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1.
J Nanobiotechnology ; 22(1): 584, 2024 Sep 28.
Artículo en Inglés | MEDLINE | ID: mdl-39334378

RESUMEN

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.


Asunto(s)
Psoriasis , Quinazolinas , Absorción Cutánea , Piel , Psoriasis/tratamiento farmacológico , Animales , Ratones , Humanos , Piel/metabolismo , Piel/efectos de los fármacos , Quinazolinas/farmacología , Quinazolinas/farmacocinética , Quinazolinas/química , Homeostasis/efectos de los fármacos , Fosfolípidos/química , Liposomas/química , Portadores de Fármacos/química , Administración Tópica , Queratinocitos/efectos de los fármacos , Queratinocitos/metabolismo , Administración Cutánea , Sistemas de Liberación de Medicamentos/métodos , Metabolismo de los Lípidos/efectos de los fármacos , Masculino , Ratones Endogámicos BALB C , Células HaCaT , Tamaño de la Partícula
2.
J Control Release ; 374: 76-88, 2024 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-39111598

RESUMEN

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.


Asunto(s)
Neoplasias de la Mama , Fenretinida , Fenretinida/administración & dosificación , Fenretinida/farmacocinética , Fenretinida/química , Animales , Femenino , Neoplasias de la Mama/prevención & control , Absorción Cutánea , Ratas Sprague-Dawley , Micelas , Lípidos/química , Piel/metabolismo , Administración Cutánea , Nanopartículas/química , Nanopartículas/administración & dosificación , Hidrogeles/química , Hidrogeles/administración & dosificación , Agujas , Solubilidad , Anticarcinógenos/administración & dosificación , Anticarcinógenos/farmacocinética , Anticarcinógenos/química , Sistemas de Liberación de Medicamentos
3.
Pharm Res ; 41(7): 1475-1491, 2024 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-38992234

RESUMEN

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.


Asunto(s)
Ácido Ascórbico , Dióxido de Silicio , Piel , Protectores Solares , Rayos Ultravioleta , Óxido de Zinc , Óxido de Zinc/química , Óxido de Zinc/farmacología , Óxido de Zinc/administración & dosificación , Animales , Dióxido de Silicio/química , Rayos Ultravioleta/efectos adversos , Ratones , Humanos , Ácido Ascórbico/química , Ácido Ascórbico/farmacología , Ácido Ascórbico/administración & dosificación , Ácido Ascórbico/análogos & derivados , Protectores Solares/química , Protectores Solares/farmacología , Protectores Solares/administración & dosificación , Piel/efectos de los fármacos , Piel/efectos de la radiación , Piel/metabolismo , Femenino , Antioxidantes/farmacología , Antioxidantes/química , Antioxidantes/administración & dosificación , Nanopartículas/química , Envejecimiento de la Piel/efectos de los fármacos , Envejecimiento de la Piel/efectos de la radiación , Masculino , Adulto , Persona de Mediana Edad
4.
Pharmaceutics ; 16(7)2024 Jun 28.
Artículo en Inglés | MEDLINE | ID: mdl-39065566

RESUMEN

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.

5.
Biomed Mater ; 19(5)2024 Jul 11.
Artículo en Inglés | MEDLINE | ID: mdl-38955335

RESUMEN

This study aimed to develop and optimize karanjin-loaded ethosomal nanogel formulation and evaluate its efficacy in alleviating symptoms of psoriasis in an animal model induced by imiquimod. These karanjin-loaded ethosomal nanogel, were formulated to enhance drug penetration into the skin and its epidermal retention. Karanjin was taken to formulate ethosomes due to its potential ani-psoriatic activity. Ethosomes were formulated using the cold method using 32full factorial designs to optimize the formulation components. 9 batches were prepared using two independent variablesX1: concentration of ethanol andX2: concentration of phospholipid whereas vesicle size (Y1) and percentage entrapment efficiency (Y2) were selected as dependent variables. All the dependent variables were found to be statistically significant. The optimized ethosomal suspension (B3) exhibited a vesicle size of 334 ± 2.89 nm with an entrapment efficiency of 94.88 ± 1.24% and showed good stability. The morphology of vesicles appeared spherical with smooth surfaces through transmission electron microscopy analysis. X-ray diffraction analysis confirmed that the drug existed in an amorphous state within the ethosomal formulation. The optimized ethosome was incorporated into carbopol 934 to develop nanogel for easy application on the skin. The nanogel underwent characterization for various parameters including spreadability, viscosity, pH, extrudability, and percentage drug content. The ethosomal formulation remarkably enhanced the skin permeation of karanjin and increased epidermal retention of the drug in psoriatic skin compared to marketed preparation and pure drug. A skin retention study showed that ethosomal nanogel formulation has 48.33% epidermal retention in 6 h.In vivo,the anti-psoriatic activity of karanjin ethosomal nanogel demonstrated significant improvement in psoriasis, indicated by a gradual decrease in skin thickness and scaling as reflected in the Psoriasis Severity Index grading. Therefore, the prepared ethosomal nanogel is a potential vehicle for improved topical delivery of karanjin for better treatment of psoriasis.


Asunto(s)
Nanogeles , Psoriasis , Absorción Cutánea , Psoriasis/tratamiento farmacológico , Psoriasis/patología , Animales , Nanogeles/química , Lecitinas/química , Piel/metabolismo , Piel/patología , Tamaño de la Partícula , Liposomas/química , Polietilenglicoles/química , Glycine max/química , Ratas , Masculino , Imiquimod/química , Portadores de Fármacos/química , Polietileneimina/química , Difracción de Rayos X , Etanol/química , Acrilatos
6.
J Microencapsul ; 41(6): 456-478, 2024 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-38990129

RESUMEN

AIMS: 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. METHODOLOGY: 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. RESULTS: 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. CONCLUSION: 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.


Asunto(s)
Portadores de Fármacos , Liposomas , Liposomas/química , Portadores de Fármacos/química , Humanos , Sistemas de Liberación de Medicamentos , Animales
7.
Int J Biol Macromol ; 272(Pt 2): 132883, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38838898

RESUMEN

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.


Asunto(s)
Vendajes , Celulosa , Glycyrrhiza , Extractos Vegetales , Spartium , Cicatrización de Heridas , Animales , Ratones , Glycyrrhiza/química , Extractos Vegetales/química , Extractos Vegetales/farmacología , Cicatrización de Heridas/efectos de los fármacos , Celulosa/química , Celulosa/farmacología , Spartium/química , Células 3T3
8.
AAPS PharmSciTech ; 25(5): 122, 2024 May 30.
Artículo en Inglés | MEDLINE | ID: mdl-38816546

RESUMEN

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.


Asunto(s)
Administración Cutánea , Tamaño de la Partícula , Aceites de Plantas , Semillas , Piel , Rayos Ultravioleta , Animales , Rayos Ultravioleta/efectos adversos , Ratones , Aceites de Plantas/farmacología , Aceites de Plantas/administración & dosificación , Aceites de Plantas/química , Piel/efectos de los fármacos , Piel/metabolismo , Piel/patología , Absorción Cutánea/efectos de los fármacos , Química Farmacéutica/métodos , Enfermedades de la Piel/tratamiento farmacológico , Enfermedades de la Piel/etiología , Masculino , Sistemas de Liberación de Medicamentos/métodos
9.
Pharm Nanotechnol ; 2024 May 28.
Artículo en Inglés | MEDLINE | ID: mdl-38808706

RESUMEN

Ethosome offers a unique solution to the challenges faced by conventional drug delivery systems. In comparison to traditional liposomes and other nanocarriers, ethosomes exhibit a unique ability to improve drug absorption, overcoming a major limitation in the Transdermal Drug Delivery System. Their soft and flexible nano-vesicular structure facilitates faster permeation, resulting in significantly higher transdermal flux. This scientific investigation effectively traverses the changing landscape of ethosomes as an innovative drug delivery system. By conducting a thorough comparative analysis, we uncover the distinct characteristics that set them apart from other nanocarriers, offering insights into their distinct advantages. The study also includes a detailed analysis of the variables that have a complex impact on performance, elucidating transport mechanisms and addressing advanced facets pivotal for refined drug delivery strategies. This comprehensive overview highlights ethosomes as a future of medicine, offering a promising future for the safe and effective treatment of diverse diseases, impacting numerous lives.

10.
Pharm Nanotechnol ; 2024 May 15.
Artículo en Inglés | MEDLINE | ID: mdl-38757163

RESUMEN

Transdermal drug delivery is an attractive and patient-friendly route for administering therapeutic agents. However, the skin's natural barrier, the stratum corneum, restricts the passage of many drugs, limiting their effectiveness. To overcome this challenge, researchers have developed various nanocarriers to enhance drug penetration through the skin. Transethosomes, a novel and promising drug delivery system, have emerged as an innovative solution for improving transdermal drug delivery. Transethosomes are a hybrid of two established nanocarriers: ethosomes and transfersomes. Ethosomes are lipid-based vesicles that can accommodate lipophilic and hydrophilic drugs, while transfersomes are deformable lipid vesicles designed to enhance skin penetration. Transethosomes combine the advantages of both systems, making them ideal candidates for efficient transdermal drug delivery. They are composed of phospholipids, ethanol, and water and exhibit high flexibility, enabling them to squeeze through the tight junctions of the stratum corneum. This abstract reviews the key characteristics of transethosomes, including their composition, preparation methods, mechanisms of action, characterization parameters, and prospects. Moreover, the recent advancements and applications of transethosomes in delivering various therapeutic agents, such as analgesics, anti-inflammatories, hormones, and skincare products, are explored. The enhanced skin penetration capabilities of transethosomes can potentially reduce systemic side effects and improve patient compliance, making them a valuable tool in the field of transdermal drug delivery. In conclusion, transethosomes represent a promising platform for overcoming the challenges of transdermal drug delivery. Their unique properties enable efficient drug permeation through the skin, offering a more controlled and effective means of administering a wide range of pharmaceutical and cosmetic products. This abstract highlights the potential of transethosomes as a valuable addition to the field of transdermal drug delivery and paves the way for further research and development in this area.

11.
J Liposome Res ; : 1-18, 2024 Apr 27.
Artículo en Inglés | MEDLINE | ID: mdl-38676416

RESUMEN

Transdermal 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.

12.
Cureus ; 16(3): e56061, 2024 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-38618434

RESUMEN

Introduction The research aimed to develop a robust, high-performance liquid chromatography (HPLC) analytical method for the quantitative assessment of rebamipide encapsulated in ethosomes. Rebamipide, a quinolinone derivative, holds promise as a therapeutic agent for dry eye, but challenges such as low bioavailability and vision clouding post-installation have prompted innovative approaches. Encapsulation in ethosomes, lipid-based nanovesicles, offers a potential solution to enhance ocular bioavailability. Materials and methods The study focused on creating a specific, linear, accurate, precise, and robust HPLC method, addressing entrapment efficiency (%EE), drug content, and drug release of rebamipide in prepared ethosomes. Statistical validation followed International Conference of Harmonization (ICH) specifications. The method's parameters were evaluated within a concentration range of 4-24 µg/ml, with recovery rates indicating accuracy and low % relative standard deviation (RSD) values confirming precision. Limits of detection (LOD) and quantification (LOQ) for rebamipide were determined. Results After preparing the ethosome dosage form by film hydrating method for rebamipide, the rebamipide entrapment efficiency in ethosomes was established at 76% ± 7, while the drug content was found to be 93% ± 6. The drug release process demonstrated zero-order kinetics and five different models of kinetics were applied for a comprehensive analysis. The method exhibited excellent system suitability, specificity, and linearity. Recovery rates for rebamipide ranged from 90% to 100%, and repeatability was confirmed by low %RSD values. The LOD and LOQ for rebamipide were determined to be 1.04 µg/mL and 3.16 µg/mL, respectively. Conclusion The developed HPLC method proved suitable for the quantitative determination of rebamipide in ethosomes, offering rapid and accurate analysis. The results underscore the method's specificity, accuracy, and precision within the specified concentration range. Overall, the validated method contributes to the advancement of ocular drug delivery systems, providing a reliable analytical tool for pharmaceutical research.

13.
J Biomed Mater Res B Appl Biomater ; 112(3): e35394, 2024 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-38433621

RESUMEN

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.


Asunto(s)
Etanol , Quempferoles , Humanos , Quempferoles/farmacología , Rastreo Diferencial de Calorimetría , Liberación de Fármacos , Cinética
14.
J Microencapsul ; 41(3): 204-225, 2024 May.
Artículo en Inglés | MEDLINE | ID: mdl-38456667

RESUMEN

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.


Asunto(s)
Absorción Cutánea , Piel , Administración Cutánea , Piel/metabolismo , Sistemas de Liberación de Medicamentos/métodos , Liposomas/química , Portadores de Fármacos/química
15.
Curr Drug Deliv ; 2024 Feb 29.
Artículo en Inglés | MEDLINE | ID: mdl-38425111

RESUMEN

Phytoconstituents have been widely used since ancient times to form a complex with phospholipids due to their various therapeutic actions. Despite having strong pharmacodynamic efficiency, numerous phytoconstituents have shown lower in vivo bioavailability and few adverse effects. Phytochemicals soluble in water exhibit poor absorption, leading to a limited therapeutic impact. Phytosome nanotechnology overcomes this limitation by creating a bound of phytochemicals with phospholipids. This method exhibits improved absorption because phytosomes inhibit significant herbal extract components from being degraded by gastric juices and gut flora. This improves bioavailability, increases clinical benefit, and ensures delivery to tissues without compromising nutritional stability. This review also aims to highlight those vesicular systems that could be used in phytosome technology. Additionally, this review highlights the preparation, advantage, characterization, applications, and recent development of phytosome and ethosome with a list of recent patents and marketed formulations and their uses.

16.
Pharmaceutics ; 16(3)2024 Feb 22.
Artículo en Inglés | MEDLINE | ID: mdl-38543203

RESUMEN

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.

17.
Microbiol Spectr ; 12(4): e0424723, 2024 Apr 02.
Artículo en Inglés | MEDLINE | ID: mdl-38415658

RESUMEN

Cutaneous 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. IMPORTANCE: Cutaneous 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.


Asunto(s)
Candida albicans , Candidiasis , Humanos , Animales , Ratones , Farnesol/farmacología , Farnesol/metabolismo , Farnesol/uso terapéutico , Administración Cutánea , Candidiasis/tratamiento farmacológico , Candidiasis/microbiología , Antifúngicos/farmacología , Biopelículas
18.
J Colloid Interface Sci ; 662: 342-356, 2024 May 15.
Artículo en Inglés | MEDLINE | ID: mdl-38354561

RESUMEN

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.

19.
BMC Pharmacol Toxicol ; 25(1): 21, 2024 Feb 26.
Artículo en Inglés | MEDLINE | ID: mdl-38409046

RESUMEN

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.


Asunto(s)
Alcaloides , Sesquiterpenos , Piel , Espectrometría de Masas en Tándem , Ratones , Animales , Cromatografía Liquida , Administración Cutánea , Liposomas
20.
Curr Drug Deliv ; 2024 Jan 24.
Artículo en Inglés | MEDLINE | ID: mdl-38279739

RESUMEN

BACKGROUND: Polyphenols are naturally occurring compounds having more than one hydroxy functional group. They are ubiquitous secondary plant metabolites possessing a wide range of pharmacological activity. Brightly colored fruits and vegetables are the natural source of polyphenols. Majorly, they possess antioxidant, anti-inflammatory and antimicrobial properties which make them suitable candidates to target skin related disorders. OBJECTIVE: This study is focused to explore the potential of polyphenols loaded nanovesicles for skin related disorders. The aim of the study is to review the applicability and efficacy of different vesicular systems encapsulated with various classes of polyphenols for skin related disorders, thus opening the opportunity for future studies based on these drug delivery systems. METHOD: Web of Science, PubMed, Scopus database, and the search engine Google Scholar were accessed for the literature search. The results were then filtered based on the titles, abstracts, and accessibility of the complete texts. RESULTS: The expository evaluation of the literature revealed that various nanovesicles like liposomes, niosomes, ethosomes and transferosomes incorporating polyphenol have been formulated to address issues pertaining to delivery across the skin. These developed nano vesicular systems have shown improvement in the physicochemical properties and pharmacological action. CONCLUSION: Polyphenol based nano-vesicular formulations have proved to be an effective system for topical delivery and henceforth, they might curtail the use of other skin therapies having limited applicability.

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