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Introduction <p>Bupropion (marketed as Wellbutrin), a potent antidepressant, eludes the typical side effects of somnolence, weight gain, and sexual dysfunction. It is also marketed under the brand name Zyban, which has been demonstrated to be effective as an antismoking medicine. The current research work focuses on establishing the antismoking potential of bupropion biochemically and then developing a nanoemulstick to improve the therapeutic potential of bupropion by minimizing its skin retention and enhancing its systemic delivery.</p> Methods <p>The Quality by Design (QbD) approach was used in the formulation and optimization of bupropion-laden nanoemulsion. Critical material attributes (CMAs) and critical quality attributes (CQAs) were identified based on the Quality Through Process Planning (QTPP). To determine CMAs points, the D-optimal mixture design was employed, and two CQAs were identified as globule size and percentage cumulative drug release (CDR%). Based on the desirability criteria, the optimized nanoemulsion was selected. The optimized nanoemulsion was transformed into a nanoemulstick, which was further evaluated for its skin permeation abilities and other parameters.</p> Results <p>As results of response surface analysis demonstrate, the optimized nanoemulsion with a particle size of 263.5&#xa0;nm exhibited good cumulative drug release of 81.01%. The physicochemical integrity of the formulation was validated through the test period by stability studies. According to the permeation investigation, the nanoemulstick of bupropion exhibited 16.676 ± 0.911% skin retention and 221.521 ± 5.765 (µg/cm<sup>2</sup>/h) steady-state flux, whereas the conventional stick showed 64.678 ± 3.337% skin retention and 32.675 ± 4.946 (µg/cm<sup>2</sup>/h) steady-state flux, highlighting the superior skin permeation characteristics of the nanoemulstick compared to the conventional stick.</p> Conclusion <p>By avoiding first-pass metabolism, the nanoemulstick dramatically improves drug absorption, making it a viable substitute for traditional oral smoking cessation formulations. This study creates the framework for future clinical testing and possible translabial nanoemulstick commercialization as a successful treatment option.</p>

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QbD-Based Development of Translabial Bupropion-Loaded Nanoemulstick for Brain-Targeted Dopamine Modulation in Smoking Cessation using PC12 Cell Lines

  • 期刊论文

  • 发表日期：

    2025年7月14日

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  • Sneh Lata,
  • Sanju Nanda

摘要

Introduction

Bupropion (marketed as Wellbutrin), a potent antidepressant, eludes the typical side effects of somnolence, weight gain, and sexual dysfunction. It is also marketed under the brand name Zyban, which has been demonstrated to be effective as an antismoking medicine. The current research work focuses on establishing the antismoking potential of bupropion biochemically and then developing a nanoemulstick to improve the therapeutic potential of bupropion by minimizing its skin retention and enhancing its systemic delivery.

Methods

The Quality by Design (QbD) approach was used in the formulation and optimization of bupropion-laden nanoemulsion. Critical material attributes (CMAs) and critical quality attributes (CQAs) were identified based on the Quality Through Process Planning (QTPP). To determine CMAs points, the D-optimal mixture design was employed, and two CQAs were identified as globule size and percentage cumulative drug release (CDR%). Based on the desirability criteria, the optimized nanoemulsion was selected. The optimized nanoemulsion was transformed into a nanoemulstick, which was further evaluated for its skin permeation abilities and other parameters.

Results

As results of response surface analysis demonstrate, the optimized nanoemulsion with a particle size of 263.5 nm exhibited good cumulative drug release of 81.01%. The physicochemical integrity of the formulation was validated through the test period by stability studies. According to the permeation investigation, the nanoemulstick of bupropion exhibited 16.676 ± 0.911% skin retention and 221.521 ± 5.765 (µg/cm2/h) steady-state flux, whereas the conventional stick showed 64.678 ± 3.337% skin retention and 32.675 ± 4.946 (µg/cm2/h) steady-state flux, highlighting the superior skin permeation characteristics of the nanoemulstick compared to the conventional stick.

Conclusion

By avoiding first-pass metabolism, the nanoemulstick dramatically improves drug absorption, making it a viable substitute for traditional oral smoking cessation formulations. This study creates the framework for future clinical testing and possible translabial nanoemulstick commercialization as a successful treatment option.