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2000
Volume 31, Issue 29
  • ISSN: 1381-6128
  • E-ISSN: 1873-4286

Abstract

Background

Tamoxifen citrate (TMC), an antiestrogenic drug, is employed in the healing of advanced breast cancer. However, its oral and parenteral route-associated side effects and solubility issues restricted its medical utilizations.

Objective

The research aimed to prepare a tamoxifen citrate-loaded transethosomal gel (TMC TEsG) to enhance TMC entrapment efficiency, dissolution, and permeation.

Methods

TMC TEs were developed employing an HPH method and optimized using 23 factorial designs. The optimized TMC TEs were converted into TMC TEsG by cold dispersion. TMC TEs and TMC TEsG were estimated for particle size, microscopic, functional group interaction, crystalline, dissolution, permeation, spreadability, TMC content, and texture analysis.

Results

The optimization study revealed the suitability and validity of 23 designs for developing TMC TEs. TMC TEs with particle size ~163.1 nm and zeta potential of ~-26.8 mV improved the physical stability and skin permeation. TMC TEs showed a high entrapment efficiency of ~84.49%. TEM depicts spherical and sealed structure vesicles of TMC TEs. Physical analysis supported the formation of TMC TEs. Vesicles improved the dissolution (~96%) compared to pure TMC (~68%). The TMC TEsG increased the permeation (~82%) compared to TMC gel (~55%). TMC TEsG with pH (~5.61), viscosity (~4077.5 cps), and spreadability (~49.84 g.cm/s) exhibiting safety and easy applicability to the skin.

Conclusion

Outcomes suggest the transdermal permeation potential of design-generated flexible TMC TEs and, thus, could be employed to treat skin-related diseases.

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2025-09-02

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QbD-Anchored Preparation and Assessment of Transethosomal Gel for Enhanced Skin Permeation of Tamoxifen Citrate
Curr. Pharm. Des. 31, 2352 (2025); https://doi.org/10.2174/0113816128344198250308022732
/content/journals/cpd/10.2174/0113816128344198250308022732
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  • Article Type:     Research Article
Keyword(s): antiestrogenic drug; ex vivo permeation; in vitro dissolution; Tamoxifen citrate; transethosomes entrapment efficiency; transmission electron microscopy

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