Department of Pharmaceutical Sciences, College of Pharmacy & Health Sciences, St. John's University, Jamaica, NY 11439, USA.
Nanomedicine (Lond). 2024;19(18-20):1601-1613. doi: 10.1080/17435889.2024.2370225. Epub 2024 Jul 29.
Development of an inhalable nanoformulation of dacomitinib (DMB) encapsulated in poly-(lactic-co-glycolic acid) nanoparticles (NPs) to improve solubility, facilitate direct lung delivery and overcome the systemic adverse effects. DMB-loaded poly-(lactic-co-glycolic acid) NPs were prepared using solvent evaporation and characterized for particle size, polydispersity index and zeta-potential. The NPs were evaluated for drug release, aerosolization performance and efficacy studies. The NPs showed excellent particle characteristics and displayed a cumulative release of ∼40% in 5 days. The NPs demonstrated a mass median aerodynamic diameter of ∼3 μm and fine particle fraction of ∼80%. Further, cell culture studies showed improved cytotoxic potential of DMB-loaded NPs compared with free drug. The study underscores the potential of DMB-loaded NPs as a viable approach for non-small cell lung cancer treatment.
研制一种可吸入的、以聚（乳酸-共-乙醇酸）纳米粒为载体的达可替尼（DMB）纳米制剂，以提高其溶解度，便于直接肺部给药，并克服全身不良反应。采用溶剂蒸发法制备载达可替尼的聚（乳酸-共-乙醇酸）纳米粒，并对其粒径、多分散指数和zeta 电位进行了表征。对纳米粒进行了药物释放、雾化性能和疗效研究。纳米粒显示出优异的颗粒特性，在 5 天内累积释放约 40%。纳米粒的质量中值空气动力学直径约为 3μm，细颗粒分数约为 80%。此外，细胞培养研究表明，与游离药物相比，载达可替尼纳米粒具有更高的细胞毒性潜力。该研究强调了载达可替尼纳米粒作为治疗非小细胞肺癌的一种可行方法的潜力。
