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Summary

This study enhanced clotrimazole (CT) drug stability in hot-melt extrusion (HME) films using hydroxypropyl cellulose (HPC) and poly(ethylene oxide) (PEO) blends. Optimal stability and drug release were achieved with a 55:35:10 HPC:PEO:CT ratio.

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Area of Science:

  • Pharmaceutical Sciences
  • Materials Science

Background:

  • Hot-melt extrusion (HME) is a viable technique for amorphous solid dispersion formulation.
  • Enhancing the physical stability of amorphous solid dispersions is crucial for drug product performance.

Purpose of the Study:

  • To improve the physical stability and tailor drug release of clotrimazole (CT) in HME films.
  • To investigate the impact of hydroxypropyl cellulose (HPC) and poly(ethylene oxide) (PEO) blends on HME film properties.

Main Methods:

  • HME films were prepared using varying ratios of HPC and PEO with CT.
  • Solid-state characterization included differential scanning calorimetry (DSC), X-ray diffractometry (XRD), and dynamic mechanical analysis (DMA).
  • Bioadhesive, mechanical, moisture sorption, and drug release properties were evaluated over 12 months.

Main Results:

  • Clotrimazole (CT) was successfully incorporated in a solid solution within all HME films.
  • Increasing HPC concentration enhanced the physical stability of CT and PEO but reduced bioadhesivity and flexibility.
  • A 55:35:10 HPC:PEO:CT ratio yielded optimal physical-mechanical, bioadhesive, and drug release characteristics.

Conclusions:

  • Polymer blends of HPC and PEO effectively enhance the physical stability of CT in HME films.
  • The HPC:PEO ratio can be optimized to tailor drug release, mechanical, and bioadhesive properties.
  • HME films offer a promising platform for stable amorphous solid dispersions of poorly soluble drugs.