The Effect of Various Vehicles on the Naproxen Permeability through Rat Skin: A Mechanistic Study by DSC and FT-IR Techniques

Salimi, Anayatollah; Hedayatipour, Najme; Moghimipour, Eskandar

doi:10.15171/apb.2016.03

Cited by 29 publications

(15 citation statements)

References 20 publications

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“…In fact, the similarity among aliphatic molecules is sometimes associated with a potentiation of the enhancer activities [ 71 ]. For example, the effect of polysorbate 80 over the permeation of lipophilic drugs (logP above 4.15) through rat mucosal membranes [ 72 ] is related to an increase in diffusion coefficient, and thus, the drug transport, similarly with econazole [ 16 ]. A significant increase in skin deposition means improved cutaneous drug availability, and thus, the feasibility of an enlarged interval of administration.…”

Section: Discussionmentioning

confidence: 99%

Biopharmaceutical Development of a Bifonazole Multiple Emulsion for Enhanced Epidermal Delivery

et al. 2019

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Efficient topical delivery of imidazolic antifungals faces the challenge of overcoming its limited water solubility and its required long-lasting duration of treatments. In this paper, a hydrophilic multiple emulsion (ME) of Bifonazole (BFZ) is shown to maximize its skin retention, minimize its skin permeation, and maintain an acceptable level of being harmless in vivo. The formulations were pharmaceutically characterized and application properties were assessed based on viscosity measurements. Non-Newtonian pseudoplastic shear thinning with apparent thixotropy was observed, facilitating the formulation retention over the skin. The in vitro release profile with vertical diffusion cells showed a predominant square-root release kinetic suggesting an infinite dose depletion from the formulation. Ex vivo human skin permeation and penetration was additionally evaluated. Respective skin permeation was lower than values obtained with a commercial O/W formulation. The combination of amphoteric and non-ionic surfactants increased the bifonazole epidermal accumulation by a factor of twenty. This fact makes the possibility of increasing its current 24 h administration frequency more likely. Eventual alterations of skin integrity caused by the formulations were examined with epidermal histological analysis and in vivo preclinical measurements of skin elasticity and water retrograde permeation. Histological analysis demonstrated that the multiple emulsions were harmless. Additionally, modifications of in vivo skin integrity descriptors were considered as negligible.

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Section: Discussionmentioning

confidence: 99%

Biopharmaceutical Development of a Bifonazole Multiple Emulsion for Enhanced Epidermal Delivery

et al. 2019

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“…[29] Oleic acid, propylene glycol, and water in our ME formulations are considered as permeation enhancers that acting by several mechanisms including disruption of the organized intercellular lipid structure of the stratum corneum, fluidization of the stratum corneum lipids. [30] Therefore, it is reasonable to believe that the developed MEs in this study should be effective; however, additional in vivo efficacy studies are recommended to show the potential of these ME systems as a dermal delivery system of HQ. …”

Section: Characterization Of Hq Mesmentioning

confidence: 95%

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Salimi¹

2017

AJP

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Introduction: Hydroquinone (HQ), a famous anti-hyperpigmentation agent, suffers from several weaknesses such as instability due to rapid oxidation and insufficient skin penetration because of the hydrophilic structure. The aim of this research was to formulate, characterize and evaluation of in vitro skin permeability of HQ-loaded microemulsion (ME). Methods: HQ MEs were prepared by pseudoternary phase diagram method, the appropriate ratios of oil, s/c mixture, and water were chosen, and full factorial design was used with three variables at two levels for preparing eight formulations. The prepared MEs were evaluated regarding their droplet size, viscosity, pH, differential scanning calorimetry, stability, in vitro drug release, and in vitro skin permeability. Results and Discussion:The results showed that the mean droplet size range of ME samples was in the range of 7.05-79.56 nm and pH was 5.3-5.7, respectively. Viscosity range of MEs was 109-195 cps. Drug release profile showed that 90.51% of the drug released (ME-HQ-8) in the 24 h of the experiment. The kinetics of drug release from all selected MEs were approximately described by Higuchi model and showed prolonged release when compared to HQ solution. All ME formulations with different compositions and properties significantly increased flux and permeability coefficient from rat skin. J ss and Papp parameters in ME-HQ-2 formulation were 0.404 mg/cm 2 h, 0.02 cm/h, and 4 times higher than those of control, respectively. The selective MEs have 99.9% HQ amount after 6 months storage. They have visually cleared and no any color changes, thus HQ MEs can could been protect drug for a long time without antioxidant. Conclusion: The present research established that the amount of components of water, oil, and S + C in ME formulation plays an important role in the physicochemical properties and permeability parameters. This study showed that any change in content and composition of MEs could be changed physicochemical properties and permeability parameters during drug permeation from ME samples. The studied MEs increased permeation rate and permeability coefficient through rat skin. Our results were showed that ME formulation could not be increase diffusivity of HQ in stratum corneum.

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“…An increase in wave number and width of -CH2 stretching peaks is due fluidization of the SC lipids [9]. If the shift is to higher wavenumber (blueshift), it indicates SC membrane (lipid bilayer) fluidization that in change contribute to the disruption of the barrier properties that probably causes the substance permeation enhancement through the SC [10]. On the other hand, lipid groups are oriented again, a phenomenon that causes a shift to lower wave number (e.g., redshift) and strengthening of subcutaneous barrier properties which finally slows down the entrance of permeant through the skin [11].…”

Section: Saadatzadeh Et Almentioning

confidence: 99%

“…The samples were heat treated (20-200°C) repeatedly at a rate of 5°C/min. All experiments were conducted three times and every time the DSC analyzer was calibrated with indium standard [21].…”

Section: Dscmentioning

confidence: 99%

Influence of Permeation Enhancers on the in Vitro Skin Permeation of Ketorolac Tromethamine Through Excised Rat Skin: A Mechanistic Study

Saadatzadeh

Salimi

Zarooni

2018

Asian J Pharm Clin Res

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Objective: Ketorolac tromethamine (KT) is considered as a member of Non-steroidal anti-inflammatory drugs that used as an analgesic and antipyretic agent. The main aim of this research was to investigate the effect of some herbal and chemical permeation enhancers on the in vitro skin permeability of KT.Method: Ketorolac permeability experiments through rat skin pre-treated with some of permeation enhancers, namely urea, eucalyptus oil, olive oil, and menthol, were performed in fabricated Franz diffusion cells and compared with hydrated rat skin as control. The permeability parameters evaluated include steady-state flux (Jss), permeability coefficient (Kp), and diffusion coefficient (D). The penetration enhancers permeability enhancement mechanisms were investigated by comparing changes in peak position and their intensities of asymmetric (Asy) and symmetric (Sym) C-H stretching, C=O stretching, C=O stretching (Amide I), and C-N stretching of keratin (Amide II) absorbance using fourier transform infrared spectroscopy (FT-IR), as well as by comparing mean transition temperature (Tm) and their enthalpies (ΔH) using differential scanning calorimetery (DSC). KT permeability parameters through rat skin were evaluated with and without chemical enhancers such as eucalyptus oil, olive oil, menthol, and urea.Result: The skin showed barrier for ketorolac permeability through the whole skin and that diffusion into the skin was the rate-limiting step for drug flux. Urea, eucalyptus oil, olive oil, and menthol were the most effective enhancers as they increased flux 0.02, 0.017, 0.016, and 0.012 times and diffusion coefficient 0.079, 0.194, 0.129, and 1.35 folds in comparison with hydrated skin, respectively.Conclusion: FT-IR and DSC results showed lipid fluidization, extraction, disruption of lipid structure, and irreversible denaturation of proteins in the stratum corneum layer of the skin by permeation enhancers.

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The Effect of Various Vehicles on the Naproxen Permeability through Rat Skin: A Mechanistic Study by DSC and FT-IR Techniques

Cited by 29 publications

References 20 publications

Biopharmaceutical Development of a Bifonazole Multiple Emulsion for Enhanced Epidermal Delivery

Biopharmaceutical Development of a Bifonazole Multiple Emulsion for Enhanced Epidermal Delivery

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Influence of Permeation Enhancers on the in Vitro Skin Permeation of Ketorolac Tromethamine Through Excised Rat Skin: A Mechanistic Study

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