Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China.
College of Pharmacy, Jiangsu University, Zhenjiang 212013, China.
Mini Rev Med Chem. 2020;20(13):1258-1271. doi: 10.2174/1389557520666200509235945.
Pulmonary pharmaceutical formulations are targeted for the treatment of respiratory diseases. However, their application is limited due to the physiological characteristics of the lungs, such as branching structure, mucociliary and macrophages, as well as certain properties of the drugs like particle size and solubility. Nano-formulations can ameliorate particle sizes and improve drug solubility to enhance bioavailability in the lungs. The nano-formulations for lungs reviewed in this article can be classified into nanocarriers, no-carrier-added nanosuspensions and polymer-drug conjugates. Compared with conventional inhalation preparations, these novel pulmonary pharmaceutical formulations have their own advantages, such as increasing drug solubility for better absorption and less inflammatory reaction caused by the aggregation of insoluble drugs; prolonging pulmonary retention time and reducing drug clearance; improving the patient compliance by avoiding multiple repeated administrations. This review will provide the reader with some background information for pulmonary drug delivery and give an overview of the existing literature about nano-formulations for pulmonary application to explore nano-strategies for improving the bioavailability of pulmonary pharmaceutical formulations.
肺部药物制剂是针对呼吸系统疾病治疗的靶向制剂。然而,由于肺部的生理特征,如分支结构、黏液纤毛和巨噬细胞,以及药物的某些性质,如粒径和溶解度,它们的应用受到限制。纳米制剂可以改善粒径并提高药物溶解度,从而提高肺部的生物利用度。本文综述了肺部用的纳米制剂,可分为纳米载体、无载体纳米混悬剂和聚合物-药物偶联物。与传统的吸入制剂相比,这些新型肺部药物制剂具有自身的优势,如增加药物溶解度以提高吸收效果和减少不溶性药物聚集引起的炎症反应;延长肺部滞留时间和减少药物清除率;通过避免多次重复给药提高患者顺应性。本文将为读者提供肺部药物传递的一些背景信息,并概述关于肺部应用的纳米制剂的现有文献,以探讨提高肺部药物制剂生物利用度的纳米策略。