口服吸入达科米替尼纳米载体作为非小细胞肺癌的治疗策略。

IF 3.9 Nanomedicine (London, England) Pub Date : 2024-01-01 Epub Date: 2024-07-29 DOI:10.1080/17435889.2024.2370225
Druva Sarika Rongala, Suyash M Patil, Nitesh K Kunda
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引用次数: 0

摘要

背景:开发一种可吸入的纳米制剂,将达科替尼(DMB)封装在聚(乳酸-共-乙醇酸)纳米颗粒(NPs)中,以提高溶解度、促进直接肺部给药并克服全身不良反应。研究方法采用溶剂蒸发法制备了负载 DMB 的聚(乳酸-共聚-乙醇酸)NPs,并对其粒度、多分散指数和 zeta 电位进行了表征。对 NPs 的体外药物释放、气溶胶性能和体外药效研究进行了评估。结果显示NPs 表现出优异的颗粒特性,5 天内的累积释放量达到 40%。NPs 的质量中值气动直径为 ∼3 μm,细颗粒比例为 ∼80%。此外,体外细胞培养研究表明,与游离药物相比,负载 DMB 的 NPs 具有更好的细胞毒性潜力。结论该研究强调了 DMB 负载 NPs 作为治疗非小细胞肺癌的一种可行方法的潜力。
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Oral inhalation of dacomitinib nanocarriers as a therapeutic strategy for non-small cell lung cancer.

Background: 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.Methods: 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 in vitro drug release, aerosolization performance and in vitro efficacy studies.Results: 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, in vitro cell culture studies showed improved cytotoxic potential of DMB-loaded NPs compared with free drug.Conclusion: The study underscores the potential of DMB-loaded NPs as a viable approach for non-small cell lung cancer treatment.

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