Antifungal activity of topical microemulsion containing a thiophene derivative

Guimarães, Geovani Pereira; Reis, Mysrayn Yargo de Freitas Araújo; Silva, Dayanne Tomaz Casimiro da; Mendonça-Júnior, Francisco Jaime Bezerra; Converti, Attílio; Pessoa, Adalberto; Damasceno, Bolívar Ponciano Goulart de Lima; Silva, José Alexsandro da

doi:10.1590/s1517-83822014000200024

Cited by 22 publications

(11 citation statements)

References 24 publications

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“…Additionally, w/o µEs are particularly interesting for oral protein delivery due to their increased oral bioavailability through the gastrointestinal tract and their protection capacity [ 144 ]. A large number of drugs, such as antibiotics [ 141 , 142 , 143 , 144 , 145 , 146 ], antifungals [ 147 , 148 , 149 ], anti-inflammatory [ 150 , 151 , 152 , 153 , 154 ] and immunosuppressive [ 155 ] molecules have been used in μEs systems.…”

Section: Achievements and Challengesmentioning

confidence: 99%

Microemulsion Microstructure(s): A Tutorial Review

et al. 2020

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Microemulsions are thermodynamically stable, transparent, isotropic single-phase mixtures of two immiscible liquids stabilized by surfactants (and possibly other compounds). The assortment of very different microstructures behind such a univocal macroscopic definition is presented together with the experimental approaches to their determination. This tutorial review includes a necessary overview of the microemulsion phase behavior including the effect of temperature and salinity and of the features of living polymerlike micelles and living networks. Once these key learning points have been acquired, the different theoretical models proposed to rationalize the microemulsion microstructures are reviewed. The focus is on the use of these models as a rationale for the formulation of microemulsions with suitable features. Finally, current achievements and challenges of the use of microemulsions are reviewed.

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Section: Achievements and Challengesmentioning

confidence: 99%

Microemulsion Microstructure(s): A Tutorial Review

et al. 2020

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“…After being equilibrated, the mixtures were assessed visually and determined as a microemulsion or coarse emulsions. The phase diagram constructed using PROSIM software 4, [14][15][16] .…”

Section: Construction Of Pseudo-ternary Phase Diagramsmentioning

confidence: 99%

“…The prepared microemulsion diluted with Water with proper dilution. After ensuring complete dispersion of the formulation the droplet size of resultant ME was determined by photon correlation spectroscopy that analyzes the fluctuation in light scattering due to the Brownian motion of the droplets as a function of time using a DLS spectrophotometer (Model DLS700, Malvern Electronics Company Ltd., Japan).The average diameter (Z-AVE) and polydispersity index (PDI) of ME were determined by using a Malvern (Model DLS700, Malvern Electronics Company Ltd., Japan) at a fixed angle of 90˚ and at 25˚C 14,15,17 .…”

Section: Droplet Size Analysismentioning

confidence: 99%

Preparation, Characterization, and Optimization of Microemulsion for Topical Delivery of Itraconazole

Patel

Suhagia

2018

J. Drug Delivery Ther.

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Microemulsions (ME) have been proved to increase the cutaneous absorption of both lipophilic and hydrophilic medicaments when compared to conventional vehicles (emulsions, pure oils, aqueous solutions). Hence the aim of the present investigation is to prepare, characterize and optimize microemulsion of Itraconazole (ITZ). Itraconazole is an anti fungal agent, most widely used in the ringworm infection. It is classified as class III drug as per BCS classification. It indicates lower permeability through the skin. Therefore the objective of the research is to improve permeability of Itraconazole through the skin. The microemulsion was prepared using eucalyptus oil, tween 20 and methanol as the oil phase, surfactant and co-surfactant respectively. Pseudo-ternary phase diagrams were constructed to find out the optimum ratio of oil: S mix (surfactant: Co-Surfactant): water. A 3 2 full factorial design was applied to the optimization of the prepared microemulsion. The microemulsion was evaluated for globule size, zeta potential, in-vitro diffusion study etc. Results of globule size measurements and zeta potential indicated ME7 had high stability than other formulation of the microemulsion. For the optimization transdermal flux and %Q6 was selected as dependant variables. Results of optimization study also revealed ME 7 as optimized microemulsion for high permeability to the skin. Further ME7 was compared to marketed Itraconazole preparation (ITASPORE) and evaluated using similarity factor F 2. Results of F 2 value was not near to 100 indicated there is no similarity in diffusion profiles of ME7 and ITASPORE. Hence, indirectly it suggests there was increased in permeability of drug by preparing microemulsion.

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“…The clear zone formed surrounding each disc if observed and taken as the minimal inhibitory concentration of the curcumin oil. [10,11] …”

Section: Susceptibility Testmentioning

confidence: 99%

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2017

AJP

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Objective: Fungal infection on the skin is one of the common dermatological diseases especially for the people living in hot and humid climatic conditions. Conventional topical formulations suffer from its own limitations such as lack of site-specific delivery, drug bioavailability, and patient compliance. Curcumin oil was selected as bioactive molecules which target fungal infection which also act as an oil phase for microemulsion preparation. Another strategy was implemented in this research study was to protect the skin from excessive exposure from free radicals by supporting the skin endogenous antioxidant system by adding ascorbic acid (Vitamin C) as an adjunct. Materials and Methods: Micro emulsion gel was formulated with curcumin oil as an active ingredient as well as an oil phase along with ascorbic acid as an adjunct (antioxidant), tween 20, and isopropanol as surfactant and cosurfactant, respectively. Carbopol 940 was chosen as a polymer for the preparation of gel. Pseudoternary phase diagram of microemulsion with various surfactant/ cosurfactant ratios (1:1-4:1) were constructed to study the phase behavior. Minimum inhibitory concentration study and Fourier transform infrared (FTIR) study was conducted to check antifungal activity and possible drug-excipient interactions, respectively. The developed formulations were characterized for physicochemical parameters such as globule size, zeta potential, viscosity, pH, etc. The optimized microemulsion formulations were further loaded into the carbopol gel base and evaluated. Results: Surfactant/cosurfactant weight ratio 3:1 was found to be largest in the percentage area of micro emulsion region. FTIR study did not show any potential drug-excipient interaction and curcumin oil showed considerably greater antifungal activity as compared to clotrimazole. The physical appearances of all the formulations were found to be yellowish, transparent, clear, glossy, and consistent. The pH, viscosity, droplet size of all the formulations was found to be in the acceptable range. From the results of in vitro drug release, approximately 90% of drug released was noted at the end of 10 h and ex vivo release study showed possible permeation mechanism of drug. In vitro antioxidant activity showed that microemulsion gel containing ascorbic acid possess significant free radical scavenging activity in a concentration-dependent manner. In vivo study showed that microemulsion gel containing curcumin oil and ascorbic acid has significant antifungal and antioxidant effect. Conclusions: Curcumin oil was successfully incorporated into topical microemulsion gel prepared with Vitamin C used as an adjunct and showed good spreadability, viscosity, drug release, in vitro antioxidant activity, and in vivo antifungal activity.

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Antifungal activity of topical microemulsion containing a thiophene derivative

Cited by 22 publications

References 24 publications

Microemulsion Microstructure(s): A Tutorial Review

Microemulsion Microstructure(s): A Tutorial Review

Preparation, Characterization, and Optimization of Microemulsion for Topical Delivery of Itraconazole

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