Enhancement of skin permeation of miconazole by phospholipid and dodecyl 2-(N,N-dimethyl amino)propionate (DDAIP)

Fujii, Makiko; Büyüktimkin, Servet; Büyüktimkin, Nadir; Rytting, J. Howard

doi:10.1016/s0378-5173(01)00951-6

Cited by 16 publications

(8 citation statements)

References 10 publications

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“…By fl uorescence spectroscopic studies dodecyl-N,Ndimethylaminoacetate was shown to alter molecular movement on the surface of the bilayers, resulting in a decrease in anisotropy of 19% [53] . By use of DDAIP as an enhancer in penetration studies of miconazole through shed snake skin, the permeation increased 11-fold compared with that of the suspension without DDAIP pretreatment [54] . The concentration of the azole in the skin increased 8-fold, indicating that the enhancement effect is connected with high partition of miconazole into the skin.…”

Section: Urea and Derivativesmentioning

confidence: 99%

Overcoming the Stratum Corneum: The Modulation of Skin Penetration

Trommer

Neubert

2006

Skin Pharmacol Physiol

460

279

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It is preferred that topically administered drugs act either dermally or transdermally. For that reason they have to penetrate into the deeper skin layers or permeate the skin. The outermost layer of the human skin, the stratum corneum, is responsible for its barrier function. Most topically administered drugs do not have the ability to penetrate the stratum corneum. In these cases modulations of the skin penetration profiles of these drugs and skin barrier manipulations are necessary. A skin penetration enhancement can be achieved either chemically, physically or by use of appropriate formulations. Numerous chemical compounds have been evaluated for penetration-enhancing activity, and different modes of action have been identified for skin penetration enhancement. In addition to chemical methods, skin penetration of drugs can be improved by physical options such as iontophoresis and phonophoresis, as well as by combinations of both chemical and physical methods or by combinations of several physical methods. There are cases where skin penetration of the drug used in the formulation is not the aim of the topical administration. Penetration reducers can be used to prevent chemicals entering the systemic circulation. This article concentrates on the progress made mainly over the last decade by use of chemical penetration enhancers. The different action modes of these substances are explained, including the basic principles of the physical skin penetration enhancement techniques and examples for their application.

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Section: Urea and Derivativesmentioning

confidence: 99%

Overcoming the Stratum Corneum: The Modulation of Skin Penetration

Trommer

Neubert

2006

Skin Pharmacol Physiol

460

279

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“…MN release was monitored using a dialysis method for separating released drug from liposomes (22,28). MN liposomes (dispersion or in gel form, equivalent to 6 mg MN) were placed in dialysis bags, suspended in 100 ml of the release medium (acetate buffer, pH 5, containing 25% methanol) in capped flasks, and shaken (100 strokes per minute) at 32±0.3°C.…”

Section: Drug Release Studiesmentioning

confidence: 99%

Propylene Glycol Liposomes as a Topical Delivery System for Miconazole Nitrate: Comparison with Conventional Liposomes

et al. 2012

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Abstract. Propylene glycol (PG)-phospholipid vesicles have been advocated as flexible lipid vesicles for enhanced skin delivery of drugs. To further characterize the performance of these vesicles and to address some relevant pharmaceutical issues, miconazole nitrate(MN)-loaded PG nanoliposomes were prepared and characterized for vesicle size, entrapment efficiency, in vitro release, and vesicle stability. An issue of pharmaceutical importance is the time-dependent, dilution-driven diffusion of propylene glycol out of the vesicles. This was addressed by assessing propylene glycol using gas chromatography in the separated vesicles and monitoring its buildup in the medium after repeated dispersion of separated vesicles in fresh medium. Further, the antifungal activity of liposomal formulations under study was assessed using Candida albicans, and their in vitro skin permeation and retention were studied using human skin. At all instances, blank and drug-loaded conventional liposomes were included for comparison. The results provided evidence of controlled MN delivery, constant percent PG uptake in the vesicles (≈45.5%) in the PG concentration range 2.5 to 10%, improved vesicle stability, and enhanced skin deposition of MN with minimum skin permeation. These are key issues for different formulation and performance aspects of propylene glycol-phospholipid vesicles.

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“…Significant differences were found in AUC 0-24 h as well as in C max and t 1/2 between the test and reference formulations as shown in the Table 6. The hypothesized mechanism is the interaction and fluidization of membrane phospholipids thereby assisting in drug transport by enhancing the lipid solubility [12] as in the case of 1-deamino-8-D-arginine-vasopressin where the transport of lysophosphatidyl choline treatment increased the apparent permeability coefficient, P app even under circumstances where the cell monolayer integrity was only slightly altered and also evidenced by 8 fold increase in concentration of miconazole indicating that the enhancement effect involved high partition of miconazole into the skin by the use of phospholipid and dodecyl 2-(N,N-dimethyl amino) propionate [13,14]. Therefore phosphatidylcholine embedded micellar systems are responsible for enhanced permeability.…”

Section: Test For Comparison Of Means Of Reference and Optimized Tagumentioning

confidence: 99%

“…Therefore phosphatidylcholine embedded micellar systems are responsible for enhanced permeability. The difference in three types of phospholipids may be owed to the difference in percentage of phosphatidyl choline (PC) as evidenced by the solubility of miconazole that increased in proportion to the hydrogenated phosphatidylcholine concentration [14]. Run with Phospholipon 90H containing 90% PC and 4% of lyso phosphatidyl choline, the byproduct of PC resulted in better in vitro dissolution and higher drug release.…”

Section: Test For Comparison Of Means Of Reference and Optimized Tagumentioning

confidence: 99%

Enhancement of Bioavailability of Fenofibrate with Alpha Tocopherol and Phospholipids as Solubilizers

Indira¹

2012

JBB

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The purpose of this study was to investigate the effect of different solubilizers namely alpha tocopherol, soy phosphatidylcholine 70, Phospholipon 80H, and Phospholipon 90H on the bioavailability of sustained release fenofibrate pellets using fluid bed coating by applying Taguchi design to optimize the type and concentration of solubilizer at four levels namely 0.5%, 1%, 1.5%, and 2%. The pellets were prepared by loading the fenofibrate blended with other excipients onto the core sugar pellets with the aid of the binder solution. Taguchi experimental runs with alpha tocopherol 1% and Phospholipon 90H 2% (test) showed significant differences in in vitro dissolution behavior of drug compared to the pure drug. The pharmacokinetics of pure drug and test was evaluated in healthy male Wistar rats and found that t 1/2 was reduced significantly (4.36 and 4.02 hours) while AUC 0-t (32.14 ± 6.38 μg h/ml, 36.94 ± 6.2 μg h/ml), C max (8.7 ± 2.31 μg/ml, 9.8 ± 2.2 μg/ml) were improved markedly compared to the pure drug with t 1/2 (7.339314 ± 3.1 hours), AUC 0-t (11.89 ± 8.13 μg h/ml), and C max (5.137 ± 3.37 μg/ml). The extent of the mean plasma exposure of fenofibrate was 2.7 and 3.1 fold higher in animals treated with test. The ANOVA results revealed that type and concentration of solubilizer are crucial for enhancement of in vitro dissolution profile. Hence use of solubilizers may be the promising way to improve the oral bioavailability of fenofibrate. Enhancement of Bioavailability of MethodsDrug loading: Drug was loaded onto sugar spheres using fluidized bed processor . The sugar spheres were loaded into the fluidized bed processor and warmed for about 10 -15 minutes. Binder solution was prepared by dissolving Povidone K30 and sugar in purified water under constant stirring. Unmicronized fenofibrate which was pre blended and pulverized (0.5 mm screen pulverizer) with other excipients was incorporated intermittently into the solution under constant stirring. The obtained solution was loaded onto the circulating sugar spheres (800 μm). The wet spheres were dried simultaneously during the process of circulation in wurster chamber. The process was continued till the complete solution was consumed. The various processing variables namely inlet air temperature (40-45°C), outlet air temperature (30-33°C), product temperature (36-40°C), chamber humidity (58-60%), air flow (85 m 3 /hr), compressed air pressure (1.5-3.0 kg/cm 2 )The peristaltic pump rpm (10-35) and spray rate (2 ml/min) were optimized in the preliminary trials.Design of experiment to optimize drug loaded fenofibrate pellets: Taguchi L16 design of experiment was used to study the effect of two variables namely, type of solubilizer and concentration of solubilizer at four different levels as given in Table 1 and Table 2. All the experimental runs were analyzed using Minitab statistical software package (version 15). Characterization methodsInfrared Spectroscopy analysis of drug and excipients: FT-IR spectra were obtained using FT-IR spectrometer (Model Nic...

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Enhancement of skin permeation of miconazole by phospholipid and dodecyl 2-(N,N-dimethyl amino)propionate (DDAIP)

Cited by 16 publications

References 10 publications

Overcoming the Stratum Corneum: The Modulation of Skin Penetration

Overcoming the Stratum Corneum: The Modulation of Skin Penetration

Propylene Glycol Liposomes as a Topical Delivery System for Miconazole Nitrate: Comparison with Conventional Liposomes

Enhancement of Bioavailability of Fenofibrate with Alpha Tocopherol and Phospholipids as Solubilizers

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