Concentration-Dependent Enhancement of 1 -Dodecylazacycloheptan-2-one on the Percutaneous Penetration Kinetics of Triamcinolone Acetonide

Chow, Dar‐Chone; Kaka, Idris; Wang, T.I.

doi:10.1002/jps.2600731234

Cited by 69 publications

(14 citation statements)

References 13 publications

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“…They have made great efforts to understand the penetration of drugs through the skin. The permeation data, however, were frequently analyzed on simplistic assumptions such as a single layer skin, a constant diffusivity, a steady-state condition, a simplified boundary condition, a compartment model of skin, etc>l- 3,6,8,9,[12][13][14]18,21,23,37,43,44) A mQre^^^_ proach is needed, at this stage of transdermal drug delivery studies, to elucidate the mechanism of percutaneous absorption.…”

Section: Introductionmentioning

confidence: 99%

Mathematical modeling of transdermal drug delivery.

Tojo

1987

J. Chem. Eng. Japan

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A dynamic mathematical model for transdermal drug delivery is developed on the basis of the bi-layer skin/twocompartment body model. The effects of metabolism reaction in the viable skin, the drug binding and reservoir function in the stratum corneum, and the solubility and diffusivity of the drug in the skin on the permeation ratetime profile are extensively simulated. The effects of the pharmacokinetic parameters on the plasma concentration profile are also analyzed. The present model is useful not only for analyzing the rate of skin permeation but also for predicting the plasma concentration after transdermal drug delivery.

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Section: Introductionmentioning

confidence: 99%

Mathematical modeling of transdermal drug delivery.

Tojo

1987

J. Chem. Eng. Japan

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“…The percutaneous absorption might be described by zero-order kinetics during the time of study (9). The concentration of enhancer in the system under investigation can influence the permeation of transdermal drug delivery (14,15). Thus, the amount of permeation enhancer present in the skin is an important factor in the enhancing effect (16).…”

Section: In Vitro Permeation Studiesmentioning

confidence: 99%

Permeation Kinetics Studies of Physical Mixtures of Artemisinin in Polyvinylpyrrolidone

Shah¹,

Shahzad²,

Ansari³

et al. 2012

Dissolution Technol.

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Artemisinin (ART), the parent compound of a novel family of antimalarial drugs, was used as a model drug that is lipophilic and has low bioavailability (32%) after oral delivery. The primary objective was to study the effect of polyvinylpyrrolidone (PVP) on the permeation enhancement and solubility of physical mixtures (PM) of ART in PVP-K30 in various solvent systems (i.e., distilled water, phosphate buffered saline [PBS], and methanol). PMs of drug-PVP in 1:0.5, 1:1, 1:2, 1:4, and 1:9 ratios were prepared by simple mixing in a mortar and pestle. Fourier transform infrared (FTIR) spectrophotometry and X-ray powder diffraction (XRPD) were applied to characterize the PMs. The solubility of ART was investigated at 37 ± 0.5 °C in three solvents. Permeation of ART-saturated solutions across a silicone membrane in Franz diffusion cells was studied using Fick's law of diffusion. FTIR and XRPD studies have shown some interactions, and there was a phase change of artemisinin from crystalline to amorphous form as the concentration of PVP-K30 in PM ratios increased. Solubility order increased with an increase in PVP-K30 concentration for the water-PBS solvent system, while in methanol, it was erratic. Flux rate and permeability coefficient were enhanced with an increase in PVP-K30 concentration. In less permeable solvents like water and PBS, the enhancement ratio was high, while the enhancement ratio was low in a highly permeable solvent like methanol. In conclusion, with an increase in concentration of PVP, the permeation rate and solubility of ART increased.

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“…Although 4% TCL increased the NAP flux value, the change was not significant when compared with the control formulation. It has been reported that the concentration of enhancer in a formulation markedly influences the promotion of transdermal drug delivery (36,38). Thus, the amount of enhancer present in the skin is an important factor in the enhancing effect.…”

Section: Permeation Of Nap From the Gel Containing Variousmentioning

confidence: 99%

Evaluation of Glycofurol-Based Gel as a New Vehicle for Topical Application of Naproxen

Barakat

2010

AAPS PharmSciTech

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Abstract. In view of the good skin tolerability, glycofurol was used as a vehicle-based gel, and its effect in the topical penetration of Naproxen (NAP) was investigated. The aims of this study were to develop a suitable gel with bioadhesive property, spreadability, and viscosity for topical anti-inflammatory effect. Three gelling and adhesive agents were examined: Carbopol 974P, Gantrez AN 119, and polyvinylpyrollidone K30. Skin permeation rates and lag times of NAP were evaluated using the Franz-type diffusion cell in order to optimize the gel formulation. The permeation rate of NAP-based gel across the excised rat skin was investigated. A significant increase in permeability parameters such as steady-state flux (J ss ), permeability coefficient (K p ), and penetration index (PI) was observed in optimized formulation containing 2% Transcutol as an permeation enhancer. From skin irritation test, it was concluded that the optimized novel glycofurol-based gel formulation was safe to be used for topical drug delivery. The developed glycofurol-based gel appeared promising for dermal and transdermal delivery of naproxen and could be applicable with water-insoluble drugs, which would circumvent most of the problems associated with drug therapy.

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Concentration-Dependent Enhancement of 1 -Dodecylazacycloheptan-2-one on the Percutaneous Penetration Kinetics of Triamcinolone Acetonide

Cited by 69 publications

References 13 publications

Mathematical modeling of transdermal drug delivery.

Mathematical modeling of transdermal drug delivery.

Permeation Kinetics Studies of Physical Mixtures of Artemisinin in Polyvinylpyrrolidone

Evaluation of Glycofurol-Based Gel as a New Vehicle for Topical Application of Naproxen

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