Designing, Optimization and Characterization of Trifluralin Transfersomal Gel to Passively Target Cutaneous Leishmaniasis

Khan, Atif Ullah; Jamshaid, Humzah; Din, Fakhar ud; Zeb, Alam; Khan, Gul Majid

doi:10.1016/j.xphs.2022.01.010

Cited by 27 publications

(11 citation statements)

References 59 publications

(77 reference statements)

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“…TEM (Joel JEM 1230, Tokyo, Japan) was utilized to detect the optimum TNs morphologically. A negatively stained sample with an aqueous solution of phosphotungstic acid (Khan et al., 2022 ) was applied to a copper-covered carbon grid and let for drying until TEM examinations were performed (Basha et al., 2013 ).…”

Section: Methodsmentioning

confidence: 99%

Fenticonazole nitrate loaded trans-novasomes for effective management of tinea corporis: design characterization, in silico study, and exploratory clinical appraisal

Albash

Ragaie

Hassab³

et al. 2022

Drug Delivery

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The current investigation aimed for loading fenticonazole nitrate (FTN), an antifungal agent with low aqueous solubility, into trans-novasomes (TNs) for management of tinea corporis topically. TNs contain Brij ® as an edge activator besides the components of novasomes (cholesterol, Span 60, and oleic acid) owing to augment the topical delivery of FTN. TNs were fabricated applying ethanol injection method based on D-optimal experiment. TNs were evaluated with regard to entrapment efficiency percent (EE%), particle size (PS), polydispersity index (PDI), and zeta potential (ZP). Further explorations were conducted on the optimum formulation (F7). F7 showed spherical appearance with EE%, PS, PDI, and ZP of 100.00 ± 1.10%, 358.60 ± 10.76 nm, 0.51 ± 0.004, and −30.00 ± 0.80 mV, respectively. The in silico study revealed the ability of the FTN–cholesterol complex to maintain favorable interactions throughout the molecular dynamics simulation (MDS) study. Moreover, Trichophyton mentagrophytes growth was inhibited effectively by F7 than by FTN suspension applying 2,3-bis(2-methyloxy-4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilide (XTT) reduction assay. Furthermore, a clinical appraisal on patients with tinea corporis fungal lesions confirmed the superiority of F7 compared to Miconaz ® cream in the magnitude of clinical cure of tinea corporis. Thereby, TNs could be considered as promising vesicles for enhancing the antifungal potential of FTN for the topical management of tinea corporis.

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Section: Methodsmentioning

confidence: 99%

Fenticonazole nitrate loaded trans-novasomes for effective management of tinea corporis: design characterization, in silico study, and exploratory clinical appraisal

Albash

Ragaie

Hassab³

et al. 2022

Drug Delivery

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“…In the present study, we constructed HA-modified transfersomes (IND-HTs; Figure 1 ) as an efficient nanovesicular carrier of IND for improved percutaneous permeation. To increase the skin retention property of IND-HTs, carbopol 940 hydrogel was employed as a reservoir to entrap the IND-HTs (Batool et al., 2021 ; Khan et al., 2022 ). The IND-HTs-embedded hydrogel (IND-HTs/Gel) could be painted as a patch on the skin with prolonged retention time in comparison with the IND-HTs solution.…”

Section: Introductionmentioning

confidence: 99%

Hyaluronan-modified transfersomes based hydrogel for enhanced transdermal delivery of indomethacin

et al. 2022

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Hyaluronic acid (HA), as a hygroscopic and biocompatible molecule, has displayed unique permeation enhancement in transdermal delivery systems. Hence, indomethacin (IND) was encapsulated in HA-modified transfersomes (IND-HTs) to enhance transdermal IND delivery to reduce adverse effects in this study. The physiochemical properties of IND-HTs were characterized. Results showed that the prepared IND-HTs were spherical and revealed good entrapment efficiency (87.88 ± 2.03%), with a nanometric particle size (221.8 ± 93.34 nm). Then, IND-HTs were further incorporated into a carbopol 940 hydrogel (IND-HTs/Gel) to prolong retention capacity on the skin. The in vitro release and skin permeation experiments of IND-HTs/Gel were carried out with the Franz diffusion cells. It was found that IND-HTs/Gel exhibited sustained drug release, as well as superior drug permeation and flux across the skin. Confocal laser scanning microscopy showed improved penetration of HTs/Gel with a wider distribution and higher fluorescence intensity. The hematoxylin–eosin stained showed that HA improved the transdermal effect by changing the microstructure of skin layers and decreasing skin barrier function. In addition, IND-HTs/Gel showed significant analgesic activity in hot plate test and no potentially hazardous skin irritation. This study indicated that the developed IND-HTs/Gel could be a promising alternative to conventional oral delivery of IND by topical administration.

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“…The vesicular carrier system can entrap drug molecules by acting as a drug carrier and increase the permeation of drugs into the stratum corneum. As far as topical vesicular systems are concerned, unfortunately, the first-generation nanovesicular systems including liposomes and niosomes were accompanied with drawbacks, particularly weak stratum corneum (SC) penetration because of their inflexible nature [ 7 ]. Among all other vesicular carriers, ultradeformable vesicular drug carrier system “Transfersomes”(TFS) have been considered as surrogate vehicles for transdermal drug delivery of a wide range of hydrophilic as well as hydrophobic drug molecules.…”

Section: Introductionmentioning

confidence: 99%

Development and In Vitro/Ex Vivo Evaluation of Lecithin-Based Deformable Transfersomes and Transfersome-Based Gels for Combined Dermal Delivery of Meloxicam and Dexamethasone

Khan

Yaqoob

Madni

et al. 2022

BioMed Research International

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Transfersomes (TFS) are the promising carriers for transdermal delivery of various low and high molecular weight drugs, owing to their self-regulating and self-optimizing nature. Herein, we report synthesis and characterization of TFS loaded with meloxicam (MLX), an NSAID, and dexamethasone (DEX), a steroid, for simultaneous transdermal delivery. The different formulations of TFS containing varying amounts of lecithin, Span 80, and Tween 80 (TFS-1 to TFS-6) were successfully prepared by thin-film hydration method. The size of ranged between 248 and 273 nm, zeta potential values covering from –62.6 to –69.5 mV, polydispersity index (PDI) values in between 0.329 and 0.526, and entrapment efficiency of MLX and DEX ranged between 63-96% and 48-81%, respectively. Release experiments at pH 7.4 demonstrated higher cumulative drug release attained with Tween 80 compared to Span 80-based TFS. The scanning electron microscopy (SEM) of selected formulations -1 and TFS-3 revealed spherical shape of vesicles. Furthermore, three optimized transfersomal formulations (based on entrapment efficiency, TFS-1, TFS-3, and TFS-5) were incorporated into carbopol-940 gels coded as TF-G1, TF-G3, and TF-G5. These transfersomal gels were subjected to pH, spreadability, viscosity, homogeneity, skin irritation, in vitro drug release, and ex vivo skin permeation studies, and the results were compared with plain (nontransfersomal) gel having MLX and DEX. TFS released 71.72% to 81.87% MLX in 12 h; whereas, DEX release was quantified as 74.72% to 83.72% in same time. Nevertheless, TF-based gels showed slower drug release; 51.54% to 59.60% for MLX and 48.98% to 61.23% for DEX. The TF-G systems showed 85.87% permeation of MLX (TF-G1), 68.15% (TF-G3), and 68.94% (TF-G5); whereas, 78.59%, 70.54%, and 75.97% of DEX was permeated by TF-G1, TF-G3, and TF-G5, respectively. Kinetic modeling of release and permeation data indicated to follow Korsmeyer-Peppas model showing diffusion diffusion-based drug moment. Conversely, plain gel influx was found mere 26.18% and 22.94% for MLX and DEX, respectively. These results suggest that TF-G loaded with MLX and DEX can be proposed as an alternate drug carriers for improved transdermal flux that will certainly increase therapeutic outcomes.

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Designing, Optimization and Characterization of Trifluralin Transfersomal Gel to Passively Target Cutaneous Leishmaniasis

Cited by 27 publications

References 59 publications

Fenticonazole nitrate loaded trans-novasomes for effective management of tinea corporis: design characterization, in silico study, and exploratory clinical appraisal

Fenticonazole nitrate loaded trans-novasomes for effective management of tinea corporis: design characterization, in silico study, and exploratory clinical appraisal

Hyaluronan-modified transfersomes based hydrogel for enhanced transdermal delivery of indomethacin

Development and In Vitro/Ex Vivo Evaluation of Lecithin-Based Deformable Transfersomes and Transfersome-Based Gels for Combined Dermal Delivery of Meloxicam and Dexamethasone

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