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Purpose <p>The aim of this study was to evaluate the in vitro anticancer activity and apoptotic potential of an optimized mechlormethamine topical formulation developed using a Quality by Design approach.</p> Methodology <p>Cytotoxic activity was assessed in A431 human skin cancer cells using the MTT assay over a concentration range of 0.5–32 µM. Cell viability, growth inhibition, and half-maximal inhibitory concentration (IC₅₀) were determined from dose–response curves. Apoptosis was evaluated by nuclear morphology using 4′,6-diamidino-2-phenylindole (DAPI) staining following treatment at the IC₅₀ concentration.</p> Results <p>The mechlormethamine formulation induced a concentration-dependent decrease in cell viability, with survival declining from 80.42% at 0.5 µM to 5.02% at 32 µM. The IC₅₀ value was 1.86 ± 0.15 µM, indicating strong antiproliferative activity. DAPI staining revealed characteristic apoptotic changes in treated cells, including chromatin condensation, nuclear fragmentation, and apoptotic body formation, while untreated cells maintained normal nuclear morphology.</p> Conclusion <p>The optimized mechlormethamine topical formulation demonstrated significant cytotoxic and apoptosis-inducing activity in vitro. These findings support its potential for further preclinical evaluation and highlight its relevance as a promising topical therapeutic approach for CTCL.</p> Graphical Abstract <p></p>

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In-Vitro Cytotoxic and Apoptotic Evaluation of an Optimized Mechlorethamine Topical Formulation in A431 Skin Cancer Cells

  • 期刊论文

  • 发表日期：

    2026年5月19日

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  • Hemil Shah,
  • Prachi Pandey,
  • Priyal Patel

摘要

Purpose

The aim of this study was to evaluate the in vitro anticancer activity and apoptotic potential of an optimized mechlormethamine topical formulation developed using a Quality by Design approach.

Methodology

Cytotoxic activity was assessed in A431 human skin cancer cells using the MTT assay over a concentration range of 0.5–32 µM. Cell viability, growth inhibition, and half-maximal inhibitory concentration (IC₅₀) were determined from dose–response curves. Apoptosis was evaluated by nuclear morphology using 4′,6-diamidino-2-phenylindole (DAPI) staining following treatment at the IC₅₀ concentration.

Results

The mechlormethamine formulation induced a concentration-dependent decrease in cell viability, with survival declining from 80.42% at 0.5 µM to 5.02% at 32 µM. The IC₅₀ value was 1.86 ± 0.15 µM, indicating strong antiproliferative activity. DAPI staining revealed characteristic apoptotic changes in treated cells, including chromatin condensation, nuclear fragmentation, and apoptotic body formation, while untreated cells maintained normal nuclear morphology.

Conclusion

The optimized mechlormethamine topical formulation demonstrated significant cytotoxic and apoptosis-inducing activity in vitro. These findings support its potential for further preclinical evaluation and highlight its relevance as a promising topical therapeutic approach for CTCL.

Graphical Abstract