Preparation, Characterization, and Evaluation of Breviscapine Nanosuspension and Its Freeze-Dried Powder

• Main Authors: Ting Zhang (Author), Xixi Li (Author), Juewen Xu (Author), Jingbao Shao (Author), Meihong Ding (Author), Senlin Shi (Author)
• Formato: Livro
• Publicado em: MDPI AG, 2022-04-01T00:00:00Z.
• Assuntos: article
• Acesso em linha: Connect to this object online.
• Notes: 10.3390/pharmaceutics14050923; 1999-4923
• Keywords: breviscapine; nanosuspension; Box-Behnken design; Pharmacy and materia medica; RS1-441
• Source: Pharmaceutics, Vol 14, Iss 5, p 923 (2022)

As a biopharmaceutics classification system (BCS) class IV drug, breviscapine (Bre) has low solubility in water, poor chemical stability, a short biological half-life and rapid removal from plasma. This paper prepared a Bre nanosuspension (Bre-NS) by an ultrasound-assisted anti-solvent precipitation method. Characterization of Bre-NS was studied using a Box-Behnken design concerning drug concentration in DMSO, an anti-solvent-to-solvent ratio, and sonication time. Under the optimized conditions of 170 mg/mL for the drug concentration, a 1:60 solvent-to-anti-solvent ratio, and a 9 min sonication time, the particle size of Bre-NS was 303.7 ± 7.3 nm, the polydispersity index was 0.178 ± 0.015, and the zeta potential was −31.10 ± 0.26 mV. Combined with the results from differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and Fourier transform-infrared spectroscopy (FT-IR), the findings indicated that the crystal form and chemical structure of Bre-NS did not change during the entire process. The optimized formulation displayed good stability, increased solubility, and better in vitro release. Therefore, the results of this study can be a reference for the delivery system design of insoluble active components and effective parts in traditional Chinese medicine.