scholarly journals Topical Delivery of Curcumin by Choline-Calix[4]arene-Based Nanohydrogel Improves Its Therapeutic Effect on a Psoriasis Mouse Model

2020 ◽  
Vol 21 (14) ◽  
pp. 5053 ◽  
Author(s):  
Alessia Filippone ◽  
Grazia M. L. Consoli ◽  
Giuseppe Granata ◽  
Giovanna Casili ◽  
Marika Lanza ◽  
...  
Keyword(s):  
Transdermal Delivery ◽  
Water Solubility ◽  
Skin Diseases ◽  
Local Skin ◽  
Nitric Oxide Synthetase ◽  
Skin Delivery ◽  
Abnormal Distribution ◽  
Tnf Α ◽  
Enhanced Expression ◽  
Inducible Nitric Oxide

Curcumin (CUR) has shown remarkable efficacy in the treatment of skin diseases, but its effective transdermal delivery is still a major challenge and stimulates interest in the design of novel systems for CUR dispersion, preservation, and delivery facilitation to the deeper layers of the skin. The present work aimed to investigate the potential of a nanohydrogel, formed by a micellar choline-calix[4]arene amphiphile (CALIX) and CUR, in the treatment of skin diseases through an imiquimod (IMQ)-induced psoriasis model. Psoriasis plaques are associated with aberrant keratinization, abnormal distribution of tight junctions (TJs) proteins, and enhanced expression of inflammatory markers. The nanohydrogel restored the normal distribution of TJs proteins ZO1 and occludin and reduced the expression of TNF-α and inducible nitric oxide synthetase (iNOS) compared to the untreated IMQ group. The novelty lies in the calix[4]arene-based nanohydrogel as a potential new soft material for the topical skin delivery of CUR. The nanohydrogel, due to its physicochemical and mechanical properties, enhances the drug water-solubility, preserves CUR from rapid degradation, and eases the local skin administration and penetration.

scholarly journals Freeze-Dried Softisan® 649-Based Lipid Nanoparticles for Enhanced Skin Delivery of Cyclosporine A

Nanomaterials ◽  
2020 ◽  
Vol 10 (5) ◽  
pp. 986 ◽  
Author(s):  
Maria Inês Silva ◽  
Ana Isabel Barbosa ◽  
Sofia A. Costa Lima ◽  
Paulo Costa ◽  
Tiago Torres ◽  
...  
Keyword(s):  
Cyclosporine A ◽  
Water Solubility ◽  
Skin Diseases ◽  
Skin Permeation ◽  
Topical Administration ◽  
Lipid Nanoparticles ◽  
World Population ◽  
Inflammatory Skin Diseases ◽  
Skin Delivery ◽  
Freeze Dried

Inflammatory skin diseases, including psoriasis and atopic dermatitis, affect around one quarter to one third of the world population. Systemic cyclosporine A, an immunosuppressant agent, is included in the current therapeutic armamentarium of these diseases. Despite being highly effective, it is associated with several side effects, and its topical administration is limited by its high molecular weight and poor water solubility. To overcome these limitations, cyclosporine A was incorporated into solid lipid nanoparticles obtained from Softisan® 649, a commonly used cosmetic ingredient, aiming to develop a vehicle for application to the skin. The nanoparticles presented sizes of around 200 nm, low polydispersity, negative surface charge, and stability when stored for 8 weeks at room temperature or 4 °C. An effective incorporation of 88% of cyclosporine A within the nanoparticles was observed, without affecting its morphology. After the freeze-drying process, the Softisan® 649-based nanoparticles formed an oleogel. Skin permeation studies using pig ear as a model revealed low permeation of the applied cyclosporine A in the freeze-dried form of the nanoparticles in relation to free drug and the freshly prepared nanoparticles. About 1.0 mg of cyclosporine A was delivered to the skin with reduced transdermal permeation. These results confirm local delivery of cyclosporine A, indicating its promising topical administration.

scholarly journals Gomisin M2 Ameliorates Atopic Dermatitis-like Skin Lesions via Inhibition of STAT1 and NF-κB Activation in 2,4-Dinitrochlorobenzene/Dermatophagoides farinae Extract-Induced BALB/c Mice

Molecules ◽  
2021 ◽  
Vol 26 (15) ◽  
pp. 4409
Author(s):  
Jinjoo Kang ◽  
Soyoung Lee ◽  
Namkyung Kim ◽  
Hima Dhakal ◽  
Taeg-Kyu Kwon ◽  
...  
Keyword(s):  
Atopic Dermatitis ◽  
Oral Administration ◽  
Skin Diseases ◽  
Nuclear Translocation ◽  
Skin Lesions ◽  
Biologically Active ◽  
Therapeutic Effects ◽  
Dermatophagoides Farinae ◽  
Tnf Α ◽  
Ifn Γ

The extracts of Schisandra chinensis (Turcz.) Baill. (Schisandraceae) have various therapeutic effects, including inflammation and allergy. In this study, gomisin M2 (GM2) was isolated from S. chinensis and its beneficial effects were assessed against atopic dermatitis (AD). We evaluated the therapeutic effects of GM2 on 2,4-dinitrochlorobenzene (DNCB) and Dermatophagoides farinae extract (DFE)-induced AD-like skin lesions with BALB/c mice ears and within the tumor necrosis factor (TNF)-α and interferon (IFN)-γ-stimulated keratinocytes. The oral administration of GM2 resulted in reduced epidermal and dermal thickness, infiltration of tissue eosinophils, mast cells, and helper T cells in AD-like lesions. GM2 suppressed the expression of IL-1β, IL-4, IL-5, IL-6, IL-12a, and TSLP in ear tissue and the expression of IFN-γ, IL-4, and IL-17A in auricular lymph nodes. GM2 also inhibited STAT1 and NF-κB phosphorylation in DNCB/DFE-induced AD-like lesions. The oral administration of GM2 reduced levels of IgE (DFE-specific and total) and IgG2a in the mice sera, as well as protein levels of IL-4, IL-6, and TSLP in ear tissues. In TNF-α/IFN-γ-stimulated keratinocytes, GM2 significantly inhibited IL-1β, IL-6, CXCL8, and CCL22 through the suppression of STAT1 phosphorylation and the nuclear translocation of NF-κB. Taken together, these results indicate that GM2 is a biologically active compound that exhibits inhibitory effects on skin inflammation and suggests that GM2 might serve as a remedy in inflammatory skin diseases, specifically on AD.

scholarly journals The Use of Micro- and Nanocarriers for Resveratrol Delivery into and across the Skin in Different Skin Diseases—A Literature Review

Pharmaceutics ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 451
Author(s):  
Beata Szulc-Musioł ◽  
Beata Sarecka-Hujar
Keyword(s):  
Transdermal Delivery ◽  
Bacterial Infections ◽  
Skin Diseases ◽  
Skin Surface ◽  
Non Invasive ◽  
Skin Abnormalities ◽  
Low Solubility ◽  
Active Substances ◽  
Poor Stability

In recent years, polyphenols have been extensively studied due to their antioxidant, anticancer, and anti-inflammatory properties. It has been shown that anthocyanins, flavonols, and flavan-3-ols play an important role in the prevention of bacterial infections, as well as vascular or skin diseases. Particularly, resveratrol, as a multi-potent agent, may prevent or mitigate the effects of oxidative stress. As the largest organ of the human body, skin is an extremely desirable target for the possible delivery of active substances. The transdermal route of administration of active compounds shows many advantages, including avoidance of gastrointestinal irritation and the first-pass effect. Moreover, it is non-invasive and can be self-administered. However, this delivery is limited, mainly due to the need to overpassing the stratum corneum, the possible decomposition of the substances in contact with the skin surface or in the deeper layers thereof. In addition, using resveratrol for topical and transdermal delivery faces the problems of its low solubility and poor stability. To overcome this, novel systems of delivery are being developed for the effective transport of resveratrol across the skin. Carriers in the micro and nano size were demonstrated to be more efficient for safe and faster topical and transdermal delivery of active substances. The present review aimed to discuss the role of resveratrol in the treatment of skin abnormalities with a special emphasis on technologies enhancing transdermal delivery of resveratrol.

scholarly journals Water Extract of Rubus coreanus Prevents Inflammatory Skin Diseases In Vitro Models

Plants ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 1230
Author(s):  
Sumin Pyeon ◽  
Ok-Kyung Kim ◽  
Ho-Geun Yoon ◽  
Shintae Kim ◽  
Kyung-Chul Choi ◽  
...  
Keyword(s):  
Mrna Expression ◽  
Skin Diseases ◽  
Water Extract ◽  
Total Phenolic ◽  
Hacat Cells ◽  
Rubus Coreanus ◽  
Tnf Α ◽  
Ifn Γ ◽  
Inflammatory Skin

Atopic dermatitis (AD) is a chronic inflammatory skin disease caused by immune hypersensitivity reaction. The cause of AD is unclear, but its symptoms have a negative effect on quality of life; various treatment methods to alleviate these symptoms are underway. In the present study, we aimed to evaluate in vitro antioxidant and anti-inflammatory effects of Rubus coreanus water extract (RCW) on AD. Total phenolic compounds and flavonoid content of RCW were 4242.40 ± 54.84 mg GAE/g RCE and 1010.99 ± 14.75 mg CE/g RCW, respectively. RCW reduced intracellular reactive oxygen species level and increased the action of antioxidant enzymes, such as catalase, superoxide dismutase, and glutathione peroxidase in tumor necrosis factor-α (TNF-α)/interferon-γ (IFN-γ)-stimulated HaCaT cells. Moreover, mRNA expression of the pro-inflammatory cytokines, including TNF-α, interleukin-1β, and interleukin-6, was downregulated by RCW in the TNF-α/IFN-γ-stimulated cells. The levels of inflammatory chemokines (thymus- and activation-regulated chemokine; eotaxin; macrophage-derived chemokine; regulated on activation, normal T-cell expressed and secreted; and granulocyte-macrophage colony-stimulating factor) and intercellular adhesion molecule-1 were decreased in the TNF-α/IFN-γ-stimulated HaCaT cells after RCW treatment. Additionally, the mRNA expression levels of filaggrin and involucrin, proteins that form the skin, were increased by RCW. Furthermore, RCW inhibited the nuclear factor kappa-light-chain-enhancer of the activated B cells pathway in the TNF-α/IFN-γ-stimulated HaCaT cells. Collectively, the present investigation indicates that RCW is a potent substance that inhibits AD.

scholarly journals Down-regulation of NF-κB signalling by polyphenolic compounds prevents endotoxin-induced liver injury in a rat model

2011 ◽  
Vol 18 (1) ◽  
pp. 70-79 ◽  
Author(s):  
Sushma Bharrhan ◽  
Kanwaljit Chopra ◽  
Sunil K Arora ◽  
Jaideep S Toor ◽  
Praveen Rishi
Keyword(s):  
Liver Injury ◽  
Therapeutic Agent ◽  
Polyphenolic Compounds ◽  
Oxygen Species ◽  
Enhanced Production ◽  
Signalling Molecule ◽  
Tnf Α ◽  
Oxide Synthase ◽  
Inducible Nitric Oxide ◽  
Pharmacological Basis

Activation of NF-κB has been reported to play a key role in causing endotoxin-induced hepatic damage through enhanced production of reactive oxygen species and pro-inflammatory mediators. In this context, the potential of polyphenolic phytochemicals in preventing endotoxin-induced liver damage remains unclear. Here, we demonstrate that catechin and quercetin have the potential to down-regulate the initial signalling molecule NF-κB which may further inhibit the downstream cascade including TNF-α and NO. These results were confirmed using N-nitro-L-arginine methyl ester (L-NAME), the inhibitor of inducible nitric oxide synthase (iNOS) along with the biochemical and histological alterations occurring in the presence and absence of supplementation with both the polyphenols. However, catechin was found to be more effective than quercetin against endotoxin-induced liver injury. These findings suggest that these polyphenols may form a pharmacological basis for designing a therapeutic agent against endotoxin-mediated oxidative damage.

Physical characterisation and stability study of formulated Chromolaena odorata gel

2021 ◽  
Vol 18 ◽  
Author(s):  
Qurratul Ain Zakirah Mohd Zamram ◽  
Hannis Fadzillah Mohsin ◽  
Mashani Mohamad Mohamad ◽  
Nurul Aqmar Mohamad Nor Hazalin ◽  
Khuriah Abdul Hamid
Keyword(s):  
High Performance ◽  
Skin Diseases ◽  
Loss Modulus ◽  
Viscosity Index ◽  
Stability Study ◽  
Wound Management ◽  
Flavonoid Compound ◽  
Chromolaena Odorata ◽  
Skin Delivery ◽  
Materials Used

Aim: Formulating topical products for skin delivery has always been a challenge for pharmaceutical scientists to fulfil good formulation criteria. Despite the challenges, gel-based drug delivery offers some advantages such that it is non-invasive, painless, avoidance of the first-pass metabolism and has satisfactory patient compliance. Objectives: In this study, Chromolaena odorata gel and quercetin gel (bioactive flavonoid compound) were successfully formulated and compared with placebo and conventional wound aid gel. The chromatographic profilling was conducted to screen the presence of phytoconstituents. Subsequently, all formulated gels were subjected to physical characteristic and stability study. Methods: Reverse Phase High-Performance Liquid Chromatography (RP-HPLC) of C.odorata methanolic leaves extract shows a distinct compound separation at retention time 8.4min to 34.8 min at 254nm. All gels were characterised by evaluating their rheological properties including storage modulus, loss modulus and plastic viscosity. Besides, texture analysis was performed to measure the gels’ firmness, consistency, cohesiveness, and viscosity index. Results: From the observation, C. odorata gel demonstrated better spreadability as compared to the other gels, which acquired less work and favourable to be applied onto the skin. Moreover, C. odorata gel showed no changes in organoleptic properties and proven to be stable after 30 days of accelerated stability study at 40°C ± 2°C with relative humidity (RH) of 75%± 5%. Conclusion: C. odorata gel has shown to be stable, reflecting the combination of materials used in the formulation, which did not degrade throughout the study. This work suggests the potential of this gel as a vehicle to deliver the active ingredients of C. odorata to the skin, which can be further explored as a topical application in antimicrobial wound management or other skin diseases study.

Elegant flexible vesicular nanocarriers for the efficient skin delivery of topically applied drugs-

2021 ◽  
Vol 18 ◽  
Author(s):  
Waleed Albalawi ◽  
Surur Alharbi ◽  
Fahad Alanazi ◽  
Hameed Alahmadi ◽  
Mothib Alghamdi ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Skin Diseases ◽  
Fungal Infections ◽  
Skin Barrier ◽  
Therapeutic Outcome ◽  
Health Concern ◽  
Inflammatory Skin Diseases ◽  
Skin Delivery ◽  
Pubmed Database ◽  
Vesicular Carriers

Background: Skin diseases represent a major health concern worldwide and negatively impact patients’ quality of life. Despite the availability of various efficacious drugs, their therapeutic outcome is often limited due to shortcomings related to the formidable skin barrier and unfavorable physicochemical properties of drugs. Flexible nano-vesicles have shown tremendous potential to overcome these hurdles and improve the local therapeutic effect of these drugs. Objective: This review article is aimed to shed light on flexible nano-vesicular carriers as a means to combat skin diseases. Methods: The literature was reviewed using PubMed database using various keywords such as liposomes, flexible (deformable liposomes) (transferosomes), ethosomes, transethosomes, niosomes, and spanlastics. Results: Liposomes and niosomes were found effective for the loading and release of both hydrophilic and lipophilic drugs. However, their limited skin penetration led to drug delivery to the outermost layers of skin only. This necessitates the search for innovative vesicular carriers, including liposomes, flexible (deformable liposomes), ethosomes, transethosomes, and spanlastics. These flexible nano-vesicular carriers showed enhanced drug delivery and deposition across various skin layers, which was better than their corresponding conventional vesicles. This resulted in superior drug efficacy against various skin diseases such as skin cancer, inflammatory skin diseases, superficial fungal infections, etc. Conclusion: Flexible nano-vesicular carriers have proven themselves as efficient drug delivery systems that are able to deliver their cargo into the deep skin layers and thus, improve the therapeutic outcome of various skin diseases. However, there remain some challenges that need to be addressed before these nanocarriers can be translated from the lab to clinics.

scholarly journals Enhanced Transdermal Delivery of Pranoprofen Using a Thermo-Reversible Hydrogel Loaded with Lipid Nanocarriers for the Treatment of Local Inflammation

2021 ◽  
Vol 15 (1) ◽  
pp. 22
Author(s):  
María Rincón ◽  
Marcelle Silva-Abreu ◽  
Lupe Carolina Espinoza ◽  
Lilian Sosa ◽  
Ana Cristina Calpena ◽  
...  
Keyword(s):  
Human Skin ◽  
Topical Application ◽  
Topical Treatment ◽  
Transdermal Delivery ◽  
Ex Vivo ◽  
Skin Permeation ◽  
In Vitro Release ◽  
Heterogeneous Structure ◽  
Clinical Environment ◽  
Local Skin

A biocompatible topical thermo-reversible hydrogel containing Pranoprofen (PF)-loaded nanostructured lipid carriers (NLCs) was studied as an innovative strategy for the topical treatment of skin inflammatory diseases. The PF-NLCs-F127 hydrogel was characterized physiochemically and short-time stability tests were carried out over 60 days. In vitro release and ex vivo human skin permeation studies were carried out in Franz diffusion cells. In addition, a cytotoxicity assay was studied using the HaCat cell line and in vivo tolerance study was performed in humans by evaluating the biomechanical properties. The anti-inflammatory effect of the PF-NLCs-F127 was evaluated in adult male Sprague Daw-ley® rats using a model of inflammation induced by the topical application of xylol for 1 h. The developed PF-NLCs-F127 exhibited a heterogeneous structure with spherical PF-NLCs in the hydrogel. Furthermore, a thermo-reversible behaviour was determined with a gelling temperature of 32.5 °C, being close to human cutaneous temperature and thus favouring the retention of PF. Furthermore, in the ex vivo study, the amount of PF retained and detected in human skin was high and no systemic effects were observed. The hydrogel was found to be non-cytotoxic, showing cell viability of around 95%. The PF-NLCs-F127 is shown to be well tolerated and no signs of irritancy or alterations of the skin’s biophysical properties were detected. The topical application of PF-NLCs-F127 hydrogel was shown to be efficient in an inflammatory animal model, preventing the loss of stratum corneum and reducing the presence of leukocyte infiltration. The results from this study confirm that the developed hydrogel is a suitable drug delivery carrier for the transdermal delivery of PF, improving its dermal retention, opening the possibility of using it as a promising candidate and safer alternative to topical treatment for local skin inflammation and indicating that it could be useful in the clinical environment.

scholarly journals Improvement of Imiquimod Solubilization and Skin Retention via TPGS Micelles: Exploiting the Co-Solubilizing Effect of Oleic Acid

Pharmaceutics ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 1476
Author(s):  
Martina Ghezzi ◽  
Silvia Pescina ◽  
Andrea Delledonne ◽  
Ilaria Ferraboschi ◽  
Cristina Sissa ◽  
...  
Keyword(s):  
Oleic Acid ◽  
Water Solubility ◽  
Skin Penetration ◽  
Water Soluble ◽  
Drug Solubility ◽  
Two Photon Microscopy ◽  
Skin Delivery ◽  
Polyethylene Glycol 1000 ◽  
The One ◽  
Skin Retention

Imiquimod (IMQ) is an immunostimulant drug approved for the topical treatment of actinic keratosis, external genital-perianal warts as well as superficial basal cell carcinoma that is used off-label for the treatment of different forms of skin cancers, including some malignant melanocytic proliferations such as lentigo maligna, atypical nevi and other in situ melanoma-related diseases. Imiquimod skin delivery has proven to be a real challenge due to its very low water-solubility and reduced skin penetration capacity. The aim of the work was to improve the drug solubility and skin retention using micelles of d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS), a water-soluble derivative of vitamin E, co-encapsulating various lipophilic compounds with the potential ability to improve imiquimod affinity for the micellar core, and thus its loading into the nanocarrier. The formulations were characterized in terms of particle size, zeta potential and stability over time and micelles performance on the skin was evaluated through the quantification of imiquimod retention in the skin layers and the visualization of a micelle-loaded fluorescent dye by two-photon microscopy. The results showed that imiquimod solubility strictly depends on the nature and concentration of the co-encapsulated compounds. The micellar formulation based on TPGS and oleic acid was identified as the most interesting in terms of both drug solubility (which was increased from few µg/mL to 1154.01 ± 112.78 µg/mL) and micellar stability (which was evaluated up to 6 months from micelles preparation). The delivery efficiency after the application of this formulation alone or incorporated in hydrogels showed to be 42- and 25-folds higher than the one of the commercial creams.

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