Journal
CHEMISTRY AND PHYSICS OF LIPIDS
Volume 234, Issue -, Pages -Publisher
ELSEVIER IRELAND LTD
DOI: 10.1016/j.chemphyslip.2020.105028
Keywords
Luliconazole; Lipid nanoparticles; Liquid crystals; Antifungal; Quality by design; Central composite design; Dermatokinetics; Fungal infections
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The study focuses on the formulation and characterization of luliconazole loaded lyotropic liquid crystalline nanoparticles (LCNP), which demonstrated promising drug release and skin permeation properties, suggesting LCNP as an effective carrier system for antifungal drugs.
Fungal infections are an important cause of morbidity and pose a serious health concern especially in immunocompromised patients. Luliconazole (LUL) is a topical imidazole antifungal drug with a broad spectrum of activity. To overcome the limitations of conventional dosage forms, LUL loaded lyotropic liquid crystalline nanoparticles (LCNP) were formulated and characterized using a three-factor, five-level Central Composite Design of Response Surface Methodology. LUL loaded LCNP showed particle size of 181 +/- 12.3 nm with an entrapment efficiency of 91.49 +/- 1.61 %. The LUL-LCNP dispersion in-vitro drug release showed extended release up to 54 h. Ex-vivo skin permeation studies revealed transdermal flux value (J) of LUL-LCNP gel (7.582 mu g/h/cm(2)) 2 folds higher compared to marketed cream (3.3706 mu g/h/cm(2)). The retention of LUL in the stratum corneum was similar to 1.5 folds higher and similar to 2 folds higher in the epidermis and other deeper layers in comparison to the marketed cream. The total amount of drug penetrated (AUC(0-infinity)) with LCNP formulation was 4.7 folds higher in epidermis and 6.5 folds higher in dermis than marketed cream. The study's findings vouch that LCNP can be a promising and effective carrier system for the delivery of antifungal drugs with enhanced skin permeation.
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