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Background and Objective <p>The present study aimed to optimize the preparation of electrospun nanofibers using a two-factor, three-level central composite design and to evaluate their potential as a gastroretentive drug delivery system in comparison with a marketed sustained-release capsule (Ganaton® SR).</p> Methods <p>Electrospun nanofibers were formulated and optimized, followed by in vitro drug release and release kinetic modeling. The optimized formulation and marketed preparation (drug equivalent to 10 mg) were compared for cumulative drug release in simulated gastric fluid. Characterization was performed using FTIR, DSC, XRD, and SEM. Pharmacokinetic studies were conducted in New Zealand white rabbits with blood sampling from the marginal ear vein analyzed via HPLC. X-ray imaging was employed to determine gastroretention.</p> Results <p>The optimized nanofiber formulation exhibited 80.00 ± 0.17% drug release in 10 h, compared to 96.78 ± 0.39% from Ganaton® SR. Release data best fitted the Hixon-Crowell kinetic model (R² = 0.969) with an ‘n’ value of 0.685. Pharmacokinetic evaluation revealed improved bioavailability of the optimized nanofibers (Cmax: 5.107 ± 0.14 µg/mL; AUC: 54.50 ± 1.62 µg/mL·h; t½: 4.923 ± 0.68 h) compared to Ganaton® SR. X-ray imaging confirmed prolonged gastroretention of the nanofibers in the stomach.</p> Conclusion <p>The optimized electrospun nanofibers demonstrated controlled drug release, enhanced bioavailability, and prolonged gastric residence, providing both local and systemic therapeutic effects. These findings suggest that nanofiber-based formulations hold promise as an effective gastroretentive drug delivery system for the treatment of gastroesophageal reflux disease. In the present study, preparation of electrospun nanofibers was optimized using 2-factor, 3 level central composite experimental design. The cumulative drug release from an optimized formulation batch was compared with the marketed capsule preparation (Ganaton® SR). The percentage of drug release carried out in simulated gastric fluid from an optimized batch of nanofiber formulation and marketed preparation, containing drug equivalent to 10&#xa0;mg, was observed to be 80.00 ± 0.17% and 96.78 ± 0.39%, respectively, in 10&#xa0;h study The data was best fitted in the Hixon-Crowell release kinetic model with an R2 value of 0.969. however, the value of 'n = 0.685'. The nanofibers were characterized using FTIR, DSC, XRD, and SEM techniques. The optimized batch of nanofiber formulation was further compared with marketed preparation (Ganaton SR®) for and pharmacokinetic study. The optimized batch showed a Cmax of 5.107 ± 0.14&#xa0;µg/mL, AUC of 54.50 ± 1.62&#xa0;µg/mL·h, and t1/2 of 4.923 ± 0.68&#xa0;h, demonstrating superior bioavailability over Ganaton® SR For pharmacokinetics studies, blood samples from the marginal ear vein of New Zealand white rabbits were collected and analyzed using HPLC. X-ray photographic images of rabbits' stomachs were taken to locate the dosage form in the stomach region at different time intervals to find the gastroretention time. Thus, from the studies carried out here, it is clinched that the prepared nanofibers provided both local and systemic effects in stomach and proved to be a promising drug delivery system for the treatment of gastroesophageal reflux disease.</p> Graphical Abstract <p></p>

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Optimization and Evaluation of Itopride Hydrochloride-Loaded Eudragit S100/Ethylcellulose Gastroretentive Electrospun Nanofibers for the Treatment of Gastroesophageal Reflux Disease

  • 期刊论文

  • 发表日期：

    2025年10月17日

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  • Rameshwar Dass,
  • Pooja Rani,
  • Harish Dureja,
  • Priya Dhiman,
  • Vikas Verma,
  • Dinesh Kumar,
  • Meenakshi Bhatia,
  • Syed Mahmood

摘要

Background and Objective

The present study aimed to optimize the preparation of electrospun nanofibers using a two-factor, three-level central composite design and to evaluate their potential as a gastroretentive drug delivery system in comparison with a marketed sustained-release capsule (Ganaton® SR).

Methods

Electrospun nanofibers were formulated and optimized, followed by in vitro drug release and release kinetic modeling. The optimized formulation and marketed preparation (drug equivalent to 10 mg) were compared for cumulative drug release in simulated gastric fluid. Characterization was performed using FTIR, DSC, XRD, and SEM. Pharmacokinetic studies were conducted in New Zealand white rabbits with blood sampling from the marginal ear vein analyzed via HPLC. X-ray imaging was employed to determine gastroretention.

Results

The optimized nanofiber formulation exhibited 80.00 ± 0.17% drug release in 10 h, compared to 96.78 ± 0.39% from Ganaton® SR. Release data best fitted the Hixon-Crowell kinetic model (R² = 0.969) with an ‘n’ value of 0.685. Pharmacokinetic evaluation revealed improved bioavailability of the optimized nanofibers (Cmax: 5.107 ± 0.14 µg/mL; AUC: 54.50 ± 1.62 µg/mL·h; t½: 4.923 ± 0.68 h) compared to Ganaton® SR. X-ray imaging confirmed prolonged gastroretention of the nanofibers in the stomach.

Conclusion

The optimized electrospun nanofibers demonstrated controlled drug release, enhanced bioavailability, and prolonged gastric residence, providing both local and systemic therapeutic effects. These findings suggest that nanofiber-based formulations hold promise as an effective gastroretentive drug delivery system for the treatment of gastroesophageal reflux disease. In the present study, preparation of electrospun nanofibers was optimized using 2-factor, 3 level central composite experimental design. The cumulative drug release from an optimized formulation batch was compared with the marketed capsule preparation (Ganaton® SR). The percentage of drug release carried out in simulated gastric fluid from an optimized batch of nanofiber formulation and marketed preparation, containing drug equivalent to 10 mg, was observed to be 80.00 ± 0.17% and 96.78 ± 0.39%, respectively, in 10 h study The data was best fitted in the Hixon-Crowell release kinetic model with an R2 value of 0.969. however, the value of 'n = 0.685'. The nanofibers were characterized using FTIR, DSC, XRD, and SEM techniques. The optimized batch of nanofiber formulation was further compared with marketed preparation (Ganaton SR®) for and pharmacokinetic study. The optimized batch showed a Cmax of 5.107 ± 0.14 µg/mL, AUC of 54.50 ± 1.62 µg/mL·h, and t1/2 of 4.923 ± 0.68 h, demonstrating superior bioavailability over Ganaton® SR For pharmacokinetics studies, blood samples from the marginal ear vein of New Zealand white rabbits were collected and analyzed using HPLC. X-ray photographic images of rabbits' stomachs were taken to locate the dosage form in the stomach region at different time intervals to find the gastroretention time. Thus, from the studies carried out here, it is clinched that the prepared nanofibers provided both local and systemic effects in stomach and proved to be a promising drug delivery system for the treatment of gastroesophageal reflux disease.

Graphical Abstract