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Purpose <p>Idiopathic pulmonary fibrosis (IPF) is a progressive and fatal pulmonary disorder marked by irreversible fibrotic remodeling of lung tissue and limited therapeutic options. Pirfenidone is clinically approved for IPF management; however, its therapeutic utility is restricted by poor and variable oral bioavailability, extensive first-pass metabolism, frequent dosing, and systemic adverse effects. These challenges necessitate the development of an innovative, lung-targeted delivery system capable of enhancing drug localization and sustaining therapeutic efficacy.</p> Methods <p>In this study, biodegradable pirfenidone-loaded nanocarriers were developed and systematically optimized as a potential pulmonary delivery system based on its nanoscale characteristics and sustained drug release properties. Nanoparticles were prepared using an ionic gelation technique employing chitosan and albumin as biocompatible polymeric carriers. A three-factor, three-level Box–Behnken design was applied to evaluate and optimize the influence of formulation variables on particle size and drug entrapment efficiency. Comprehensive preformulation and physicochemical characterization, including UV–visible spectroscopy, FTIR, DSC, and solubility analysis, confirmed drug integrity and excipient compatibility. </p> Results <p>The optimized formulation exhibited a nanoscale particle size (~152 nm) with high drug entrapment efficiency (~85%), supporting its suitability for deep lung deposition. In vitro release studies demonstrated a controlled and sustained release profile, achieving approximately 79% cumulative drug release over 24 hours. Release kinetics analysis revealed diffusion-controlled drug release behavior, consistent with Higuchi and Korsmeyer–Peppas models. Statistical validation confirmed strong model predictability and robustness of the optimization strategy. </p> Conclusion <p>Overall, this work presents an innovative biodegradable nanocarrier platform that addresses key limitations of conventional pirfenidone therapy. The developed system holds significant potential for improving pulmonary drug targeting, enhancing therapeutic performance, and reducing systemic side effects, thereby offering a promising pharmaceutical innovation for the effective management of idiopathic pulmonary fibrosis.</p> Graphical Abstract <p></p>

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Development and Optimization of Biodegradable Pirfenidone Loaded Nanocarriers for Targeted Therapy of Idiopathic Pulmonary Fibrosis

  • 期刊论文

  • 发表日期：

    2026年5月4日

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  • Yogendra Malviya,
  • Swapnil Goyal

摘要

Purpose

Idiopathic pulmonary fibrosis (IPF) is a progressive and fatal pulmonary disorder marked by irreversible fibrotic remodeling of lung tissue and limited therapeutic options. Pirfenidone is clinically approved for IPF management; however, its therapeutic utility is restricted by poor and variable oral bioavailability, extensive first-pass metabolism, frequent dosing, and systemic adverse effects. These challenges necessitate the development of an innovative, lung-targeted delivery system capable of enhancing drug localization and sustaining therapeutic efficacy.

Methods

In this study, biodegradable pirfenidone-loaded nanocarriers were developed and systematically optimized as a potential pulmonary delivery system based on its nanoscale characteristics and sustained drug release properties. Nanoparticles were prepared using an ionic gelation technique employing chitosan and albumin as biocompatible polymeric carriers. A three-factor, three-level Box–Behnken design was applied to evaluate and optimize the influence of formulation variables on particle size and drug entrapment efficiency. Comprehensive preformulation and physicochemical characterization, including UV–visible spectroscopy, FTIR, DSC, and solubility analysis, confirmed drug integrity and excipient compatibility.

Results

The optimized formulation exhibited a nanoscale particle size (~152 nm) with high drug entrapment efficiency (~85%), supporting its suitability for deep lung deposition. In vitro release studies demonstrated a controlled and sustained release profile, achieving approximately 79% cumulative drug release over 24 hours. Release kinetics analysis revealed diffusion-controlled drug release behavior, consistent with Higuchi and Korsmeyer–Peppas models. Statistical validation confirmed strong model predictability and robustness of the optimization strategy.

Conclusion

Overall, this work presents an innovative biodegradable nanocarrier platform that addresses key limitations of conventional pirfenidone therapy. The developed system holds significant potential for improving pulmonary drug targeting, enhancing therapeutic performance, and reducing systemic side effects, thereby offering a promising pharmaceutical innovation for the effective management of idiopathic pulmonary fibrosis.

Graphical Abstract