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Background <p>The present investigation aimed to formulate, optimize, and comparatively evaluate matrix-type transdermal patches of Carvedilol for sustained systemic delivery using different ratios of ethyl cellulose (EC) and polyvinyl pyrrolidone (PVP), with and without the penetration enhancer clove oil. Carvedilol is a non-selective β-blocker used to treat hypertension and heart failure. There are disadvantages of taking carvedilol orally such as inconsistent absorption and first-pass metabolism, which makes it an ideal drug for transdermal delivery via a patch. </p> Method <p>The patches were made using a solvent casting method with different ratios of ethyl cellulose and polyvinyl pyrrolidone along with dibutyl phthalate as a plasticizer, then evaluating in vitro permeation, release kinetics modeling, and skin irritation studies. </p> Results <p>There was no evidence of significant drug/polymer interaction determined via FT-IR analysis showing that carvedilol is compatible with the polymers utilized in this study.All formulations exhibited uniform thickness (0.10–0.16 mm), acceptable folding endurance (70–79 folds), minimal weight variation, and satisfactory flatness (&gt; 99%), confirming mechanical integrity and uniformity. Drug content complied with pharmacopeial limits, and the analytical method showed excellent linearity (R² = 0.9996). In vitro release studies demonstrated sustained drug release profiles across all formulations. Among the tested batches, the EC: PVP (1:7) formulation showed optimal performance, achieving approximately 88% cumulative drug release, while incorporation of clove oil further enhanced permeation to ~ 90%. Kinetic modeling indicated diffusion-controlled release following the Higuchi model, with Korsmeyer–Peppas analysis suggesting anomalous (non-Fickian) transport. Skin irritation studies in albino rabbits revealed no erythema or edema, confirming dermatological safety.</p> Conclusion <p>The developed formulation demonstrated promising in vitro drug release and permeation characteristics. However, these findings are preliminary and require further in vivo and pharmacokinetic studies to establish clinical efficacy and therapeutic applicability.</p>

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Formulation and Optimization of Carvedilol Transdermal Patches with Clove Oil as a Natural Penetration Enhancers

  • 期刊论文

  • 发表日期：

    2026年6月2日

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  • Neha Paramanik,
  • Arpan Sen,
  • Shreya Ghosh,
  • Alindam Ghosh,
  • Avik Dutta,
  • Sudip Das,
  • Prithviraj Chakraborty,
  • Debarupa Dutta Chakraborty

摘要

Background

The present investigation aimed to formulate, optimize, and comparatively evaluate matrix-type transdermal patches of Carvedilol for sustained systemic delivery using different ratios of ethyl cellulose (EC) and polyvinyl pyrrolidone (PVP), with and without the penetration enhancer clove oil. Carvedilol is a non-selective β-blocker used to treat hypertension and heart failure. There are disadvantages of taking carvedilol orally such as inconsistent absorption and first-pass metabolism, which makes it an ideal drug for transdermal delivery via a patch.

Method

The patches were made using a solvent casting method with different ratios of ethyl cellulose and polyvinyl pyrrolidone along with dibutyl phthalate as a plasticizer, then evaluating in vitro permeation, release kinetics modeling, and skin irritation studies.

Results

There was no evidence of significant drug/polymer interaction determined via FT-IR analysis showing that carvedilol is compatible with the polymers utilized in this study.All formulations exhibited uniform thickness (0.10–0.16 mm), acceptable folding endurance (70–79 folds), minimal weight variation, and satisfactory flatness (> 99%), confirming mechanical integrity and uniformity. Drug content complied with pharmacopeial limits, and the analytical method showed excellent linearity (R² = 0.9996). In vitro release studies demonstrated sustained drug release profiles across all formulations. Among the tested batches, the EC: PVP (1:7) formulation showed optimal performance, achieving approximately 88% cumulative drug release, while incorporation of clove oil further enhanced permeation to ~ 90%. Kinetic modeling indicated diffusion-controlled release following the Higuchi model, with Korsmeyer–Peppas analysis suggesting anomalous (non-Fickian) transport. Skin irritation studies in albino rabbits revealed no erythema or edema, confirming dermatological safety.

Conclusion

The developed formulation demonstrated promising in vitro drug release and permeation characteristics. However, these findings are preliminary and require further in vivo and pharmacokinetic studies to establish clinical efficacy and therapeutic applicability.