Background <p>Mebendazole (MBZ) is an anthelmintic drug that was repurposed as an anti-cancer agent.</p> Objectives <p>This study aimed at formulating MBZ into stearylamine tailored spanlastics dispersed in nanogel for enhancing MBZ anti-tumor efficacy against skin cancer.</p> Methods <p>MBZ spanlastics were prepared by thin film hydration using 2<sup>1</sup> × 3<sup>1</sup> factorial design. The formulation variables were the total amount (mg) of Span 60 and Tween 80 in the formulations and the ratio between Span 60 and Tween 80.</p> Results <p>Optimal spanlastics formulation was composed of 400&#xa0;mg of Span 60 and Tween 80 in a ratio of 2:1 and showed EE% of 78 ± 2.9% and PS of 284.00 ± 35.36&#xa0;nm. Stearylamine (20&#xa0;mg) was added to the optimized formulation and showed acceptable positive charge (zeta potential = 47.53 ± 1.50&#xa0;mV). It was dispersed in 30% Tetronic<sup>®</sup>1107 solution to form a nanogel. MBZ nanogel was assessed for their cytotoxic effect on cell proliferation against human malignant melanoma and epidermoid carcinoma cell lines and showed 38.70 ± 1.70% and 48.60 ± 0.50% (respectively) cell proliferation compared to the control group (100%). Finally, its permeation through Wistar rat skin was tested.</p> Conclusion <p>SA-spanlastics nanogel holds potential as an effective nanocarrier for boosting MBZ anti-cancer efficacy.</p> Graphical Abstract <p></p>

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Stearyl amine tailored spanlastics embedded within tetronic® nanogel for boosting the repurposed anticancer potential of mebendazole: formulation, in vitro profiling, cytotoxicity assessment, and in vivo permeation analysis

  • Mai El Halawany,
  • Marwa Sharaky,
  • Diana Aziz

摘要

Background

Mebendazole (MBZ) is an anthelmintic drug that was repurposed as an anti-cancer agent.

Objectives

This study aimed at formulating MBZ into stearylamine tailored spanlastics dispersed in nanogel for enhancing MBZ anti-tumor efficacy against skin cancer.

Methods

MBZ spanlastics were prepared by thin film hydration using 21 × 31 factorial design. The formulation variables were the total amount (mg) of Span 60 and Tween 80 in the formulations and the ratio between Span 60 and Tween 80.

Results

Optimal spanlastics formulation was composed of 400 mg of Span 60 and Tween 80 in a ratio of 2:1 and showed EE% of 78 ± 2.9% and PS of 284.00 ± 35.36 nm. Stearylamine (20 mg) was added to the optimized formulation and showed acceptable positive charge (zeta potential = 47.53 ± 1.50 mV). It was dispersed in 30% Tetronic®1107 solution to form a nanogel. MBZ nanogel was assessed for their cytotoxic effect on cell proliferation against human malignant melanoma and epidermoid carcinoma cell lines and showed 38.70 ± 1.70% and 48.60 ± 0.50% (respectively) cell proliferation compared to the control group (100%). Finally, its permeation through Wistar rat skin was tested.

Conclusion

SA-spanlastics nanogel holds potential as an effective nanocarrier for boosting MBZ anti-cancer efficacy.

Graphical Abstract