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Purpose <p>Chemotherapy-induced nausea and vomiting (CINV) significantly impairs children’s quality of life and treatment adherence. This study developed pullulan-based lyophilized orodispersible wafers of Fosaprepitant diglutamine as a non-invasive alternative to injections. The rapidly dissolving formulation aims to enhance comfort, ease of administration, and overall pediatric treatment acceptance.</p> Methods <p>Orodispersible wafers were prepared using a lyophilization technique and optimized by adjusting polymer concentration, superdisintegrant, cryoprotectant, and natural sweetener levels. The prepared formulations were evaluated for thickness uniformity, surface pH, tensile strength, swelling index, disintegration time, and drug content. Drug–excipient compatibility was assessed using ATR-IR and DSC studies. In vitro dissolution, ex vivo permeation through goat buccal mucosa, pharmacokinetic analysis, stability testing, and antiemetic activity in a cisplatin-induced model were performed.</p> Results <p>The optimized formulation (F3) showed uniform drug distribution, a swelling index of 143–150%, and rapid disintegration within 40&#xa0;s. It achieved 96.55% drug release within 5&#xa0;min. Ex vivo permeation reached 95.65% at 30&#xa0;min, markedly higher than pure drug solution (60.83%). Pharmacokinetic evaluation demonstrated effective systemic exposure (Cmax 254.15&#xa0;µg/mL; Tmax 1&#xa0;h), comparable to the marketed formulation. Antiemetic studies confirmed reduced nausea-related behavior and improved feed intake.</p> Conclusion <p>The developed lyophilized wafers offer a stable, fast-disintegrating, and child-friendly alternative to injectable therapy, with strong potential to improve comfort, compliance, and therapeutic outcomes in pediatric CINV management.</p> Graphical Abstract <p></p>

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Advancing Pediatric Chemotherapy care: Innovative Fosaprepitant Orodispersible Wafers for Nausea and Vomiting

  • 期刊论文

  • 发表日期：

    2026年4月1日

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  • Tanushree Chakraborty,
  • R Suma,
  • Aisha Khanum,
  • Mohammed Afshan,
  • Rupesh Kumar,
  • Umme Hani,
  • Riyaz Ali M Osmani

摘要

Purpose

Chemotherapy-induced nausea and vomiting (CINV) significantly impairs children’s quality of life and treatment adherence. This study developed pullulan-based lyophilized orodispersible wafers of Fosaprepitant diglutamine as a non-invasive alternative to injections. The rapidly dissolving formulation aims to enhance comfort, ease of administration, and overall pediatric treatment acceptance.

Methods

Orodispersible wafers were prepared using a lyophilization technique and optimized by adjusting polymer concentration, superdisintegrant, cryoprotectant, and natural sweetener levels. The prepared formulations were evaluated for thickness uniformity, surface pH, tensile strength, swelling index, disintegration time, and drug content. Drug–excipient compatibility was assessed using ATR-IR and DSC studies. In vitro dissolution, ex vivo permeation through goat buccal mucosa, pharmacokinetic analysis, stability testing, and antiemetic activity in a cisplatin-induced model were performed.

Results

The optimized formulation (F3) showed uniform drug distribution, a swelling index of 143–150%, and rapid disintegration within 40 s. It achieved 96.55% drug release within 5 min. Ex vivo permeation reached 95.65% at 30 min, markedly higher than pure drug solution (60.83%). Pharmacokinetic evaluation demonstrated effective systemic exposure (Cmax 254.15 µg/mL; Tmax 1 h), comparable to the marketed formulation. Antiemetic studies confirmed reduced nausea-related behavior and improved feed intake.

Conclusion

The developed lyophilized wafers offer a stable, fast-disintegrating, and child-friendly alternative to injectable therapy, with strong potential to improve comfort, compliance, and therapeutic outcomes in pediatric CINV management.

Graphical Abstract