scholarly journals Biocompatibility and Antimicrobial Activity of Nanostructured Lipid Carriers for Topical Applications Are Affected by Type of Oils Used in Their Composition

Pharmaceutics ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 1950
Author(s):  
Dragana P. C. de Barros ◽  
Patricia Reed ◽  
Marta Alves ◽  
Rafaela Santos ◽  
Abel Oliva
Keyword(s):  
Antimicrobial Activity ◽  
Therapeutic Potential ◽  
Antimicrobial Properties ◽  
Dermal Fibroblasts ◽  
Nanostructured Lipid Carriers ◽  
Epidermal Keratinocytes ◽  
Drug Bioavailability ◽  
Human Epidermal Keratinocytes ◽  
Strong Argument ◽  
Natural Oils

Nanostructured lipid carriers (NLCs) have gained significant attention as tools for the dermal delivery of therapeutics due to their stability, biocompatibility, and ability to improve drug bioavailability. The use of natural plant oils (NPO) in NLC formulations has numerous benefits for the skin due to their therapeutic potential. This work shows the effect of NLC composition on bioavailability in epidermal cells and antimicrobial activity against Staphylococcus aureus. Sixteen systems containing fixed (sunflower, olive, corn, peanut, coconut, castor, and sweet almond) and essential (eucalyptus) oils, with different solid lipid (SL): liquid lipid (LL) ratios, were engineered. The structural properties, bioavailability, and antimicrobial action of the particles was studied. The choice of NPO influenced the physicochemical stability by changing the diameter of NLC formulations (between 160 nm and 185 nm) and Z-potential (between −46 mV and −61 mV). All of the systems were characterized by concentration-dependent cytocompatibility with human epidermal keratinocytes (HaCaT) and human dermal fibroblasts (HDFn). The SL:LL ratio in some NLC systems impacted cell cytotoxicity differently. Antimicrobial properties were observed in all 16 systems; however, the type of oil and SL:LL ratio affected the activity of the formulations. Two NLC-NPO systems were found to be non-cytotoxic to human cells lines at concentrations that completely inhibited bacterial growth. These results present a strong argument that the use of natural oils in NLC formulations presents a promising tool for the treatment of skin infections.

scholarly journals Nanostructured Lipid Carriers Engineered as Topical Delivery of Etodolac: Optimization and Cytotoxicity Studies

Materials ◽  
2021 ◽  
Vol 14 (3) ◽  
pp. 596
Author(s):  
Anna Czajkowska-Kośnik ◽  
Emilia Szymańska ◽  
Robert Czarnomysy ◽  
Julia Jacyna ◽  
Michał Markuszewski ◽  
...  
Keyword(s):  
Drug Release ◽  
Entrapment Efficiency ◽  
Dermal Fibroblasts ◽  
Nanostructured Lipid Carriers ◽  
Tween 20 ◽  
Epidermal Keratinocytes ◽  
Human Epidermal Keratinocytes ◽  
Cytotoxicity Studies ◽  
Prolonged Drug Release

Etodolac (ETD), a nonsteroidal anti-inflammatory drug, exhibits antinflammatory, analgesic, and antipyretic activity. The main type of ETD administration is oral route, which is associated with significant systemic side effects. Nanostructured lipid carriers (NLC), a modern lipid formulation, are non-toxic, biocompatible, can improve the solubility and stability of drugs. Nanostructured lipid carriers (NLC) containing etodolac were prepared by a melt-emulsification and ultrasonication technique. Full factorial design (FFD) was applied to optimize the composition of NLC and their properties such as zeta potential, polidyspersity index, and entrapment efficiency. Formulations consisting of Capryol 90, glicerol monostearate, and Tween 20 displayed particle size below 300 nm, encapsulated drug with efficiency of approximately 87% and prolonged drug release up to 24 h. Stable formulations displayed moderately negative surface charge suggesting their limited ability to interact with skin surface but simultaneously presenting their lower risk to cause cell-membrane disruption. In fact, cytotoxicity assessment using human dermal fibroblasts and human epidermal keratinocytes revealed that etodolac-loaded NLC had no important impact on skin cells viability evaluated in vitro, which might evidence that NLC formulations are safe for dermal delivery. The studies developed were relatively fast and simple, requiring no specialized equipment method to prepare NLC as ETD carriers ensuring better solubility and prolonged drug release.

Keratinocyte growth regulation in fibroblast cocultures via a double paracrine mechanism

1999 ◽  
Vol 112 (12) ◽  
pp. 1843-1853 ◽  
Author(s):  
N. Maas-Szabowski ◽  
A. Shimotoyodome ◽  
N.E. Fusenig
Keyword(s):  
Neutralizing Antibodies ◽  
Growth Regulation ◽  
Keratinocyte Growth Factor ◽  
Dermal Fibroblasts ◽  
Tissue Homeostasis ◽  
Epidermal Keratinocytes ◽  
Human Epidermal Keratinocytes ◽  
Keratinocyte Proliferation ◽  
Normal Human ◽  
Kinetics Of

Epithelial-mesenchymal interactions play an important role in regulating tissue homeostasis and repair. For skin, the regulatory mechanisms of epidermal-dermal interactions were studied in cocultures of normal human epidermal keratinocytes (NEK) and dermal fibroblasts (HDF) rendered postmitotic by alpha-irradiation (HDFi). The expression kinetics of different cytokines and their receptors with presumed signalling function in skin were determined at the RNA and protein level in mono- and cocultured NEK and HDFi. In cocultured HDFi, mRNA and protein synthesis of keratinocyte growth factor (KGF) (FGF-7) was strongly enhanced, whereas in cocultured keratinocytes interleukin (IL)-1alpha and -1beta mRNA expression increased compared to monocultures. Thus we postulated that IL-1, which had no effect on keratinocyte proliferation, induced in fibroblasts the expression of factors stimulating keratinocyte proliferation, such as KGF. The functional significance of this reciprocal modulation was substantiated by blocking experiments. Both IL-1alpha and -1beta-neutralizing antibodies and IL-1 receptor antagonist significantly reduced keratinocyte proliferation supposedly through abrogation of KGF production, because IL-1 antibodies blocked the induced KGF production. These data indicate a regulation of keratinocyte growth by a double paracrine mechanism through release of IL-1 which induces KGF in cocultured fibroblasts. Thus IL-1, in addition to its proinflammatory function in skin, may play an essential role in regulating tissue homeostasis.

scholarly journals Persea americanaMill. Seed: Fractionation, Characterization, and Effects on Human Keratinocytes and Fibroblasts

2013 ◽  
Vol 2013 ◽  
pp. 1-12 ◽  
Author(s):  
Maria del R. Ramos-Jerz ◽  
Socorro Villanueva ◽  
Gerold Jerz ◽  
Peter Winterhalter ◽  
Alexandra M. Deters
Keyword(s):  
Chlorogenic Acid ◽  
Dermal Fibroblasts ◽  
Persea Americana ◽  
Epidermal Keratinocytes ◽  
Hacat Keratinocytes ◽  
Human Epidermal Keratinocytes ◽  
Residual Solvent ◽  
Keratinocyte Proliferation ◽  
Normal Human

Methanolic avocado (Persea americanaMill., Lauraceae) seed extracts were separated by preparative HSCCC. Partition and HSCCC fractions were principally characterized by LC-ESI-MS/MS analysis. Theirin vitroinfluence was investigated on proliferation, differentiation, cell viability, and gene expression on HaCaT and normal human epidermal keratinocytes (NHEK) and normal human dermal fibroblasts (NHDF). The methanol-water partition (M) from avocado seeds and HSCCC fraction 3 (M.3) were mostly composed of chlorogenic acid and its isomers. Both reduced NHDF but enhanced HaCaT keratinocytes proliferation. HSCCC fractionM.2composed of quinic acid among chlorogenic acid and its isomers inhibited proliferation and directly induced differentiation of keratinocytes as observed on gene and protein level. Furthermore,M.2increased NHDF proliferation via upregulation of growth factor receptors. Salidrosides and ABA derivatives present in HSCCC fractionM.6increased NHDF and keratinocyte proliferation that resulted in differentiation. The residual solvent fractionM.7contained among low concentrations of ABA derivatives high amounts of proanthocyanidins B1 and B2 as well as an A-type trimer and stimulated proliferation of normal cells and inhibited the proliferation of immortalized HaCaT keratinocytes.

scholarly journals In Vitro and Clinical Evaluation of Cannabigerol (CBG) Produced via Yeast Biosynthesis: A Cannabinoid with a Broad Range of Anti-Inflammatory and Skin Health-Boosting Properties

Molecules ◽  
2022 ◽  
Vol 27 (2) ◽  
pp. 491
Author(s):  
Eduardo Perez ◽  
Jose R. Fernandez ◽  
Corey Fitzgerald ◽  
Karl Rouzard ◽  
Masanori Tamura ◽  
...  
Keyword(s):  
Human Skin ◽  
Cannabis Sativa ◽  
Transepidermal Water Loss ◽  
Dermal Fibroblasts ◽  
Ultraviolet B ◽  
Epidermal Keratinocytes ◽  
Yeast Fermentation ◽  
Lauryl Sulfate ◽  
Human Epidermal Keratinocytes

Cannabigerol (CBG) is a minor non-psychoactive cannabinoid present in Cannabis sativa L. (C. sativa) at low levels (<1% per dry weight) that serves as the direct precursor to both cannabidiol (CBD) and tetrahydrocannabinol (THC). Consequently, efforts to extract and purify CBG from C. sativa is both challenging and expensive. However, utilizing a novel yeast fermentation technology platform, minor cannabinoids such as CBG can be produced in a more sustainable, cost-effective, and timely process as compared to plant-based production. While CBD has been studied extensively, demonstrating several beneficial skin properties, there are a paucity of studies characterizing the activity of CBG in human skin. Therefore, our aim was to characterize and compare the in vitro activity profile of non-psychoactive CBG and CBD in skin and be the first group to test CBG clinically on human skin. Gene microarray analysis conducted using 3D human skin equivalents demonstrates that CBG regulates more genes than CBD, including several key skin targets. Human dermal fibroblasts (HDFs) and normal human epidermal keratinocytes (NHEKs) were exposed in culture to pro-inflammatory inducers to trigger cytokine production and oxidative stress. Results demonstrate that CBG and CBD reduce reactive oxygen species levels in HDFs better than vitamin C. Moreover, CBG inhibits pro-inflammatory cytokine (Interleukin-1β, -6, -8, tumor necrosis factor α) release from several inflammatory inducers, such as ultraviolet A (UVA), ultraviolet B (UVB), chemical, C. acnes, and in several instances does so more potently than CBD. A 20-subject vehicle-controlled clinical study was performed with 0.1% CBG serum and placebo applied topically for 2 weeks after sodium lauryl sulfate (SLS)-induced irritation. CBG serum showed statistically significant improvement above placebo for transepidermal water loss (TEWL) and reduction in the appearance of redness. Altogether, CBG’s broad range of in vitro and clinical skin health-promoting activities demonstrates its strong potential as a safe, effective ingredient for topical use and suggests there are areas where it may be more effective than CBD.

scholarly journals N-Succinyl-S-Farnesyl-L-Cysteine (SFC): A Novel Isoprenylcysteine Analog with In Vitro Anti-Inflammatory Activity and Clinical Skin Protecting Properties

Cosmetics ◽  
2021 ◽  
Vol 8 (4) ◽  
pp. 110
Author(s):  
José R. Fernández ◽  
Karl Rouzard ◽  
Corey Fitzgerald ◽  
Jason Healy ◽  
Masanori Tamura ◽  
...  
Keyword(s):  
Small Molecule ◽  
Dermal Fibroblasts ◽  
Epidermal Keratinocytes ◽  
Double Blind ◽  
Human Epidermal Keratinocytes ◽  
New Class ◽  
Normal Human ◽  
Anti Inflammatory ◽  
Split Face

Over the past 15 years, small molecule isoprenylcysteine (IPC) analogs have been identified as a potential new class of topical anti-inflammatories. Clinical studies have demonstrated that IPCs are both safe and effective in promoting healthy skin when applied topically. This work aims to demonstrate N-Succinyl-S-farnesyl-L-cysteine (SFC) as a novel IPC molecule that provides a broad spectrum of benefits for skin. Human promyelocytic cell line HL-60, human dermal microvascular endothelial cells (HDMECs), human dermal fibroblasts (HDFs), and normal human epidermal keratinocytes (NHEKs) were exposed in culture to various inducers to trigger reactive oxygen species, cytokines, or collagenase production. A 49-subject randomized double-blind, vehicle-controlled, split face trial was performed with 1% SFC gel, or 5% niacinamide and vehicle applied for 12 weeks to evaluate anti-wrinkle and anti-aging endpoints. We demonstrated that SFC inhibited GPCR and TLR-induced pro-inflammatory cytokine release in NHEKs and HDMECs from several inflammatory inducers such as UVB, chemicals, cathelicidin, and bacteria. SFC successfully reduced GPCR-induced oxidation in differentiated neutrophils. Moreover, photoaging studies showed that SFC reduced UVA-induced collagenase (pro-MMP-1) production in HDFs. Clinical assessment of 1% SFC gel demonstrated improvement above the vehicle for wrinkle reduction, hydration, texture, and overall appearance of skin. N-Succinyl-S-farnesyl-L-cysteine (SFC) is a novel anti-inflammatory small molecule and is the first farnesyl-cysteine IPC shown to clinically improve appearance and signs of aging, while also having the potential to ameliorate inflammatory skin disorders.

scholarly journals A Novel Substance P-Based Hydrogel for Increased Wound Healing Efficiency

Molecules ◽  
2018 ◽  
Vol 23 (9) ◽  
pp. 2215 ◽  
Author(s):  
Da Kim ◽  
Ji Jang ◽  
Song Jang ◽  
Jungsun Lee
Keyword(s):  
Wound Healing ◽  
Substance P ◽  
Dermal Fibroblasts ◽  
Epidermal Keratinocytes ◽  
Human Epidermal Keratinocytes ◽  
In Vivo Experiments ◽  
And Migration ◽  
Proliferation And Migration

The neuropeptide substance P (SP) is known to stimulate wound healing by regulating the production of relevant cytokines as well as cell proliferation and migration. However, the therapeutic application of SP is limited by its low stability under biological conditions and oxidation during purification, formulation, and storage. To address this problem, we developed a novel formulation of SP as an SP gel, and investigated its wound healing activity both in vitro and in vivo. SP in SP gel was stable at various temperatures for up to 4 weeks. In vitro, SP gel exhibited more potential as a candidate wound-healing agent than SP alone, as evidenced by the observed increases in the proliferation and migration of human epidermal keratinocytes and human dermal fibroblasts. In vivo experiments showed that SP gel treatment enhanced the healing of full-thickness wounds in mice as compared to SP alone. These results demonstrate the benefits of SP gel as a promising topical agent for wound treatment.

Demonstration of a Choline Requirement for Optimal Keratinocyte Growth in a Defined Culture Medium

1988 ◽  
Vol 118 (12) ◽  
pp. 1487-1494 ◽  
Author(s):  
Philip R. Gordon ◽  
Liebe K. Gelman ◽  
Barbara A. Gilchrest
Keyword(s):  
Culture Medium ◽  
Basal Medium ◽  
Donor Cell ◽  
Cell Types ◽  
Dermal Fibroblasts ◽  
Cell Yield ◽  
Epidermal Keratinocytes ◽  
Good Growth ◽  
Human Epidermal Keratinocytes ◽  
Defined Culture

Abstract Nutrient requirements for proliferation and differentiated function of individual cell types can be determined using cell culture methodologies. Human epidermal keratinocytes are stimulated to grow by choline supplementation in the presence of myo-inositol when grown in a commercial nutrient medium containing six other defined supplements. The optimal range of choline concentrations varied among donor cell lines, but consistently fell between 36 µM and 180 µM. Addition of 72 µM choline increased cell yield to 250 ± 38% of that produced by myo-inositol supplementation alone and 92 ± 8% of that produced by addition of a highly mitogenic hypothalamic extract, which was previously required for good growth in this culture system. Supplementation of the basal medium with both the extract and choline resulted in 165 ± 13% of the cell yield observed with the extract addition alone. Supplementation with other phospholipid precursors did not further increase keratinocyte growth. Neither dermal fibroblasts nor epidermal melanocytes were stimulated by supplementation with choline, suggesting the high keratinocyte requirement is unusual. This completely defined culture medium for keratinocyte growth should prove useful in analyzing the role of phospholipids and other nutrients in human epidermis.

scholarly journals Laminarin Effects, a β-(1,3)-Glucan, on Skin Cell Inflammation and Oxidation

Cosmetics ◽  
2020 ◽  
Vol 7 (3) ◽  
pp. 66 ◽  
Author(s):  
Hélène Ozanne ◽  
Hechmi Toumi ◽  
Benoît Roubinet ◽  
Ludovic Landemarre ◽  
Eric Lespessailles ◽  
...  
Keyword(s):  
Hyaluronic Acid ◽  
Antioxidant Activities ◽  
Dermal Fibroblasts ◽  
Epidermal Keratinocytes ◽  
Type I ◽  
Human Epidermal Keratinocytes ◽  
Procollagen Type ◽  
Skin Cells ◽  
Radiation Conditions ◽  
Uva Radiation

Laminarin, a β-(1,3)-glucan from the seaweed Laminaria digitata, is a polysaccharide which provides anti-inflammatory and anti-oxidative properties. Its influence on both human dermal fibroblasts adult (HDFa) and normal human epidermal keratinocytes (NHEK) has not been established yet. Herein, laminarin effects were examined on skin cells’ mitochondrial and antioxidant activities. Cytokines, hyaluronic acid, and procollagen type I secretions and interaction mechanisms were explored after a maximum of 72 h treatment with laminarin. Our results demonstrated a decrease in mitochondrial activities with 72 h treatment with laminarin from 500 µg.mL−1 for NHEK cells and from 100 µg.mL−1 for HDFa cells without cytotoxicity. No variation of hyaluronic acid or type I procollagen was observed for all laminarin concentrations, while an antioxidant effect was found against reactive oxygen species (ROS) from 1 µg.mL−1 for HDFa cells in both H2O2 and UVA radiation conditions, and from 10 µg.mL−1 and 1 µg.mL−1 for NHEK cells in both H2O2 and UVA radiation conditions, respectively. Laminarin treatment modulated both cells surface glycosylation and cytokine secretions of skin cells. Overall, our data suggest a positive effect of β-(1,3)-glucan on skin cells on oxidative stress and inflammation induced by environmental factors. Of note, these effects are through the modulation of glycan and receptors interactions at the skin cells surface.

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