scholarly journals Effect of Penetration Enhancers on Toenail Delivery of Efinaconazole from Hydroalcoholic Preparations

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1650
Author(s):  
Jun Soo Park ◽  
Jeong Soo Kim ◽  
Myoung Jin Ho ◽  
Dong Woo Park ◽  
Eun A. Kim ◽  
...  
Keyword(s):  
Antifungal Agents ◽  
Penetration Enhancers ◽  
Ambient Conditions ◽  
Permeation Enhancers ◽  
Drug Degradation ◽  
Franz Diffusion Cell ◽  
Promising Tool ◽  
In Vitro Permeation ◽  
Topical Solution

The incorporation of permeation enhancers in topical preparations has been recognized as a simple and valuable approach to improve the penetration of antifungal agents into toenails. In this study, to improve the toenail delivery of efinaconazole (EFN), a triazole derivative for onychomycosis treatment, topical solutions containing different penetration enhancers were designed, and the permeation profiles were evaluated using bovine hoof models. In an in vitro permeation study in a Franz diffusion cell, hydroalcoholic solutions (HSs) containing lipophilic enhancers, particularly prepared with propylene glycol dicaprylocaprate (Labrafac PG), had 41% higher penetration than the HS base. Moreover, the combination of hydroxypropyl-β-cyclodextrin with Labrafac PG further facilitated the penetration of EFN across the hoof membrane. In addition, this novel topical solution prepared with both lipophilic and hydrophilic enhancers was physicochemically stable, with no drug degradation under ambient conditions (25 °C, for 10 months). Therefore, this HS system can be a promising tool for enhancing the toenail permeability and therapeutic efficacy of EFN.

scholarly journals COMPARISON OF EFFECT OF PENETRATION ENHANCER ON DIFFERENT POLYMERS FOR DRUG DELIVERY

2019 ◽  
Vol 11 (1) ◽  
pp. 89
Author(s):  
Bhawana Sethi ◽  
Rupa Mazumder
Keyword(s):  
Oleic Acid ◽  
Permeation Enhancers ◽  
In Vitro Drug Release ◽  
Franz Diffusion Cell ◽  
In Vitro Permeation ◽  
Treatment Of Hypertension ◽  
Permeation Studies ◽  
Evaporation Technique ◽  
Polymer Interaction

Objective: Aliskiren hemifumarate is used for the treatment of hypertension. The aim of this research to study the effect on the delivery of drug using natural and synthetic permeation enhancers like limonene, cineol, β-cyclodextrin, and oleic acid by using different polymers. As different penetration acts differently with polymers.Methods: Transdermal patches were prepared by the solvent evaporation technique. The controlled release polymers were used for the preparation of patches. The patches were prepared with different polymers and different plasticizer. The drug and polymer interaction study was performed by Fourier transform infrared spectra. In vitro permeation studies were conducted using pretreated cellophane membrane using franz diffusion cell. Results: The prepared patches were evaluated for in vitro drug release, and the release profile was varied from 52.32% PGH (oleic acid) to 87.63% B (cineol). The permeability coefficient was found in the range of 5.82 to 8.32 cm/h, and corresponding flux was found between 281.61 to 729.08 µg/cm2/h on the prepared patches and statistical analysis performed using t-test (p<0.005).Conclusion: On the basis of the obtained results, it was concluded that patch prepared using methocel k 15 m as a polymer, glycerin as plasticizer and cineol as a permeation enhancer shows the maximum release. The increase in the release due to increase in the flux.

scholarly journals Validation of a Static Franz Diffusion Cell System for In Vitro Permeation Studies

2010 ◽  
Vol 11 (3) ◽  
pp. 1432-1441 ◽  
Author(s):  
Shiow-Fern Ng ◽  
Jennifer J. Rouse ◽  
Francis D. Sanderson ◽  
Victor Meidan ◽  
Gillian M. Eccleston
Keyword(s):  
Cell System ◽  
Diffusion Cell ◽  
Franz Diffusion Cell ◽  
In Vitro Permeation ◽  
Permeation Studies

scholarly journals Transdermal delivery of nobiletin using ionic liquids

2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Tadashi Hattori ◽  
Hiroki Tagawa ◽  
Makoto Inai ◽  
Toshiyuki Kan ◽  
Shin-ichiro Kimura ◽  
...  
Keyword(s):  
Transdermal Delivery ◽  
Water Solubility ◽  
Penetration Enhancers ◽  
Time Curve ◽  
Transdermal Administration ◽  
Franz Diffusion Cell ◽  
Geranic Acid ◽  
Delivery Approach

AbstractNobiletin (NOB), a flavonoid, has extremely low water solubility and low oral bioavailability; however, despite these problems, various physiological effects have been investigated in vitro. In the present study, we investigated the transdermal delivery of NOB using choline and geranic acid (CAGE), which is a biocompatible material that has been reported to be a promising transdermal delivery approach. The feasibility was evaluated by a set of in vitro and in vivo tests. A solubility evaluation demonstrated that CAGE induced excellent solubility of NOB induced by multipoint hydrogen bonding between NOB and CAGE. In vitro transdermal tests using a Franz diffusion cell showed that CAGE was effective in enhancing transdermal absorption of NOB, compared to other penetration enhancers. Subsequent in vivo tests demonstrated that CAGE significantly improved area under the concentration-time curve of NOB in vivo and NOB/CAGE sample showed 20-times higher bioavailability than oral administration of NOB crystal. Furthermore, NOB/CAGE sample also showed significant drops of the blood glucose level in rats derived from hypoglycemic activity of NOB. Thus, transdermal administration of NOB using CAGE was shown to be feasible, which indicates that the use of CAGE may be adapted for other flavonoids that also show both low water solubility and low permeability.

scholarly journals Development and Evaluation of Flupirtine Maleate Transdermal Patch Containing Different Permeation Enhancers

2021 ◽  
Vol 11 (5) ◽  
Keyword(s):  
Polyethylene Glycol ◽  
Polyvinyl Alcohol ◽  
Dimethyl Sulfoxide ◽  
Release Profile ◽  
Transdermal Patch ◽  
Permeation Enhancers ◽  
Peg 400 ◽  
Transdermal Patches ◽  
In Vitro Permeation

The present study was aimed at the formulation of transdermal patches of flupirtine maleate containing different permeation enhancers. It acts indirectly as N-methyl-D-aspartate (NMDA) receptor antagonist and activates the K+ channels; thereby acts as a skeletal muscle relaxant. Flupirtine maleate transdermal patches are intended to provide localized effect. The patches were prepared by solvent evaporation technique, using polyvinyl alcohol (PVA) as the polymer whereas dimethyl sulfoxide (DMSO) and polyethylene glycol (PEG-400) as the permeation enhancers. Methanol was used as a solvent to dissolve the drug and glycerol was used as the plasticizer. These patches were evaluated for in vitro permeation, tensile strength, percent moisture absorption, drug content uniformity, film thickness, weight variation and folding endurance. All the patches showed extended release properties. Formulation FDD8 containing 8% polymer and 2% DMSO was found to be the optimized formulation on the basis of evaluation parameters. In vitro permeation release was found to be 95.71 ± 0.01% at the end of 12 h. As the concentration of DMSO increased, the release profile of drug was enhanced. This indicated that DMSO improved the release profile of flupirtine maleate when compared to PEG-400. The release kinetics of the transdermal patches followed Higuchi matrix model. The stability studies showed that all the optimized patches were stable during their study period. From the present study, it can be concluded that addition of DMSO yields good result to enhance the permeation of the drug. Keywords: flupirtine maleate, transdermal patch, permeation enhancers, dimethyl sulfoxide DMSO, polyethylene glycol PEG-400, polyvinyl alcohol PVA.

Effect of Permeation Enhancers on Transdermal Delivery of Venlafaxine Hydrochloride from Carbopol Gel

2013 ◽  
Vol 6 (1) ◽  
pp. 1977-1982
Author(s):  
Shabnam Ain ◽  
J Dahiya ◽  
Babita K ◽  
V Gupta
Keyword(s):  
Oleic Acid ◽  
Olive Oil ◽  
Transdermal Delivery ◽  
Castor Oil ◽  
Permeation Rate ◽  
Penetration Enhancers ◽  
Permeation Enhancers ◽  
Permeable Membrane ◽  
Venlafaxine Hydrochloride

In this study, we investigated the effect of different permeation enhancers at different concentrations viz. oleic acid, olive oil and castor oil from transdermal gel for transdermal delivery of venlafaxine, a newer antidepressant. It is a first line drug in the treatment of depression and inhibits brain serotonin and norepinephrine neuronal reuptake. It is also used in the treatment of anxiety disorders. Transdermal delivery of venlafaxine hydrochloride may result in enhanced patient compliance by reducing the incidence of the undesirable GI problems associated with its multiple oral dosing. The differential scanning colorimetry study was used to investigate the drug-polymer interaction. The prepared gels were evaluated for several physico-chemical parameters such as drug content, spreadability, pH, viscosity and physical appearance to justify their suitability for topical use. The in vitro permeation studies were performed by using Franz diffusion cell and rat skin as a semi permeable membrane. This indicate that penetration enhancers in 5% v/w concentration enhance the permeation of venlafaxine hydrochloride but oleic acid show maximum permeation rate was 197 µg/cm2/hr as compared to olive oil (154.69µg/cm2/hr) and castor oil (175.8µg/cm2/hr). It is further optimized by increasing the concentration of permeation enhancer at levels as high as 10% v/w and 15% v/w. The result indicates that increase in the concentration of enhancer enhances the percutaneous permeation of venlafaxine. Oleic acid was found to be superior to olive oil and castor oil implying the ability of oleic acid to increase the drug diffusion by SC lipid disruption and increase partition coefficient into SC. The permeation rate of venlafaxine hydrochloride with 15% v/w oleic acid was higher (rat abdominal skin flux = 8.507 µg/cm2/h) than with 15% v/w olive oil and castor oil.  These studies show promising potential of transdermal patches of venlafaxine. 

scholarly journals Microemulsions as Solubilizers and Penetration Enhancers for Minoxidil Release from Gels

Gels ◽  
2021 ◽  
Vol 7 (1) ◽  
pp. 26
Author(s):  
Miroslava Špaglová ◽  
Mária Čuchorová ◽  
Martina Čierna ◽  
Silvester Poništ ◽  
Katarína Bauerová
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Penetration Enhancers ◽  
Permeation Enhancers ◽  
Permeable Membrane ◽  
Ex Vivo Permeation ◽  
Residual Amount ◽  
Natural Surfactants

Micro- and nanoemulsions are potential drug solubilizers and penetration enhancers through the high surfactant/co-surfactant content. This study aimed to evaluate the influence of minoxidil (MXD) solubilized in the microemulsions (MEs) on drug release by in vitro/ex vivo diffusion through the semi-permeable membrane Spectra/Por® (Spectrum Laboratory, Gardena, CA, USA) and porcine ear skin. Moreover, a residual amount of drug in the skin after ex vivo diffusion was evaluated. The reference MER, lecithin-containing MEL, and gelatin-containing MEG were characterized in terms of their size, polydispersity index, density, viscosity, electrical conductivity and surface tension. Based on the in vitro diffusion, it can be argued that MEL slowed down the drug release, while MER and MEG have no significant effect compared to the sample, in which propylene glycol (PG) was used as a solubilizer. Determination of the residual drug amount in the skin after 6 h of the ex vivo permeation was demonstrated as the most valuable method to evaluate the effectiveness of the ME’s application. The results indicate that the most optimal MXD permeation enhancers in alginate gel were the natural surfactants containing MEs. MXD solubilization in MEG and MEL had caused more than 5% of the drug remaining in the skin, which is almost a 1.5-fold higher amount compared to the reference gel.

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