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Purpose <p>Tacrolimus, a critical immunosuppressive agent used in autoimmune disorders and organ transplantation, requires rigorous stability assessment to ensure therapeutic efficacy. This study aimed to evaluate the stability of tacrolimus capsules under stress conditions using Response Surface Methodology (RSM), correlating degradation with both chemical and colorimetric changes.</p> Methods <p>The experimental design included four independent variables: exposure time (A), temperature (B), relative humidity (C), and hydrogen peroxide concentration (D). Two key responses were measured: the percentage of remaining tacrolimus using HPLC-UV, and the color change (ΔE) between untreated and stress-exposed tacrolimus capsules.</p> Results <p>The stability of tacrolimus (% remaining) was significantly affected by all variables (A–D), their interactions (AB, AC), and quadratic terms (A², C²). Color change (ΔE) was primarily driven by time, temperature, their interaction (AB), and the quadratic effect of humidity (C²). Logistic regression confirmed ΔE as a highly accurate predictor of degradation (92.6% correct classification, <i>p</i> = 0.007), with each unit increase in ΔE raising the odds of tacrolimus dropping below 95% stability by 8%.</p> Conclusion <p>The study demonstrated that RSM effectively models tacrolimus degradation under stress conditions, enabling precise shelf-life predictions based on time, temperature, humidity, and oxidative exposure. Colorimetric analysis (ΔE) was a rapid, non-destructive compare to HPLC. To minimize degradation, tacrolimus capsules should be stored at controlled temperatures (≤ 25&#xa0;°C) and low relative humidity (≤ 60% RH), with protection from prolonged heat and oxidizing agents.</p> Graphical Abstract <p></p>

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Experimental Design Approach for Evaluating the Stability of Tacrolimus Capsules during Various Stress Conditions: HPLC and Colored Image Analysis

  • 期刊论文

  • 发表日期：

    2026年1月7日

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  • Sara Sajjadi,
  • Ali Shayanfar,
  • Farhad Kiafar,
  • Mohammadreza Siahi-Shadbad

摘要

Purpose

Tacrolimus, a critical immunosuppressive agent used in autoimmune disorders and organ transplantation, requires rigorous stability assessment to ensure therapeutic efficacy. This study aimed to evaluate the stability of tacrolimus capsules under stress conditions using Response Surface Methodology (RSM), correlating degradation with both chemical and colorimetric changes.

Methods

The experimental design included four independent variables: exposure time (A), temperature (B), relative humidity (C), and hydrogen peroxide concentration (D). Two key responses were measured: the percentage of remaining tacrolimus using HPLC-UV, and the color change (ΔE) between untreated and stress-exposed tacrolimus capsules.

Results

The stability of tacrolimus (% remaining) was significantly affected by all variables (A–D), their interactions (AB, AC), and quadratic terms (A², C²). Color change (ΔE) was primarily driven by time, temperature, their interaction (AB), and the quadratic effect of humidity (C²). Logistic regression confirmed ΔE as a highly accurate predictor of degradation (92.6% correct classification, p = 0.007), with each unit increase in ΔE raising the odds of tacrolimus dropping below 95% stability by 8%.

Conclusion

The study demonstrated that RSM effectively models tacrolimus degradation under stress conditions, enabling precise shelf-life predictions based on time, temperature, humidity, and oxidative exposure. Colorimetric analysis (ΔE) was a rapid, non-destructive compare to HPLC. To minimize degradation, tacrolimus capsules should be stored at controlled temperatures (≤ 25 °C) and low relative humidity (≤ 60% RH), with protection from prolonged heat and oxidizing agents.

Graphical Abstract