scholarly journals Enhanced skin permeation of a novel peptide via structural modification, chemical enhancement, and microneedles

2020 ◽  
Author(s):  
Jungen Chen ◽  
Junxing Bian ◽  
Basil M. Hantash ◽  
David E. Hibbs ◽  
Chunyong Wu ◽  
...  
Keyword(s):  
Structural Modification ◽  
Skin Permeation ◽  
Skin Condition ◽  
Penetration Enhancers ◽  
Chemical Enhancement ◽  
Large Molecular Weight ◽  
Psychosocial Consequences ◽  
Common Skin ◽  
Microneedle Patch

AbstractHyperpigmentation is a common skin condition with serious psychosocial consequences. Decapeptide-12, a novel peptide, has been found to be safer than hydroquinone in reducing content of melanin, with efficacy up to more than 50% upon 16 weeks of twice daily treatment. However, the peptide suffers from limited transcutaneous penetration due to its hydrophilicity and large molecular weight. Therefore, decapeptide-12 was modified by adding a palmitate chain in an attempt to overcome this limitation. We also tested the effects of chemical penetration enhancers and microneedles to deliver two peptides through skin. Enhanced skin permeation was found using an in vitro human skin permeation model. Moreover, we examined peptide retention of different formulations in skin. Our data showed that palm-peptides in microneedle patch was the most effective.

scholarly journals FORMULATION AND EVALUATION OF TRANSDERMAL PATCHES OF METOPROLOL TARTRATE USING PERMEATION ENHANCERS OF NATURAL AND SYNTHETIC ORIGIN

2019 ◽  
pp. 317-323
Author(s):  
SHIKHA BAGHEL CHAUHAN ◽  
SUSHILA SAINI
Keyword(s):  
Moisture Absorption ◽  
Skin Permeation ◽  
Penetration Enhancers ◽  
Moisture Loss ◽  
Metoprolol Tartrate ◽  
Peg 400 ◽  
Transdermal Patches ◽  
Weight Variation ◽  
Basil Oil

Objective: Oral metoprolol tartrate has a short elimination half-life (2-3h) and low bioavailability undergoes extensive first-pass metabolism and frequent dosing. The aim of the present investigation was to formulate, develop and evaluate metoprolol tartrate transdermal patches using various synthetic and natural penetration enhancers. Methods: Enhancers used were eugenol, limonene, basil oil, urea and SLS (sodium lauryl sulphate). Polymer used was chitosan and PEG 400 used as a plasticizer. Transdermal Films were prepared by using solvent casting method. FTIR and DSC were studied to assess any interaction between the drug and polymers. Films were evaluated for Physico-chemical Characteristics like thickness, weight variation, folding endurance, moisture loss, moisture absorption and drug content. In vitro skin permeation studies were performed using Keshary chien cell For 24 h across rat skin. Results: Chitosan was found to be a suitable polymer for matrix formation. 3.5% w/w was used to optimize to formulate transdermal patches. 1.5% of total solution v/v lactic acid was used for dissolution of chitosan. 2.5%v/v of total solution PEG 400 was used to provide plasticity and smoothness to the patches. From the evaluation of patches formulation, F10 containing Basil oil as penetration enhancer in the concentration of 1.5% v/v was found to be best among all batches because of its consistent release rate For 24 h and extent of drug release was 85.20%. It can be concluded that naturally occurring volatile oils i.e., terpenes appear acceptable permeation enhancer and shows the best permeation across skin as indicated by high percutaneous enhancement ability. Conclusion: The developed transdermal patches are stable, non-irritating, and had increased efficacy of metoprolol and therefore had a good potential for hypertension treatment.

scholarly journals Evaluation of Skin Permeation and Analgesic Activity Effects of Carbopol Lornoxicam Topical Gels Containing Penetration Enhancer

2014 ◽  
Vol 2014 ◽  
pp. 1-9 ◽  
Author(s):  
Saleh A. Al-Suwayeh ◽  
Ehab I. Taha ◽  
Fahad M. Al-Qahtani ◽  
Mahrous O. Ahmed ◽  
Mohamed M. Badran
Keyword(s):  
Analgesic Activity ◽  
Skin Permeation ◽  
Tween 80 ◽  
Skin Penetration ◽  
Penetration Enhancers ◽  
Topical Gel ◽  
Carbopol Gel ◽  
Franz Diffusion Cells ◽  
Gel Formulations

The current study was designed to develop a topical gel formulation for improved skin penetration of lornoxicam (LOR) for enhancement of its analgesic activity. Moreover, the effect of different penetration enhancers on LOR was studied. The LOR gel formulations were prepared by using hydroxylpropyl methylcellulose (HPMC) and carbopol. The carbopol gels in presence of propylene glycol (PG) and ethanol were developed. The formulated gels were characterized for pH, viscosity, and LOR release using Franz diffusion cells. Also,in vitroskin permeation of LOR was conducted. The effect of hydroxypropylβ-cyclodextrin (HPβ-CD), beta-cyclodextrin (β-CD), Tween 80, and oleic acid on LOR permeation was evaluated. The optimized LOR gel formulation (LORF8) showed the highest flux (14.31 μg/cm2/h) with ER of 18.34 when compared to LORF3. Incorporation of PG and HPβ-CD in gel formulation (LORF8) enhanced the permeation of LOR significantly. It was observed that LORF3 and LORF8 show similar analgesic activity compared to marketed LOR injection (Xefo). This work shows that LOR can be formulated into carbopol gel in presence of PG and HPβ-CD and may be promising in enhancing permeation.

Influence of different penetration enhancers on in vitro skin permeation and in vivo photoprotective effect of flavonoids

1998 ◽  
Vol 175 (1) ◽  
pp. 85-94 ◽  
Author(s):  
Antonella Saija ◽  
Antonio Tomaino ◽  
Domenico Trombetta ◽  
Marcella Giacchi ◽  
Anna De Pasquale ◽  
...  
Keyword(s):  
Skin Permeation ◽  
Penetration Enhancers ◽  
In Vitro Skin Permeation

scholarly journals 1105 The effect of chemical penetration enhancers and dosage form on in vitro skin permeation

2018 ◽  
Vol 138 (5) ◽  
pp. S187
Author(s):  
G. Krishnan ◽  
M. Patel ◽  
B. Upadhyay ◽  
L. Garcowski ◽  
A. Anthony ◽  
...  
Keyword(s):  
Dosage Form ◽  
Skin Permeation ◽  
Penetration Enhancers ◽  
In Vitro Skin Permeation ◽  
Chemical Penetration Enhancers

scholarly journals Formulation of Novel Liquid Crystal (LC) Formulations with Skin-Permeation-Enhancing Abilities of Plantago lanceolata (PL) Extract and Their Assessment on HaCaT Cells

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 1023
Author(s):  
Dóra Kósa ◽  
Ágota Pető ◽  
Ferenc Fenyvesi ◽  
Judit Váradi ◽  
Miklós Vecsernyés ◽  
...  
Keyword(s):  
Liquid Crystal ◽  
Skin Permeation ◽  
Plantago Lanceolata ◽  
Antioxidant Properties ◽  
Pharmaceutical Formulations ◽  
Biological Properties ◽  
Penetration Enhancers ◽  
Hacat Cells ◽  
Toxicity Screening

Exposure to reactive oxygen species can easily result in serious diseases, such as hyperproliferative skin disorders or skin cancer. Herbal extracts are widely used as antioxidant sources in different compositions. The importance of antioxidant therapy in inflammatory conditions has increased. Innovative formulations can be used to improve the effects of these phytopharmacons. The bioactive compounds of Plantago lanceolata (PL) possess different effects, such as anti-inflammatory, antioxidant, and bactericidal pharmacological effects. The objective of this study was to formulate novel liquid crystal (LC) compositions to protect Plantago lanceolata extract from hydrolysis and to improve its effect. Since safety is an important aspect of pharmaceutical formulations, the biological properties of applied excipients and blends were evaluated using assorted in vitro methods on HaCaT cells. According to the antecedent toxicity screening evaluation, three surfactants were selected (Gelucire 44/14, Labrasol, and Lauroglycol 90) for the formulation. The dissolution rate of PL from the PL-LC systems was evaluated using a Franz diffusion chamber apparatus. The antioxidant properties of the PL-LC systems were evaluated with 2,2-diphenyl-1-picrylhydrazyl (DPPH) and malondialdehyde (MDA) assessments. Our results suggest that these compositions use a nontraditional, rapid-permeation pathway for the delivery of drugs, as the applied penetration enhancers reversibly alter the barrier properties of the outer stratum corneum. These excipients can be safe and highly tolerable thus, they could improve the patient’s experience and promote adherence.

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 Permeability of Ibuprofen in the Form of Free Acid and Salts of L-Valine Alkyl Esters from a Hydrogel Formulation through Strat-M™ Membrane and Human Skin

Materials ◽  
2021 ◽  
Vol 14 (21) ◽  
pp. 6678
Author(s):  
Joanna Klebeko ◽  
Paula Ossowicz-Rupniewska ◽  
Anna Nowak ◽  
Ewa Janus ◽  
Wiktoria Duchnik ◽  
...  
Keyword(s):  
Human Skin ◽  
Free Acid ◽  
Skin Permeation ◽  
Skin Penetration ◽  
Hplc Method ◽  
Penetration Enhancers ◽  
In Vitro Permeation ◽  
Cumulative Mass ◽  
Permeation Test

This paper aimed to evaluate the effect of vehicle and chemical modifications of the structure of active compounds on the skin permeation and accumulation of ibuprofen [IBU]. In vitro permeation experiments were performed using human abdominal skin and Strat-M™ membrane. The HPLC method was used for quantitative determinations. The formulations tested were hydrogels containing IBU and its derivatives and commercial gel with ibuprofen. The results obtained indicate that Celugel® had an enhancing effect on the skin penetration of IBU. The average cumulative mass of [IBU] after 24 h permeation test from Celugel® formulation through human skin was over 3 times higher than for the commercial product. Three ibuprofen derivatives containing [ValOiPr][IBU], [ValOPr][IBU], and [ValOBu][IBU] cation were evaluated as chemical penetration enhancers. The cumulative mass after 24 h of penetration was 790.526 ± 41.426, 682.201 ± 29.910, and 684.538 ± 5.599 μg IBU cm−2, respectively, compared to the formulation containing unmodified IBU-429.672 ± 60.151 μg IBU cm−2. This study demonstrates the perspective of the transdermal hydrogel vehicle in conjunction with the modification of the drug as a potential faster drug delivery system.

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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