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 Omega-3- and Resveratrol-Loaded Lipid Nanosystems for Potential Use as Topical Formulations in Autoimmune, Inflammatory, and Cancerous Skin Diseases

Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1202
Author(s):  
Ana R. Caldas ◽  
José Catita ◽  
Raul Machado ◽  
Artur Ribeiro ◽  
Fátima Cerqueira ◽  
...  
Keyword(s):  
Skin Diseases ◽  
Skin Permeation ◽  
Chemical Properties ◽  
Topical Administration ◽  
Skin Surface ◽  
Lipid Nanoparticles ◽  
Skin Layer ◽  
No Production ◽  
Omega 3 ◽  
Pharmaceutical Industries

Resveratrol (RSV) and omega 3 (ω3), because of their biological favorable properties, have become subjects of interest for researchers in dermocosmetic and pharmaceutical industries; however, these bioactives present technological limitations that hinder their effective delivery to the target skin layer. To overcome the stability and skin permeation limitations of free bioactives, this work proposes a combined strategy involving two different lipid nanosystems (liposomes and lipid nanoparticles) that include ω3 in their lipid matrix. Additionaly, RSV is only encapsulated in liposomes that provid an adequate amphiphilic environment. Each formulation is thoroughly characterized regarding their physical–chemical properties. Subsequently, the therapeutic performance of the lipid nanosystems is evaluated based on their protective roles against lipid peroxidation, as well as inhibition of cicloxygenase (COX) and nitric oxid (NO) production in the RWA264.7 cell line. Finally, the lipid nanosystems are incorporated in hydrogel to allow their topical administration, then rheology, occlusion, and RSV release–diffusion assays are performed. Lipid nanoparticles provide occlusive effects at the skin surface. Liposomes provide sustained RSV release and their flexibility conferred by edge activator components enhances RSV diffusion, which is required to reach NO production cells and COX cell membrane enzymes. Overall, the inclusion of both lipid nanosystems in the same semisolid base constitutes a promising strategy for autoimmune, inflammatory, and cancerous skin diseases.

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 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 Lipid Nanocarriers for Hyperproliferative Skin Diseases

Cancers ◽  
2021 ◽  
Vol 13 (22) ◽  
pp. 5619
Author(s):  
Eliana B. Souto ◽  
Ana L. R. de Souza ◽  
Fernanda K. dos Santos ◽  
Elena Sanchez-Lopez ◽  
Amanda Cano ◽  
...  
Keyword(s):  
Side Effects ◽  
Topical Treatment ◽  
Skin Diseases ◽  
Aminolevulinic Acid ◽  
Skin Permeation ◽  
Aqueous Solubility ◽  
Lipid Nanoparticles ◽  
Unknown Etiology ◽  
Skin Manifestations ◽  
Lipid Nanocarriers

Hyperproliferative skin diseases (HSD) are a group of diseases that include cancers, pre-cancerous lesions and diseases of unknown etiology that present different skin manifestations in terms of the degree and distribution of the injuries. Anti-proliferative agents used to treat these diseases are so diverse, including 5-aminolevulinic acid, 5-fluorouracil, imiquimod, methotrexate, paclitaxel, podophyllotoxin, realgar, and corticosteroids in general. These drugs usually have low aqueous solubility, which consequently decreases skin permeation. Thus, their incorporation in lipid nanocarriers has been proposed with the main objective to increase the effectiveness of topical treatment and reduce side effects. This manuscript aims to describe the advantages of using lipid nanoparticles and liposomes that can be used to load diversity of chemically different drugs for the treatment of HSD.

scholarly journals Topical Allopurinol-Loaded Nanostructured Lipid Carriers: A Novel Approach for Wound Healing Management

2021 ◽  
Vol 8 (12) ◽  
pp. 192
Author(s):  
Carla Varrica ◽  
Manuela Carvalheiro ◽  
Catarina Faria-Silva ◽  
Carla Eleutério ◽  
Giuseppina Sandri ◽  
...  
Keyword(s):  
Wound Healing ◽  
Water Solubility ◽  
Drug Carrier ◽  
Skin Permeation ◽  
Skin Lesions ◽  
Nanostructured Lipid Carriers ◽  
Hacat Cells ◽  
Xanthine Oxidase Inhibitor ◽  
Skin Delivery

Nanostructured lipid carriers (NLC) have been widely studied as delivery systems for a variety of routes, including the skin. Their composition results in an imperfect lipid matrix, allowing increased drug encapsulation. Allopurinol (AP), a xanthine oxidase inhibitor, is characterized by low water solubility and high melting point, which has hampered its use through the topical route. In this work, AP was incorporated in a NLC formulation to enhance drug-carrier association and skin delivery as a topical approach to treat wounds. AP-NLC system was characterized in terms of size, charge, rheological behavior, and in vitro skin permeation. The in vitro cytotoxicity was evaluated using HaCaT cells. The wound healing efficacy of the AP-NLC formulation on animal skin lesions was evaluated in male Wistar rats. The AP-NLC presented a mean size of 193 ± 15 nm with a PdI of 0.240 ± 0.02, zeta potential values around −49.6 mV, and an encapsulation efficiency of 52.2%. The AP-NLC formulation presented an adequate profile to be used topically, since epidermal and dermal drug retention were achieved. No reduction in HaCaT cells viability was observed at the tested concentrations (AP < 10 μg/mL). The in vivo application of the AP-NLC formulation resulted in the regeneration of skin lesions when compared with non-treated controls.

scholarly journals Mechanistic Evaluation of Enhanced Curcumin Delivery through Human Skin In Vitro from Optimised Nanoemulsion Formulations Fabricated with Different Penetration Enhancers

Pharmaceutics ◽  
2019 ◽  
Vol 11 (12) ◽  
pp. 639 ◽  
Author(s):  
Shereen A. Yousef ◽  
Yousuf H. Mohammed ◽  
Sarika Namjoshi ◽  
Jeffrey E. Grice ◽  
Heather A. E. Benson ◽  
...  
Keyword(s):  
Zeta Potential ◽  
Droplet Size ◽  
Skin Diseases ◽  
Skin Permeation ◽  
Storage Period ◽  
Penetration Enhancers ◽  
Log P ◽  
Water Control ◽  
Skin Delivery

Curcumin is a natural product with chemopreventive and other properties that are potentially useful in treating skin diseases, including psoriasis and melanoma. However, because of the excellent barrier function of the stratum corneum and the relatively high lipophilicity of curcumin (log P 3.6), skin delivery of curcumin is challenging. We used the principles of a Quality by Design (QbD) approach to develop nanoemulsion formulations containing biocompatible components, including Labrasol and Lecithin as surfactants and Transcutol and ethanol as cosurfactants, to enhance the skin delivery of curcumin. The nanoemulsions were characterised by cryo-SEM, Zeta potential, droplet size, pH, electrical conductivity (EC) and viscosity (η). Physicochemical long-term stability (6 months) was also investigated. The mean droplet sizes as determined by dynamic light scattering (DLS) were in the lower submicron range (20–50 nm) and the average Zeta potential values were low (range: −0.12 to −2.98 mV). Newtonian flow was suggested for the nanoemulsions investigated, with dynamic viscosity of the nanoemulsion formulations ranging from 5.8 to 31 cP. The droplet size of curcumin loaded formulations remained largely constant over a 6-month storage period. The inclusion of terpenes to further enhance skin permeation was also examined. All nanoemulsions significantly enhanced the permeation of curcumin through heat-separated human epidermal membranes, with the greatest effect being a 28-fold increase in maximum flux (Jmax) achieved with a limonene-based nanoemulsion, compared to a 60% ethanol in water control vehicle. The increases in curcumin flux were associated with increased skin diffusivity. In summary, we demonstrated the effectiveness of nanoemulsions for the skin delivery of the lipophilic active compound curcumin, and elucidated the mechanism of permeation enhancement. These formulations show promise as delivery vehicles for curcumin to target psoriasis and skin cancer, and more broadly for other skin delivery applications.

scholarly journals Improved Dermal Delivery of Cyclosporine A Loaded in Solid Lipid Nanoparticles

Nanomaterials ◽  
2019 ◽  
Vol 9 (9) ◽  
pp. 1204 ◽  
Author(s):  
Abderrazzaq Essaghraoui ◽  
Ahmed Belfkira ◽  
Bassou Hamdaoui ◽  
Cláudia Nunes ◽  
Sofia A. Costa Lima ◽  
...  
Keyword(s):  
Cyclosporine A ◽  
Solid Lipid Nanoparticles ◽  
Topical Administration ◽  
Lipid Nanoparticles ◽  
Homogenization Method ◽  
Solid Lipid ◽  
Ic50 Values ◽  
Negative Surface ◽  
Dermal Delivery

Cyclosporine A (CsA) is an immunosuppressant frequently used in the therapy of autoimmune disorders, including skin-related diseases. Aiming towards topical delivery, CsA was successfully incorporated into lipid nanoparticles of Lipocire DM and Pluronic F-127 using the hot homogenization method. Two different nanocarriers were optimized: solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) where oleic acid was the liquid lipid. The developed nanoparticles showed mean sizes around 200 nm, a negative surface charge, and drug entrapment efficiencies around 85% and 70% for SLNs and NLCs, respectively. The spherical CsA-loaded lipid nanoparticles were stable for 9 weeks when stored at room temperature, and exhibited in vitro pH-dependent release under skin mimetic conditions, following the Peppas–Korsmeyer model. CsA, when loaded in SLNs, was safe to be used up to 140 μg mL−1 in fibroblasts and keratinocytes, while CsA-loaded NLCs and free drug exhibited IC50 values of 55 and 95 μg mL−1 (fibroblasts) and 28 and 30 μg mL−1 (keratinocytes), respectively. The developed SLNs were able to retain the drug in pork skin with a reduced permeation rate in relation to NLCs. These findings suggest that SLNs are a potential alternative to produce stable and safe CsA nanocarriers for topical administration.

scholarly journals In Vitro Skin Permeation of Idebenone from Lipid Nanoparticles Containing Chemical Penetration Enhancers

Pharmaceutics ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 1027
Author(s):  
Lucia Montenegro ◽  
Ludovica Maria Santagati ◽  
Maria Grazia Sarpietro ◽  
Francesco Castelli ◽  
Annamaria Panico ◽  
...  
Keyword(s):  
Skin Permeation ◽  
Skin Penetration ◽  
Lipid Nanoparticles ◽  
Penetration Enhancers ◽  
Isopropyl Myristate ◽  
Skin Delivery ◽  
Rate Limiting Step ◽  
In Vitro Skin Permeation ◽  
Chemical Penetration Enhancers

Lipid nanoparticles (LNPs) have been proposed as carriers for drug skin delivery and targeting. As LNPs effectiveness could be increased by the addition of chemical penetration enhancers (PE), in this work, the feasibility of incorporating PE into LNPs to improve idebenone (IDE) targeting to the skin was investigated. LNPs loading IDE 0.7% w/w were prepared using hydrophilic (propylene glycol, PG, 10% w/w or N-methylpyrrolidone, NMP, 10% w/w) and/or lipophilic PE (oleic acid, OA, 1% w/w; isopropyl myristate, IPM, 3.5% w/w; a mixture of 0.5% w/w OA and 2.5% w/w IPM). All LNPs showed small sizes (<60 nm), low polydispersity index and good stability. According to the obtained results, IDE release from LNPs was not the rate-limiting step in IDE skin penetration. No IDE permeation was observed through excised pigskin from all LNPs, while the greatest increase of IDE penetration into the different skin layers was obtained using the mixture OA/IPM. The antioxidant activity of IDE-loaded LNPs, determined by the oxygen radical absorbance capacity assay, was greater than that of free IDE. These results suggest that the use of suitable PE as LNPs components could be regarded as a promising strategy to improve drug targeting to the skin.

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