fluconazole loaded nanostructured lipid carriers (FLZ-NLCs), the possible advantages of NLCs over SLNs have not yet been fully established. Studies performed so far have given several contradictory results.Materials and Methods:Both formulations of fluconazole were synthesized using probe ultrasonication method and the characteristics were analyzed. Antifungal susceptibility testing (AFST) was performed with FLZ, FLZ-SLNs, and FLZ-NLCs using CLSI document M60 against some common fluconazole-resistant Candida species.Results:A significant decrease was observed in minimum inhibitory concentration values when both formulations were applied. Nonetheless, FLZ-NLCs were significantly more effective (P<0.05). However, three species groups were not statistically different in terms of the activity of FLZ-NLCs.Conclusion:Based on the obtained results, FLZ-NLCs could reverse the azole-resistance phenomenon in the most common Candida species more effectively, as compared to FLZ-SLNs.
Highlights
Background and PurposeEncapsulation can lead to improved efficacy and safety of antifungal compounds
The main mechanisms of resistant against fluconazole include target gene mutation (ERG11 mutations resulted in less target binding), target upregulation (UPC2, Duplication of chromosome 5 Iso chromosomes), and efflux pumps (CDR, MFS CgSNQ2, PDH1 ( C. glabrata [21]) [23]
The present study investigated the effectiveness of two formulations of FLZ-loaded nanoparticles (i.e., FLZ-solid lipid nanoparticles (SLNs) and fluconazole loaded nanostructured lipid carriers (FLZNLCs)).The nanoparticles with spherical shape and small size were synthesized with excellent zeta potential and entrapment efficiency
Summary
Background and PurposeEncapsulation can lead to improved efficacy and safety of antifungal compounds. The attention of scientists has recently turned to biocompatible lipids as the carriers for the delivery of antifungal drugs, such as fluconazole. Several research reports have already been published on fluconazole loaded solid lipid nanoparticles (FLZ-SLNs) and fluconazole loaded nanostructured lipid carriers (FLZNLCs), the possible advantages of NLCs over SLNs have not yet been fully established. Studies performed so far have given several contradictory results. Antifungal susceptibility testing (AFST) was performed with FLZ, FLZ-SLNs, and FLZ-NLCs using CLSI document M60 against some common fluconazole-resistant Candida species. Three species groups were not statistically different in terms of the activity of FLZ-NLCs. Conclusion: Based on the obtained results, FLZ-NLCs could reverse the azoleresistance phenomenon in the most common Candida species more effectively, as compared to FLZ-SLNs
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