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Acne vulgaris is a common dermatologic disorder that affects approximately 85% of teenagers, which significantly impacts the quality of life in adolescents. It is a chronic disease of the sebaceous follicles that is multifactorial in etiology. Topical treatment is the first choice for mild and moderate acne, while systemic therapy is reserved for severe and certain moderate cases. Topical treatments include retinoids (e.g., tretinoin and adapalene), antibiotics (e.g., clindamycine), and other agents (e.g., benzoyl peroxide and azelaic acid), often applied in combination. The mechanisms of action include antimicrobial, anti-inflammatory, and keratolytic activities, as well as sebum secretion reduction, and the normalization of follicular keratinization. However, these topical agents commonly induce side effects, such as dryness, burning, stinging, peeling, redness, erythema, and photosensitivity. Therefore, there is a need to reduce the side effects of anti-acne drugs, while maintaining or enhancing their therapeutic effectiveness. This article aims to comprehensively outline nanotechnology strategies, particularly the use of phospholipid-based nanocarriers like liposomes and related vesicles, to enhance therapeutic efficacy, skin tolerability, and patient compliance in the treatment of acne vulgaris. In addition, novel active ingredients encapsulated in vesicles beyond those recommended in official guidelines are discussed.

The retinoid fenretinide (FENR) is a promising compound for preventing breast cancer recurrence but faces challenges due to poor solubility and low bioavailability. This study explores the development of dissolving microneedles (MNs) containing FENR-loaded ethosomes for minimally invasive breast cancer chemoprevention, aiming to enhance local drug distribution. Ethosomes were formulated using ethanol, propylene glycol, soya lecithin, water, and polysorbate 80 micelles. MNs were created from poly(vinyl alcohol) and poly(vinylpyrrolidone) hydrogels by adding polymer powder directly into ethosomes suspensions, reducing manufacturing time and cost. Two methods were used to load ethosomes into high-density moulds: 1) only in the needle area, and 2) in both the needle area and baseplate. Dynamic light scattering confirmed nanostructures in the hydrogels and MNs. Micelle-based ethosomes dissolved MNs in 15 min, compared to 30 min for other MNs. Skin deposition studies showed greater drug deposition (up to 10 μg/patch) and enhanced skin permeation of FENR (up to 40 μg) with Method 2. In-vivo studies in rats demonstrated that oral administration resulted in plasma FENR levels below 10 ng/g in the first three hours, whereas MN administration delayed delivery, reaching a maximum plasma concentration of 52 ng/g at 48 h. Skin deposition of FENR from MNs decreased from 3 μg/g on day 1 to <0.3 μg/g by the last day. This study indicates that MNs are a potential minimally invasive dosage form for delivering FENR, offering a new approach for breast cancer chemoprevention. [Display omitted] [ABSTRACT FROM AUTHOR]

Psoriasis is a chronic, relapsing, and refractory immune-mediated skin disease with the etiology and pharmaceutical targets remaining unsatisfactorily addressed. Topical herbal-derived compounds, such as tryptanthrin (Tryp), have been considered as an alternative therapy for psoriasis due to their lower costs and fewer side effects compared to other therapies. However, the effectiveness of topically administered drugs is substantially limited by the thickened pathological skin barrier and the low bioavailability of drugs in the deeper layers of the lesion. Ethosomes, being a novel phospholipid-based vesicle system with high content of ethanol, have been implicated in enhancing topical drug absorption and restoring psoriatic lesions. In this study, taking advantages of ethosomes as a soft and malleable drug carrier, we constructed the Tryp-loaded ethosome (Tryp-ES) through a one-step microfluidics-based technique. The optimal formulation of Tryp-ES was achieved by adding amino-acid-derived surfactant sodium lauroyl glutamate, and Tryp-ES exhibited homogeneous particle size and favorable stability at room temperature. In vitro evaluations showed that Tryp of Tryp-ES could be easily internalized into cells and accumulated in cell nuclei, hence inhibited the abnormally proliferated keratinocytes by inducing apoptosis. In vivo and in vitro assessment using psoritic skin of mice revealed that Tryp-ES had preferred skin retention and permeation of loaded drugs within the initial 1 h of topical administration, which could be attributed to transient disintegrations of cell membranes by ethosomes, thus improved cellular fluidity and permeability. Notably, a synergistic effect of ethosomes and Tryp was found in psoriatic mice. Tryp-ES-treated mice showed substantially ameliorated symptoms of psoriasis and reduced pathological alterations due to hyperplasia, inflammation and angiogenesis, without detectable local or systemic toxicities. Interestingly, lipidomics analysis confirmed that the supplementation of phospholipids, as in the form of ethosome vehicles, was an alterantive strategy to relieve psoriatic pathologies. Taken together, this study provides a novel impact for ethosomal topical delivery of Tryp and underlines their potential as an effective therapy for the management of psoriasis. [ABSTRACT FROM AUTHOR]

There are around 24 distinct lipid vesicles described in the literature that are similar to vesicular systems such as liposomes. Liposome-like structures are formed by combining certain amphiphilic lipids with a suitable stabiliser. Since their discovery and classification, self-assembled liposome-like structures as active drug delivery vehicles captured researchers' curiosity. This comprehensive study included an in-depth literature search using electronic databases such as PubMed, ScienceDirect and Google Scholar, focusing on studies on liposome and liposomes like structure, discussed in literature till 2024, their sizes, benefits, drawback, method of preparation, characterisation and pharmaceutical applications. Pharmacosomes, cubosomes, ethosomes, transethosomes, and genosomes, all liposome-like structures, have the most potential due to their smaller size with high loading capacity, ease of absorption, and ability to treat inflammatory illnesses. Genosomes are futuristic because of its affinity for DNA/gene transport, which is an area of focus in today's treatments. This review will critically analyse the composition, preparation procedures, drug encapsulating technologies, drug loading, release mechanism, and related applications of all liposome-like structures, highlighting their potential benefits with enhanced efficacy over each other and over traditional carriers by paving the way for exploring novel drug delivery systems in the Pharma industry. [ABSTRACT FROM AUTHOR]

Abstract Psoriasis is a chronic, relapsing, and refractory immune-mediated skin disease with the etiology and pharmaceutical targets remaining unsatisfactorily addressed. Topical herbal-derived compounds, such as tryptanthrin (Tryp), have been considered as an alternative therapy for psoriasis due to their lower costs and fewer side effects compared to other therapies. However, the effectiveness of topically administered drugs is substantially limited by the thickened pathological skin barrier and the low bioavailability of drugs in the deeper layers of the lesion. Ethosomes, being a novel phospholipid-based vesicle system with high content of ethanol, have been implicated in enhancing topical drug absorption and restoring psoriatic lesions. In this study, taking advantages of ethosomes as a soft and malleable drug carrier, we constructed the Tryp-loaded ethosome (Tryp-ES) through a one-step microfluidics-based technique. The optimal formulation of Tryp-ES was achieved by adding amino-acid-derived surfactant sodium lauroyl glutamate, and Tryp-ES exhibited homogeneous particle size and favorable stability at room temperature. In vitro evaluations showed that Tryp of Tryp-ES could be easily internalized into cells and accumulated in cell nuclei, hence inhibited the abnormally proliferated keratinocytes by inducing apoptosis. In vivo and in vitro assessment using psoritic skin of mice revealed that Tryp-ES had preferred skin retention and permeation of loaded drugs within the initial 1 h of topical administration, which could be attributed to transient disintegrations of cell membranes by ethosomes, thus improved cellular fluidity and permeability. Notably, a synergistic effect of ethosomes and Tryp was found in psoriatic mice. Tryp-ES-treated mice showed substantially ameliorated symptoms of psoriasis and reduced pathological alterations due to hyperplasia, inflammation and angiogenesis, without detectable local or systemic toxicities. Interestingly, lipidomics analysis confirmed that the supplementation of phospholipids, as in the form of ethosome vehicles, was an alterantive strategy to relieve psoriatic pathologies. Taken together, this study provides a novel impact for ethosomal topical delivery of Tryp and underlines their potential as an effective therapy for the management of psoriasis.

Introduction: Ethosomes are non-invasive drug delivery systems that enable drugs to enter the bloodstream or deep layers of the skin and these are phospholipid-based elastic Nano vesicles with a high ethanol concentration (20-45%). In vesicular systems, ethanol is a well-known permeability enhancer that has been utilized to produce elastic Nano vesicles. Quercetin (QT) is one of the most prevalent polyphenolic flavonoids found in fruits and vegetables, and it has several biological and health-promoting effects in a variety of disorders. The current study sought to formulate ethosomal gel and hydrogel as topical drug delivery. Materials and Methods: The ethosomes formulations were made by hot method using phospholipid and ethanol (20% to 40%) and then tested for particle size, PDI, percentage entrapment efficiency and Scanning Electron Microscopy (SEM), in vitro drug release study, zeta potential, Then quercetin-loaded ethosomal gel and quercetin hydrogel were prepared and tested for pH, spreadability, viscosity, washability, drug content, visual observation, and extrudability. Results and Discussion: FT-IR investigations demonstrated that there was no interaction between the medication and the excipients. Compared to regular hydrogel, the results suggested that ethosomal gel might be a useful transdermal delivery system for quercetin in the treatment of inflammation. [ABSTRACT FROM AUTHOR]

Objective: Zinc Oxide nanoparticles (ZnO NPs) are used widely in nowadays personal care products, especially sunscreens, as a protector against UV irradiation. Yet, they have some reports of potential toxicity. Silica is widely used to cage ZnO NPs to reduce their potential toxicity. Vitamin C derivative, Magnesium Ascorpyl Phosphate (MAP), is a potent antioxidant that can efficiently protect human skin from harmful impacts of UV irradiation and oxidative stress. The combination of silica coated ZnO NPs and MAP nanovesicles could have potential synergistic protective effect against skin photodamage. Methods: Silica coated ZnO NPs and MAP nanovesicles (ethosomes and niosomes) were synthesized, formulated, and evaluated as topical gels. These gel formulations were evaluated in mice for their photoprotective effect against UV irradiation through histopathology and immuno-histochemistry study. Split-face clinical study was conducted to compare the effect of application of silica coated ZnO NPs either alone or combined with MAP nanovesicles. Their photoprotective action was evaluated, using Antera 3D® camera, for melanin level, roughness index and wrinkles depth. Results: Silica coated ZnO NPs when combined with MAP nanovesicles protected mice skin from UV irradiation and decreased the expression of the proinflammatory cytokines, NF-κB. Clinically, silica coated ZnO NPs, alone or combined with MAP nanovesicles, could have significant effect to decrease melanin level, roughness index and wrinkles depth with higher effect for the combination. Conclusion: A composite of silica coated ZnO NPs and MAP nanovesicles could be a promising cosmetic formulation for skin protection against photodamage signs such as hyperpigmentation, roughness, and wrinkles. [ABSTRACT FROM AUTHOR]

Since the earliest days, people have been employing herbal treatments extensively around the world. The development of phytochemical and phytopharmacological sciences has made it possible to understand the chemical composition and biological properties of a number of medicinal plant products. Due to certain challenges like large molecular weight and low bioavailability, some components of herbal extracts are not utilized for therapeutic purposes. It has been suggested that herbal medicine and nanotechnology can be combined to enhance the benefits of plant extracts by lowering dosage requirements and adverse effects and increasing therapeutic activity. Using nanotechnology, the active ingredient can be delivered in an adequate concentration and transported to the targeted site of action. Conventional therapy does not fulfill these requirements. This review focuses on different skin diseases and nanotechnology-based herbal medicines that have been utilized to treat them. [ABSTRACT FROM AUTHOR]

Thymoquinone (TQ), a bioactive compound found in Nigella sativa seeds, possesses diverse therapeutic properties for skin conditions. However, formulating TQ presents challenges due to its hydrophobic nature and chemical instability, which hinder its skin penetration. Transethosomes, as a formulation, offer an environment conducive to enhancing TQ's solubility, stability, and skin permeation. To optimize TQ transethosomal formulations, we introduced a combination of ionic and nonionic surfactants, namely Tween 20 and sodium lauryl sulfate (SLS) or sodium lauroyl glutamate (SLG). Surfactants play a crucial role in stabilizing the formulation, reducing aggregation, improving biocompatibility, and minimizing potential toxicity. We fine-tuned the formulation composition and gained insights into its interfacial behavior using the Langmuir monolayer technique. This method elucidated the interfacial properties and behavior of phospholipids in ethosome and transethosome formulations. Our findings suggest that monolayer studies can serve as the initial step in selecting surfactants for nanocarrier formulations based on their interfacial dilational rheology studies. It was found that the addition of surfactant to the formulation increased the elasticity considering the capability of transethosomes to significantly decrease their radius when permeating the skin barrier. The results of the dilational rheology experiments were most relevant to drug permeation through the skin for the largest amplitude of deformation. The combination of Tween 20 and SLS efficiently modified the rheological behavior of lipids, increasing their elasticity. This conclusion was supported by in vitro studies, where formulation F2 composed of Tween 20 and SLS demonstrated the highest permeation after 24 h (300.23 µg/cm2). Furthermore, the F2 formulation showed the highest encapsulation efficiency (EE) of 94%, surpassing those of the control and ethosomal formulations. Additionally, this transethosomal formulation exhibited antimicrobial activity against S. aureus, with a zone of inhibition of 26.4 ± 0.3 mm. Importantly, we assessed the cytotoxicity of both ethosomes and transethosomes at concentrations ranging from 3.5 µM to 50 µM on HaCaT cell lines and found no cytotoxic effects compared to TQ hydroethanolic solution. These results suggest the potential safety and efficacy of TQ transethosomal formulations. [ABSTRACT FROM AUTHOR]

Prinsepia utilis seed oil (PUSO) is a natural medication obtained from Prinsepia utilis Rogle seed, which has been used for the treatment of skin diseases. The study aims to prepare ethosomes with high drug loading as a water-soluble transdermal vehicle to enhance the transdermal delivery of PUSO. PUSO-loaded ethosomes (PEs) were prepared using a cold method, and optimized by an orthogonal experimental design with entrapment efficiency (EE) as the dependent variable. The PEs prepared with the optimized formulation showed good stability, with a spherical shape under transmission electron microscopy (TEM), average particle size of 39.12 ± 0.85 nm, PDI of 0.270 ± 0.01, zeta potential of -11.3 ± 0.24 mV, and EE of 95.93 ± 0.43%. PEs significantly increased the skin deposition of PUSO compared to the PUSO suspension (P < 0.001). Moreover, the optimum formula showed significant ameliorative effects on ultraviolet B (UVB) irradiation-associated macroscopic and histopathological changes in mice skin. Therefore, PEs represent a promising therapeutic approach for the treatment of UVB-induced skin inflammation, with the potential for industrialization. [ABSTRACT FROM AUTHOR]

[Display omitted] • The effects of destruction and reassembly of vesicular structure of niosomes as a result of purification by centrifugation. • Significant loss of the encapsulated cargo due to centrifugation. • Mechanism and energy landscape of niosome reassembly. • Elastic niosomes (ethosomes) as a way to decrease a destruction of nanocarriers in the mechanical fields and preserve the content of the water core. This paper presents, for the first time, evidence for vesicle destruction and payload loss at the stage of purification of niosome dispersions by centrifugation, an important operation in the assembly of vesicular materials. The ability of niosomes of different compositions to reassemble, i.e., to restore the vesicular structure after destruction in the field of centrifugal forces, was demonstrated by dynamic light scattering and fluorescence spectroscopy. The kinetics of reassembly of vesicular structures is determined by the strength of the centrifugal field and the composition of niosomes. In contrast to ternary compositions, where particle size and modality are essentially unchanged after redispersion of the precipitate resulting from centrifugation, niosome dispersions containing anionic dicetyl phosphate includes micron-sized particles after redispersion, which vary in size over a wide range throughout the observation period. The reassembly process is complicated by the presence of charge on the surface of the niosomes. Elastic niosomes - ethosomes have been synthesised which, due to the high deformability of the shells, are less susceptible to destruction in the centrifugal field and retain the contents of the aqueous core. Using the "energy landscape" approximation, it is shown that vesicular structures assembled during hydration and reassembled after their centrifugation occupy different positions in the energetic pathway of their preparation. The results obtained should also be taken into account when determining the entrapment efficiency, since this procedure uses centrifugation to separate the load. It is important to note that the physical stability of niosomes, which is usually considered in terms of the functional activity of particles, is manifest and should be considered at the material preparation stage. [ABSTRACT FROM AUTHOR]

Ethosomes, which are liposomes like structures, mainly composed primarily of ethanol, have attracted considerable attention due to their potential to enhance the drug permeation via skin. The article discusses the formulation and preparation methods of ethosomes, offering insights into the various factors that influence their size, shape, and stability. Moreover, it explores the techniques used to assess the physicochemical properties of ethosomes and their impact on drug delivery effectiveness. The article also elucidates the mechanism by which ethosomes enhance skin permeation, emphasising their ability to modify the lipid structure and fluidity of the stratum corneum. Additionally, the review investigates the applications of ethosomes in diverse drug delivery scenarios, including the delivery of small molecules, peptides, and phytoconstituents. It highlights the potential of ethosomes to improve drug bioavailability, extend drug release, and achieve targeted delivery to specific skin layers or underlying tissues. [ABSTRACT FROM AUTHOR]

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]

The use of herbal medications has been increasing in recent years due to their perceived safety and efficacy. However, the delivery of these medications can be challenging due to their poor solubility and bioavailability. Ethosomes, which are lipid-based vesicular carriers, have been shown to enhance the delivery of various drugs, including herbal medications. In this review, we will discuss the potential of using ethosomal formulations to improve the delivery of herbal medications. We will explore the advantages of using ethosomes, such as their ability to penetrate the skin and enhance drug absorption, and the challenges associated with their formulation and stability. Additionally, we will highlight recent studies that have investigated the use of ethosomes for delivering various herbal medications, including curcumin, resveratrol and quercetin. Overall, the use of ethosomes has the potential to revolutionize the delivery of herbal medications, providing patients with more effective and efficient treatment options. Challenges in the field, such as formulation optimization, regulatory considerations and scale-up, are addressed. Future directions for research and development are outlined, emphasizing advanced formulation technologies, biocompatible materials, personalized medicine and clinical translation. [ABSTRACT FROM AUTHOR]

Transdermal drug delivery has gained significant attention as a non-invasive and convenient method for administering drugs. However, the stratum corneum, the outermost layer of the skin, poses a significant barrier to drug permeation. To overcome this challenge, vesicular carriers have emerged as promising systems for enhancing drug delivery through the skin. This review highlights recent advances in the development of vesicular carriers for transdermal drug delivery. Liposomes, niosomes, transfersomes, ethosomes, and solid lipid nanoparticles are among the commonly used vesicular carriers. These carriers offer advantages such as improved drug solubility, prolonged drug release, and enhanced drug stability. Additionally, they can encapsulate a wide range of drugs, including hydrophilic and lipophilic compounds. Various strategies have been employed to optimize vesicular carriers for transdermal drug delivery. These include modifying the vesicle composition, size, and surface charge to enhance skin penetration. The incorporation of penetration enhancers, such as surfactants, has also been explored to improve drug permeation across the skin. Furthermore, advancements in nanotechnology have led to the development of novel vesicular carriers, such as nanostructured lipid carriers and elastic liposomes. These carriers offer improved drug loading capacity, sustained release profiles, and enhanced skin penetration. Moreover, the use of vesicular carriers has shown promise in delivering a wide range of therapeutic agents, including small molecules, peptides, proteins, and genetic material. The ability to encapsulate and deliver these diverse drug entities opens new possibilities for transdermal drug delivery in various therapeutic areas. [ABSTRACT FROM AUTHOR]

Background: Tocopherols are well‐known antioxidant and moisturizing agent. Tocopherol succinate (TS) are widely used in many skin products especially used in anti‐aging and skin whitening product formulation. Aim: We previously reported the successful synthesis and preliminary characterizations of stable TS ethosomal gels (TSEG) (DOI: 10.1111/jocd.14907). Herein, we develop and further characterize TSEG to enhance the stability of the developed formulation with increased permeation through skin. Methods: Cold method technique was used to prepare TS ethosomes. The developed ethosomal vesicle size was 250 nm, which allowed TS to penetrate through the stratum corneum layer and act on melanocytes. For stability study was assessed by thermogravimetric analysis (TGA) by placing TSEG and unloaded/control ethosomal gel (CEG) at various temperature conditions, that is, 8°C, 25°C, 40°C, and 40°C ± 75% RH for 3 months. Organoleptic evaluation was done in terms of color, odor, and phase separation. Transmission electron microscopy (TEM), Fourier Transform infrared spectroscopy (FTIR), x‐ray diffraction spectroscopy (XRD), zeta potential (ZP) and particle size (PS) was used for TSEG physical characterizations. In vitro dissolution and ex‐vivo permeation studies (using Franz diffusion cell) were performed for both TSEG and CEG formulations. Human women (N = 34) were used to evaluate in vivo biophysical parameters including erythema, melanin, moisture content, sebum level, and skin elasticity. Results: Developed formulation was highly thermostable during the 3 months. Erythema, melanin, and sebum level decreased while marked improvement (p < 0.05) in moisture content and elasticity have been observed for the developed TSEG. Conclusion: The developed TSEG formulation was found to be efficient, safe (no adverse effects observed), stable (at least for 3 months), and easy to use for topical application with improved skin complexation and skin integrity. [ABSTRACT FROM AUTHOR]

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 (33)). 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/cm2 was determined and compared with pure KMP (118.46 ± 0.3 μg/cm2) 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. [ABSTRACT FROM AUTHOR]

This study aimed to design and evaluate the transdermal permeation of Huperzine A ethosomes gel in vitro. Huperzine A ethosomes were prepared using the injection method, and their physical and chemical properties were characterized. A comparison was made between Huperzine A ethosomes gel, ordinary gel, and cream. The Franz diffusion cell test on mouse abdominal skin was conducted, and Huperzine A concentration was determined using LC-MS/MS. Transdermal volume, skin retention, and transdermal rate were used to assess the percutaneous permeability of the three preparations. Results demonstrated that Huperzine A ethosomes gel exhibited significantly higher accumulative permeation, transdermal rate, and skin retention compared to ordinary gel and cream. The findings suggest that Huperzine A ethosomes gel, with its controllable quality and favorable transdermal absorption properties, holds potential as a safe option for clinical administration. [ABSTRACT FROM AUTHOR]

The skin's protective mechanisms, in some cases, are not able to counteract the destructive effects induced by UV radiations, resulting in dermatological diseases, as well as skin aging. Nutlin-3, a potent drug with antiproliferative activity in keratinocytes, can block UV-induced apoptosis by activation of p53. In the present investigation, ethosomes and transethosomes were designed as delivery systems for nutlin-3, with the aim to protect the skin against UV damage. Vesicle size distribution was evaluated by photon correlation spectroscopy and morphology was investigated by cryogenic transmission electron microscopy, while nutlin-3 entrapment capacity was evaluated by ultrafiltration and HPLC. The in vitro diffusion kinetic of nutlin-3 from ethosomes and transethosomes was studied by Franz cell. Moreover, the efficiency of ethosomes and transethosomes in delivering nutlin-3 and its protective role were evaluated in ex vivo skin explants exposed to UV radiations. The results indicate that ethosomes and transethosomes efficaciously entrapped nutlin-3 (0.3% w/w). The ethosome vesicles were spherical and oligolamellar, with a 224 nm mean diameter, while in transethosome the presence of polysorbate 80 resulted in unilamellar vesicles with a 146 nm mean diameter. The fastest nutlin-3 kinetic was detected in the case of transethosomes, with permeability coefficients 7.4-fold higher, with respect to ethosomes and diffusion values 250-fold higher, with respect to the drug in solution. Ex vivo data suggest a better efficacy of transethosomes to promote nutlin-3 delivery within the skin, with respect to ethosomes. Indeed, nutlin-3 loaded transethosomes could prevent UV effect on cutaneous metalloproteinase activation and cell proliferative response. [ABSTRACT FROM AUTHOR]

Background: In a world where hair loss, acne, and skin whitening are common concerns, ethosomes emerge as a captivating breakthrough in cosmetic drug delivery. Method: This review provides a comprehensive overview of the ethosomal system and assesses its potential as an effective nanocarrier for delivering active ingredients to the skin. The focus is on exploring their applications in various pathologies, particularly skin disorders such as acne, hair loss, and skin pigmentation. Results: Ethosomes are a novel type of vesicular nanocarrier composed of high concentrations of ethanol (20‐45%) and phospholipids. Their unique structure and composition make them an ideal choice for transporting active ingredients through the skin, offering targeted and effective treatment. The inclusion of ethanol in ethosomes' composition gives them distinctive properties, including flexibility, deformability, and stability, facilitating deep penetration into the skin and enhancing medication deposition. Moreover, ethosomes improved theoverall drug‐loading capacity, and specificity of target treatment Conclusion: Ethosomes represent a unique and suitable approach for delivering active cosmetic ingredients in the treatment of hair loss, acne, and skin whitening, presenting a versatile alternative to traditional dermal delivery systems. Despite the challenges associated with their complex preparation and sensitivity to temperature and humidity, the remarkable potential benefits of ethosomes cannot be ignored. Further research is crucial to unlock their full potential, understand their limitations, and refine their formulations and administration methods. Ethosomes hold the promise of transforming the way we address these cosmetic concerns, offering an exciting glimpse into the future of advanced skincare solutions. [ABSTRACT FROM AUTHOR]

Diabetes mellitus is a concern of disorder globally and which is increasing continuously. Diabetic complications lead to physical, mental and societal issues to patients. Oral medications are being prescribed but these have problems like frequent dosing, side effects and non-patient compliance. Insulin therapy is also problematic due to injectable route of delivery. Dose missing of these treatments lead to fluctuations in blood glucose levels which cause severe adverse effects. Recent developments have shown the potential of transdermal drug administration in association with nanoformulations for improving the efficacy and safety of anti-diabetic medications. Nanotechnology offers modification of size and surface characteristics of nanocarriers which enhances the drug permeation through biological barriers. Transdermal drug delivery in conjunction with nanocarriers provide enhanced permeation, improved bioavailability and sustained effect with reduction in adverse effects. This article first presents the current scenarios of diabetes mellitus and important aspects of transdermal drug delivery systems. In later sections, a detailed description (pharmaceutical and preclinical characteristics) of various nanoformulation assisted transdermal drug delivery systems (polymeric nanoparticles, ethosomes, nanostructured lipid carriers, solid lipid nanoparticles, microemulsions, liposomes, niosomes, nanoemulsions, transethosomes and transfersomes) have been reviewed. Transdermal drug delivery in conjunction with nanoformulations can be utilized for the better management and control of diabetes. [ABSTRACT FROM AUTHOR]

Psoriasis is an auto-immune condition with high keratinocyte hyperproliferation due to lower p53 and p22 levels. Tacrolimus, an immune suppressor, is considered one of the most effective drugs in suppressing psoriasis. Systematic administration of tacrolimus often leads to challenging side effects, namely increased infection risk, renal toxicity, neurological symptoms such as tremors and headaches, gastrointestinal disturbances, hypertension, skin-related problems, etc. To address this, a nanocarrier-based formulation of tacrolimus along with inclusion of hyaluronic acid was developed. The optimization and formulation of ethosomes via the ethanol injection technique were done based on the Box-Behnken experimental design. The results revealed hyaluronic acid–based tacrolimus ethosomes (HA-TAC-ETH) had nanometric vesicle size (315.7 ± 2.2 nm), polydispersity index (PDI) (0.472 ± 0.07), and high entrapment efficiency (88.3 ± 2.52%). The findings of drug release and skin permeation showed sustained drug release with increased dermal flux and enhancement ratio. The effectiveness of HA-TAC-ETH was confirmed in an imiquimod (5%)–prompted psoriasis model. The skin irritation score and Psoriasis Area and Severity Index (PASI) score indicated that HA-TAC-ETH gel has validated a decline in the entire factors (erythema, edema, and thickness) in the imiquimod-induced psoriasis model in contrast with TAC-ETH gel and TAC ointment. The fabricated HA-TAC-ETH opt gel proved to be safe and effective in in vivo studies and could be employed to treat psoriasis further. [ABSTRACT FROM AUTHOR]

Although the introduction of glycerosomes has enriched strategies for efficient transdermal drug delivery, the inclusion of cholesterol as a membrane stabilizer has limited their clinical application. The current study describes the development and optimization of a new type of glycerosome (S-glycerosome) that is formed in glycerol solution with β-sitosterol as the stabilizer. Moreover, the transdermal permeation properties of lappaconitine (LA)-loaded S-glycerosomes and peppermint oil (PO)-mediated S-glycerosomes (PO-S-glycerosomes) are evaluated, and the lipid alterations in the stratum corneum are analyzed via lipidomics. The LA-loaded S-glycerosomes prepared by the preferred formulation from the uniform design have a mean size of 145.3 ± 7.81 nm and an encapsulation efficiency of 73.14 ± 0.35%. Moreover, the addition of PO positively impacts transdermal flux, peaking at 0.4% (w/v) PO. Tracing of the fluorescent probe P4 further revealed that PO-S-glycerosomes penetrate deeper into the skin than S-glycerosomes and conventional liposomes. Additionally, treatment with PO-S-glycerosomes alters the isoform type, number, and composition of sphingolipids, glycerophospholipids, glycerolipids, and fatty acids in the stratum corneum, with the most notable effect observed for ceramides, the main component of sphingolipids. Furthermore, the transdermal administration of LA-loaded PO-S-glycerosomes improved the treatment efficacy of xylene-induced inflammation in mice without skin irritation. Collectively, these findings demonstrate the feasibility of β-sitosterol as a stabilizer in glycerosomes. Additionally, the inclusion of PO improves the transdermal permeation of S-glycerosomes, potentially by altering the stratum corneum lipids. [ABSTRACT FROM AUTHOR]

The current research aims to develop and test a system of vesicular drug carriers for topical drug administration of Vitex negundo Linn. to provide sustained drug delivery. The ethosomes of V. negundo Linn. were produced using thin-film hydration, and their in vitro drug release profiles, size, drug content, and other characteristics were examined. To attain the desired results, for drug release and entrapment effectiveness, the composition of lecithin and ethanol was changed to form ethosomes. The ethosomal size of the vesicle of the optimized formulation batch was measured to be the units 13.47 nm with -3.97 mV as zeta potential. The percent drug release of ethosomal gel was 83.24 %, and the percent entrapment efficiency was 89.40 %. The formation of spherically shaped vesicles was confirmed by optical and scanning electron microscopy observations. It was observed that as the ethanol concentration increased, the formulation's in vitro profile for drug release increase, and lipid concentration decreases. [ABSTRACT FROM AUTHOR]

This study delineates the phospholipid flexible carrier systems explored till date primarily for transdermal delivery. Although they are sometimes collectively called as flexible vesicular systems or simple transferosomes. But an articulate understanding of main difference between advanced transferosomes from the conventional one is needed. This paper explains basic difference in various flexible nano carries from transferosomes and the specific terminology used for them. This study is essentially useful for researchers to diligently coin the terms to novel drug delivery systems. [ABSTRACT FROM AUTHOR]

ABSTRACTCutaneous candidiasis, caused by Candida albicans, is a severe and frustrating condition, and finding effective treatments can be challenging. Therefore, the development of farnesol-loaded nanoparticles is an exciting breakthrough. Ethosomes are a novel transdermal drug delivery carrier that incorporates a certain concentration (10–45%) of alcohols into lipid vesicles, resulting in improved permeability and encapsulation rates compared to conventional liposomes. Farnesol is a quorum-sensing molecule involved in morphogenesis regulation in C. albicans, and these ethosomes offer a promising new approach to treating this common fungal infection. This study develops the formulation of farnesol-loaded ethosomes (farnesol-ethosomes) and assesses applications in treating cutaneous candidiasis induced by C. albicans in vitro and in vivo. Farnesol-ethosomes were successfully developed by ethanol injection method. Therapeutic properties of farnesol-ethosomes, such as particle size, zeta potential, and morphology, were well characterized. According to the results, farnesol-ethosomes demonstrated an increased inhibition effect on cells’ growth and biofilm formation in C. albicans. In Animal infection models, treating farnesol-ethosomes by transdermal administration effectively relieved symptoms caused by cutaneous candidiasis and reduced fungal burdens in quantity. We also observed that ethosomes significantly enhanced drug delivery efficacy in vitro and in vivo. These results indicate that farnesol-ethosomes can provide future promising roles in curing cutaneous candidiasis.IMPORTANCECutaneous candidiasis attributed to Candida infection is a prevalent condition that impacts individuals of all age groups. As a type of microbial community, biofilms confer benefits to host infections and mitigate the clinical effects of antifungal treatments. In C. albicans, the yeast-to-hypha transition and biofilm formation are effectively suppressed by farnesol through its modulation of multiple signaling pathway. However, the characteristics of farnesol such as hydrophobicity, volatility, degradability, and instability in various conditions can impose limitations on its effectiveness. Nanotechnology holds the potential to enhance the efficiency and utilization of this molecule. Treatment of farnesol-ethosomes by transdermal administration demonstrated a very remarkable therapeutic effect against C. albicans in infection model of cutaneous candidiasis in mice. Many patients suffering fungal skin infection will benefit from this study.

Since the earliest days, people have been employing herbal treatments extensively around the world. The development of phytochemical and phytopharmacological sciences has made it possible to understand the chemical composition and biological properties of a number of medicinal plant products. Due to certain challenges like large molecular weight and low bioavailability, some components of herbal extracts are not utilized for therapeutic purposes. It has been suggested that herbal medicine and nanotechnology can be combined to enhance the benefits of plant extracts by lowering dosage requirements and adverse effects and increasing therapeutic activity. Using nanotechnology, the active ingredient can be delivered in an adequate concentration and transported to the targeted site of action. Conventional therapy does not fulfill these requirements. This review focuses on different skin diseases and nanotechnology-based herbal medicines that have been utilized to treat them.

Thymoquinone (TQ), a bioactive compound found in Nigella sativa seeds, possesses diverse therapeutic properties for skin conditions. However, formulating TQ presents challenges due to its hydrophobic nature and chemical instability, which hinder its skin penetration. Transethosomes, as a formulation, offer an environment conducive to enhancing TQ’s solubility, stability, and skin permeation. To optimize TQ transethosomal formulations, we introduced a combination of ionic and nonionic surfactants, namely Tween 20 and sodium lauryl sulfate (SLS) or sodium lauroyl glutamate (SLG). Surfactants play a crucial role in stabilizing the formulation, reducing aggregation, improving biocompatibility, and minimizing potential toxicity. We fine-tuned the formulation composition and gained insights into its interfacial behavior using the Langmuir monolayer technique. This method elucidated the interfacial properties and behavior of phospholipids in ethosome and transethosome formulations. Our findings suggest that monolayer studies can serve as the initial step in selecting surfactants for nanocarrier formulations based on their interfacial dilational rheology studies. It was found that the addition of surfactant to the formulation increased the elasticity considering the capability of transethosomes to significantly decrease their radius when permeating the skin barrier. The results of the dilational rheology experiments were most relevant to drug permeation through the skin for the largest amplitude of deformation. The combination of Tween 20 and SLS efficiently modified the rheological behavior of lipids, increasing their elasticity. This conclusion was supported by in vitro studies, where formulation F2 composed of Tween 20 and SLS demonstrated the highest permeation after 24 h (300.23 µg/cm2). Furthermore, the F2 formulation showed the highest encapsulation efficiency (EE) of 94%, surpassing those of the control and ethosomal formulations. Additionally, this transethosomal formulation exhibited antimicrobial activity against S. aureus, with a zone of inhibition of 26.4 ± 0.3 mm. Importantly, we assessed the cytotoxicity of both ethosomes and transethosomes at concentrations ranging from 3.5 µM to 50 µM on HaCaT cell lines and found no cytotoxic effects compared to TQ hydroethanolic solution. These results suggest the potential safety and efficacy of TQ transethosomal formulations.

Vismodegib, first approved in 2012 for the treatment of basal cell carcinoma, is an inhibitor of the Hedgehog signaling pathway that becomes active in certain tumors. However, its secondary effects after oral administration and systemic distribution are severe. In this study, we loaded vismodegib into conventional liposomes, which are typically unable to penetrate the stratum corneum barrier effectively after topical application. We studied its skin penetration when co-administered with empty ethosomes, aimed at transiently disrupting the skin impermeability.The drug was successfully recovered from the deeper viable epidermal layers in an in vitro model. The preparation method for the liposomal formulation is reproducible and relatively straightforward to scale up. Furthermore, it involves the use of biocompatible lipids, thus avoiding the utilization of potentially risky compounds.

Psychiatric and neurodegenerative disorders are amongst the most prevalent and debilitating diseases, but current treatments either have low success rates, greatly due to the low permeability of the blood–brain barrier, and/or are connected to severe side effects. Hence, new strategies are extremely important, and here is where liposome-derived nanosystems come in. Niosomes, transfersomes, and ethosomes are nanometric vesicular structures that allow drug encapsulation, protecting them from degradation, and increasing their solubility, permeability, brain targeting, and bioavailability. This review highlighted the great potential of these nanosystems for the treatment of Alzheimer's disease, Parkinson's disease, schizophrenia, bipolar disorder, anxiety, and depression. Studies regarding the encapsulation of synthetic and natural-derived molecules in these systems, for intravenous, oral, transdermal, or intranasal administration, have led to an increased brain bioavailability when compared to conventional pharmaceutical forms. Moreover, the developed formulations proved to have neuroprotective, anti-inflammatory, and antioxidant effects, including brain neurotransmitter level restoration and brain oxidative status improvement, and improved locomotor activity or enhancement of recognition and working memories in animal models. Hence, albeit being relatively new technologies, niosomes, transfersomes, and ethosomes have already proven to increase the brain bioavailability of psychoactive drugs, leading to increased effectiveness and decreased side effects, showing promise as future therapeutics. [ABSTRACT FROM AUTHOR]

Ethosomes are novel lipid‐based vesicular systems that demonstrate unique improvements in drug delivery with respect to other nanoparticles, especially for transdermal applications. Their high ethanol content strongly improves flexibility and deformability, which allows squeezing through the intercellular spaces without any drug leakage. The ethanol, moreover, contributes to increase the fluidity of the lipids of the cell membranes in dermal layers, allowing an in‐depth penetration of the nanostructures. Moreover, the high ethanol content of ethosomes allows the promotion of the encapsulation of either hydrophilic or lipophilic active agents, a feature particularly useful when it deals with natural extracts, a family of compounds characterized by a huge chemical variability. As a further advantage, being natural extracts often obtained in ethanol‐based solutions, their incorporation in ethosomes makes not necessarily expensive and time‐consuming procedures finalized at solvent removal. Following the initial exploitation of ethosomes, research focuses on the development of variants such as invasomes and transethosomes, which show improved drug encapsulation and delivery capacity. This review provides the state‐of‐the‐art on ethosomal research, with special attention on the encapsulation and delivery of natural extracts and their transdermal delivery. [ABSTRACT FROM AUTHOR]

Many dermatological diseases still do not have an adequate treatment, such as melanoma. The treatments are usually lengthy, complex, with low cure rates and with severe side effects. This leads to low patient compliance, generating recurrence and/or worsening of the disease. Ethosomes, which are phospholipid-based vesicles containing ethanol, have shown great potential as drug delivery systems for the treatment of melanoma and other skin diseases. The unique structure of ethosomes allows for enhanced skin penetration and efficient delivery of therapeutic agents to the target site, improving the efficacy of treatment. The use of ethosomes in melanoma treatment holds promise for overcoming the limitations of conventional therapies, offering the potential for improved patient outcomes, reduced treatment duration, and minimized side effects. In this mini-review we present the advances, challenges, limitations and advantages, and future perspectives of the use of ethosomes in the treatment of the melanoma. [ABSTRACT FROM AUTHOR]

Acne vulgaris is a common dermatologic disorder that affects approximately 85% of teenagers, which significantly impacts the quality of life in adolescents. It is a chronic disease of the sebaceous follicles that is multifactorial in etiology. Topical treatment is the first choice for mild and moderate acne, while systemic therapy is reserved for severe and certain moderate cases. Topical treatments include retinoids (e.g., tretinoin and adapalene), antibiotics (e.g., clindamycine), and other agents (e.g., benzoyl peroxide and azelaic acid), often applied in combination. The mechanisms of action include antimicrobial, anti-inflammatory, and keratolytic activities, as well as sebum secretion reduction, and the normalization of follicular keratinization. However, these topical agents commonly induce side effects, such as dryness, burning, stinging, peeling, redness, erythema, and photosensitivity. Therefore, there is a need to reduce the side effects of anti-acne drugs, while maintaining or enhancing their therapeutic effectiveness. This article aims to comprehensively outline nanotechnology strategies, particularly the use of phospholipid-based nanocarriers like liposomes and related vesicles, to enhance therapeutic efficacy, skin tolerability, and patient compliance in the treatment of acne vulgaris. In addition, novel active ingredients encapsulated in vesicles beyond those recommended in official guidelines are discussed.

Ethosomes are novel lipid‐based vesicular systems that demonstrate unique improvements in drug delivery with respect to other nanoparticles, especially for transdermal applications. Their high ethanol content strongly improves flexibility and deformability, which allows squeezing through the intercellular spaces without any drug leakage. The ethanol, moreover, contributes to increase the fluidity of the lipids of the cell membranes in dermal layers, allowing an in‐depth penetration of the nanostructures. Moreover, the high ethanol content of ethosomes allows the promotion of the encapsulation of either hydrophilic or lipophilic active agents, a feature particularly useful when it deals with natural extracts, a family of compounds characterized by a huge chemical variability. As a further advantage, being natural extracts often obtained in ethanol‐based solutions, their incorporation in ethosomes makes not necessarily expensive and time‐consuming procedures finalized at solvent removal. Following the initial exploitation of ethosomes, research focuses on the development of variants such as invasomes and transethosomes, which show improved drug encapsulation and delivery capacity. This review provides the state‐of‐the‐art on ethosomal research, with special attention on the encapsulation and delivery of natural extracts and their transdermal delivery.

Alpha arbutin is a skin-whitening agent in cosmetics. Structurally, it is 4-hydroxyphenyl-α-glucopyranoside. Ethosomes encourage the formation of lamellar-shaped vesicles with improved solubility and entrapment of whitening agents. The objective of this study was to fabricate an optimized nanostructured ethosomal gel loaded with alpha arbutin for the treatment of skin pigmentation.Different ethosomal suspensions of alpha arbutin were prepared by the cold method. Invitro evaluation included zeta potential, droplet size analysis, polydispersity index, entrapment efficiency (EE), scanning electron microscopy (SEM) and Fourier transform infrared (FTIR) spectroscopy. Stability studies of the optimized ethosomal and control gels were performed for three months under different temperature conditions. The optimized ethosomal gel loaded with alpha arbutin was further analyzed on human volunteers for skin benefits by measuring melanin level, moisture content and elasticity.It was concluded that the optimized formulation had a size, zeta potential, polydispersity index and entrapment efficiency of 196.87 nm, −45.140 mV, 0.217 and 93.458343%, respectively. Scanning electron microscopy (SEM) depicted spherical ethosomal vesicles. Stability data was obtained in terms of pH and conductivity. Rheological analysis revealed non-Newtonian flow. The cumulative drug permeated for ethosomal gel was 78.4%. Moreover, encapsulation of alpha arbutin causes significant improvement in skin melanin, moisture content and elasticity.The overall findings suggested that the arbutin-loaded ethosomal formulation was stable and could be a better approach than conventional formulation for cosmeceutical purposes such as for depigmentation and moisturizing effects.

Objective: This study aimed to develop an innovative ocular delivery system for posaconazole (PSC) using a gellan gum-based in situ ethosomal formulation, addressing the challenges posed by the poor solubility of PSC and the need for an effective treatment for fungal keratitis. Materials and Methods: Ethosomes were prepared using a thin-film hydration method with a mixture of ethanol, soya phosphatidylcholine, and cholesterol. A 32 factorial design was employed, with soya phosphatidylcholine (X1) and cholesterol (X2) concentrations as independent variables, and particle size (Y1) and % entrapment efficiency (Y2) as dependent variables. Compatibility studies using Fourier-transform infrared (FTIR) spectroscopy were conducted to assess potential drug-excipient interactions. Transmission electron microscopy (TEM) analysis was performed to evaluate the morphology of the developed ethosomes. In vitro drug release studies were carried out to investigate the permeation of PSC from plain and loaded ethosomes. Ex vivo studies using a goat cornea model were conducted to evaluate the corneal retention and permeation of the formulations. Results: The optimized F1 batch demonstrated a high % entrapment efficiency of 89.00±1.03% and smaller vesicles with a particle size of 239.4±1.21 nm. FTIR analysis confirmed the absence of drug-excipient interactions. TEM analysis revealed uniform spherical vesicles in the ethosomes. In vitro drug release studies demonstrated the sustained permeation of 81.23% of plain PSC and 51.50% of PSC-loaded ethosomes after 24 h. Ex vivo studies demonstrated the quick permeation of the developed in situ gel formulation in the goat cornea. Conclusion: The developed in-situ gel formulation loaded with PSC-loaded ethosomal vesicles offers a promising ocular delivery system for the effective treatment of deep fungal eye infections. The enhanced solubility, sustained drug release, and efficient corneal permeation of PSC make it a potential therapeutic option for fungal keratitis. Further, investigations and clinical studies are warranted to validate the efficacy and safety of this ocular delivery system. [ABSTRACT FROM AUTHOR]

Hyaluronic Acid (HA) has been applied as an anti-ageing molecule in the form of topical products. Current topical commercial formulations of HA face the limitations of very small and stagnant skin permeation, thereby demanding enduring administration of the formulation to sustain its action. In this study, Lipid-based nanocarriers in the form of ethosomes were formulated in a 1% w/w HA strength and were extensively evaluated in vitro, ex-vivo, and in vivo parameters along with a comparison to it's commercial counterpart. The optimised ethosomes-based HA gel formulation revealed required pH (6.9 ± 0.2), small globule size (1024 ± 9 nm), zeta potential of −6.39 ± 0.2 mV, and 98 ± 1.1% HA content. The ex vivo skin permeation and deposition potenwere conferred on synthetic membrane Strat-M, Human cadaver skin, mice skin, rat skin, and pig skin, and both parameters were found to be much higher in comparison to the commercial topical formulation. Skin deposition capacity of the optimised HA formulation was further confirmed by Scan Electron Microscopy (SEM) and Confocal Laser Scanning Microscopy (CLSM) and it was observed that the developed ethosomal gel formulation got deposited more on the treated skin. The in vivo anti-ageing effect of optimised ethosomal gel on rats was found to be greater when compared to commercial formulation of HA and the developed carrier-based system proved to deliver the HA molecule in very small amounts into the systemic circulation. The results endorse the ethosomal carrier-based formulation of HA as a attractive technique for better local bioavailability of HA. [ABSTRACT FROM AUTHOR]

Nanovesicular carriers called ethosomes are used for dermal delivery. Nanovesicular drug deliveries provide thorough insights into the most up-to-date and complete discussion about the preparation of drugs. Sebaceous glands, hair follicles, and the pilosebaceous unit are all impacted by the chronic inflammatory disorder known as acne vulgaris. It is among the most prevalent dermatological problems in the globe. Water, ethanol in quite high concentrations (up to 50%), and phospholipids are the main components of ethosomes. Due to the presence of ethanol, ethosomes are referred to as "soft vesicles" with fluid bilayers. The vesicle form and content make them able to carry more molecules with a variety of physicochemical qualities to the skin's deep layers. Ethosomal systems have been the subject of intensive study ever since they were initially proposed for a variety of purposes. In addition to the face, the back and chest can also be affected by acne, which can manifest as non-inflammatory lesions, combustible sores, or a mix of these two types. Ethosomes improve the drug's penetration of the skin via transdermal and dermal distribution. A wide range of medications, including peptides and protein compounds, may be delivered via ethosomes. This review is about the ethosomes used for the treatment of acne vulgaris. [ABSTRACT FROM AUTHOR]

A wide range of literature sources report on the potential benefits of transdermal drug delivery. Among these advantages, the following are distinguished – minimal injury, reduction of side effects, and prevention of degradation or metabolism in the gastrointestinal tract or liver. However, transdermal delivery of most molecules often excludes due to the barrier function of the skin, which prevents the penetration of exogenous substances. To overcome this barrier and increase skin absorption, ethosomal complexes use, by means penetration into the deep layers of the skin and/or systemic circulation is possible. This work devotes to the development of a non-invasive method for assessing the depth of penetration by ethosomes with methylene blue (MB) into the skin during application and photodynamic exposure. MB as photosensitizer (PS) was chosen, since there are a sufficient number of publications on its positive effect on the restoration of the cell’s respiratory chain of various organs and therefore the restoration of their metabolism. Besides MB has proven to be an effective PS, destructed pathogenic microbes and viruses, including SARS-CoV-2. However, for more effective Covid-19 therapy and antibiotic-resistant microbial diseases, the penetration of MB into the vascular system of the epidermis or mucous tissue is required. Nowadays, the existing methods for assessing the penetration depth of PS are time consuming and require the use of animal skin or model samples. The LESA-01 BIOSPEC system with specially designed optical adapters that allow assessing the drug fluorescence intensity on skin surface and at a depth of up to 2 mm in the investigation was used.

Challenges associated with topical analgesics and anti-inflammatory drugs include poor drug penetration and retention at the desired lesion site. Therefore, improving these challenges would help to reduce the toxic and side effects caused by drug absorption into the systemic circulation and improve the therapeutic efficacy of topical therapeutic drugs. Pentapeptide (KTTKS) is a signal peptide in skin tissue, it can be recognized and bound by signal recognition particles. In the current study, we successfully prepared novel indomethacin (IMC) loaded KTTKS-modified ethosomes (IMC-KTTKS-Es), and the physicochemical properties and topical efficacy were investigated. Results showed that the prepared IMC-KTTKS-Es displayed a particle size of about 244 nm, a negative charge, good deformability, and encapsulation efficiency (EE) exceeding 80% for IMC, with a sustained release pattern. In vitro percutaneous permeation studies revealed that the skin retention was increased after the drug was loaded in the IMC-KTTKS-Es. Confocal laser scanning microscopy also showed improved skin retention of IMC-KTTKS-Es. In addition, IMC-KTTKS-Es showed improved topical analgesic and anti-inflammatory activity with no potentially hazardous skin irritation. This study suggested that the IMC-KTTKS-Es might be an effective drug carrier for topical skin therapy with a good safety profile.

Ascorbic acid (vitamin C) is an antioxidant that is widely used in cosmetics in skincare products. Due to the excessive low stability of ascorbic acid in cosmetic formulations, the stabilized ascorbic acid derivative, magnesium ascorbyl phosphate (MAP) was formulated as vesicular carriers; ethosomes and niosomes. The aim was to deliver MAP at the intended site of action, the skin, for sufficient time with enhanced permeation to get an effective response. Ethosomes were formulated using a full 32 factorial design to study ethanol and phospholipid concentration effect on ethosomes properties. Niosomes were formulated using 23 factorial designs to study the effect of surfactant type, surfactant concentration and cholesterol concentration on niosomes properties. The prepared formulations were evaluated for their Entrapment efficiency, particle size, polydispersity index, zeta potential and % drug permeated. The optimized ethosomal and niosomal formulations were incorporated into carbopol gel and evaluated for their permeation, skin retention and stability. A comparative split-face clinical study was done between the ethosomal and niosomal formulations for melasma treatment using Antera 3 D® camera. The optimized ethosomal and niosomal gels showed comparable controlled permeation and higher skin retention over their ethosomes and niosomes formulations respectively. Magnesium ascorbyl phosphate ethosomal gel showed clinically and statistically significant melanin level decrease after one month while MAP niosomal gel showed clinically and statistically significant melanin level decrease after six months. A combination of MAP ethosomes and niosomes could be promising skincare formulations for melasma and hyperpigmentation short and long-term treatment.

Despite high efficiency of domperidone (DOM) in prophylaxis of emesis accompanied with radiotherapy and chemotherapy, it still can bother cancer patients by its powerful side effects and difficulty of its oral administration. The study was designed to develop and optimize DOM loaded ethosomal gel for rectal transmucosal delivery. Ethosomal formulations were prepared using a 21, 51 full-factorial design where the impact of lecithin concentration and additives were investigated. The optimum ethosomal vesicles were subsequently incorporated in Carbopol gel base where rheological behavior, spreadability, mucoadhesion, and in vivo pharmacokinetic parameters were studied. Based on Design Expert® software (Stat Ease, Inc., Minneapolis, MN), the optimum formulation illustrated entrapment efficiency of 70.02%±5.52%, and vesicular size of 112 ± 3.3 nm, polydispersity index of 0.32 ± 0.01, zeta potential of −59 ± 0.28 mV, and % drug released after 6 h of 76.30%±2.45%. Moreover, ex vivo permeation through rabbit intestinal mucosa increased four times compared to free DOM suspension. The gel loaded with ethosomes showed excellent mucoadhesion to rectal mucosa. DOM ethosomal gel showed a raise in Cmax and AUC0–48 of DOM by twofolds compared to free DOM gel. The study suggested that ethosomes incorporated in gels could be an efficient candidate for rectal transmucosal delivery of DOM.

This study was performed with the main objective of formulating and evaluating the potential of ethosomesl gel (Etho gel) to deliver nimodipine (NiM) for cardiovascular disease, a potent water insoluble anti-hypertensive drug via skin to reach the deeper layers of skin. The Box-Behnken design (BBD) was used to optimize the NiM-Eth to determine the impact of the independent and depended variables. The effectiveness of drug entrapment, vesicle size, and cumulative drug release were assessed for the NiM loaded ethosomes and NiM-Eth gel using carbopol 934 as a gelling agent. Fourier transform infrared spectroscopy (FTIR), Differential scanning calorimetry (DSC), Power X-ray diffraction (PXRD), and scanning electron microscopy (SEM) analysis were performed and analysed their physicochemical characters. Rat abdomen skin was used to investigate drug permeability and deposition. As compared to marketed products, NiM-Eth gel produced an improved drug permeability in ex vivo experiments. The mean AUC0 to AUC0-∞ of NiM-Eth gel when compared to oral formulation (Nymalize oral preparation) was found to be increased from 4.1 to 5.9 folds which was found to be resulted from first pass effect. Histophatlogical findings revealed that the maximum amount of NiM penetrated the stratum corneum of the skin and create drug depots in the deep layer. In summary, it can be said that NiM might be successfully prepared in NiM-Eth gel for transdermal drug delivery.

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.

In recent years, nanotechnology has a new era of drug delivery for many drug systems. Transdermal drug delivery is one of the few systems that have recently become a major focal point of research. When compared to traditional drug delivery systems, the Transdermal Drug Delivery System (TDDS) has various advantages. Due to the barrier properties of the Stratum Corneum, TDDS has had limited market success. The introduction of ethosomes, which are soft, malleable vesicular carriers containing ethanol and are tailored for enhanced delivery of active agents, has opened up a new area of vesicular research for transdermal drug delivery. According to various reports, ethosomes have a promising future in improving the efficacy of transdermal delivery of various agents. Ethosomes are also useful for the non-invasive delivery of small, medium and large drug molecules. Ethosome preparation is simple, requires no complicated equipment, and can thus be scaled up to industrial levels. The review emphasises introduction to ethosomes, their composition and preparation methods, evaluation, and their efficiency in penetrating the skin and the use of ethosomes in transdermal medication delivery as being more effective than liposomes or hydroalcoholic solution in terms of quantity and depth. [ABSTRACT FROM AUTHOR]