Transdermal delivery of naloxone: effect of water, propylene glycol, ethanol and their binary combinations on permeation through rat skin

Panchagnula, Ramesh; Salve, Pramod S.; Thomas, Narisetty Sunil; Jain, Amit; Ramarao, P.

doi:10.1016/s0378-5173(01)00634-2

Cited by 122 publications

(75 citation statements)

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“…Ethanol enhances permeation by various mechanisms such as push and pull effect, fluidization of stratum corneum lipids and vesicular lipid bilayers providing malleability to vesicles to penetrate skin pores smaller than their diameter (Panchagnula et al, 2001;Kowatsu and Okada, 1996).…”

Section: Resultsmentioning

confidence: 99%

Development of ethosomes with taguchi robust design-based studies for transdermal delivery of alfuzosin hydrochloride

Prasanthi

Lakshmi

2012

Int Curr Pharm J

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In the present investigation efficiency of ethosomes as novel lipid carriers for transdermal delivery of Alfuzosin Hydrochloride (AH) has been evaluated. Taguchi robust design method was used for optimization of ethosomal formulations. Phospholipid type, concentration of phospholipid and concentration of ethanol was selected as independent variables and their effect on the dependent variables (entrapment efficiency and flux) was studied. Ethosomal formulation (EA8) with soya phosphatidylcholine (3%) and ethanol 20% were optimized. Vesicles were spherical, unilamellar with smooth surface. The optimized formulation exhibited vesicle size (6.85 ± 1.35µm), zeta potential (-8.14 ± 0.62mv), entrapment efficiency (91.86 ± 3.25%), flux (27.42 ± 0.04µg/cm2/hr), lag time (0.26±0.20hr) and skin deposition (298.01 ± 15.4µg/g). Transdermal flux was enhanced by 6.92 times over drug solution. Vesicle skin interaction studies showed fatty change in the dermis. The formulations were stable at 4°C for 120 days. Results suggested ethosomes as efficient carriers for AH transdermal delivery.DOI: http://dx.doi.org/10.3329/icpj.v1i11.12063 International Current Pharmaceutical Journal 2012, 1(11): 370-375

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Section: Resultsmentioning

confidence: 99%

Development of ethosomes with taguchi robust design-based studies for transdermal delivery of alfuzosin hydrochloride

Prasanthi

Lakshmi

2012

Int Curr Pharm J

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“…With the addition of water, however, ethanol may have a disruptive effect on stratum corneum lipid structure causing increased permeability. Other suggested mechanisms include effects on the putative pore pathway, increased solubility in stratum corneum lipids and ethanol copermeation (Berner et al 1989;Kurihara-Bergstrom et al 1990;Megrab et al 1995;Kim et al 1996;Levang et al 1999;Panchagnula et al 2001).…”

Section: Discussionmentioning

confidence: 99%

“…A 66% aqueous solution of propylene glycol, however, enhances permeability (Panchagnula et al 2001). Proposed mechanisms of absorption enhancement include a cosolvency effect (Barry 1983) and a carrier mechanism (Hoelgaard & Mollgaard 1985).…”

Section: Discussionmentioning

confidence: 99%

“…Water, ethanol and propylene glycol are common solvents and their effects on dermal absorption across a range of compounds have been described (Berner et al 1989;Kurihara-Bergstrom et al 1990;Megrab et al 1995;Kim et al 1996;Levang et al 1999;Panchagnula et al 2001). Comparing the dermal absorption of a range of compounds from these solvents with and without the addition of SLS offers an opportunity to study SLS effects on absorption when in combination with solvents relevant to a significant number of real-world dermal exposure hazards.…”

Section: Introductionmentioning

confidence: 99%

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Effect of vehicles and sodium lauryl sulphate on xenobiotic permeability and stratum corneum partitioning in porcine skin

Merwe

Riviere

2005

Toxicology

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Dermal contact with potentially toxic agricultural and industrial chemicals is a common hazard encountered in occupational, accidental spill and environmental contamination scenarios. Different solvents and chemical mixtures may influence dermal absorption. The effects of sodium lauryl sulphate (SLS) on the stratum corneum partitioning and permeability in porcine skin of 10 agricultural and industrial chemicals in water, ethanol and propylene glycol were investigated. The chemicals were phenol, p-nitrophenol, pentachlorophenol, methyl parathion, ethyl parathion, chlorpyrifos, fenthion, simazine, atrazine and propazine. SLS decreased partitioning into stratum corneum from water for lipophilic compounds, decreased partitioning from propylene glycol and did not alter partitioning from ethanol. SLS effects on permeability were less consistent, but generally decreased permeability from water, increased permeability from ethanol and had an inconsistent effect on permeability from propylene glycol. It was concluded that, for the compounds tested, partitioning into the stratum corneum was determined by the relative solubility of the solute in the donor solvent and the stratum corneum lipids.Permeability, however, reflected the result of successive, complex processes and was not predictable from stratum corneum partitioning alone. Addition of SLS to solvents altered partitioning and absorption characteristics across a range of compounds, which indicates that partition coefficients or skin permeability from neat chemical exposure should be used with caution in risk assessment procedures for chemical mixtures.

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“…However, the percutaneous absorption of drugs with a high molecular weight and hydrophilic properties is not sufficient due to the barrier function of the skin. To enhance the absorption, several investigations using vehicles, 1,2) chemical enhancers, [3][4][5][6] iontophoresis, [7][8][9] electroporation 10,11) and phonophoresis 12,13) have been performed. We have focused on iontophoresis in terms of the enhancement of the amount of drug delivered by current with low skin irritation.…”

mentioning

confidence: 99%

Evaluation of Skin Barrier Function Using Direct Current III: Effects of Electrode Distance, Boundary Length and Shape

Kanebako¹,

Inagi²,

Takayama

2003

Biological & Pharmaceutical Bulletin

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Transdermal drug delivery can avoid first-pass metabolism, which is the greatest disadvantage of oral administration. However, the percutaneous absorption of drugs with a high molecular weight and hydrophilic properties is not sufficient due to the barrier function of the skin. To enhance the absorption, several investigations using vehicles, 1,2) chemical enhancers, [3][4][5][6] iontophoresis, 7-9) electroporation 10,11) and phonophoresis 12,13) have been performed. We have focused on iontophoresis in terms of the enhancement of the amount of drug delivered by current with low skin irritation. In a previous study, we predicted that the amount of drug that migrated in the skin was determined by a synergistic effect of both current application and enhanced passive diffusion due to the reduction in barrier function.14)The prediction was proved by the measurement of the distribution using indomethacin as a model drug. 15) In these studies, the accumulation of drug in the stratum corneum contributed to enhanced passive diffusion due to the reduction in barrier function. On the other hand, the accumulation from dermis to upper dermis was attributed to a passage of current. Further, a novel method for analyzing the reduction in barrier function under constant voltage was proposed.16) With this method, the barrier function was defined as resistance, which represented the sum of exponential functions of surface and skin resistance. In addition, the evaluation was carried out using the initial value and rate constant of the surface resistance. Using this method, effects of conductivity in the adhesive pad, voltage, the distance between electrodes and electrode area on the barrier function were evaluated. Furthermore, the influence of a pulsed direct current, which could prevent skin polarization and irritation was investigated. 17)The reduction in barrier function brought about by the application of sine and rectangular waveforms with a 75% duty cycle was almost the same as that caused by the application of direct current. Considering the skin polarization, the pulsed currents were more suitable.In the evaluation of changing electrode area, 16) although the initial value of surface resistance increased with increasing electrode area, no change of rate constant was observed. The rate constant showed the damping of the surface resistance, i.e., the barrier function. These phenomena contributed to the higher current density in the portion adjacent to the other electrode. Therefore, we investigated the electrode disposition and shape considering the reduction in barrier function as well as effective delivery of drugs into the skin. Similar results were reported by Haga et al. 18) They prepared electrodes with different boundary lengths using a photoeching technique, and then observed the skin distribution of 6-carboxyfluorescein (6-CF) under constant voltage. In that paper, the topical distribution of 6-CF in the skin was recognized in both boundary portions, i.e., the portion adjacent to the other electrode. They suggested ...

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Transdermal delivery of naloxone: effect of water, propylene glycol, ethanol and their binary combinations on permeation through rat skin

Cited by 122 publications

References 10 publications

Development of ethosomes with taguchi robust design-based studies for transdermal delivery of alfuzosin hydrochloride

Development of ethosomes with taguchi robust design-based studies for transdermal delivery of alfuzosin hydrochloride

Effect of vehicles and sodium lauryl sulphate on xenobiotic permeability and stratum corneum partitioning in porcine skin

Evaluation of Skin Barrier Function Using Direct Current III: Effects of Electrode Distance, Boundary Length and Shape

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