ethosomes

乙醇体
  • 文章类型: Journal Article
    维甲酸维甲酸维甲酸(FENR)是用于预防乳腺癌复发的有前途的化合物,但由于溶解性差和生物利用度低而面临挑战。这项研究探讨了含有FENR负载的醇质体的溶解微针(MNs)的发展,用于微创乳腺癌化学预防,旨在加强本地药物分销。乙醇体使用乙醇配制,丙二醇,大豆卵磷脂,水,和聚山梨酯80胶束。通过将聚合物粉末直接添加到乙醇体悬浮液中,由聚(乙烯醇)和聚(乙烯基吡咯烷酮)水凝胶产生MN,减少制造时间和成本。使用两种方法将乙醇体加载到高密度模具中:1)仅在针区,和2)在针区域和基板。动态光散射证实了水凝胶和MN中的纳米结构。基于胶束的醇质体在15分钟内溶解了MNs,与其他MN的30分钟相比。皮肤沉积研究显示使用方法2的更大的药物沉积(高达10μg/片)和增强的FENR的皮肤渗透(高达40μg)。在大鼠体内研究表明,口服导致血浆FENR水平低于10ng/g在前三小时,而MN管理延迟交付,在48小时达到52ng/g的最大血浆浓度。来自MNs的FENR的皮肤沉积从第1天的3μg/g减少到最后一天的<0.3μg/g。这项研究表明,MNs是一种潜在的微创剂型,用于递送FENR,为乳腺癌化学预防提供了新的途径。
    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.
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  • 文章类型: Journal Article
    从最早的日子开始,人们在世界各地广泛使用草药治疗。植物化学和植物生理学的发展使人们有可能了解许多药用植物产品的化学成分和生物学特性。由于某些挑战,如大分子量和低生物利用度,草药提取物的一些成分不用于治疗目的。有人建议,可以将草药和纳米技术结合起来,通过降低剂量要求和不良反应以及增加治疗活性来增强植物提取物的益处。利用纳米技术,活性成分可以以足够的浓度递送并运输到目标作用部位。常规治疗不能满足这些要求。这篇综述的重点是不同的皮肤病和纳米技术为基础的草药,已用于治疗它们。
    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.
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  • 文章类型: Journal Article
    目的:氧化锌纳米颗粒(ZnONPs)广泛应用于当今的个人护理产品中,尤其是防晒霜,作为紫外线照射的保护者。然而,他们有一些潜在毒性的报道。二氧化硅广泛用于笼罩着ZnONPs以降低其潜在的毒性。维生素C衍生物,抗坏血酸磷酸镁(MAP),是一种有效的抗氧化剂,可以有效地保护人类皮肤免受紫外线照射和氧化应激的有害影响。二氧化硅涂覆的ZnONP和MAP纳米囊泡的组合可以具有针对皮肤光损伤的潜在协同保护作用。
    方法:合成了二氧化硅包覆的ZnONPs和MAP纳米囊泡(乙醇体和囊泡),制定,并评估为局部凝胶。通过组织病理学和免疫组织化学研究,在小鼠中评估了这些凝胶制剂对紫外线照射的光保护作用。进行了分面临床研究,以比较单独或与MAP纳米囊泡组合使用二氧化硅包覆的ZnONP的效果。评估了它们的光保护作用,使用Antera3D®相机,黑色素水平,粗糙度指数和皱纹深度。
    结果:二氧化硅包覆的ZnONPs与MAP纳米囊泡结合时,可保护小鼠皮肤免受紫外线照射,并降低促炎细胞因子的表达,NF-κB.临床上,二氧化硅包覆ZnONPs,单独或与MAP纳米囊泡结合,可能对降低黑色素水平有显著影响,粗糙度指数和皱纹深度具有较高的组合效果。
    结论:二氧化硅涂覆的ZnONP和MAP纳米囊泡的复合材料可能是一种有前途的化妆品配方,用于保护皮肤免受光损伤迹象,如色素沉着过度,粗糙度,和皱纹。
    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.
    CONCLUSIONS: 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.
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  • 文章类型: Journal Article
    文献中描述了约24种不同的脂质囊泡,其类似于囊泡系统如脂质体。脂质体样结构通过将某些两亲性脂质与合适的稳定剂组合而形成。自从他们的发现和分类以来,自组装的脂质体样结构作为活性药物递送载体引起了研究人员的好奇心。
    这项综合研究包括使用PubMed等电子数据库进行深入的文献检索,科学直接和谷歌学者,重点研究脂质体和脂质体样结构,直到2024年在文献中讨论,它们的大小,好处,缺点,制备方法,表征和药物应用。
    药物组,立方体,乙醇体,跨丝小体,和基因组,所有的脂质体样结构,具有最大的潜力,因为它们具有较小的尺寸和高的承载能力,易于吸收,和治疗炎症性疾病的能力。基因组是未来的,因为它对DNA/基因运输的亲和力,这是当今治疗的重点领域。
    这篇评论将批判性地分析其组成,准备程序,药物封装技术,药物装载,释放机构,以及所有脂质体样结构的相关应用,通过为在制药行业中探索新型药物输送系统铺平道路,强调它们的潜在益处,增强彼此之间和传统载体的功效。
    UNASSIGNED: 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.
    UNASSIGNED: 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.
    UNASSIGNED: 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.
    UNASSIGNED: 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.
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  • 文章类型: Journal Article
    本研究旨在开发和优化karanjin负载的乙醇粒纳米凝胶制剂,并在咪喹莫特诱导的动物模型中评估其缓解银屑病症状的功效。.这些载有karanjin的乙醇纳米凝胶,配制以增强药物渗透到皮肤中及其表皮保留。Karanjin由于其潜在的肛门牛皮癣活性而被用来配制乙醇体。使用冷方法,使用32个全因子设计来配制乙醇体以优化制剂组分。使用两个独立变量X1:乙醇浓度和X2:磷脂浓度制备9批次,而囊泡尺寸(Y1)和包封效率百分比(Y2)被选择为因变量。发现所有因变量均具有统计学意义。优化的乙醇悬浮液(B3)的囊泡尺寸为334±2.89nm,包封率为94.88±1.24%,并显示出良好的稳定性。通过透射电子显微镜(TEM)分析,囊泡的形态呈球形,表面光滑。X-射线衍射(XRD)分析证实药物以无定形状态存在于乙醇体制剂中。将优化的乙醇体掺入到卡波姆934中以开发易于在皮肤上应用的纳米凝胶。纳米凝胶经历了各种参数的表征,包括铺展性,粘度,pH值,可挤出性,和药物含量百分比。与市售制剂和纯药物相比,该脂质体制剂显着增强了karanjin的皮肤渗透,并增加了该药物在银屑病皮肤中的表皮滞留。皮肤保留研究显示,醇脂质体纳米凝胶制剂在6h内具有48.33%的表皮保留。在体内,karanjin的抗银屑病活性在银屑病中表现出显着的改善,如PSI分级所示,皮肤厚度和结垢逐渐减少。因此,制备的乙醇纳米凝胶是改善karanjin局部递送以更好地治疗银屑病的潜在载体。 .
    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.
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  • 文章类型: Journal Article
    甘草提取物因其抗氧化和抗炎特性而广为人知,可以改善伤口愈合过程。这项工作的目的是通过使用基于西班牙扫帚柔性纤维素织物的生态可持续伤口敷料,通过浸渍G.glabra提取物负载的乙醇体,缩短愈合过程的时间。通过LC-DAD-MS/MS进行G.glabra提取物的化学分析,并且使用乙醇注射方法获得其在醇质体中的包封。脂质囊泡的特征在于大小,多分散指数,截留效率,zeta电位,和稳定性。体外释放研究,生物相容性,对3个T3成纤维细胞进行划痕试验。此外,西班牙扫帚敷料的结构及其吸收伤口渗出物的能力通过同步加速器X射线相衬显微断层扫描(SR-PCmicroCT)进行了表征。乙醇体表现出良好的包封效率,纳米尺寸,与游离提取物相比,随着时间的推移具有良好的稳定性和多酚的缓慢释放,并且没有细胞毒性。最后,结果表明,载有G.glabra醇质体的西班牙扫帚伤口敷料能够通过减少伤口愈合时间来加速伤口闭合。总而言之,西班牙扫帚伤口敷料可能是生物医学应用的潜在新绿色工具。
    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.
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  • 文章类型: Journal Article
    Prinsepiautilis种子油(PUSO)是从PrinsepiautilisRogle种子中获得的天然药物,已用于治疗皮肤病。本研究旨在制备具有高载药量的醇质体作为水溶性透皮载体,以增强PUSO的透皮递送。使用冷方法制备了负载PUSO的乙醇体(PE),并通过正交实验设计进行优化,以包封效率(EE)为因变量。优化配方制备的PEs具有良好的稳定性,在透射电子显微镜(TEM)下具有球形,平均粒径为39.12±0.85nm,PDI为0.270±0.01,zeta电位为-11.3±0.24mV,EE为95.93±0.43%。与PUSO悬浮液相比,PE显著增加了PUSO的皮肤沉积(P<0.001)。此外,最佳配方对紫外线B(UVB)照射相关的小鼠皮肤宏观和组织病理学变化具有明显的改善作用。因此,PE代表了治疗UVB引起的皮肤炎症的一种有前途的治疗方法,具有工业化的潜力。
    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.
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  • 文章类型: Journal Article
    Ethosome为常规药物递送系统所面临的挑战提供了独特的解决方案。与传统的脂质体和其他纳米载体相比,乙醇体表现出独特的改善药物吸收的能力,克服了经皮给药系统的主要限制。它们柔软灵活的纳米囊泡结构有助于更快的渗透,导致明显更高的透皮通量。这项科学研究有效地穿越了作为创新药物输送系统的醇体不断变化的格局。通过进行彻底的比较分析,我们发现了将它们与其他纳米载体区分开来的独特特征,提供对其独特优势的见解。该研究还包括对对绩效有复杂影响的变量的详细分析,阐明运输机制和解决先进的方面是精制药物输送策略的关键。这份全面的概述强调了乙醇体是医学的未来,为各种疾病的安全有效治疗提供了一个充满希望的未来,影响无数人的生活。
    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.
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  • 文章类型: Journal Article
    经皮药物递送是用于施用治疗剂的有吸引力且患者友好的途径。然而,皮肤的天然屏障,角质层,限制了许多药物的通过,限制其有效性。为了克服这一挑战,研究人员开发了各种纳米载体来增强药物通过皮肤的渗透。跨细胞小体,一种新颖且有前途的药物递送系统,已成为改善透皮给药的创新解决方案。跨核小体是两种已建立的纳米载体的杂种:醇核体和传递体。醇质体是基于脂质的囊泡,可以容纳亲脂性和亲水性药物,而传递体是可变形的脂质囊泡,旨在增强皮肤渗透。经塞小体结合了两个系统的优点,使它们成为有效透皮给药的理想候选者。它们由磷脂组成,乙醇,和水,表现出很高的灵活性,使它们能够挤压角质层的紧密连接。这篇摘要回顾了跨丝体的关键特征,包括他们的组成,制备方法,行动机制,表征参数,和前景。此外,最近的进展和应用的转塞体在提供各种治疗剂,如镇痛药,抗炎药,荷尔蒙,和护肤品,正在探索。增强的跨囊体的皮肤渗透能力可以潜在地减少全身副作用并提高患者的依从性。使它们成为透皮给药领域的有价值的工具。总之,跨囊体代表了克服经皮药物递送挑战的有前途的平台。它们独特的特性使药物能够有效地通过皮肤渗透,提供了一种更加可控和有效的方法来管理各种药物和化妆品。该摘要突出了转体作为经皮药物递送领域的有价值的补充的潜力,并为该领域的进一步研究和开发铺平了道路。
    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.
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  • 文章类型: Journal Article
    近年来,经皮给药系统(TDDS)受到了广泛的关注。TDDS是将活性组分运输到皮肤以通过皮肤局部或全身递送药物的柔性系统。在三个主要的皮肤层中,最外层,称为角质层(SC),防止嗜水细菌和高分子量药物的进入。挑战在于成功地通过皮肤输送药物,穿过角质层。近年来,基于脂质的囊泡递送系统的普及由于其递送亲水性和疏水性药物的能力而增加。醇质体是由磷脂制成的专门囊泡,可以储存大量的乙醇。乙醇体结构和物质促进皮肤渗透性和生物利用度。这篇文章涵盖了乙醇体成分,类型,药物输送技术,稳定性,和安全。除此之外,还讨论了醇质体在广泛疾病的药物递送应用中的应用的深入分析。这篇综述文章强调了乙醇体的不同方面,比如他们的合成,表征,上市配方,TDDS的最新进展,和应用。
    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.
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