Ahmed Lamiaa M, Mohamed Fergany A, Elfaham Tahani H
Department of pharmaceutics, Faculty of pharmacy, Assiut University, Assiut, 71526, Egypt.
Sci Rep. 2025 Aug 11;15(1):29347. doi: 10.1038/s41598-025-12837-3.
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.
药物的低溶解度是药物递送的主要障碍,因此制药行业正在探索使用纳米晶体作为一种有前景的方法,以提高那些药物的生物利用度并改善其药代动力学。本研究旨在通过酸碱沉淀法以纳米晶体形式改善依托考昔的性质。该方法简单、环保,且更倾向于使用非有机溶剂和化学品,从而克服了剂型开发中的挑战。针对稳定剂类型和浓度、药物用量、匀化时间和速度等多个因素对制备的纳米晶体进行了优化。对优化后的纳米晶体配方进行了傅里叶变换红外光谱(FT-IR)、差示扫描量热法(DSC)、X射线衍射和透射电子显微镜(TEM)表征。结果表明成功制备了依托考昔纳米晶体,其平均粒径为210.30±10.20 nm,多分散指数(PDI)为0.277±0.01,zeta电位为-74.10±0.61 mV。TEM成像显示纳米颗粒呈规则的立方体形,表明形态均匀且与辅料相容。溶解度研究表明,与纯药物(87.70±1.41 μg/mL)相比,依托考昔纳米晶体的水溶解度显著提高(137.75±1.34 μg/mL)。此外,纳米晶体表现出快速溶解特性,在5分钟内药物释放率达到91.49±0.01%。这些结果表明,使用纳米晶体来提高低溶解度药物的水溶解度和溶出度是一种潜在策略。