Transdermal Delivery of Telmisartan: Formulation, in vitro, ex vivo, Iontophoretic Permeation Enhancement and Comparative Pharmacokinetic Study in Rats

Teaima, Mahmoud H.; Abdelmonem, Rehab; Adel, Yomna A; El-Nabarawi, Mohamed A.; El-Nawawy, Tayseer M

doi:10.2147/dddt.s327860

Cited by 12 publications

(7 citation statements)

References 36 publications

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“…Vesicle size is essential for transdermal delivery of drug-loaded nanocarriers and so submicron sizes permit an effective penetration into the stratum corneum [30]. As revealed in (table 2), the values for PDI and ZP ranged from 0.133±0.09 to 0.466±0.05 for the former and-19.00±1.50 mV to-27.5±1.75 mV for the latter.…”

Section: Influence Of Formulation Variables On Vesicle Sizementioning

confidence: 95%

“…Concerning the impact of X2 on %SE where other factors are constant, altering SAA concentration from 0.2% to 0.8% cause a significant decrease in %SE of DKT loaded TE from 86.08±1.05% (0.2% SAA) to 59.70±1.21% (0.8% SAA) and this is confirmed by the negative sign of the coefficient of estimates (-12.49). It was reported that increasing concentration of SAA or edge activator causes a reduction in vesicular size and hence causes a decrease in %SE [30]. As well, the decrease in %SE with a high level of SAA concentration (Labrafil or Cremophore) may be indicative of the presence of micelle structure in conjunction with vesicles in the formulation; micelles tend to have a lower entrapment capability over vesicles [28].…”

Section: Influence Of Formulation Variables On Solubilization Efficiencymentioning

confidence: 99%

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Transethosomes as Breakthrough Tool for Controlled Transdermal Delivery of Dexketoprofen Trometamol: Design, Fabrication, Statistical Optimization, in Vitro, and Ex Vivo Characterization

Soliman

RASHWAN²,

Teaima³

et al. 2022

Int J App Pharm

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Objective: Transethosomes (TEs) have introduced an emerging avenue of interest in vesicular research for transdermal delivery of drugs and can be a proper delivery system for painkillers like NSAIDS. This study aimed to formulate and characterize the potential of TE to enhance the transdermal transport of Dexketoprofen trometamol (DKT) to achieve controlled pain management compared to DKT solution. Methods: Factorial design (23) was adopted to appraise the influence of independent variables, namely, Lipoid S100 and surfactant concentrations and surfactant type (X3) on the % solubilization efficiency (% SE), vesicle size (VS), and % release efficiency (% RE). Thin film hydration was the preferred approach for preparing TEs where vesicle size, zeta potential, polydispersity index, %SE and %RE were investigated. The optimized formula was nominated and subjected to several studies. For the permeation study, optimum TE was incorporated into carbapol gel base for comparison with DKT solution. Also, an accelerated stability study was assessed for optimized formula. Results: All the prepared DKT-loaded TEs revealed acceptable VS, PDI, and ZP. The highest %SE (86.08±1.05 %) and lowest %RE (44.62±1.36 %) were observed in case of F1. The optimized formula (F1) displayed VS of 133.2±1.62 nm, PDI of 0.342±0.03 and ZP of-21.6±2.45 mV. F1 revealed enhanced skin permeation of a 2.6-fold increase compared with DKT solution. Moreover, F1 was stable upon storage and a non-significant change (P>0.05) was observed. Conclusion: DKT was successfully incorporated into vesicle carrier and can signify an alternative option for providing this therapy, bypassing the poor bioavailability and considerable adverse consequences of using the oral route besides improved patient compliance.

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Section: Influence Of Formulation Variables On Vesicle Sizementioning

confidence: 95%

Section: Influence Of Formulation Variables On Solubilization Efficiencymentioning

confidence: 99%

Transethosomes as Breakthrough Tool for Controlled Transdermal Delivery of Dexketoprofen Trometamol: Design, Fabrication, Statistical Optimization, in Vitro, and Ex Vivo Characterization

Soliman

RASHWAN²,

Teaima³

et al. 2022

Int J App Pharm

Self Cite

View full text Add to dashboard Cite

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“…An identical empty pan was used as a reference. Thermograms were analyzed using a Shimadzu TA-60 software system (Lbsolutions TA workstation) [ 47 ]. The various obtained thermograms were evaluated for peak shift as well as appearance and disappearance of new peaks.…”

Section: Methodsmentioning

confidence: 99%

Anti-Tumor Activity of Orally Administered Gefitinib-Loaded Nanosized Cubosomes against Colon Cancer

et al. 2023

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Gefitinib (GFT) is a tyrosine kinase inhibitor drug used as a first-line treatment for patients with advanced or metastatic non-small cell lung, colon, and breast cancer. GFT exhibits low solubility and hence low oral bioavailability, which restricts its clinical application. One of the most important trends in overcoming such problems is the use of a vesicular system. Cubosomes are considered one of the most important vesicular systems used to improve solubility and oral bioavailability. In this study, GFT cubosomal nanoparticles (GFT-CNPs) were prepared by the emulsification method. The selected formulation variables were analyzed and optimized by full factorial design and response surface methodology. Drug entrapment efficiency (EE%), transmission electron microscopy, particle size, polydispersity index, in vitro release and its kinetics, and the effect of storage studies were estimated. The chosen GFT-CNPs were subjected to further investigations as gene expression levels of tissue inhibitors of metalloproteinases-1 (TIMP-1) and matrix metalloproteinases-7 (MMP-7), colon biomarkers, and histopathological examination of colon tissues. The prepared GFT-CNPs were semi-cubic in shape, with high EE%, smaller vesicle size, and higher zeta potential values. The in vivo data showed a significant decrease in the serum level of embryonic antigen (CEA), carbohydrate antigen 19-9 (CA 19-9), and gene expression level of TIMP-1 and MMP-7. Histopathological examination showed enhancement in cancer tissue and highly decreased focal infiltration in the lamina propria after treatment with GFT-CNPs.

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“…In Vitro Release of AzA from the Optimized Formula The in vitro release behavior of the AzA-TEs optimized formula was performed via the dialysis bag technique and compared with free AzA [27]. Before using the cellulose dialysis bag, it was soaked in phosphate-buffered saline pH 7.4 for 24 h. AzA-Tes equivalent to 10 mg of AzA was accurately weighed and the same amount of free AzA was dispersed in phosphate-buffered saline pH 7.4 and then subjected to 5 min vortexing.…”

Section: Fourier Transform Infrared (Ftir) Spectroscopymentioning

confidence: 99%

“…Ex Vivo Permeation of AzA from the Optimized Formula Mouse skin was utilized as a model to simulate human skin [29]. The ex vivo permeation experiment was performed via Franz diffusion cells with a diffusional area of 1.76 cm 2 using the same conditions of the in vitro drug release study, except that the cellulose membrane was substituted by dorsal hairless mouse skin [27,29]. The sacrifice of male mice (weighing between 25-30 g) was first carried out, followed by hair removal, and excision of the ventral and dorsal abdominal skins.…”

Section: Fourier Transform Infrared (Ftir) Spectroscopymentioning

confidence: 99%

Development, Optimization, and In Vitro/In Vivo Evaluation of Azelaic Acid Transethosomal Gel for Antidermatophyte Activity

et al. 2023

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Treatment of dermatophytosis is quite challenging. This work aims to investigate the antidermatophyte action of Azelaic acid (AzA) and evaluate its efficacy upon entrapment into transethosomes (TEs) and incorporation into a gel to enhance its application. Optimization of formulation variables of TEs was carried out after preparation using the thin film hydration technique. The antidermatophyte activity of AzA-TEs was first evaluated in vitro. In addition, two guinea pig infection models with Trichophyton (T.) mentagrophytes and Microsporum (M.) canis were established for the in vivo assessment. The optimized formula showed a mean particle size of 219.8 ± 4.7 nm and a zeta potential of −36.5 ± 0.73 mV, while the entrapment efficiency value was 81.9 ± 1.4%. Moreover, the ex vivo permeation study showed enhanced skin penetration for the AzA-TEs (3056 µg/cm2) compared to the free AzA (590 µg/cm2) after 48 h. AzA-TEs induced a greater inhibition in vitro on the tested dermatophyte species than free AzA (MIC90 was 0.01% vs. 0.32% for T. rubrum and 0.032% for T. mentagrophytes and M. canis vs. 0.56%). The mycological cure rate was improved in all treated groups, specially for our optimized AzA-TEs formula in the T. mentagrophytes model, in which it reached 83% in this treated group, while it was 66.76% in the itraconazole and free AzA treated groups. Significant (p < 0.05) lower scores of erythema, scales, and alopecia were observed in the treated groups in comparison with the untreated control and plain groups. In essence, the TEs could be a promising carrier for AzA delivery into deeper skin layers with enhanced antidermatophyte activity.

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Transdermal Delivery of Telmisartan: Formulation, in vitro, ex vivo, Iontophoretic Permeation Enhancement and Comparative Pharmacokinetic Study in Rats

Cited by 12 publications

References 36 publications

Transethosomes as Breakthrough Tool for Controlled Transdermal Delivery of Dexketoprofen Trometamol: Design, Fabrication, Statistical Optimization, in Vitro, and Ex Vivo Characterization

Transethosomes as Breakthrough Tool for Controlled Transdermal Delivery of Dexketoprofen Trometamol: Design, Fabrication, Statistical Optimization, in Vitro, and Ex Vivo Characterization

Anti-Tumor Activity of Orally Administered Gefitinib-Loaded Nanosized Cubosomes against Colon Cancer

Development, Optimization, and In Vitro/In Vivo Evaluation of Azelaic Acid Transethosomal Gel for Antidermatophyte Activity

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