Innovative inhalable dry powder: nanoparticles loaded with Crizotinib for targeted lung cancer therapy.

IF 3.4 2区 医学 Q2 ONCOLOGY
Faiza Naureen, Yasar Shah, Maqsood Ur Rehman, Fazli Nasir Fazli Nasir, Abdul Saboor Pirzada, Jamelah Saleh Al-Otaibi, Maria Daglia, Haroon Khan
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引用次数: 0

Abstract

Crizotinib is a targeted therapy for metastatic non-small cell lung cancer (NSCLC) that is ALK- or ROS1-positive, as well as for conditions such as ALK-positive anaplastic large cell lymphoma and inflammatory myofibroblastic tumor. However, the associated toxicity poses a significant challenge to its use. To mitigate this issue, a novel dry powder inhalation formulation was developed using Crizotinib-loaded polyethylene glycol-based polymeric nanoparticles (NPs). These nanoparticles were created through a nanoprecipitation approach and improved employing central composite design. The capabilities of the formulation were assessed with Anderson Cascade Impactor, revealing a fine particle fraction of 56.2% and a mass median aerodynamic diameter of around 1.5 μm, indicating appropriate aerodynamic characteristics for inhalation. Key properties of the optimized nanoparticles included Encapsulation efficiency (82.3%, Zeta potential (-31.9 mV), Particle size (167 nm), Polydispersity index (0.462) and Release efficiency (60.6%) In vitro studies indicated that the polymeric nanoparticles exhibited greater anticancer activity compared to free Crizotinib. Additional characterization using techniques like XRD, DSC, FTIR, and SEM confirmed that the polymeric nanoparticle formulation has promising physicochemical properties, suggesting it could enhance local drug delivery and efficacy in lung cancer treatment while potentially reducing systemic toxicity.

创新的可吸入干粉:纳米颗粒载克唑替尼靶向肺癌治疗。
克唑替尼是一种靶向治疗ALK-或ros1阳性的转移性非小细胞肺癌(NSCLC),以及ALK阳性间变性大细胞淋巴瘤和炎症性肌纤维母细胞瘤等疾病。然而,相关的毒性对其使用构成了重大挑战。为了缓解这一问题,研究人员开发了一种新型干粉吸入制剂,该制剂使用了含有克唑替尼的聚乙二醇基聚合物纳米颗粒(NPs)。这些纳米颗粒是通过纳米沉淀法制造的,并采用中心复合设计进行改进。采用安德森级联冲击器对配方进行了性能评估,细颗粒分数为56.2%,质量气动直径中位数约为1.5 μm,表明该配方具有合适的吸入气动特性。优化后的纳米颗粒的主要性能为包封率(82.3%)、Zeta电位(-31.9 mV)、粒径(167 nm)、多分散指数(0.462)和释放效率(60.6%)。体外研究表明,与游离的克唑替尼相比,聚合物纳米颗粒具有更强的抗癌活性。使用XRD、DSC、FTIR和SEM等技术进行的进一步表征证实,聚合物纳米颗粒配方具有良好的物理化学性质,表明它可以增强局部药物传递和肺癌治疗的有效性,同时潜在地降低全身毒性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
BMC Cancer
BMC Cancer 医学-肿瘤学
CiteScore
6.00
自引率
2.60%
发文量
1204
审稿时长
6.8 months
期刊介绍: BMC Cancer is an open access, peer-reviewed journal that considers articles on all aspects of cancer research, including the pathophysiology, prevention, diagnosis and treatment of cancers. The journal welcomes submissions concerning molecular and cellular biology, genetics, epidemiology, and clinical trials.
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