Department of Pharmaceutical Engineering & Technology, Indian Institute of Technology (BHU) , Varanasi, India.
Expert Opin Drug Deliv. 2020 Oct;17(10):1459-1472. doi: 10.1080/17425247.2020.1798401. Epub 2020 Aug 13.
Lung cancer and metastases are major concerns worldwide. Although systemic chemotherapy is the recommended treatment, it is associated with various disadvantages, including nonselective drug distribution and systemic toxicity. In contrast, the pulmonary route ensures the localized delivery of drugs to the lung. Still, the pulmonary route is prone to clearance, limited drug dissolution, and local toxicity to healthy lung cells. Drug nanocrystals provide a potential strategy to enhance the therapeutic efficacy and mitigate the limitations of pulmonary delivery.
The development and potential application of nanocrystals in pulmonary delivery, their role in overcoming associated barriers, and strategies for site-specific and stimuli-responsive pulmonary delivery are outlined. This review also traces different pulmonary models for assessments of the performance of drug nanocrystals and nanocrystals loaded carriers in pulmonary delivery.
Enhanced stability, high aerosolization performance, better particle size distribution, improved penetration, sustained release of the drug, and minimal excipients usage makes drug nanocrystal an ideal candidate for pulmonary delivery. Besides, drug nanocrystals may provide selective cellular internalization with minimum clearance and maximum deposition. Furthermore, surface modified nanocrystals and nanocrystals in nanocarriers can exhibit a more prolonged, and site-specific release of the drug to cancer cells in the lungs.
肺癌和转移是全球主要关注的问题。尽管全身化疗是推荐的治疗方法,但它存在各种缺点,包括药物分布的非选择性和全身毒性。相比之下,肺部途径可确保药物局部递送至肺部。然而,肺部途径容易被清除、药物溶解有限,并且对健康肺细胞有局部毒性。药物纳米晶体提供了一种增强治疗效果和减轻肺部递药局限性的潜在策略。
本文概述了纳米晶体在肺部递药中的开发和潜在应用,它们在克服相关障碍方面的作用,以及用于肺部递药的靶向和刺激响应性的策略。本文还追溯了不同的肺部模型,以评估药物纳米晶体和负载纳米晶体的载体在肺部递药中的性能。
增强的稳定性、高雾化性能、更好的粒径分布、改善的穿透性、药物的持续释放以及最小的赋形剂使用,使药物纳米晶体成为肺部递药的理想候选物。此外,药物纳米晶体可能提供最小清除和最大沉积的选择性细胞内化。此外,表面修饰的纳米晶体和纳米载体中的纳米晶体可以使药物在肺部癌细胞中表现出更持久和靶向的释放。