<p>Poor solubility of drugs represents a major obstacle against drug delivery, so pharmaceutical industry is exploring the use of nanocrystals as a promising approach to enhance the bioavailability of those medications with improving their pharmacokinetics. This study aims to improve etoricoxib properties via nanocrystal form using an acid-base precipitation method. This method is simple, environment- friendly, and prefers non-organic solvents and chemicals, thus overcoming challenges in developing dosage forms. Prepared nanocrystals were optimized for several factors such as stabilizer type and concentration, amount of drug, time and speed of homogenization. FT-IR, DSC, X-ray diffraction, and TEM characterizations were conducted on the optimized nanocrystal formula. The findings showed a successful inclusion of etoricoxib as nanocrystals with a mean particle size of 210.30 ± 10.20&#xa0;nm, PDI of 0.277 ± 0.01, and a zeta potential of − 74.10 ± 0.61 mV. TEM imaging revealed well-defined cubic-shaped nanoparticles, indicating morphological uniformity and excipient compatibility. Solubility studies demonstrated notable enhancement in the aqueous solubility of etoricoxib nanocrystals (137.75 ± 1.34&#xa0;µg/mL) compared to the pure drug (87.70 ± 1.41&#xa0;µg/mL). Additionally, the nanocrystals exhibited rapid dissolution profile, achieving 91.49 ± 0.01% drug release within 5&#xa0;min. These results suggest that using nanocrystals to improve the aqueous solubility and dissolution of medications with poor solubility is a potential strategy.</p>

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Nanocrystals as a promising approach for enhancing solubility and dissolution of etoricoxib using Box–Behnken design

  • Lamiaa M. Ahmed,
  • Fergany A. Mohamed,
  • Tahani H. Elfaham

摘要

Poor solubility of drugs represents a major obstacle against drug delivery, so pharmaceutical industry is exploring the use of nanocrystals as a promising approach to enhance the bioavailability of those medications with improving their pharmacokinetics. This study aims to improve etoricoxib properties via nanocrystal form using an acid-base precipitation method. This method is simple, environment- friendly, and prefers non-organic solvents and chemicals, thus overcoming challenges in developing dosage forms. Prepared nanocrystals were optimized for several factors such as stabilizer type and concentration, amount of drug, time and speed of homogenization. FT-IR, DSC, X-ray diffraction, and TEM characterizations were conducted on the optimized nanocrystal formula. The findings showed a successful inclusion of etoricoxib as nanocrystals with a mean particle size of 210.30 ± 10.20 nm, PDI of 0.277 ± 0.01, and a zeta potential of − 74.10 ± 0.61 mV. TEM imaging revealed well-defined cubic-shaped nanoparticles, indicating morphological uniformity and excipient compatibility. Solubility studies demonstrated notable enhancement in the aqueous solubility of etoricoxib nanocrystals (137.75 ± 1.34 µg/mL) compared to the pure drug (87.70 ± 1.41 µg/mL). Additionally, the nanocrystals exhibited rapid dissolution profile, achieving 91.49 ± 0.01% drug release within 5 min. These results suggest that using nanocrystals to improve the aqueous solubility and dissolution of medications with poor solubility is a potential strategy.