Objective <p>This research aimed to develop the amorphous solid dispersion (ASD) of piroxicam (PRX) using Neusilin<sup>®</sup> US2 as a porous carrier via incipient wetness impregnation and to investigate the effect of polymers on stabilizing the amorphous PRX to enhance its aqueous solubility.</p> Methods <p>Three types of polymers (hydroxypropyl methylcellulose, polyvinyl alcohol, and poloxamer) were selected as stabilizers for the ASD and co-incorporated with PRX onto Neusilin<sup>®</sup> US2. Physicochemical properties of PRX-impregnated composites, including morphology, particle size, specific surface area, total pore volume, solid-state characteristics, drug loading, and dissolution were evaluated to confirm successful impregnation. Stability of PRX-impregnated composites was also assessed at 40&#xa0;°C and 75% relative humidity.</p> Results <p>The actual drug loading in the poloxamer formulation was 18.51 ± 0.02%, and after 3 months of storage, it remained at 16.39 ± 0.07%, indicating good retention relative to the 20% target drug loading. Compared with other polymers, poloxamer was found to be the most effective in stabilizing the amorphous PRX and preventing its recrystallization.</p> Conclusions <p>Impregnation of the drug in its amorphous state along with poloxamer onto Neusilin<sup>®</sup> US2 could be a promising approach to improve the dissolution rate of poorly water-soluble drug.</p>

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The Effect of Polymers on Physicochemical Properties and Stability of Amorphous Piroxicam-Impregnated Neusilin® US2 Composite Particles Prepared by Incipient Wetness Impregnation

  • Malina Thepphaya,
  • Thamer A. Omar,
  • Veerakiet Boonkanokwong

摘要

Objective

This research aimed to develop the amorphous solid dispersion (ASD) of piroxicam (PRX) using Neusilin® US2 as a porous carrier via incipient wetness impregnation and to investigate the effect of polymers on stabilizing the amorphous PRX to enhance its aqueous solubility.

Methods

Three types of polymers (hydroxypropyl methylcellulose, polyvinyl alcohol, and poloxamer) were selected as stabilizers for the ASD and co-incorporated with PRX onto Neusilin® US2. Physicochemical properties of PRX-impregnated composites, including morphology, particle size, specific surface area, total pore volume, solid-state characteristics, drug loading, and dissolution were evaluated to confirm successful impregnation. Stability of PRX-impregnated composites was also assessed at 40 °C and 75% relative humidity.

Results

The actual drug loading in the poloxamer formulation was 18.51 ± 0.02%, and after 3 months of storage, it remained at 16.39 ± 0.07%, indicating good retention relative to the 20% target drug loading. Compared with other polymers, poloxamer was found to be the most effective in stabilizing the amorphous PRX and preventing its recrystallization.

Conclusions

Impregnation of the drug in its amorphous state along with poloxamer onto Neusilin® US2 could be a promising approach to improve the dissolution rate of poorly water-soluble drug.