Enhancing the nail permeability of topically applied drugs

Murdan, Sudaxshina

doi:10.1517/17425240802497218

Cited by 124 publications

(120 citation statements)

References 75 publications

Supporting

Mentioning

111

Contrasting

Unclassified

Order By: Relevance

“…Hydration and especially penetration enhancer treatment significantly decreased the absorbance maximum of the amide I band and significantly increased those of the amide II and amide III bands; iontophoresis also decreased amide I but had no significant effect on the other two (Table II, Figure 4), a finding which is consistent with previous IR measurements on SC protein post-current passage (27,30), and with earlier work on human nails using near-IR FT-Raman spectroscopy that revealed only minor changes in protein-associated bands post-hydration (24). The effects of N-acetyl-L-cysteine on the amide signals are the most notable of the treatments considered in the current work, in accord with this enhancer's ability to break disulphide bonds and to provoke conformational changes and increased water access to additional sites in the protein (6,7,8). Corroborating this deduction is recent evidence from scanning electron microscopy and mercury intrusion porosimetry (9) that N-acetyl-L-cysteine increases the apparent surface porosity of human nails to a significantly greater extent than simple hydration.…”

Section: Discussionsupporting

confidence: 65%

“…While topical treatments minimize systemic adverse effects, and avoid the pain associated with intralesional injections, they have limited efficacy (1-4) due primarily to the nature and structure of the nail plate that severely limit drug penetration to the target site of action (5,6). Much research has examined strategies to improve drug delivery to and across the nail (6)(7) including the use of penetration enhancers, such as N-acetyl-L-cysteine which breaks disulphide bonds in keratin, the main constituent of the nail plate (6)(7)(8)(9). Another approach is iontophoresis (10) which involves drug administration to the nail with the application of a small electrical current to enhance molecular transport.…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Effects of Iontophoresis, Hydration, and Permeation Enhancers on Human Nail Plate: Infrared and Impedance Spectroscopy Assessment

et al. 2013

View full text Add to dashboard Cite

Infrared and impedance spectroscopies were used to investigate the effects of hydration, iontophoresis and chemical enhancer (N-acetyl-L-cysteine) treatment on the healthy human nail.Although significant shifts to higher wavenumbers were observed for the symmetric and asymmetric -CH 2 stretching vibrations, the fact that these changes were essentially the same for the three treatments suggested that they were principally due to hydration alone. Spectral changes associated with amide bonds from nail protein were particularly evident post-treatment with Nacetyl-L-cysteine. The alternating current conductivity and permittivity of the nail, particularly at low frequencies, increased with hydration. Iontophoresis increased the low frequency ac conductivity of the nail but had less effect on the nail capacitance/permittivity. Further, the effects seemed to return gradually to baseline after termination of current passage. Treatment with N-acetyl-L-cysteine produced a greater perturbation, leading to increased low-frequency conductivity and a shift of the frequency-dependent conductivity region to a higher frequency. Overall, the effects of iontophoresis on both the IR and impedance spectroscopic profiles of the nail were attributable simply to increased hydration and similar to those observed after skin iontophoresis. In contrast, both spectroscopy techniques indicated that N-acetyl-L-cysteine disrupted nail structure in line with the enhancer's known effect on keratin.

show abstract

Section: Discussionsupporting

confidence: 65%

Section: Introductionmentioning

confidence: 99%

Effects of Iontophoresis, Hydration, and Permeation Enhancers on Human Nail Plate: Infrared and Impedance Spectroscopy Assessment

et al. 2013

View full text Add to dashboard Cite

show abstract

“…One of the approaches to improve the passive transungual drug delivery is the use of chemical penetration enhancers. Various methods have been investigated and reported to screen these penetration enhancers (4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15)(16)(17)(18)(19). Although these screening methods are high throughput and give reasonable estimate on the ability of the penetration enhancers to increase drug delivery into and across the human nail, the results have to be confirmed in a transungual permeation study.…”

Section: Introductionmentioning

confidence: 99%

Lateral Drug Diffusion in Human Nails

et al. 2014

View full text Add to dashboard Cite

Abstract. The main objective of the current work is to demonstrate the process of passive lateral diffusion in the human nail plate and its effect on the passive transungual permeation of antifungal drug ciclopirox olamine (CPO). A water soluble dye, methyl red sodium salt (MR) was used to visualize the process of lateral diffusion using a novel suspended nail experiment. The decline in concentration of CPO correlates with that of concentration of MR from the proximal to the distal end of the nail in suspended nail study. Three toenails each were trimmed to 5 mm×5 mm (25 mm 2 ), 7 mm×7 mm (49 mm 2 ), and 9 mm×9 mm (81 mm 2 ) to study the extent and effect of lateral diffusion of the CPO on its in vitro transungual permeation. The permeation flux of CPO decreased as the surface area of the toenail increased. There was a positive correlation between the concentrations of CPO and MR in the area of application and in the peripheral area of the toenails of the three surface areas, confirming the findings in the suspended nail experiment. Profound lateral diffusion of CPO was demonstrated and shown to reduce the in vitro passive transungual drug permeation and prolong the lag-time in human toenails. The study data implies that during passive in vitro transungual permeation experiments, the peripheral nail around the area of drug application has to be kept to a minimum, in order to get reliable data which mimics the in vivo situation.

show abstract

“…Diseased nail plate could detach from the nail bed (onycholysis) within few weeks as the disease progresses; which imposes a resistance to drug permeation from formulation to nail bed (10). But, onycholysis creates the cavity between the nail plate and nail bed, where drug formulations could be applied, thus providing a direct contact of drug with the nail bed facilitating the drug delivery on the infected areas over and under the nail bed more easily.…”

Section: Introductionmentioning

confidence: 99%

Microemulsion-Based Gel of Terbinafine for the Treatment of Onychomycosis: Optimization of Formulation Using D-Optimal Design

Barot¹,

Parejiya²,

Patel³

et al. 2011

AAPS PharmSciTech

115

View full text Add to dashboard Cite

Abstract. The aim of the present investigation was to evaluate microemulsion as a vehicle for dermal drug delivery and to develop microemulsion-based gel of terbinafine for the treatment of onychomycosis. Doptimal mixture experimental design was adopted to optimize the amount of oil (X 1 ), Smix (mixture of surfactant and cosurfactant; X 2 ) and water (X 3 ) in the microemulsion. The formulations were assessed for globule size (in nanometers; Y 1 ) and solubility of drug in microemulsion (in milligrams per milliliter; Y 2 ). The microemulsion containing 5.75% oil, 53.75% surfactant-cosurfactant mixture and 40.5% water was selected as the optimized batch. The globule size and solubility of the optimized batch were 18.14 nm and 43.71 mg/ml, respectively. Transmission electron microscopy showed that globules were spherical in shape. Drug containing microemulsion was converted into gel employing 0.75% w/w carbopol 934P. The optimized gel showed better penetration and retention in the human cadaver skin as compared to the commercial cream. The cumulative amount of terbinafine permeated after 12 h was 244.65±18.43 μg cm −2 which was three times more than the selected commercial cream. Terbinafine microemulsion in the gel form showed better activity against Candida albicans and Trichophyton rubrum than the commercial cream. It was concluded that drug-loaded gel could be a promising formulation for effective treatment of onychomycosis.

show abstract

Enhancing the nail permeability of topically applied drugs

Cited by 124 publications

References 75 publications

Effects of Iontophoresis, Hydration, and Permeation Enhancers on Human Nail Plate: Infrared and Impedance Spectroscopy Assessment

Effects of Iontophoresis, Hydration, and Permeation Enhancers on Human Nail Plate: Infrared and Impedance Spectroscopy Assessment

Lateral Drug Diffusion in Human Nails

Microemulsion-Based Gel of Terbinafine for the Treatment of Onychomycosis: Optimization of Formulation Using D-Optimal Design

Contact Info

Product

Resources

About