scholarly journals Comparison of Synthetic Membranes to Heat-Separated Human Epidermis in Skin Permeation Studies In Vitro

Pharmaceutics ◽  
2021 ◽  
Vol 13 (12) ◽  
pp. 2106
Author(s):  
Anita Kovács ◽  
Stella Zsikó ◽  
Fanni Falusi ◽  
Erzsébet Csányi ◽  
Mária Budai-Szűcs ◽  
...  
Keyword(s):  
Gold Standard ◽  
Skin Permeation ◽  
Diclofenac Sodium ◽  
Human Epidermis ◽  
Formulation Development ◽  
Early Screening ◽  
Synthetic Membranes ◽  
Screening Model ◽  
Permeation Studies

In recent years, the study of dermal preparations has received increased attention. There are more and more modern approaches to evaluate transdermal formulations, which are crucial in proving the efficacy of a formulation. The aim of this study was to compare permeation across innovative synthetic membranes (Strat-M and Skin PAMPA membranes) and heat-separated human epidermis (HSE, gold standard membrane) using four different dermal formulations. The Strat-M and Skin PAMPA membranes were designed to mimic the stratum corneum layer of the human epidermis. There have also been some publications on their use in dermal formulation development, but further information is needed. Drug permeation was measured using formulations containing diclofenac sodium (two hydrogels and two creams). The HSE, Strat-M, and Skin PAMPA membranes proved to be significantly different, but based on the results, the Strat-M membrane showed the greatest similarity to HSE. The permeation data of the different formulations across different membranes showed good correlations with formulations similar to these four, which allows the prediction of permeation across HSE using these synthetic membranes. In addition, Strat-M and Skin PAMPA membranes have the potential to select and differentiate a dermal formulation containing diclofenac sodium as an early screening model.

Anti-Inflammatory Activity of Human Lens Crystallin Derived Peptide

2021 ◽  
Vol 18 ◽  
Author(s):  
Anuraag Muralidharan ◽  
Tenzin Tender ◽  
Pallavi K Shetty ◽  
Srinivas Mutalik ◽  
Krishna Sharma K ◽  
...  
Keyword(s):  
Free Radical ◽  
Skin Permeation ◽  
Diclofenac Sodium ◽  
Radical Scavenging ◽  
Free Radical Scavenging ◽  
Inflammatory Activity ◽  
Human Lens ◽  
Permeation Studies ◽  
Anti Inflammatory

Background: Inflammation has become the culmination point for several chronic diseases like skin diseases, asthma, neurological disorders, cancer and cardiovascular disorders. Mini αA-crystallin peptide, identified from a highly conserved region of human lens protein αA-crystallin, is known to have a chaperone-like function, hence has generated interest in exploring the anti-inflammatory potential of the peptide. Objective: The objective of the study was to evaluate anti-inflammatory potential of mini αA chaperone using in vitro, ex-vivo and in vivo models. Methods: The peptide was tested for its phosphodiestarase4 B inhibition, anti-inflammatory and free radical scavenging abilities in HaCat cells. Carbopol gel formulations with varying concentrations of mini αA-crystallin peptide and diclofenac sodium were prepared and optimized. Skin permeation studies of prepared formulations were carried out on excised abdominal skin of Wistar rat using a vertical type diffusion cell. Carrageenan induced rat paw oedema model was used for determining the anti-inflammatory potential of the peptide in prepared gel formulation with or without diclofenac sodium. Results: The peptide exhibited appreciable free radical scavenging and weak PDE4B inhibition. Gel formulation with 1% Tween-80, 1% carbopol and 10% ethanol showed better permeation compared to other formulations. The in vitro skin permeation studies revealed good improvement in permeation characteristics of diclofenac and peptide from the gels. The peptide was retained within the skin tissue, which is an ideal requirement for the delivery of anti-inflammatory topical formulation. In preclinical anti-inflammatory studies, gel formulation containing mini αA-peptide and diclofenac sodium showed a significant decrease in paw volume compared to other combinations tested. Conclusion: The study revealed the additive effect in anti-inflammatory activity by combining mini-αA peptide and diclofenac sodium which effectively reduced the inflammation.

scholarly journals Penetration of Chlorhexidine into Human Skin

2008 ◽  
Vol 52 (10) ◽  
pp. 3633-3636 ◽  
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.

scholarly journals FORMULATION DEVELOPMENT AND EVALUATION OF PRONIOSOMAL GEL OF ETHINYLESTRADIOL AND LEVONORGESTREL FOR ANTIFERTILITY TREATMENT

2019 ◽  
Vol 12 (1) ◽  
pp. 364
Author(s):  
Shikha Baghel Chauhan ◽  
Tanveer Naved ◽  
Nayyar Parvez
Keyword(s):  
Optical Microscopy ◽  
Encapsulation Efficiency ◽  
In Vitro Release ◽  
Stability Studies ◽  
Formulation Development ◽  
Promising Alternative ◽  
Size And Shape ◽  
Permeation Studies ◽  
Gel Formulations

Objective: The purpose of this research was to develop and formulate proniosomal gel drug delivery system of ethinylestradiol and levonorgestrel for antifertility treatment that is capable of efficiently delivering entrapped drug over an extended period of time.Methods: Ethinylestradiol and levonorgestrel are encapsulated in various formulations of proniosomal gel composed of various ratios of span surfactant, cholesterol, soya lecithin, and alcohol as aqueous phase prepared by coacervation-phase separation method. The prepared formulations characterized for drug encapsulation efficiency, size distribution, in vitro release studies, and vesicular stability at different storage conditions were carried. Stability studies for proniosomal gel were carried out for a few weeks. Morphological size and shape of the vesicles are characterized using optical microscopy and scanning electron microscopy (SEM). Stability studies for proniosomal gel were carried out for 3 months.Results: Morphological size and shape of the vesicles are characterized using optical microscopy and SEM, particles are found to be spherical, size of the particles is in the range of 46.4–80.6 nm, and permeation studies showed good control release for prolonged period of time. The encapsulation efficiency of proniosomal gel formulations is in the range of 74–80% and in vitro permeation studies proved that good amount of drug is permeated and has reasonably good stability characteristics as well.Conclusions: The results suggest that proniosomal gel formulations of ethinylestradiol and levonorgestrel may be used for transdermal delivery for antifertility treatment. The dried proniosomal formulation could act as a promising alternative to niosomes.

scholarly journals Determination of Diclofenac Sodium in Eagle's Minimum Essential Medium with Earle's Balanced Salt Solution

2003 ◽  
Vol 86 (4) ◽  
pp. 681-684
Author(s):  
Patrícia S Lopes ◽  
Telma M Kaneko ◽  
Carolina Y Takano ◽  
Aurea C L Lacerda ◽  
Leandro R Latorre ◽  
...  
Keyword(s):  
Salt Solution ◽  
Diclofenac Sodium ◽  
Reversed Phase ◽  
Minimum Essential Medium ◽  
In Vitro Permeation ◽  
Hydrophilic Drug ◽  
Permeation Studies ◽  
The Mean

Abstract A validated method was developed for determination of diclofenac sodium, considered a model hydrophilic drug for in vitro permeation studies, in Eagle's Minimum Essential Medium (MEM) with Earle's balanced salt solution. Liquid chromatography was used to determine diclofenac sodium. This method was developed with a reversed-phase column Supercosil LC 18, DB 25 cm × 4.5 mm; the mobile phase was methanol with 3% (v/v) acetic acid–Milli-Q water (74 + 26), and detection was at 283 nm. The detection and quantitation limits were 2.41 × 10–8 and 3.31 × 10–5 μg/μL, respectively. The accuracy within-day (n = 3) and day-to-day (n = 7) was 98.83%; the mean variation coefficient for inter- (n = 7) and intraday precision (n = 3) was 12.20%, thus, not exceeding 15%. This method can be used as an analytical procedure for the determination of diclofenac sodium in MEM for in vitro permeation studies.

scholarly journals A stepwise protocol for drug permeation assessment that combines heat-separated porcine ear epidermis and vertical diffusion cells

2018 ◽  
Vol 72 (1) ◽  
pp. 47-53 ◽  
Author(s):  
Ivana Pantelic ◽  
Tanja Ilic ◽  
Bojan Markovic ◽  
Sanela Savic ◽  
Milica Lukic ◽  
...  
Keyword(s):  
Evaluation Method ◽  
In Vitro Test ◽  
Formulation Development ◽  
Vertical Diffusion ◽  
Synthetic Membranes ◽  
Drug Permeation ◽  
Diffusion Cells ◽  
Drug Sample ◽  
Model Drug

After decades long absence of an official consensus on the most appropriate evaluation method for in vitro skin performance of topical semisolid drugs, United States Pharmacopoeia (USP 39) finally suggested three types of testing equipment; however, all these provide data on drug release using inert synthetic membranes. Considering the need for a readily available membrane that would be more structurally similar to human skin, this paper provides a detailed protocol of a method for drug permeation assessment that uses heat-separated porcine ear epidermis and modified Franz diffusion cells. Phases that were shown to be critical for variability of the results are identified (e.g., membrane preparation), and process parameters optimized. Applicability of the method was tested on four cream samples loaded with aceclofenac as a model drug. Sample compositions were designed in such a way to provide ?large? variations (variation of the main stabilizer: natural-origin versus synthetic emulsifier) and relatively ?minor? variations (co-solvent variation: none/isopropanol/glycerol). The developed protocol is a straightforward and reliable in vitro test for the evaluation of rate and extent of drug delivery into/through the skin. Moreover, this protocol may be routinely applied even in averagely equipped laboratories during formulation development or preliminary bioequivalence assessment of generic topical semisolids.

scholarly journals EFFECT OF HYDROPHILIC AND HYDROPHOBIC POLYMER MATRIX ON THE TRANSDERMAL DRUG DELIVERY OF ETHINYLESTRADIOL AND MEDROXYPROGESTERONE ACETATE

2019 ◽  
Vol 11 (1) ◽  
pp. 210
Author(s):  
Shikha Baghel Chauhan ◽  
Tanveer Naved ◽  
Nayyar Parvez
Keyword(s):  
Medroxyprogesterone Acetate ◽  
Ethyl Cellulose ◽  
Skin Permeation ◽  
Eudragit Rs ◽  
Hydrophobic Polymer ◽  
In Vitro Permeation ◽  
In Vitro Skin Permeation ◽  
Permeation Studies ◽  
Eudragit Rl

Objective: The aims of the present study were to develop different matrix patches with various ratios of hydrophilic and hydrophobic polymer combinations such as ethyl cellulose (EC) and polyvinylpyrrolidone (PVP) and eudragit RL 100 (ERL) and eudragit RS 100 (ERS) containing ethinylestradiol and medroxyprogesterone acetate and to perform physicochemical characterization and in vitro permeation studies through rat skin.Methods: Six formulations (F1 to F6) were developed by varying the concentration of both hydrophilic and hydrophobic polymer and keeping the drug load constant. Physical parameters and drug excipient interaction studies were evaluated in all the formulations. In vitro, skin permeation profiles of ethinylestradiol and medroxyprogesterone acetate from various formulations were simultaneously characterized in a thermostatically controlled modified Franz Diffusion cell. The physicochemical compatibility of the drug and the polymers was studied by differential scanning calorimetry.Results: The results suggested no physicochemical incompatibility between the drug and the polymers. In vitro permeation studies were performed by using Franz diffusion cells, patches coded as F3 (ethyl cellulose: polyvinylpyrrolidone, 7.5:2.5) and F6 (eudragit RL 100 (ERL) and eudragit RS 100 (ERS), 8:2) can be chosen for further in vivo studies. The results followed Higuchi kinetics (r = 0.9953-0.9979), and the mechanism of release was diffusion mediated. Based on physicochemical and in vitro skin permeation studies of 85.64% (for F3) and 88.62% (for F6) of ethinylestradiol and medroxyprogesterone acetate.Conclusion: The developed transdermal patches are stable, non-irritating and had increased efficacy of ethinylestradiol and medroxyprogesterone acetate and therefore had a good potential for antifertility treatment.

Ketorolac amide prodrugs for transdermal delivery: stability and in vitro rat skin permeation studies

2005 ◽  
Vol 293 (1-2) ◽  
pp. 193-202 ◽  
Author(s):  
Bo-Yeon Kim ◽  
Hea-Jeong Doh ◽  
Thanh Nguyen Le ◽  
Won-Jea Cho ◽  
Chul-Soon Yong ◽  
...  
Keyword(s):  
Transdermal Delivery ◽  
Skin Permeation ◽  
Rat Skin ◽  
Permeation Studies

scholarly journals Lipid-based nanocarriers to enhance skin permeation and antioxidant activity of Centella asiatica extract

2018 ◽  
Vol 192 ◽  
pp. 01016
Author(s):  
Boonnada Pamornpathomkul ◽  
Worranan Rangsimawong ◽  
Theerasak Rojanarata ◽  
Praneet Opanasopit ◽  
Chuleerath Chaiyodsilp ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Skin Permeation ◽  
Centella Asiatica ◽  
Entrapment Efficiency ◽  
Dpph Assay ◽  
Significant Difference ◽  
In Vitro Skin Permeation ◽  
Permeation Studies ◽  
Solution Formulation

The purpose of this study was to evaluate the use of different formulations, including solution, gel, liposome and niosome for in vitro skin permeation and antioxidant activity of Centella asiatica (CA) extract. The liposomes and niosomes loaded with CA were characterized to observe the physicochemical properties i.e., particle size, zeta potential, percentage of entrapment efficiency (%EE) and percentage of loading efficiency (%LE). In vitro skin permeation studies revealed that liposome formulations had a superior enhancing effect on skin permeation compared to niosome, gel and solution formulation. Upon applied niosome formulations for the delivery of CA extract at 24 hours (h), the antioxidant activity was higher than liposome, gel and solution formulation, as evidenced by the increased in percent inhibition using 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. However, there was no significant difference in antioxidant activity between niosome and liposome formulations. Accordingly, both the liposome and noisome formulations are promising approaches for transdermal delivery of CA extract for promoting successful antioxidant activity.

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