Preeti S. Bobade, Ayush S. Mishra, Saurabh B. Ganorkar, Darshan R. Telange* and Shailesh S. Chalikwar Pages 1 - 18 ( 18 )
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 utilization.
Objective: The research aimed to prepare a tamoxifen citrate-loaded transethosomal gel (TMC TEsG) to enhance TMC entrapment efficiency, in vitro dissolution, and ex vivo 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, in vitro dissolution, ex vivo permeation, spreadability, TMC content, and texture analysis.
Results: The optimization study revealed the suitability and validity of 23 designs for developing TMC TE. 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.
Tamoxifen citrate, transethosomes entrapment efficiency, in vitro dissolution, ex vivo permeation.