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Purpose <p>This study explores the potential of carboxymethyl ethyl cellulose (CMEC) as a carrier for preparing amorphous solid dispersion (ASDs) of itraconazole (ITZ), a poorly water-soluble drug.</p> Methods <p>ASDs were prepared via solvent evaporation at drug-to-polymer ratios of 1:1–1:5 and characterized by FTIR, PXRD, and DSC to assess drug–polymer interactions and amorphization. Solubility was evaluated in pH 1.2 and pH 6.8 media, furthermore, in vitro dissolution was studied in both acidic and basic environments. ASD tablets were formulated to assess performance in solid dosage form. Pharmacokinetic studies were conducted in rats, and accelerated stability testing was performed on the optimized formulation.</p> Results <p>FTIR confirmed hydrogen bonding between ITZ and CMEC, while PXRD and DSC indicated complete amorphization in optimized ASDs. Solubility and dissolution studies showed negligible release at pH 1.2 but a marked improvement at pH 6.8, with up to 91% release from ASDs versus 4% from pure ITZ. The ASD tablets retained this dissolution advantage, achieving 93% release in basic medium. Pharmacokinetic analysis revealed significantly higher systemic exposure for ITZ: CMEC (1:5), followed by 1:4, compared to pure ITZ. The optimized ASD remained stable under accelerated conditions.</p> Conclusion <p>CMEC-based ASDs effectively improved the solubility, dissolution, and bioavailability of ITZ, demonstrating the potential of CMEC as a promising carrier for poorly soluble, weakly basic drugs.</p> Graphical Abstract <p></p>

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Carboxymethyl Ethyl Cellulose-based Solid Dispersions: a Promising Approach to Enhance the Dissolution and Oral Bioavailability of Itraconazole

  • 期刊论文

  • 发表日期：

    2026年1月27日

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  • Madhur Kulkarni,
  • Vaishali Shirsat,
  • Pratiksha More,
  • Shreya Mohite,
  • Ayush Jaiswal

摘要

Purpose

This study explores the potential of carboxymethyl ethyl cellulose (CMEC) as a carrier for preparing amorphous solid dispersion (ASDs) of itraconazole (ITZ), a poorly water-soluble drug.

Methods

ASDs were prepared via solvent evaporation at drug-to-polymer ratios of 1:1–1:5 and characterized by FTIR, PXRD, and DSC to assess drug–polymer interactions and amorphization. Solubility was evaluated in pH 1.2 and pH 6.8 media, furthermore, in vitro dissolution was studied in both acidic and basic environments. ASD tablets were formulated to assess performance in solid dosage form. Pharmacokinetic studies were conducted in rats, and accelerated stability testing was performed on the optimized formulation.

Results

FTIR confirmed hydrogen bonding between ITZ and CMEC, while PXRD and DSC indicated complete amorphization in optimized ASDs. Solubility and dissolution studies showed negligible release at pH 1.2 but a marked improvement at pH 6.8, with up to 91% release from ASDs versus 4% from pure ITZ. The ASD tablets retained this dissolution advantage, achieving 93% release in basic medium. Pharmacokinetic analysis revealed significantly higher systemic exposure for ITZ: CMEC (1:5), followed by 1:4, compared to pure ITZ. The optimized ASD remained stable under accelerated conditions.

Conclusion

CMEC-based ASDs effectively improved the solubility, dissolution, and bioavailability of ITZ, demonstrating the potential of CMEC as a promising carrier for poorly soluble, weakly basic drugs.

Graphical Abstract