Development, optimization, and evaluation of a nanostructured lipid carrier of sesame oil loaded with miconazole for the treatment of oral candidiasis

Abstract

Candida albicans is the fungus responsible for oral candidiasis, a prevalent disease. The development of antifungal-based delivery systems has always been a major challenge for researchers. This study was designed to develop a nanostructured lipid carrier (NLC) of sesame oil (SO) loaded with miconazole (MZ) that could overcome the solubility problems of MZ and enhance its antifungal activity against oral candidiasis. In the formulation of this study, SO was used as a component of a liquid lipid that showed an improved antifungal effect of MZ. An optimized MZ-loaded NLC of SO (MZ-SO NLC) was used, based on a central composite design-based experimental design; the particle size, dissolution efficiency, and inhibition zone against oral candidiasis were chosen as dependent variables. A software analysis provided an optimized MZ-SO NLC with a particle size of 92 nm, dissolution efficiency of 88%, and inhibition zone of 29 mm. Concurrently, the ex vivo permeation rate of the sheep buccal mucosa was shown to be significantly ( p < .05) higher for MZ-SO NLC (1472 µg/cm 2 ) as compared with a marketed MZ formulation (1215 µg/cm 2 ) and an aqueous MZ suspension (470 µg/cm 2 ). Additionally, an in vivo efficacy study in terms of the ulcer index against C. albicans found a superior result for the optimized MZ-SO NLC (0.5 ± 0.50) in a treated group of animals. Hence, it can be concluded that MZ, through an optimized NLC of SO, can treat candidiasis effectively by inhibiting the growth of C. albicans .

Antifungal Cationic Nanoemulsion Ferrying Miconazole Nitrate with Synergism to Control Fungal Infections:In Vitro,Ex Vivo, andIn VivoEvaluations

“…13 Recently, oral delivery of the drug was reported in an NLC (nanostructured lipid carrier) despite the limited oral pharmacokinetics. 14 Furthermore, localized infection with Candida albicans often penetrates to deeper viable epidermis, and miconazole nitrate has low bioavailability in skin strata causing drug resistance and recurrence of infections in the skin. 7 Hence, there is a need to develop a new strategy for localizing the drug to the target site for efficient and effective therapy.…”

“…Considering the aforementioned issues, several attempts have been made to employ nanotechnology-based nanocarriers such as liposomes, ethosomes, and niosome. 8 , 14 , 15 However, these formulations did not show the promised results to eradicate the complete infections from the skin (viable epidermis) due to physical, chemical, and storage instability of vesicular carrier systems.…”

Design, Characterization, and In Vitro Assays on Muscle Cells of Endocannabinoid-like Molecule Loaded Lipid Nanoparticles for a Therapeutic Anti-Inflammatory Approach to Sarcopenia

“…The solubility of PEA in the selected lipids (namely, stearic acid and cholesteryl stearate) was determined at the temperature of 85 °C under 200 rpm magnetic stirring [ 32 ]. Exactly weighted amounts of PEA were gradually added to known amounts of stearic acid or cholesteryl stearate and a mixture thereof with the same ratio used for SLNs preparation; the progressive additions were made at 30 min intervals until concentrations exceeded saturation solubility.…”

Molecular Mapping of Antifungal Mechanisms Accessing Biomaterials and New Agents to Target Oral Candidiasis

“…According to the evaluation of the ulcer index on rats treated with C. albicans colonies, the synergism between miconazole and sesame oil in alleviating mucosal ulcerations was proved. This fact can be justified by the antioxidant activity of the natural oil, associated with the molecular action of miconazole [ 162 ].…”