Topical Delivery of Niacinamide to Skin Using Hybrid Nanogels Enhances Photoprotection Effect

Niacinamide (NIA) has been widely used in halting the features of ageing by acting as an antioxidant and preventing dehydration. NIA’s physicochemical properties suggest difficulties in surpassing the barrier imposed by the stratum corneum layer to reach the target in the skin. To improve cutaneous delivery of NIA, a hybrid nanogel was designed using carrageenan and polyvinylpyrrolidone polymers combined with jojoba oil as a permeation enhancer. Three different types of transethosomes were prepared by the thin-film hydration method, made distinct by the presence of either an edge activator or a permeation enhancer, to allow for a controlled delivery of NIA. Formulations were characterized by measurements of size, polydispersity index, zeta potential, encapsulation efficiency, and loading capacity, and by evaluating their chemical interactions and morphology. Skin permeation assays were performed using Franz diffusion cells. The hybrid hydrogels exhibited robust, porous, and highly aligned macrostructures, and when present, jojoba oil changed their morphology. Skin permeation studies with transethosomes-loaded hydrogels showed that nanogels per se exhibit a more controlled and enhanced permeation, in particular when jojoba oil was present in the transethosomes. These promising nanogels protected the human keratinocytes from UV radiation, and thus can be added to sunscreens or after-sun lotions to improve skin protection.

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Penetration of Chlorhexidine into Human Skin

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.00637-08 ◽

2008 ◽

Vol 52 (10) ◽

pp. 3633-3636 ◽

Cited By ~ 38

Author(s):

T. J. Karpanen ◽

T. Worthington ◽

B. R. Conway ◽

A. C. Hilton ◽

T. S. J. Elliott ◽

...

Keyword(s):

Human Skin ◽

High Performance ◽

Skin Permeation ◽

Full Thickness ◽

Alternative Strategies ◽

Thickness Skin ◽

Skin Antisepsis ◽

Permeation Studies ◽

Franz Diffusion Cells

ABSTRACT This study evaluated a model of skin permeation to determine the depth of delivery of chlorhexidine into full-thickness excised human skin following topical application of 2% (wt/vol) aqueous chlorhexidine digluconate. Skin permeation studies were performed on full-thickness human skin using Franz diffusion cells with exposure to chlorhexidine for 2 min, 30 min, and 24 h. The concentration of chlorhexidine extracted from skin sections was determined to a depth of 1,500 μm following serial sectioning of the skin using a microtome and analysis by high-performance liquid chromatography. Poor penetration of chlorhexidine into skin following 2-min and 30-min exposures to chlorhexidine was observed (0.157 ± 0.047 and 0.077 ± 0.015 μg/mg tissue within the top 100 μm), and levels of chlorhexidine were minimal at deeper skin depths (less than 0.002 μg/mg tissue below 300 μm). After 24 h of exposure, there was more chlorhexidine within the upper 100-μm sections (7.88 ± 1.37 μg/mg tissue); however, the levels remained low (less than 1 μg/mg tissue) at depths below 300 μm. There was no detectable penetration through the full-thickness skin. The model presented in this study can be used to assess the permeation of antiseptic agents through various layers of skin in vitro. Aqueous chlorhexidine demonstrated poor permeation into the deeper layers of the skin, which may restrict the efficacy of skin antisepsis with this agent. This study lays the foundation for further research in adopting alternative strategies for enhanced skin antisepsis in clinical practice.

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Grape Pomace for Topical Application: Green NaDES Sustainable Extraction, Skin Permeation Studies, Antioxidant and Anti-Inflammatory Activities Characterization in 3D Human Keratinocytes

Biomolecules ◽

10.3390/biom11081181 ◽

2021 ◽

Vol 11 (8) ◽

pp. 1181

Author(s):

Angela Punzo ◽

Emanuele Porru ◽

Alessia Silla ◽

Patrizia Simoni ◽

Paola Galletti ◽

...

Keyword(s):

Skin Permeation ◽

Deep Eutectic Solvents ◽

Human Keratinocytes ◽

Skin Aging ◽

Grape Pomace ◽

Natural Deep Eutectic Solvents ◽

Franz Cells ◽

Permeation Studies ◽

Red Grape ◽

Potential Use

Food waste is a global problem due to its environmental and economic impact, so there is great demand for the exploitation of new functional applications. The winemaking process leads to an incomplete extraction of high-value compounds, leaving the pomace still rich in polyphenols. This study was aimed at optimising and validating sustainable routes toward the extraction and further valorisation of these polyphenols, particularly for cosmeceutical applications. New formulations based on red grape pomace polyphenols and natural deep eutectic solvents (NaDESs) were here investigated, namely betaine combined with citric acid (BET-CA), urea (BET-U) and ethylene glycol (BET-EG), in which DESs were used both as extracting and carrying agents for polyphenols. The flavonoid profile determined by HPLC-MS/MS analysis showed similar malvidin content (51–56 μg mL−1) in the DES combinations, while BET-CA gave the best permeation performance in Franz cells, so it was further investigated in 3D human keratinocytes (HaCat spheroids) injured with the pro-oxidant agent menadione. BET-CA treatment showed good intracellular antioxidant activity (IC50 0.15 ± 0.02 μg mL−1 in malvidin content) and significantly decreased (p < 0.001) the release of the pro-inflammatory cytokine IL-8, improving cell viability. Thus, BET-CA formulation is worthy of investigation for potential use as a cosmetic ingredient to reduce oxidative stress and inflammation, which are causes of skin aging.

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Stimuli Responsive Matrices for Medical Applications

Key Engineering Materials ◽

10.4028/www.scientific.net/kem.638.249 ◽

2015 ◽

Vol 638 ◽

pp. 249-254

Author(s):

Raluca Petronela Dumitriu ◽

Daniela Pamfil ◽

Manuela Tatiana Nistor ◽

Cornelia Vasile

Keyword(s):

Tissue Engineering ◽

Medical Application ◽

Controlled Delivery ◽

Hydroxyethyl Methacrylate ◽

Stimuli Responsive ◽

Stimuli Responsive Polymers ◽

Responsive Polymers ◽

Hybrid Hydrogels ◽

Isopropyl Acrylamide ◽

Different Types

Different types of stimuli responsive polymers that respond with a property change to a variation in the environmental conditions are an attractive class of materials for advanced applications in biomedical or pharmaceutical fields. Three types of responsive biocompatible and biodegradable polymer matrices are presented as potential biomaterials for medical application as carriers for various drugs and tissue engineering substitutes. Hybrid hydrogels based on collagen/ N-isopropyl acrylamide containing montmorillonite nanoparticles are promising materials for tissue engineering and also as carriers for norfloxacin, a chemotherapeutic antibacterial agent. Semi-interpenetrated hydrogels based either on substituted anhydride modified collagen and 2-hydroxyethyl methacrylate or on alginate and poly (N-isopropylacrylamide) were tested as matrices for the controlled delivery of bisoprolol fumarate, an antihypertensive drug and respectively of ketoprofen, a non-steroidal anti-inflammatory drug.

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Formulation and Evaluation of DHA Oil based Nicotinamide Nanoemulsion Gel for Treating Atopic Dermatitis

Nanoscience &Nanotechnology-Asia ◽

10.2174/2210681210666200210115526 ◽

2020 ◽

Vol 10 (6) ◽

pp. 892-901

Author(s):

Gayathri P. Pradeep ◽

Vidya Viswanad

Keyword(s):

Drug Release ◽

Cell Line ◽

Skin Permeation ◽

Skin Irritation ◽

In Vitro Drug Release ◽

Release Studies ◽

Nanoemulsion Gel ◽

Permeation Studies ◽

Franz Diffusion Cells

Background: Atopic dermatitis (or eczema) can be defined as a chronic inflammatory condition accompanied by severe pruritus. Objective: The prepared gel was evaluated for in vitro drug release, in vitro occlusion studies, transepidermal water loss studies, skin permeation studies, in vitro skin irritation studies and antiinflammatory cell line studies. Methods: In vitro drug release studies were performed using Franz diffusion cells. The in vitro occlusion studies were carried out by the procedure reported by Wissing et al. TEWL determination was done by the method proposed by Reiger. The skin permeation studies were carried out using porcine skin using Franz diffusion cells. In vitro skin irritation study was carried out using HETCAM (Hen’s Egg Test on the Chorioallantoic Membrane) method. Anti-inflammatory cell line studies were carried out using RAW 264.7 cell lines. Results: In vitro drug release studies,drug release of nicotinamide from nanoemulsion gel was found to be more than marketed gel. Kinetic modelling showed a higuchi model with non-fickian diffusion. In vitro occlusion study showed the percentage of evaporated water from prepared nanoemulsion formulation after 72 h is very less compared with the other formulations. The TEWL measurement shows the reduction in TEWL has more in prepared nanoemulsion gel than other formulations. Anti-inflammatory cell line studies proved that the nanoemulsion gel has inhibition capacity on COX activity, LOX activity, Inducibe nitric oxide synthase and cellular nitrate levels. Conclusion: DHA oil based nicotinamidenanoemulsion gel were prepared successfully and the evaluation of prepared gel showed better drug release and skin permeation with better antiinflammatory activity.

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Lamivudine Liposomes for Transdermal Delivery - Formulation, Characterization, Stability and In vitro Evaluation

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2008.1.4.1 ◽

2009 ◽

Vol 1 (4) ◽

pp. 317-326

Author(s):

Roopa Pai S. ◽

Kusum Devi V.

Keyword(s):

Drug Delivery ◽

Particle Size ◽

Oral Administration ◽

Skin Permeation ◽

Hiv Infections ◽

Permeation Studies ◽

Formulation Parameters ◽

Lower Temperature ◽

Franz Diffusion Cells

: Lamivudine, an antiretroviral is commonly used in the treatment of HIV infections. Upon oral administration, it exhibits dose dependent toxic effects such as hepatotoxicity, hyperglycemia, hyperlipidemia, lactic acidosis, lipodystropy, osteonecrosis. These side effects often require dosage reduction or even cessation of treatment. Thus, the problems associated with oral administration led us to explore the possibilities of designing novel drug delivery system for lamivudine with an alternative route of administration. In the present study, liposomes of lamivudine were prepared by thin film hydration and their potential for transdermal drug delivery has been evaluated in vitro. In the preparation of liposomes, process and formulation parameters were standardized. Liposomes were evaluated for their physicochemical properties such as appearance, particle size, particle size distribution and drug entrapment. Liposomes stored at lower temperature conditions, retained 96 % of the incorporated drug. Residual solvents in the formulation were determined by Gas Chromatography and content of lipids was estimated by Stewart assay. Permeation studies of liposomal formulations were carried out across rat abdominal skin using modified Franz diffusion cells. The lamivudine liposomes with good stability and appreciably controlled skin permeation with minimal retention of drug in the skin were successfully prepared

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Secretion of different types of gelatinases from cultured human keratinocytes

Journal of Dermatological Science ◽

10.1016/0923-1811(94)90417-0 ◽

1994 ◽

Vol 8 (1) ◽

pp. 70

Author(s):

T. Kobayash ◽

K. Sakuraoka ◽

S. Hattori ◽

Y. Nagai ◽

T. Nishikawa

Keyword(s):

Human Keratinocytes ◽

Different Types

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Development and evaluation of a heparin gel for transdermal delivery via laser-generated micropores

Therapeutic Delivery ◽

10.4155/tde-2020-0024 ◽

2021 ◽

Vol 12 (2) ◽

pp. 133-144

Author(s):

Deepal Vora ◽

Yujin Kim ◽

Ajay K Banga

Keyword(s):

Transdermal Delivery ◽

Continuous Intravenous Infusion ◽

In Vitro Permeation ◽

Assisted Delivery ◽

Permeation Studies ◽

Franz Diffusion Cells ◽

Transdermal Route ◽

Poloxamer Gel ◽

Ablative Laser

Aim: Our study investigated the feasibility of transdermal delivery of heparin, an anticoagulant used against venous thromboembolism, as an alternative to intravenous administration. Materials & methods: Skin was pretreated using ablative laser (Precise Laser Epidermal System [P.L.E.A.S.E.®] technology) for enhanced delivery of heparin. In vitro permeation studies using static Franz diffusion cells provided a comparison between delivery from 0.3% w/v heparin-loaded poloxamer gel and solution across untreated and laser-treated dermatomed porcine ear skin. Results: No passive delivery of heparin was observed. Laser-assisted delivery from solution (26.07 ± 1.82 μg/cm2) was higher (p < 0.05) than delivery from heparin gel (11.28 ± 5.32 μg/cm2). However, gel is likely to sustain the delivery over prolonged periods like a maintenance dose via continuous intravenous infusion. Conclusion: Thus, ablative laser pretreatment successfully delivered heparin, establishing the feasibility of delivering hydrophilic macromolecules using the transdermal route.

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Transdermal Nitroglycerin Delivery Using Acrylic Matrices: Design, Formulation, and In Vitro Characterization

ISRN Pharmaceutics ◽

10.1155/2014/493245 ◽

2014 ◽

Vol 2014 ◽

pp. 1-9 ◽

Cited By ~ 2

Author(s):

Houman Savoji ◽

Amir Mehdizadeh ◽

Ahmad Ramazani Saadat Abadi

Keyword(s):

Skin Permeation ◽

Peel Strength ◽

Adhesion Properties ◽

Pressure Sensitive Adhesives ◽

In Vitro Characterization ◽

Chemical Permeation Enhancers ◽

Transdermal Drug Delivery Systems ◽

Franz Diffusion Cells ◽

Chemical Permeation

Nitroglycerin (TNG) transdermal drug delivery systems (TDDSs) with different acrylic pressure-sensitive adhesives (PSAs) and chemical permeation enhancers (CPEs) were prepared. The effects of PSAs and CPEs types and concentrations on skin permeation and in vitro drug release from devices were evaluated using the dissolution method as well as the modified-jacketed Franz diffusion cells fitted with excised rat abdominal skin. It was demonstrated that the permeation rate or steady state flux (Jss) of the drug through the excised rat skin was dependent on the viscosity and type of acrylic PSA as well as the type of CPE. Among different acrylic PSAs, Duro-Tak 2516 and Duro-Tak 2054 showed the highest and Duro-Tak 2051 showed the lowest Jss. Among the various CPEs, propylene glycol and cetyl alcohol showed the highest and the lowest enhancement of the skin permeation of TNG, respectively. The adhesion properties of devices such as 180° peel strength and probe tack values were obtained. It was shown that increasing the concentration of CPE led to reduction in the adhesion property of PSA. Moreover, after optimization of the formulation, it was found that the use of 10% PG as a CPE and 25% nitroglycerin loading in Duro-Tak 2054 is an effective monolithic DIAP for the development of a transdermal therapeutic system for nitroglycerin.

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