Fan Fan, Zhou Feng, Zhang Jiayu, Yang Junhui, Zhuang Kai, Shan Yudong, Jiang Lei, Zhang Jiantao
Laboratory of Advanced Theranostic Materials and Technology, Ningbo Institute of Materials Technology and Engineering, Chinese Academy of Sciences, Ningbo, 315201, China.
Ningbo Cixi Institute of Biomedical Engineering, Cixi, 315300, China.
AAPS PharmSciTech. 2025 Jan 29;26(1):47. doi: 10.1208/s12249-025-03041-7.
Amorphous solid dispersion (ASD) is one of the most studied strategies for improving the dissolution performance of poorly water-soluble drugs, but ASDs often have low drug loadings, thereby necessitating larger dosage sizes. This study intended to create Soluplus® (SOL)-based microparticle ASDs with high drug loading (up to 60 w/w%) and long-term stability (at least 16 months) using electrospraying to enhance the dissolution of poorly water-soluble celecoxib (CEL). X-ray diffraction (XRD) and differential scanning calorimetry (DSC) analyses showed that the electrosprayed SOL-CEL microparticles were amorphous, and Fourier transform infrared spectroscopy (FTIR) data indicated the presence of hydrogen bonding between SOL and CEL in the microparticles, which helped stabilize the ASDs. In vitro dissolution studies demonstrated that these ASDs improved the CEL dissolution rate by up to 8.2-fold compared to the crystalline form. Electrospraying presents a promising alternative to conventional methods like hot-melt extrusion (HME) and spraying drying (SD) for the production of ASDs, providing simplicity, high drug loading capability and long-term stability, thus catering to a variety of poorly water-soluble drugs.
无定形固体分散体（ASD）是改善难溶性药物溶解性能研究最多的策略之一，但ASD的药物载量往往较低，因此需要更大的剂量。本研究旨在通过电喷雾法制备基于Solupuls®（SOL）的高载药量（高达60 w/w%）和长期稳定性（至少16个月）的微粒型ASD，以提高难溶性塞来昔布（CEL）的溶出度。X射线衍射（XRD）和差示扫描量热法（DSC）分析表明，电喷雾制备的SOL-CEL微粒为无定形，傅里叶变换红外光谱（FTIR）数据表明微粒中SOL和CEL之间存在氢键，这有助于稳定ASD。体外溶出度研究表明，与结晶形式相比，这些ASD将CEL的溶出速率提高了8.2倍。对于ASD的生产，电喷雾是热熔挤出（HME）和喷雾干燥（SD）等传统方法的一种有前景的替代方法，具有操作简单、高载药能力和长期稳定性等优点，因此适用于多种难溶性药物。
