Abstract:This research aimed to develop and evaluate a novel multi-ethosome (ME) system for the dermal delivery of terbinafine hydrochloride (TH) as a new approach to fungal infection treatment. TH-loaded MEs were successfully prepared using cinnamaldehyde as a penetration enhancer. Mean diameter of ME was found as ~100 nm with monodispersed size distribution. Drug entrapment efficiency reached up to 86% ± 1.4%. MEs exhibited excellent colloid stability and no drug leakage after 2 months of storage. In contrast to a co… Show more
“…As reported by Zhang et al. while targeting dermal fungus infection using vesicle nanocarrier loaded with terbinafine hydrochloride, a maximizing in ZP contributed to higher repulsive forces that enhanced vesicle stability and improved the interaction with the skin layers, which is in agreement with current findings (L. Zhang et al., 2020 ).…”
Cutaneous fungal infection therapy confronts several issues concerning skin permeation in addition to drug resistance and adverse effects of conventional drugs. The repurposing strategy is supposed to overcome some of those therapeutic obstacles. Recently, atorvastatin (ATO) revealed antifungal activity. ATO is an antihyperlipidemic drug with pH-dependent solubility, which limits skin permeation. This study aims to improve ATO antifungal activity by encapsulation in an emulsomes (EMLs) system, which seeks to ameliorate skin penetration. Therefore, multiple factors were investigated according to the One-Factor-at-a-Time (OFAT) design to achieve the optimum formula with targeted characteristics. Minimizing particle-size and polydispersity-index, besides elevating zeta-potential (ZP) and entrapment-efficiency were the desirable responses during assessing 11 factors. The selected ATO-EMLs formula (E21) recorded 250.5 nm in particle size, polydispersity index of 0.4, ZP of –25.93 mV, and 83.12% of drug entrapped. Morphological study of E21 revealed spherical core–shell vesicles in nanosize. DSC, XRD, and FTIR were conducted to discover the physicochemical properties and confirm emulsomes formation. Optimized ATO-EMLs slowed drug release rate as only 75% of ATO was released after 72 h. Stability study recommended storage between 2 and 8 °C. The
in vivo
permeation study remarked a homogeneous penetration of EMLs in different skin layers. The
in vivo
skin irritation test revealed limited histopathological changes. The
in vitro
and
in vivo
microbiological studies demonstrated a good antifungal activity of ATO-EMLs. ATO-EMLs system improved antifungal activity as the MIC values reduced from 650 µg/mL for free ATO to 550 µg/mL for ATO-EMLs. These findings may shed light on ATO as an antifungal drug and nanosystems as a tool to support drug repurposing.
“…As reported by Zhang et al. while targeting dermal fungus infection using vesicle nanocarrier loaded with terbinafine hydrochloride, a maximizing in ZP contributed to higher repulsive forces that enhanced vesicle stability and improved the interaction with the skin layers, which is in agreement with current findings (L. Zhang et al., 2020 ).…”
Cutaneous fungal infection therapy confronts several issues concerning skin permeation in addition to drug resistance and adverse effects of conventional drugs. The repurposing strategy is supposed to overcome some of those therapeutic obstacles. Recently, atorvastatin (ATO) revealed antifungal activity. ATO is an antihyperlipidemic drug with pH-dependent solubility, which limits skin permeation. This study aims to improve ATO antifungal activity by encapsulation in an emulsomes (EMLs) system, which seeks to ameliorate skin penetration. Therefore, multiple factors were investigated according to the One-Factor-at-a-Time (OFAT) design to achieve the optimum formula with targeted characteristics. Minimizing particle-size and polydispersity-index, besides elevating zeta-potential (ZP) and entrapment-efficiency were the desirable responses during assessing 11 factors. The selected ATO-EMLs formula (E21) recorded 250.5 nm in particle size, polydispersity index of 0.4, ZP of –25.93 mV, and 83.12% of drug entrapped. Morphological study of E21 revealed spherical core–shell vesicles in nanosize. DSC, XRD, and FTIR were conducted to discover the physicochemical properties and confirm emulsomes formation. Optimized ATO-EMLs slowed drug release rate as only 75% of ATO was released after 72 h. Stability study recommended storage between 2 and 8 °C. The
in vivo
permeation study remarked a homogeneous penetration of EMLs in different skin layers. The
in vivo
skin irritation test revealed limited histopathological changes. The
in vitro
and
in vivo
microbiological studies demonstrated a good antifungal activity of ATO-EMLs. ATO-EMLs system improved antifungal activity as the MIC values reduced from 650 µg/mL for free ATO to 550 µg/mL for ATO-EMLs. These findings may shed light on ATO as an antifungal drug and nanosystems as a tool to support drug repurposing.
“…It was found that ME significantly improved the targeting efficiency as compared commercial Lamisil ® cream. The improved antifungal activity of ME confirmed by in vitro minimum inhibitory concentration (MIC) assay on Candida albicans strains [55].…”
Section: Application Of Ethosomal Formulations In Fungal Therapeuticsmentioning
Fungal infections have become a subject of great concern and the incidence of fungal infections is increasing, presenting an enormous challenge to healthcare professionals. Since most of the fungal infections are occurring over the skin, the treatment option of these infections always involves topical application. However, in topical delivery drug reaches into systemic circulation through different barriers of skin. Nevertheless, due to the low permeability, skin restricts the movement of many drugs. Hence, a delivery system is required, which deliver the medicament into the skin layers or through the skin and into the systemic circulation. Ethosomes or Soft malleable vesicles are the novel lipid vesicular carrier that offer improved skin permeability and efficient delivery due to their structure and composition. They contain high concentration of ethanol, which increases the fluidity of the skin. Therefore, in the present paper, we have explored the utility of ethosomal systems in the topical treatment of fungal infections. Structure, compositions types, mechanism and techniques of preparation of ethosome also discussed in the paper.
“…The microdilution method determined the minimum inhibitory concentration (MIC) values of evaluated samples against C.albicans and A.fumigatus ( Zhang et al, 2020 ). The assay was performed on the free ATO, blank EML-foam, and ATO-EMLs foam system.…”
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