scholarly journals Lipid-Based Nanosystems as a Tool to Overcome Skin Barrier

2021 ◽  
Vol 22 (15) ◽  
pp. 8319
Author(s):  
Maddalena Sguizzato ◽  
Elisabetta Esposito ◽  
Rita Cortesi
Keyword(s):  
Skin Barrier ◽  
Structural Similarity ◽  
Lipophilic Compounds ◽  
Aqueous Dispersions ◽  
Skin Lipids ◽  
Efficient Delivery ◽  
Lipid Nanocarriers ◽  
Mechanism Of Interaction ◽  
Cutaneous Application ◽  
Topical Applications

Skin may be affected by many disorders that can be treated by topical applications of drugs on the action site. With the advent of nanotechnologies, new efficient delivery systems have been developed. Particularly, lipid-based nanosystems such as liposomes, ethosomes, transferosomes, solid lipid nanoparticles, nanostructured lipid carriers, cubosomes, and monoolein aqueous dispersions have been proposed for cutaneous application, reaching in some cases the market or clinical trials. This review aims to provide an overview of the different lipid-based nanosystems, focusing on their use for topical application. Particularly, biocompatible nanosystems able to dissolve lipophilic compounds and to control the release of carried drug, possibly reducing side effects, are described. Notably, the rationale to topically administer antioxidant molecules by lipid nanocarriers is described. Indeed, the structural similarity between the nanosystem lipid matrix and the skin lipids allows the achievement of a transdermal effect. Surely, more research is required to better understand the mechanism of interaction between lipid-based nanosystems and skin. However, this attempt to summarize and highlight the possibilities offered by lipid-based nanosystems could help the scientific community to take advantage of the benefits derived from this kind of nanosystem.

Fucose decorated solid-lipid nanocarriers mediate efficient delivery of methotrexate in breast cancer therapeutics

2016 ◽  
Vol 146 ◽  
pp. 114-126 ◽  
Author(s):  
Neeraj K. Garg ◽  
Bhupinder Singh ◽  
Ashay Jain ◽  
Pradip Nirbhavane ◽  
Rajeev Sharma ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Therapeutics ◽  
Solid Lipid ◽  
Efficient Delivery ◽  
Lipid Nanocarriers

scholarly journals A distributed residue network permits conformational binding specificity in a conserved family of actin remodelers

2021 ◽  
Author(s):  
Theresa Hwang ◽  
Robert A Grant ◽  
Amy E Keating
Keyword(s):  
Cell Invasion ◽  
Structural Similarity ◽  
Cancer Cell Invasion ◽  
High Sequence Identity ◽  
High Affinity ◽  
Sequence Identity ◽  
Binding Partners ◽  
Ciliary Protein ◽  
Mechanism Of Interaction ◽  
A Site

Metazoan proteomes contain many protein families wherein paralogs with high sequence and structural similarity have evolved unique functions and binding profiles. We uncovered a region from ciliary protein PCARE is highly specific to Ena/VASP paralog ENAH, but not VASP and EVL (Hwang et al., 2021). Here, we show that despite binding at a site that is identical between paralogs, PCARE stabilizes a conformation of the EVH1 domain of ENAH that is inaccessible to family members VASP and EVL to achieve its high affinity and ~100-fold specificity. Structure-based modeling rapidly identified seven residues distributed throughout EVL that, when mutated to residues of ENAH, are sufficient to confer high-affinity binding of PCARE. By exploiting the ENAH-specific EVH1 conformation, we rationally designed the tightest and most selective ENAH binder to date, providing a tool for dissecting paralog-specific Ena/VASP functions in processes including cancer cell invasion. Our work uncovers a mechanism of interaction specificity that distinguishes paralogs that share high sequence identity and many common binding partners.

scholarly journals Characterisation of Drug Delivery Efficacy Using Microstructure-Assisted Application of a Range of APIs

Pharmaceutics ◽  
2020 ◽  
Vol 12 (12) ◽  
pp. 1213
Author(s):  
Raha Rahbari ◽  
Ionut Ichim ◽  
Ryan Bamsey ◽  
Jemma Burridge ◽  
Owen J. Guy ◽  
...  
Keyword(s):  
Dissociation Constants ◽  
Skin Barrier ◽  
Acid Dissociation ◽  
Acid Dissociation Constant ◽  
Molecular Weights ◽  
Patch Application ◽  
In Vitro Permeation ◽  
Franz Diffusion Cells ◽  
Topical Applications

Polymer-based solid microstructures (MSts) have the potential to significantly increase the quantity and range of drugs that can be administered across the skin. MSt arrays are used to demonstrate their capacity to bypass the skin barrier and enhance permeability by creating microchannels through the stratum corneum, in a minimally invasive manner. This study is designed to demonstrate the ability of MSts to exceed the current boundaries for transdermal delivery of compounds with different molecular weights, partition coefficients, acid dissociation constants, melting points, and water solubilities. In vitro permeation of a range of selected molecules, including acetyl salicylic acid (aspirin), galantamine, selegiline hydrochloride (Sel-HCl), insulin, caffeine, hydrocortisone (HC), hydrocortisone 21-hemisuccinate sodium salt (HC-HS) and bovine serum albumin (BSA) has been studied across excised porcine skin with and without poke and patch application of MSts. Permeation of the molecules was monitored using Franz diffusion cells over 24 h. MSts significantly increased the permeation of all selected molecules up to 40 times, compared to topical applications of the molecules without MSts. The greatest increase in permeation was observed for caffeine with 70 ± 8% permeation and the lowest enhancement was observed for HC with a 2.4 ± 1.3% increase in permeation. The highest obtained flux was BSA (8133 ± 1365 μg/cm2/h) and the lowest flux observed for HC (11 ± 4 μg/cm2/h). BSA and HC also showed the highest (16,275 ± 3078 μg) and the lowest (73 ± 47 μg) permeation amount after 24 h respectively. MSt-treated skin exhibits greatly increased permeation. The molecule parameters (size, acid dissociation constant, partition coefficient and solubility)—traditional hurdles associated with passive diffusion through intact skin—are overcome using MSt skin treatment.

Dynamics of Skin Barrier Repair following Topical Applications of Miconazole Nitrate

2006 ◽  
Vol 19 (5) ◽  
pp. 290-294 ◽  
Author(s):  
E. Xhauflaire-Uhoda ◽  
V. Vroome ◽  
G. Cauwenbergh ◽  
G.E. Piérard
Keyword(s):  
Skin Barrier ◽  
Miconazole Nitrate ◽  
Barrier Repair ◽  
Skin Barrier Repair ◽  
Topical Applications

Ceramide liposomes for skin barrier recovery: A novel formulation based on natural skin lipids

2021 ◽  
Vol 596 ◽  
pp. 120264
Author(s):  
Aneta Vovesná ◽  
Alexander Zhigunov ◽  
Martin Balouch ◽  
Jarmila Zbytovská
Keyword(s):  
Skin Barrier ◽  
Skin Lipids

scholarly journals Nanodelivery Strategies for Skin Diseases with Barrier Impairment: Focusing on Ceramides and Glucocorticoids

Nanomaterials ◽  
2022 ◽  
Vol 12 (2) ◽  
pp. 275
Author(s):  
Cíntia Almeida ◽  
Patrícia Filipe ◽  
Catarina Rosado ◽  
Catarina Pereira-Leite
Keyword(s):  
Atopic Dermatitis ◽  
Stratum Corneum ◽  
Safety Profile ◽  
Topical Treatment ◽  
Crucial Role ◽  
Skin Diseases ◽  
Skin Barrier ◽  
Treatment Efficiency ◽  
Efficient Delivery ◽  
Water Holding

The human epidermis has a characteristic lipidic composition in the stratum corneum, where ceramides play a crucial role in the skin barrier homeostasis and in water-holding capacity. Several skin diseases, such as atopic dermatitis and psoriasis, exhibit a dysfunction in the lipid barrier with altered ceramide levels and increased loss of transepidermal water. Glucocorticoids are normally employed in the therapeutical management of these pathologies. However, they have shown a poor safety profile and reduced treatment efficiency. The main objective of this review is to, within the framework of the limitations of the currently available therapeutical approaches, establish the relevance of nanocarriers as a safe and efficient delivery strategy for glucocorticoids and ceramides in the topical treatment of skin disorders with barrier impairment.

scholarly journals Systematic Investigation of the Effect of Non-Ionic Emulsifiers on Skin by Confocal Raman Spectroscopy—A Comprehensive Lipid Analysis

Pharmaceutics ◽  
2020 ◽  
Vol 12 (3) ◽  
pp. 223 ◽  
Author(s):  
Yali Liu ◽  
Dominique Jasmin Lunter
Keyword(s):  
Raman Spectroscopy ◽  
Polyethylene Glycol ◽  
Lipid Content ◽  
Deep Understanding ◽  
Skin Barrier ◽  
Fatty Acid Esters ◽  
Skin Barrier Function ◽  
Confocal Raman Spectroscopy ◽  
Skin Lipids ◽  
Confocal Raman

Non-ionic emulsifiers are commonly found in existing pharmaceutical and cosmetic formulations and have been widely employed to enhance the penetration and permeation of active ingredients into the skin. With the potential of disrupting skin barrier function and increasing fluidity of stratum corneum (SC) lipids, we herein examined the effects of two kinds of non-ionic emulsifiers on intercellular lipids of skin, using confocal Raman spectroscopy (CRS) with lipid signals on skin CRS spectrum. Non-ionic emulsifiers of polyethylene glycol alkyl ethers and sorbitan fatty acid esters were studied to obtain a deep understanding of the mechanism between non-ionic emulsifiers and SC lipids. Emulsifier solutions and dispersions were prepared and applied onto excised porcine skin. Water and sodium laureth sulfate solution (SLS) served as controls. SC lipid signals were analysed by CRS regarding lipid content, conformation and lateral packing order. Polyethylene glycol (PEG) sorbitan esters revealed no alteration of intercellular lipid properties while PEG-20 ethers appeared to have the most significant effects on reducing lipid content and interrupting lipid organization. In general, the polyoxyethylene chain and alkyl chain of PEG derivative emulsifiers might indicate their ability of interaction with SC components. HLB values remained critical for complete explanation of emulsifier effects on skin lipids. With this study, it is possible to characterize the molecular effects of non-ionic emulsifiers on skin lipids and further deepen the understanding of enhancing substance penetration with reduced skin barrier properties and increased lipid fluidity.

scholarly journals Revealing the Correlation between Altered Skin Lipids Composition and Skin Disorders

Cosmetics ◽  
2021 ◽  
Vol 8 (3) ◽  
pp. 88
Author(s):  
Katerina Drakou ◽  
Andrea Tsianni ◽  
Faye Vrani ◽  
Valia Kefala ◽  
Efstathios Rallis
Keyword(s):  
Atopic Dermatitis ◽  
Lipid Composition ◽  
Acne Vulgaris ◽  
Skin Barrier ◽  
The Body ◽  
Microbiome Composition ◽  
Skin Lipids ◽  
Key Players ◽  
Dermatological Disorders

Human skin layers serve as a barrier between the body and the environment, by preventing water loss and blocking the entry of chemicals, allergens, and microbes. Recent data showed that skin lipids are vital ‘key players’ of several functions and mechanisms performing in the skin, such as, barrier function and microbiome composition. Abnormalities in lipid composition have been observed in inflammatory cutaneous diseases with a disrupted skin barrier. This review aims to demonstrate the fundamental role of keratinocytes, sebocytes, and microbiome-derived lipids in the maintenance of the skin barrier. Furthermore, it would reveal the correlation between altered skin lipids’ composition, microbiome, and the occurrence of certain dermatological disorders such as acne vulgaris, atopic dermatitis, psoriasis, and rosacea.

scholarly journals Bacterial invasion across the human skin barrier – mechanisms and ensuing tissue degradation.

2021 ◽  
Author(s):  
Zachary W Lipsky ◽  
Marissa K Patsy ◽  
Claudia N. H. Marques ◽  
Guy K German
Keyword(s):  
Human Skin ◽  
Skin Barrier ◽  
Theoretical Models ◽  
Structural Defects ◽  
Bacterial Invasion ◽  
Outermost Layer ◽  
Skin Lipids ◽  
Bacterial Penetration ◽  
Tissue Degradation ◽  
Temperature Controlled

Atopic Dermatitis (AD) is associated with a deficiency of skin lipids, increased populations of Staphylococcus aureus in the microbiome, and structural defects in the stratum corneum (SC), the outermost layer of human skin. However, the pathogenesis of AD is ambiguous as it is unclear whether observed changes are the result of AD or contribute to the pathogenesis of the disease. Previous studies have shown that S. aureus is capable of permeating across isolated human SC tissue when lipids are depleted to levels consistent with AD conditions. In this study, we expand upon this discovery to determine the mechanisms of bacterial penetration into the SC barrier. Specifically, we establish whether bacteria are permeating intercellularly, between corneocytes, or employing a combination pathway of both inter- and intra-cellular travel. The mechanical implications of bacterial invasion, lipid depletion, and media immersion are also evaluated using a newly developed, physiologically relevant, temperature-controlled drip chamber. Results reveal that S. aureus can be internalized by corneocytes, indicating transcellular movement through the tissue during permeation, consistent with previous theoretical models. S. aureus also degrades the mechanical integrity of human SC, particularly when the tissue is partially depleted of lipids. These observed mechanical changes are likely the cause of broken or ruptured tissue seen as exudative lesions in AD flares. This work further highlights the necessity of lipids in skin microbial barrier function.

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