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Kaempferol (KMP) belong to flavonoid class have developed in ethosomal formulation and were evaluated for their potential to treat diabetic foot ulcers. Even though ethosomes are highly deformable, they can pass through human skin intact. KMP ethosomes were formulated using the cold method and optimized by Box-Behnken design (BBD) (three-factor, three-level (3 3 )). The formulation variables used for optimization are drug concentration of KMP, soylecithin content, and ethanol percentage. The optimized formulation was examined using transmission electronic microscopy (TEM), differential scanning calorimetry (DSC), Fourier transform infrared (FTIR) spectroscopy, in-vitro release, ex-vivo permeation studies, and storage stability. The optimized KMP ethosomes was found to have vesicle size (VS) of 283 ± 0.3 nm and zeta potential (ZP) of -29.67 ± 0.3 mV, polydispersity index (PDI) of 0.36, % entrapment efficiency (%EE) of 91.02 ± 0.21%, drug loading (%) of 46.23 ± 2.5% followed by good storage stability at 4°C/60 ± 5% RH. In vitro drug release of optimized KMP ethosomes was 88.2 ± 2.75%, which was approximately double when compared with pure KMP release, that is 49.9 ± 1.89%. The release kinetics for optimized KMP ethosomes follows the Korsmeyer-Peppas model. An apparent permeation coefficient of 356.25 ± 0.5 μg/cm 2 was determined and compared with pure KMP (118.46 ± 0.3 μg/cm 2 ) for 24 h. According to the study, ethosomes can be a cutting-edge strategy that offers a new delivery method for prolonged and targeted distribution of KMP in a variety of dosage forms including oral, topical, transdermal, and so forth., (© 2024 Wiley Periodicals LLC.)

The use of nanotechnology has been extensively explored for developing efficient drug delivery systems towards topical and transdermal applications. Ethosomes constitute a vesicular nanocarrier containing a relatively high concentration of ethanol (20-45%). Ethanol is a well-known permeation enhancer, which confers ethosomes unique features, including high elasticity and deformability, allowing them to penetrate deeply across the skin and enhance drug permeation and deposition. The improved composition of ethosomes offer, thereby, significant advantages in the delivery of therapeutic agents over particularly the conventional liposomes regarding different pathologies, including acne, psoriasis, alopecia, skin infections, hormonal deficiencies, among others. This review provides a comprehensive overview of the ethosomal system and an assessment of its potential as an efficient nanocarrier towards the skin delivery of active ingredients. Special attention is given to the composition of ethosomes and the mechanism of skin permeation, as well as their potential applications in different pathologies, particularly skin pathologies (acne, psoriasis, atopic dermatitis, skin cancer and skin infections). Some examples of ethosome-based formulations for the management of skin disorders are also highlighted. Besides the need for further studies, particularly in humans, ethosomal-based formulations hold great promise in the skin delivery of active ingredients, which increasingly asserts oneself as a viable alternative to the oral route.

Aim: The aim of the current work was to develop vardenafil hydrochloride (VRD)-loaded ethosome-derived invasomes as a possible transdermal system which could be used for patients suffering from pulmonary arterial hypertension., Methods: VRD-loaded ethosomes were developed at three concentrations of phosphatidylcholine (5, 10 and 15 mg/mL) and three percentages of ethanol (20%, 30% and 40%, v/v). The best achieved VRD-loaded ethosomes (ETH9) were optimized to invasomes via incorporation of terpenes (limonene, cineole and a 1:1 mixture) at three concentrations (0.5%, 1% and 2%, v/v). All systems were evaluated for vesicle size, zeta potential, drug entrapment efficiency (EE%), cumulative drug permeated percentages after 0.5hrs (Q 0.5h ) and 12hrs (Q 12h ) and steady-state flux (J ss ). The optimized system (ETH9-INV8) was further characterized for morphology, histopathology and confocal laser scanning microscopy (CLSM). Physiologically based pharmacokinetic (PBPK) modeling was employed to estimate VRD pharmacokinetic parameters from the optimized transdermal system and an oral aqueous drug dispersion, in adults and geriatrics., Results: The optimized invasomal system (ETH9-INV8) was characterized with spherical vesicles (159.9 nm) possessing negative zeta potential (-20.3 mV), promising EE% (81.3%), low Q 0.5h (25.4%), high Q 12h (85.3%) and the largest steady-state flux (6.4 µg.cm -2 h -1 ). Following a leave-on period of 12hrs in rats, it showed minor histopathologic changes. CLSM studies proved its ability to deeply permeate rat skin. Lower C max values, delayed T max estimates and greater AUC 0-24h folds in adults and geriatrics (≈ 2.18 and 1.69, respectively) were estimated following the transdermal application of ETH9-INV8 system., Conclusion: ETH9-INV8 is a promising transdermal system for VRD., Competing Interests: The authors report no conflicts of interest for this work., (© 2020 Ammar et al.)

This is a comprehensive review on the use of phospholipid nanovesicles for dermal/transdermal and nasal drug administration. Phospholipid-based vesicular carriers have been widely investigated for enhanced drug delivery via dermal/transdermal routes. Classic phospholipid vesicles, liposomes, do not penetrate the deep layers of the skin, but remain confined to the upper stratum corneum. The literature describes several approaches with the aim of altering the properties of these vesicles to improve their penetration properties. Transfersomes and ethosomes are the most investigated penetration-enhancing phospholipid nanovesicles, obtained by the incorporation of surfactant edge activators and high concentrations of ethanol, respectively. These two types of vesicles differ in terms of their structure, characteristics, mechanism of action and mode of application on the skin. Edge activators contribute to the deformability and elasticity of transfersomes, enabling them to penetrate through pores much smaller than their own size. The ethanol high concentration in ethosomes generates a soft vesicle by fluidizing the phospholipid bilayers, allowing the vesicle to penetrate deeper into the skin. Glycerosomes and transethosomes, phospholipid vesicles containing glycerol or a mixture of ethanol and edge activators, respectively, are also covered. This review discusses the effects of edge activators, ethanol and glycerol on the phospholipid vesicle, emphasizing the differences between a soft and an elastic nanovesicle, and presents their different preparation methods. To date, these differences have not been comparatively discussed. The review presents a large number of active molecules incorporated in these carriers and investigated in vitro, in vivo or in clinical human tests.

Purpose: Thymosin β-4(Tβ-4) is a macromolecular protein drug with potential for drug development in wound repair but is limited by the shortcomings of macromolecular protein, such as large volumes, poor membrane permeability, and unstable physicochemical characteristics. Ethosomes could enhance cell membrane fluidity and reduce epidermal membrane density to make macromolecular drugs through the stratum corneum into the deeper layers of the skin easily. Herein, we developed and characterized a novel transdermal delivery vehicle to load macromolecular protein peptides and use Tβ-4 as a model drug wrapped into ethosomes., Methods: We used the orthogonal method to optimize the formulation of the ethosome preparation prepared by the ethonal infusion method. Ethosomal gels were characterized by using different analytical methods. Transdermal release rate in vitro have been demonstrated in Franz diffusion cells and the efficacy of drug-loaded nanocarriers in vivo was investigated in a mouse model., Results: Optimized Tβ-4 ethosomal gels have good physicochemical properties. The drug amounts of the cumulative release in the ethosomal gel within 5 hours were 1.67 times that of the T-β4 gel in vitro release study, and the wound healing time of ethosomal gel group was only half of the T-β4 gel group in vivo pharmacokinetic study. Compared with the free drug group, the ethosome preparation not only promotes the percutaneous absorption process of the macromolecular protein drugs but also shortened wound recovery time., Conclusion: Hence, we provide a possible good design for ethosomal gel system that can load macromolecular protein peptide drugs to achieve transdermal drug administration, promoting the percutaneous absorption of the drug and improving the effect., Competing Interests: The authors report no conflicts of interest in this work., (© 2019 Fu et al.)

Liposomes containing a certain amount of ethanol are often referred to in the literature as ethosomes. Liposomes vary in size from 25 nm to 25,000 nm. Ethosomes are defined as lipids composed of phospholipids, ethanol, or isopropyl alcohol in quite high concentrations, and water. They enable active substances to reach the deep skin layers or even the general circulation. The structure of ethosomes allows for an increased penetration of the drug through two effects: the ethanolic effect and the ethosomal effect. Ethosomes can be obtained using three methods: the hot method, the cold method, and the classic method of mechanical dispersion. The literature describes many of the therapeutic groups of drugs that can be enclosed in ethosomal formulations. These include anti-viral drugs, antineoplastic drugs, antifungal drugs, hypnotic drugs, hormones, and many others. Ethosomes show important practical advantages compared to classic liposomes. It is necessary to conduct research with regard to real pharmaceutical systems using advanced physicochemical techniques.

Raloxifene HCl belongs to a class of selective estrogen receptor modulators (SERMs) which is used for the management of breast cancer. The major problem reported with raloxifene is its poor bioavailability which is only up to 2%. The main objective of the present work was to formulate raloxifene loaded ethosomal preparation for transdermal application and compare it with an oral formulation of the drug. Five ethosomal formulations with different concentrations of ethanol and a conventional liposomes formulation were prepared by rotary evaporation method. The prepared systems were characterised by high resolution transmission electron microscopy (HRTEM), force emission electron microscopy (FESEM), atomic force microscopy (AFM), X-ray diffraction (XRD) and 31 P NMR study. All these advanced characterization study established that the ethosome formulation was well defined by its size, shape and its bilayer formation. Transdermal flux of the optimized ethosome formulation was 22.14 ± 0.83 µg/ml/cm 2 which was 21 times higher when compared to the conventional liposomes. Confocal microscopy study revealed an enhanced permeation of coumarin-6 dye loaded ethosomes to much deeper layers of skin when compared with conventional liposomes. The gel was found to be pseudoplastic with elastic behaviour. In-vivo studies on rats showed a higher bioavailability of RXL (157% times) for ethosomal formulation when compared with the oral formulation. In conclusion, RXL loaded ethosomal formulation via transdermal route showed superior drug delivery properties as compared to oral formulation., (Copyright © 2018 Elsevier B.V. All rights reserved.)

The primary objective of this study was to develop, evaluate and compare the effectiveness and stability of ethosomal carbomer gels in different solvents. The optimal ethosomal formulation was isolated to create ethosomal gels using carbomer in either pure water (water gel) or PBS containing 30% ethanol (PBS gel). In vitro release of the ethosomal gels were tested using Franz apparatus on hydrophilic and hydrophobic artificial membranes. In vitro stability of two ethosomal gels was systematically evaluated. Transdermal antigen delivery of ethosomal gel was finally performed on the skin of hair removal mice. Both solvent and concentration effects on the in vitro release performance of ethosomal gel of carbomer have been confirmed. Penetration depth has been found to be dependent on the nature of the membranes such that penetration rate is higher in the hydrophobic membrane than the hydrophilic ones. Furthermore, in vitro stability test indicated that ethosomal PBS gel was more stable than ethosomal water gel. In vivo immunoassay confirmed that the ethosomal PBS gel could deliver the antigenic molecules into the skin of mice and stimulate specific IgG secretion. Using the same solvent for lipid vesicular formulation when making polymeric hydrogel may help to provide a more conducive environment for lipid vesicles and hence enhance their roles in transdermal antigen delivery., (Copyright © 2017 Elsevier B.V. All rights reserved.)

Cytarabine is a pyrimidine nucleoside analog used predominantly for acute myeloid leukemia (AML) and also for other indications, including acute lymphocytic leukemia, chronic myelogenous leukemia, and lymphoma by parenteral route due to its low oral bioavailability. Parenteral administration requires constant plasma level, monitoring for its fluctuation and poor patients compliances. Hence the objective of this work is to construct optimized nanosized malleable liposomes of cytarabine to accentuate transdermal delivery of drug to circumvent previously mentioned drawbacks. We also investigated its characteristics and therapeutic efficiency and attempted to systematically explore the penetration enhancing property. Well characterized ethanolic liposomes were also biologically tested for dermatological safety and systemic bioavailability. Ethanolic liposomes were found to be spherical having nanometric size with low polydispersity and high encapsulation efficiency. Skin permeation and deposition studies revealed significant enhancement. In vivo, skin irritation study of developed formulation showed no erythema or scaling vis-à-vis the liposomes. Blood profile of this novel formulation indicated lower lag time with the high amount of drug within 3-12 h after transdermal administration demonstrating the enhanced percutaneous penetration of cytarabine with no erythema, thus leading to patient's compliance by alternative delivery of drug for the treatment of leukemia.

Ethosomal systems are novel lipid vesicular carriers containing a relatively high percentage of ethanol. These nanocarriers are especially designed for the efficient delivery of therapeutic agents with different physicochemical properties into deep skin layers and across the skin. Ethosomes have undergone extensive research since they were invented in 1996; new compounds were added to their initial formula, which led to the production of new types of ethosomal systems. Different preparation techniques are used in the preparation of these novel carriers. For ease of application and stability, ethosomal dispersions are incorporated into gels, patches, and creams. Highly diverse in vivo models are used to evaluate their efficacy in dermal/transdermal delivery, in addition to clinical trials. This article provides a detailed review of the ethosomal systems and categorizes them on the basis of their constituents to classical ethosomes, binary ethosomes, and transethosomes. The differences among these systems are discussed from several perspectives, including the formulation, size, ζ-potential (zeta potential), entrapment efficiency, skin-permeation properties, and stability. This paper gives a detailed review on the effects of ethosomal system constituents, preparation methods, and their significant roles in determining the final properties of these nanocarriers. Furthermore, the novel pharmaceutical dosage forms of ethosomal gels, patches, and creams are highlighted. The article also provides detailed information regarding the in vivo studies and clinical trials conducted for the evaluation of these vesicular systems.

The aim of this study was to develop and evaluate a novel topical delivery system for apigenin by using ethosomes. An optimal apigenin-loaded ethosome formulation was identified by means of uniform design experiments. Skin deposition and transdermal flux of apigenin loaded in ethosomes, liposomes, and deformable liposomes were compared in vitro and in vivo. The efficiency of apigenin encapsulation increased with an increase in the amount of phospholipids in ethosome formulations. Moreover, skin deposition and transdermal flux of apigenin improved with an increase in the levels of phospholipids (Lipoid S 75) and short-chain alcohols (propylene glycol and ethanol), but decreased with an increase in the ratio of propylene glycol to ethanol. Profiles of skin deposition versus time for ethosomes varied markedly between in vivo and in vitro studies compared with those of liposomes or deformable liposomes. Optimized ethosomes showed superior skin targeting both in vitro and in vivo. Moreover, they had the strongest effect on reduction of cyclooxygenase-2 levels in mouse skin inflammation induced by ultraviolet B (UVB) light. Therefore, apigenin-loaded ethosomes represent a promising therapeutic approach for the treatment of UVB-induced skin inflammation., (Copyright © 2013 Elsevier B.V. All rights reserved.)

AbstractTransdermal drug delivery systems (TDDS) have received significant attention in recent years. TDDS are flexible systems that transport active components to the skin for either localized or systemic delivery of drugs through the skin. Among the three main layers of skin, the outermost layer, called the stratum corneum (SC), prevents the entry of water-loving bacteria and drugs with a high molecular weight. The challenge lies in successfully delivering drugs through the skin, which crosses the stratum corneum. The popularity of lipid-based vesicular delivery systems has increased in recent years due to their ability to deliver both hydrophilic and hydrophobic drugs. Ethosomes are specialized vesicles made of phospholipids that can store large amounts of ethanol. Ethosome structure and substance promote skin permeability and bioavailability. This article covers ethosome compositions, types, medication delivery techniques, stability, and safety. In addition to this, an in-depth analysis of the employment of ethosomes in drug delivery applications for a wide range of diseases has also been discussed. This review article highlights different aspects of ethosomes, such as their synthesis, characterization, marketed formulation, recent advancements in TDDS, and applications. [ABSTRACT FROM AUTHOR]

Ethosomes are novel ethanolic phospholipid vesicles which are significantly used for the transdermal drug delivery. Ethanol is an efficient permeation enhancer which is used in ethosomes about 20-45%. These are non-invasive in nature and have emerged as an area of active research interest because they significantly lead to enhanced skin penetration, improvement in drug delivery, increased drug entrapment efficiency it can deliver both hydrophilic and lipophilic drugs efficiently. Increased patient compliance etc. The drug penetrates the skin surface and gets absorbed by two phases i.e., the ethanol effect and ethosomes effect. Ethosomes are predominantly being used over liposomes because of their greater penetration rate which is attributed to the high concentration of ethanol. Hence it is an active area of research. The primary aim of the review is to provide a comprehensive account on the methods of preparation, properties, characterization, advantages and applications of ethosomes in the management of several skin diseases.

Skin cancer is one of the most prominent diseases, affecting all continents worldwide, and has shown a significant rise in mortality and prevalence. Conventional therapy, including chemotherapy and surgery, has a few drawbacks. The ethosomal systems would be thoroughly reviewed in this compilation, and they would be classified based on constituents: classical ethosomes, binary ethosomes, and transethosomes. Ethosomes systems are model lipid vesicular carriers with a substantial portion of ethanol. The impacts of ethosomal system components, preparation techniques, and their major roles in selecting the final characteristics of these nanocarriers are comprehensively reviewed in this chapter. The special techniques for ethosomes, including the cold approach, hot approach, injection method, mechanical dispersion method, and conventional method, are explained in this chapter. Various evaluation parameters of ethosomes were also explained. Furthermore, ethosomal gels, patches, and creams can be emphasised as innovative pharmaceutical drug formulations. Some hybrid ethosomal vesicles possessing combinatorial cancer therapy using nanomedicine could overcome the current drug resistance of specific cancer cells. Through the use of repurpose therapy, phytoconstituents may be delivered more effectively. A wide range of in vivo models are employed to assess their effectiveness. Ethosomes have provided numerous potential skin cancer therapeutic approaches in the future.

Background: Diabetic neuropathy (DN) is the most prevalent and problematic consequence of diabetes mellitus, with the highest rates of morbidity and death, as well as a significant financial burden on diabetes treatment. Aside from commercially available formulations, substantial research on herbal-based natural therapies to treat hyperglycemia and related consequences is underway. Objectives: The major aim of the study was to use an ethosomal gel to improve transdermal penetration of Curcuma longa and Boswellia serrata and to overcome the challenges of low transdermal drug delivery permeability. Materials and Methods: Curcuma longa and Boswellia serrata loaded ethosomes were made using a cold process with various amounts of ethanol and soya lecithin, and were improved based on entrapment efficiency, vesicular size, and ex-vivo investigations. Results: The optimized ethosomal formulation was then put into a gel and evaluated. Ex-vivo tests were conducted with Curcuma longa and Boswellia serrata ethosomal gels, which were compared to plain gel. The ethosomal system produced vesicles with sizes ranging from 1 to 100 nm, a spherical, smooth surface, and a maximum entrapment efficiency of Ne9. A modified ethosomal system (Ne9) was introduced into the gel and studied further. Conclusion: According to the findings, the ethosomal gel has a lot of potential for transdermal Curcuma longa and Boswellia serrata administration. [ABSTRACT FROM AUTHOR]

Ethosomes are novel ethanolic phospholipid vesicles which are significantly used for the transdermal drug delivery. Ethanol is an efficient permeation enhancer which is used in ethosomes about 20-45%. These are non-invasive in nature and have emerged as an area of active research interest because they significantly lead to enhanced skin penetration, improvement in drug delivery, increased drug entrapment efficiency it can deliver both hydrophilic and lipophilic drugs efficiently. Increased patient compliance etc. The drug penetrates the skin surface and gets absorbed by two phases i.e., the ethanol effect and ethosomes effect. Ethosomes are predominantly being used over liposomes because of their greater penetration rate which is attributed to the high concentration of ethanol. Hence it is an active area of research. The primary aim of the review is to provide a comprehensive account on the methods of preparation, properties, characterization, advantages and applications of ethosomes in the management of several skin diseases. [ABSTRACT FROM AUTHOR]

Glycyrrhiza glabra extract is widely known for its antioxidant and anti-inflammatory properties and can improve the wound healing process. The aim of this work was to shorten the time of the healing process by using an eco-sustainable wound dressing based on Spanish broom flexible cellulosic fabric by impregnation with G. glabra extract-loaded ethosomes. Chemical analysis of G. glabra extract was performed by LC-DAD-MS/MS and its encapsulation into ethosomes was obtained using the ethanol injection method. Lipid vesicles were characterized in terms of size, polydispersity index, entrapment efficiency, zeta potential, and stability. In vitro release studies, biocompatibility, and scratch test on 3T3 fibroblasts were performed. Moreover, the structure of Spanish broom dressing and its ability to absorb wound exudate was characterized by Synchrotron X-ray phase contrast microtomography (SR-PCmicroCT). Ethosomes showed a good entrapment efficiency, nanometric size, good stability over time and a slow release of polyphenols compared to the free extract, and were not cytotoxic. Lastly, the results revealed that Spanish broom wound dressing loaded with G. glabra ethosomes is able to accelerate wound closure by reducing wound healing time. To sum up, Spanish broom wound dressing could be a potential new green tool for biomedical applications. [ABSTRACT FROM AUTHOR]

Transdermal drug delivery system was first introduced more than 20 years ago. Transdermal drug delivery system is a type of convenient drug delivery system where drug goes to the systemic circulation through the protective barrier i.e. skinis the main target of topical and transdermal preparations. Major aim of transdermal drug delivery system is to cross the stratum corneum. Vesicular system is one of the most controversial methods for transdermal drug delivery system. Ethosomes are non-invasive delivery carriers that enable drugs to reach the deep skin layers and/or the systemic circulation. Ethosomes are innovative novel vesicular system. Ethosomes are composed of phospholipid, alcohol, polyglycol and water. Ethanol increases the penetration rate of the skin and delivers the drug into the deeper layers of skin. These systems are more efficient in delivering substances to the skin because of the presence of ethanol, Ethosomes are simple to prepare and safe to use. The purpose of this review is to focus on various aspects of ethosomes including their mechanism of penetration, preparation, composition, characterization, and application of ethosomes. [ABSTRACT FROM AUTHOR]

The skin is the largest organ of the human body that restricts the movement of drug to the systemic circulation. Topical drug delivery system is a system where the drug reaches the systemic circulation through the protective layer i.e. skin. The main disadvantage of this route is the low diffusion rate of the drugs which is across the stratum corneum layer of the skin. To overcome this problem to a certain extent, ethosomal delivery for drugs and herbal compounds has been recently introduced. Literature studies indicate that ethosomal formulation of acyclovir shows high therapeutic efficiency with shorter healing time in the treatment of recurrent herpes labialis than conventional Zovirax. Also, the ethosomes of minoxidil enhanced the skin permeation of minoxidil in vitro in comparison to its ethanolic or phospholipid ethanolic micellar solution or hydroethanolic solution. The advantages of this system include increased drug permeation, increased drug entrapment and improved drug delivery. Ethosomal drug delivery system opens up doors for the development of new and novel therapies for treating male pattern baldness, as it is an easier way to prepare, in addition to its safety and efficacy. In this review article, we have focused on methods of preparation of ethosomes, characterization techniques, applications, details about the various research trials for the management of androgenic alopecia and various ethosomal products in market. [ABSTRACT FROM AUTHOR]

Skin, the largest organ of the body serves as a potential route of drug delivery for local and systemic effects. However, the outermost layer of skin, the stratum corneum (SC) acts as a tough barrier that prevents penetration of hydrophilic and high molecular weight drugs. Ethosomes are a novel phospholipid vesicular carrier containing high ethanol concentrations and offer improved skin permeability and efficient bioavailability due to their structure and composition. This article gives a review of ethosomes including their compositions, types, mechanism of drug delivery, stability, and safety behaviour. This article also provides a detailed overview of drug delivery applications of ethosomes in various diseases. [ABSTRACT FROM AUTHOR]

This study aimed to formulate suitable nanovesicles (NVs) for transdermal delivery of Ondansetron. It also illustrated a practical example for the importance of Box-Cox transformation. A 2 3 full factorial design was used to enable testing transfersomes, ethosomes, and transethosomes of Ondansetron simultaneously. The independent variables (IVs) studied were sodium taurocholate amount, ethanol volume in hydration medium and sonication time. The studied dependent variables (DVs) were: particle size (PS), zeta potential (ZP) and entrapment efficiency (EE). Polynomial equations were used to study the influence of IVs on each DV. Numerical multiple response optimization was applied to select an optimized formula (OF) with the goals of minimizing PS and maximizing ZP absolute value and EE. Box-Cox transformation was adopted to enable modeling PS raised to the power of 1.2 with an excellent prediction R 2 of 1.000. ZP and EE were adequately represented directly with prediction R 2 of 0.9549 and 0.9892 respectively. Response surface plots helped in explaining the influence of IVs on each DV. Two-sided 95% prediction interval test and percent deviation of actual values from predicted ones proved the validity of the elucidated models. The OF was a transfersomal formula with desirability of 0.866 and showed promising results in ex-vivo permeation study. [ABSTRACT FROM AUTHOR]

Despite its broad-spectrum antifungal properties, voriconazole has many side effects when administered systemically. The aim of this work was to develop an ethosomal topical delivery system for voriconazole and test its potential to enhance the antifungal properties and skin delivery of the drug. Voriconazole was encapsulated into various ethosomal preparations and the effect of phospholipid and ethanol concentrations on the ethosomes properties were evaluated. The ethosomes were evaluated for drug encapsulation efficiency, particle size and morphology and antifungal efficacy. Drug permeability and deposition were tested in rat abdominal skin. Drug encapsulation efficiency of up to 46% was obtained and it increased with increasing the phospholipid concentration, whereas the opposite effect was observed for the ethanol concentration. The ethosomes had a size of 420–600 nm and negative zeta potential. The particle size of the ethosomes increased by increasing their ethanol content. The ethosomes achieved similar inhibition zones againstAspergillus flavusat a 2-fold lower drug concentration compared with drug solution in dimethyl sulfoxide. Theex vivodrug permeability through rat abdominal skin was ∼6-fold higher for the ethosomes compared with the drug hydroalcoholic solution. Similarly, the amount of drug deposited in the skin was higher for the ethosomes and was dependent on the ethanol concentration of the ethosomes. These results confirm that voriconazole ethosomal preparations are promising topical delivery systems that can enhance the drug antifungal efficacy and improve its skin delivery. [ABSTRACT FROM PUBLISHER]

Liposomes containing a certain amount of ethanol are often referred to in the literature as ethosomes. Liposomes vary in size from 25 nm to 25,000 nm. Ethosomes are defined as lipids composed of phospholipids, ethanol, or isopropyl alcohol in quite high concentrations, and water. They enable active substances to reach the deep skin layers or even the general circulation. The structure of ethosomes allows for an increased penetration of the drug through two effects: the ethanolic effect and the ethosomal effect. Ethosomes can be obtained using three methods: the hot method, the cold method, and the classic method of mechanical dispersion. The literature describes many of the therapeutic groups of drugs that can be enclosed in ethosomal formulations. These include anti-viral drugs, antineoplastic drugs, antifungal drugs, hypnotic drugs, hormones, and many others. Ethosomes show important practical advantages compared to classic liposomes. It is necessary to conduct research with regard to real pharmaceutical systems using advanced physicochemical techniques.

Purpose: To design, develop and evaluate an Azelaic acid encapsulated Ethosomal formulation for acne. Methods: Encapsulated ethosomes were prepared by three methods viz. hot method, cold method and thin film hydration method. Central Composite Design was employed for optimisation of ethosomal formulations. Concentrations of phospholipid, cholesterol and ethanol were selected as independent variables and their effect on the dependent variables (Entrapment Efficiency and Drug Diffused) was studied. The optimised vesicular carriers were evaluated for vesicle size, entrapment efficiency, in-vitro and ex-vivo diffusion studies, anti-microbial activity, skin irritation studies and stability studies as per ICH guidelines. Ethosomal formulations with varying soya phosphatidylcholine, cholesterol and ethanol were prepared. Results: Vesicles were spherical, unilamellar with a smooth surface. The optimised formulation showed a vesicle size of 4.25 ± 1.35 μm and entrapment efficiency of 91.86 ± 2.25%. In-vitro and exvivo drug diffusion of the ethosomal gel was compared with a conventional gel and a marketed cream. The developed novel formulation exhibited enhanced anti-acne activity as compared to conventional gel and a marketed cream. Conclusion: We can conclude that the ethosomal formulation is an efficient vesicular carrier system for topical delivery. [ABSTRACT FROM AUTHOR]

Transdermal drug delivery system is a type of convenient drug delivery system where drug goes to the systemic circulation through the protective barrier i.e. Skin. In transdermal drug delivery system (TDDS) specific dose of medicaments are mainly administered as transdermal patch or skin patch. Over the years it has showed promising result in comparison to oral drug delivery system as it eliminates gastrointestinal interferences and first pass metabolism of the drug but the main drawback of TDDS is it encounters the barrier properties of the Stratum Corneum i.e. only the lipophilic drugs having molecular weight < 500 Da can pass through it. So now a days, liposomes, niosomes, transferosomes and ethosomes are used to increase the permeability of drug through stratum corneum. Ethosomes have been found to be much more efficient in delivering drug to the skin, than that of liposomes or hydro-alcoholic solution. Present review addresses about ethosomes. [ABSTRACT FROM AUTHOR]

Skin acts as a major target as well as a principal barrier for topical or transdermal drug delivery. Despite many advantages of this system, the major obstacle is the low diffusion rate of drugs across the stratum corneum. Ethosomes as novel vesicles in transdermal drug delivery show significant effects on drug penetration through the biological membrane. Ethosomes are phospholipid-based elastic nanovesicles containing a high content of ethanol (20-45%). Ethosomal systems are much more efficient in delivering substances to the skin in the terms of quantity and depth, than either conventional liposomes or hydroalcoholic solutions. Enhanced delivery of bioactive molecules through the skin and cellular membranes by means of an ethosomal carrier opens numerous challenges and opportunities for the research and future development of novel improved therapies. [ABSTRACT FROM AUTHOR]

Abstract: The growing focus on nanotechnology and the increased use of nano-sized structures, e.g. vesicles, in topical formulations has led to safety concerns. We have investigated the sensitizing capacity and penetration properties of a fluorescent model compound, rhodamine B isothiocyanate (RBITC), when administered in micro- and nano-scale vesicle formulations. The sensitizing capacity of RBITC was studied using the murine local lymph node assay (LLNA) and the skin penetration properties were compared using diffusion cells in combination with two-photon microscopy (TPM). The lymph node cell proliferation, an indicator of a compounds sensitizing capacity, increased when RBITC was applied in lipid vesicles as compared to an ethanol:water (Et:W) solution. Micro-scale vesicles showed a slightly higher cell proliferative response compared to nano-scale vesicles. TPM imaging revealed that the vesicle formulations improved the skin penetration of RBITC compared to the Et:W solution. A strong fluorescent region in the stratum corneum and upper epidermis implies elevated association of RBITC to these skin layers when formulated in lipid vesicles. In conclusion, the results indicate that there could be an elevated risk of sensitization when haptens are delivered in vehicles containing lipid vesicles. Although the size of the vesicles seems to be of minor importance, further studies are needed before a more generalized conclusion can be drawn. It is likely that the enhanced sensitizing capacity is a consequence of the improved penetration and increased formation of hapten–protein complexes in epidermis when RBITC is delivered in ethosomal formulations. [Copyright &y& Elsevier]

[Display omitted] The skin embodies a relatively large and readily accessible surface area to absorb a drug through a non-invasive procedure. The vesicular carrier systems such as liposomes, ethosomes, and transethosomes have been explored as non-invasive systems for transdermal delivery of drugs. In the present study, different vesicular carriers were prepared by the thin-film hydration method with modification, and various parameters like size, elasticity, and release profiles were evaluated. Ethosomes and transethosomes have shown the smaller size of 362.21 ± 55.76 and 314.34 ± 41.21 nm, with deformity of 19.34% and 25.04%, respectively, compared with liposomes. The FTIR study of the skin before and after the application of vesicular formulation was performed. The ethosomes and transethosomes changed the orthorhombic phase to the liquid crystalline phase to move the vesicular carrier with the drug to cross the stratum corneum (SC) of the skin. The thermotropic behaviour of drug and vesicular carrier ingredients was studied using differential scanning calorimetry (DSC). Fluorescence images of vesicular-skin permeation have revealed that ethosome and transethosome formulation have shown deeper penetration across the SC and epidermis. The in vitro drug release from the ethosomes and transethosomes has shown 93.34 ± 1.23% and 95.45 ± 2.67% of drug release using Franz diffusion cell and porcine skin as a membrane. The nanostructured flexible vesicular carrier containing ethanol alone and a combination of ethanol and edge activator is a perfect carrier for drug penetration to the deeper skin layer and maintaining the sustained release of drug for a prolonged time. [ABSTRACT FROM AUTHOR]

• Extraction of phospholipids through CO2-ethanol is an efficient two-step process. • Fractions rich in phospholipids can be obtained from studied by-products. • Camelina press-cake and scallop byproducts are interesting sources of phospholipids. • Extracts rich in Phopsholipids are able to self-assemble in liposomes or ethosomes. Selective extraction of phospholipids (PLs) from camelina press cake and scallop by-products was investigated using Supercritical Fluid Extraction at 45 °C, 25 MPa, with (2–30%) ethanol (EtOH) as co-solvent. A two-step process consisting of a first extraction with CO 2 + 7% EtOH to eliminate neutral lipids followed by a second extraction with CO 2 + 30% EtOH led to extracts containing up to 40% of the PLs initially present in the matrix. The variation of the extraction conditions made it possible to recover up to 90% of PLs. The extracts enriched in PLs were able to self-assemble to form liposomes. Ethosomes, with smaller size, were also obtained when EtOH remained in the extracts. [ABSTRACT FROM AUTHOR]