Mechanism investigation of ethosomes transdermal permeation

Niu, Xiaoqian; Zhang, Dan‐Ping; Bian, Qiong; Feng, Xing-Fu; Li, Hao; Rao, Yuefeng; Shen, Yongmei; Geng, Funeng; Yuan, Anran; Ying, Xiaoying

doi:10.1016/j.ijpx.2019.100027

Cited by 48 publications

(44 citation statements)

References 57 publications

(56 reference statements)

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“…As suggested by other authors, SLN appear less efficient to promote drug permeation as compared to ETHO. Indeed, many studies have suggested that SLN can exert an occlusive effect [ 56 , 57 , 58 ], promoting the formation of a drug depot in or on the stratum corneum , while other studies have demonstrated that elastic ETHO can penetrate the stratum corneum through the intercellular spaces and release the loaded drug [ 25 , 30 , 31 , 32 ]. In this respect, the transdermal effect of ETHO-CA promotes a more intense and prolonged antioxidant activity of CA with respect to SLN-CA.…”

Section: Resultsmentioning

confidence: 99%

“…Conversely, many studies have evidenced the transdermal effect of ETHO, allowing the deep penetration of drugs through the skin strata [ 25 , 30 , 31 ]. In line with this, ethanol is supposed to disorganize the stratum corneum barrier, opening spaces through which the soft and malleable ETHO vesicles can pass, as indicated by the presence of intact ETHO in the epidermis [ 25 , 32 ]. Different nanosystems have been investigated as carriers for phenolic compounds; however, to the best of our knowledge, the influence of the nanosystem type on the antioxidant behavior and transdermal potential of the phenolic compound has not been yet investigated.…”

Section: Introductionmentioning

confidence: 99%

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The Potential of Caffeic Acid Lipid Nanoparticulate Systems for Skin Application: In Vitro Assays to Assess Delivery and Antioxidant Effect

et al. 2021

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The object of this study is a comparison between solid lipid nanoparticles and ethosomes for caffeic acid delivery through the skin. Caffeic acid is a potent antioxidant molecule whose cutaneous administration is hampered by its low solubility and scarce stability. In order to improve its therapeutic potential, caffeic acid has been encapsulated within solid lipid nanoparticles and ethosomes. The effect of lipid matrix has been evaluated on the morphology and size distribution of solid lipid nanoparticles and ethosomes loaded with caffeic acid. Particularly, morphology has been investigated by cryogenic transmission electron microscopy and small angle X-ray scattering, while mean diameters have been evaluated by photon correlation spectroscopy. The antioxidant power has been evaluated by the 2,2-diphenyl-1-picrylhydrazyl methodology. The influence of the type of nanoparticulate system on caffeic acid diffusion has been evaluated by Franz cells associated to the nylon membrane, while to evaluate caffeic acid permeation through the skin, an amperometric study has been conducted, which was based on a porcine skin-covered oxygen electrode. This apparatus allows measuring the O2 concentration changes in the membrane induced by polyphenols and H2O2 reaction in the skin. The antioxidative reactions in the skin induced by caffeic acid administered by solid lipid nanoparticles or ethosomes have been evaluated. Franz cell results indicated that caffeic acid diffusion from ethosomes was 18-fold slower with respect to solid lipid nanoparticles. The amperometric method evidenced the transdermal delivery effect of ethosome, indicating an intense antioxidant activity of caffeic acid and a very low response in the case of SLN. Finally, an irritation patch test conducted on 20 human volunteers demonstrated that both ethosomes and solid lipid nanoparticles can be safely applied on the skin.

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Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

The Potential of Caffeic Acid Lipid Nanoparticulate Systems for Skin Application: In Vitro Assays to Assess Delivery and Antioxidant Effect

et al. 2021

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“…Moreover, 0.5% HAL-ES-mediated aPDT further significantly inhibited the activity and growth of C. albicans biofilm within 48 h, mainly due to the effective reduction of biofilm hyphae. This can be because ES, as a nanocarrier, contains a high concentration of ethanol and is of reduced size, allowing the drug to effectively penetrate the structure of biofilm and cell membranes ( Zhang et al, 2014 ; Niu et al, 2019 ). Hyphae play a pivotal role in the spatial structure and compressive strength of biofilms ( Paramonova et al, 2009 ).…”

Section: Discussionmentioning

confidence: 99%

Antifungal Photodynamic Activity of Hexyl-Aminolevulinate Ethosomes Against Candida albicans Biofilm

et al. 2020

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Biofilm formation is responsible for the development of chronic and recurrent Candida albicans infections. The generation of biofilms is commonly accompanied by high resistance to conventional antifungal drugs, which can increase up to 1,000-fold. Fortunately, antimicrobial photodynamic therapy (aPDT) has shown excellent potential to treat biofilm infections. However, the current most commonly used photosensitizer (PS), aminolevulinic acid (ALA), is hydrophilic, unstable, and has low permeability, leading to unsatisfactory effects on biofilm eradication. To solve these problems, more stable lipophilic PSs and more effective permeability carriers could be considered as two effective solutions. Hexylaminolevulinate (HAL) has good bioavailability as a PS, and we proved in a previous study that ethosomes (ES), lipid-based nanocarriers, promote percutaneous drug penetration. In our previous study, a HAL-ES system presented superior photodynamic effects compared to those of ALA or HAL alone. Therefore, here, we aim to evaluate the biological effects of HAL-ES-mediated aPDT on C. albicans biofilm. An XTT sodium salt assay showed that aPDT using 0.5% HAL decreased C. albicans biofilm activity by 69.71 ± 0.43%. Moreover, aPDT with 0.5% HAL-ES further decreased biofilm activity by 92.95 ± 0.16% and inhibited growth of 25.71 ± 1.61% within 48 h, mostly via its effect on the hyphae growth, which correlated with a threefold increase in C. albicans plasma membrane permeabilization. Notably, HAL-ES-mediated aPDT significantly reduced the sessile minimum inhibitory concentration 50 (SMIC50) of fluconazole to <2.0 μg/ml, and the 21-day survival rate of C. albicans biofilm-infected mice increased from 6.7 to 73.3%. It also significantly reduced the drug resistance and in vivo pathogenicity of C. albicans biofilm. These results demonstrate that HAL-ES-mediated aPDT could be an effective therapy for C. albicans biofilm infections; while also serving as a particularly promising effective treatment for cutaneous or mucocutaneous candidiasis and the prevention of progression to systemic candidiasis.

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“…They are formed from phospholipids, water and high concentrations of alcohols (ethyl alcohol or isopropanol) [ 98 ] that provide elastic properties to the vesicles as well as increase the encapsulation efficiency of lipophilic molecules, especially compared to conventional liposomes. Halan et al [ 99 ] prepared ethosomes incorporating caffeic acid for transdermal delivery. The study revealed that the encapsulation efficiency of caffeic acid was greater compared to other systems described in the literature and that caffeic acid was stabilized, maintaining its antioxidant potential for prolonged time.…”

Section: Organic-based Delivery Systemsmentioning

confidence: 99%

Innovative Delivery Systems Loaded with Plant Bioactive Ingredients: Formulation Approaches and Applications

Kyriakoudi

Spanidi²,

Mourtzinos

et al. 2021

Plants

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Plants constitute a rich source of diverse classes of valuable phytochemicals (e.g., phenolic acids, flavonoids, carotenoids, alkaloids) with proven biological activity (e.g., antioxidant, anti-inflammatory, antimicrobial, etc.). However, factors such as low stability, poor solubility and bioavailability limit their food, cosmetics and pharmaceutical applications. In this regard, a wide range of delivery systems have been developed to increase the stability of plant-derived bioactive compounds upon processing, storage or under gastrointestinal digestion conditions, to enhance their solubility, to mask undesirable flavors as well as to efficiently deliver them to the target tissues where they can exert their biological activity and promote human health. In the present review, the latest advances regarding the design of innovative delivery systems for pure plant bioactive compounds, extracts or essential oils, in order to overcome the above-mentioned challenges, are presented. Moreover, a broad spectrum of applications along with future trends are critically discussed.

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Mechanism investigation of ethosomes transdermal permeation

Abstract: Graphical abstract

Cited by 48 publications

References 57 publications

The Potential of Caffeic Acid Lipid Nanoparticulate Systems for Skin Application: In Vitro Assays to Assess Delivery and Antioxidant Effect

The Potential of Caffeic Acid Lipid Nanoparticulate Systems for Skin Application: In Vitro Assays to Assess Delivery and Antioxidant Effect

Antifungal Photodynamic Activity of Hexyl-Aminolevulinate Ethosomes Against Candida albicans Biofilm

Innovative Delivery Systems Loaded with Plant Bioactive Ingredients: Formulation Approaches and Applications

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