In Vitro Skin Penetration of Ethylene Glycol Using Excised Skin from Mice and Humans

Sun, James D.; Frantz, Stephen W.; Beskitt, Joyce L.

doi:10.3109/15569529509037554

Cited by 18 publications

(11 citation statements)

References 14 publications

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“…In addition, the use of semi-solid formulations such as gels as a delivery system can provide a faster release of drug substances and increase the residence time on skin and good hydration for optimal penetration through the micropores. The results of this study confirm the report that Methylcellulose is effective in enhancing drug permeation through human skin [16,17].…”

Section: Figuresupporting

confidence: 91%

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Formulation and Comparative Characterization of Methylcellulose, Carbomer and Petrolatum Gels for Topical and Transdermal Delivery of Zosyn (Piperacillin/Tazobactam) Antibiotics

Yeboah¹,

Ltd²

2020

PPPS

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Piperacillin/Tazobactam otherwise known as Zosyn is a broad-spectrum combination antibiotic used to treat severe infections. It combines the high antibiotic activity of piperacillin with β-lactamase inhibitor properties of tazobactam that helps to restore the susceptibility of bacteria to the antibiotic and prevents resistance. Despite this interesting pharmacological profile, Zosyn is given intravenously because of its poor oral absorption and short half-life of between only 0.8 and 1.1 hours. However, this system of delivery is not convenient because it is invasive, requires continuous monitoring of patients, and incompatibility issues with other intravenous therapy. The purpose of this study, therefore, was to comparatively characterize an extended release gel formulation from Methylcellulose, Carbomer and Petrolatum and evaluate their suitability for topical and transdermal administration of the drug.Methodology: Gels with 1%, 5% and 10% drug loadings were prepared with the three polymers. The physical characterization of the formulations was done for: drug release using dissolution apparatus; percutaneous absorption in rat skin using microporation technique and Franz cell apparatus. Drug stability studies were conducted at 25°C, 37°C and 45°C and at skin pH of 5. The formulations were also tested for chemical degradation under acidic/ basic and oxidizing/reduction conditions similar to those found on the skin and in wounds with 0.01mol/l HCL, 0.01 mol/l NaOH, 0.1% H 2 O 2 , and 1M KI for 2 hours. Results:The results showed that the gel with 10% drug loaded Methylcellulose formulation was more stable at temperatures studied and less susceptible to chemical degradation for all the chemicals used. The release of drug from the formulations was relatively high in the Methylcellulose (40.9%) and Carbomer (27.59%) gels but were limited in the Petrolatum (3.97%). Furthermore, transdermal delivery using microporation showed high permeation of 12.7%, 6.08% and 6.97% for the 10% drug loaded gels of Methylcellulose, Carbomer and Petrolatum respectively. The drug in the Methylcellulose was found to be subjected to higher degradation in basic medium by an oxidation pathway. Conclusion:The 5% methylcellulose gel formulation containing 10% Zosyn loading was found to have the most potential for effective topical administration and extended-release transdermal delivery of the Zosyn.

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Section: Figuresupporting

confidence: 91%

“…It is especially, used to produce thixotropic gels, emulsions and sprays. The polymers have been reported to be effective in enhancing drug permeation in human skin [16,17].…”

Section: Gel Formulations From Cellulose Carbomer and Petrolatummentioning

confidence: 99%

Formulation and Comparative Characterization of Methylcellulose, Carbomer and Petrolatum Gels for Topical and Transdermal Delivery of Zosyn (Piperacillin/Tazobactam) Antibiotics

Yeboah¹,

Ltd²

2020

PPPS

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“…It is important to optimize the topical formulations to get appropriate permeation of the drug through the skin. Hydroxypropyl methylcellulose (HPMC) has been stated to be effective in enhancing the drug permeation through human skin [ 12 , 13 ]. Hence, HPMC was examined for its permeation enhancement ability in this research work.…”

Section: Introductionmentioning

confidence: 99%

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

Al‐Suwayeh

Taha

Alqahtani

et al. 2014

The Scientific World Journal

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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 vitro skin permeation of LOR was conducted. The effect of hydroxypropyl β-cyclodextrin (HP β-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 HP β-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 HP β-CD and may be promising in enhancing permeation.

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“…The reported values for the skin penetration of EG vary by up to 1300-fold across studies (Loden 17 : 118 µg/cm 2 h and Driver et al 18 : 0.02-0.9 µg/cm 2 h); therefore, it is not clear how reliable these data are for dermal exposure assessment. Sun et al 19 conducted their study using fresh full-thickness skin samples obtained from surgical procedure and obtained lower penetration rates (7-13 µg/cm 2 h) than Loden 17 who conducted the study using dermatomed skin. Driver et al 18 reported a much lower rate of penetration of EG through dermatomed skin; however, they applied very low (finite) doses of EG to skin samples.…”

Section: Introductionmentioning

confidence: 99%

Dermal Penetration of Ethylene Glycol Through Human Skin In Vitro

2010

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This study was conducted to determine the in vitro dermal absorption of ethylene glycol (EG) through dermatomed human abdominal skin (containing epidermis and dermis), obtained from cadavers within 24 hours of death and kept frozen until processed. Three formulations of EG (neat, 50%, and 10% aqueous solutions) were applied in triplicate to skin samples from 6 donors, and placed in Teflon Bronaugh flow-through diffusion cells. Barrier integrity of each sample was evaluated with (3)H-H(2)O prior to applying EG and only data from samples passing the test were used. A physiological receptor fluid was pumped beneath the skin samples and collected in a fraction collector at predetermined time points through 24 hours. Possible volatilized EG was trapped in a charcoal basket located above each skin sample. Each skin sample was treated with an infinite dose of 500 microL of EG formulation/cm(2). At the end of 24 hours, volatilized EG trapped in the headspace was collected, the unabsorbed dose was removed from the skin and the skin was rinsed, tape stripped, and solubilized along with a rinse of the flow-through cells, and total radioactivity was determined. Only a small fraction (

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In Vitro Skin Penetration of Ethylene Glycol Using Excised Skin from Mice and Humans

Cited by 18 publications

References 14 publications

Formulation and Comparative Characterization of Methylcellulose, Carbomer and Petrolatum Gels for Topical and Transdermal Delivery of Zosyn (Piperacillin/Tazobactam) Antibiotics

Formulation and Comparative Characterization of Methylcellulose, Carbomer and Petrolatum Gels for Topical and Transdermal Delivery of Zosyn (Piperacillin/Tazobactam) Antibiotics

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

Dermal Penetration of Ethylene Glycol Through Human Skin In Vitro

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