Istinye University, Faculty of Pharmacy, Department of Pharmaceutical Technology, Zeytinburnu, 34010, Istanbul, Turkey.
Istinye University, Faculty of Health Sciences, Department of Stem Cell and Tissue Engineering, Zeytinburnu, 34010, Istanbul, Turkey.
AAPS PharmSciTech. 2024 Sep 17;25(7):218. doi: 10.1208/s12249-024-02938-z.
This research aims to produce orodispersible films (ODFs) and determine their potential use in the oral delivery of montelukast sodium for asthma treatment and allergic rhinitis. ODFs were successfully developed by Three-dimensional (3D) printing using propylene glycol (PG), and hydroxypropyl methylcellulose (HPMC), polyethylene glycol 400 (PEG). Finally, the amount of montelukast sodium in the ODFs was 5% (w/w). Drug-excipients compatibility with Fourier Transformed Infrared (FTIR) spectroscopy, mass uniformity, thickness, disintegration time, folding endurance, moisture absorption, pH, in vitro drug release (dissolution), drug content, moisture loss, moisture content, mechanical properties, and cytotoxicity studies were performed on the prepared films. All formulations disintegrated in approximately 40 s. Over 98% of drug release from all films within 2 min was confirmed. It was reported that Fm1-4 (8% HPMC and 1% PEG) and Fm2-4 (10% HPMC and 3% PEG) are more suitable for drug content, but Fm2-4 may be the ideal formulation considering its durability and transportability properties. Based on the characterization results and in vitro release values, the montelukast sodium ODF can be an option for other dosage forms. It was concluded that the formulations did not show toxic potential by in vitro cytotoxicity study with 3T3 cells. This new formulation can efficiently treat allergic rhinitis and asthma diseases.
本研究旨在制备口崩片(ODF)并确定其在口服递药系统中应用于孟鲁司特钠治疗哮喘和变应性鼻炎的潜力。采用 3D 打印技术,以丙二醇(PG)和羟丙基甲基纤维素(HPMC)、聚乙二醇 400(PEG)成功制备了 ODF。最终,ODF 中孟鲁司特钠的含量为 5%(w/w)。对 ODF 进行了药物-赋形剂相容性、傅里叶变换红外(FTIR)光谱、质量均匀性、厚度、崩解时间、耐折性、吸湿性、pH 值、体外药物释放(溶出度)、药物含量、水分损失、水分含量、机械性能和细胞毒性研究。所有配方在大约 40 秒内崩解。确认所有薄膜在 2 分钟内释放超过 98%的药物。报道称,Fm1-4(8%HPMC 和 1%PEG)和 Fm2-4(10%HPMC 和 3%PEG)更适合药物含量,但考虑到其耐用性和可运输性,Fm2-4 可能是理想的配方。基于表征结果和体外释放值,孟鲁司特钠 ODF 可以作为其他剂型的选择。体外细胞毒性研究表明,该配方对 3T3 细胞无潜在毒性。这种新配方可以有效治疗变应性鼻炎和哮喘疾病。