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·综述·


          治疗肺部疾病的中药活性成分可吸入纳米给药系统研究进展
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          程方瑞 ,孙 爽,张 欢,李永吉,吕邵娃(黑龙江中医药大学药学院/教育部北药基础与应用研究重点实验室,
          哈尔滨 150040)

          中图分类号  R944      文献标志码  A      文章编号  1001-0408(2024)23-2954-05
          DOI  10.6039/j.issn.1001-0408.2024.23.19


          摘   要  肺部给药能直接将药物运送至肺部,是肺部疾病的优选给药方式。中药活性成分如槲皮素、紫杉醇等对肺部疾病具有良
          好的治疗效果,但其存在水溶性差和肺清除率高等问题。将中药活性成分负载在纳米给药系统中,可提高药物的水溶性、稳定性
          及其在肺部的渗透性和滞留性。基于此,本研究综述了治疗肺部疾病的中药活性成分可吸入纳米给药系统的研究进展,发现有基
          于壳聚糖、脂质(包括脂质体、固体脂质纳米粒、纳米结构脂质载体)、靶向配体(包括靶向叶酸受体、靶向转铁蛋白受体、外泌体)的
          中药活性成分可吸入纳米给药系统,这些纳米给药系统综合考虑了粒径、表面电荷和疏水性等关键因素,可避免药物被黏液、纤毛
          和巨噬细胞清除,具有较好的应用潜力。
          关键词  可吸入纳米给药系统;中药活性成分;肺部疾病


          Research  progress  on  inhalation  nano-drug  delivery  systems  of  active  ingredients  of  traditional  Chinese
          medicine for pulmonary diseases
          CHENG Fangrui,SUN Shuang,ZHANG Huan,LI Yongji,LYU Shaowa(College of Pharmacy/Key Lab for Basis
          and  Application  Research  of  Northern  Medicine  of  Ministry  of  Education,Heilongjiang  University  of  Chinese
          Medicine,Harbin 150040,China)

          ABSTRACT    Pulmonary administration can directly deliver drugs to the lungs, making it the preferred mode of administration for
          pulmonary  disease. Active  ingredients  of  traditional  Chinese  medicine (TCM),  such  as  quercetin  and  paclitaxel  have  demonstrated
          promising therapeutic effects on lung diseases. However, they face challenges such as poor water solubility and high lung clearance
          rates.  Loading  the  active  ingredients  of  TCM  onto  nano-drug  delivery  systems  can  enhance  their  water  solubility,  stability,
          permeability  and  retention  in  the  lungs.  Based  on  this,  this  study  reviewed  the  research  progress  on  inhalation  nano-drug  delivery
          systems for the active ingredients of TCM in the treatment of lung diseases. It was found that there are nano-drug delivery systems
          for  TCM  active  ingredients  based  on  chitosan,  lipids (including  liposomes,  solid  lipid  nanoparticles,  and  nanostructured  lipid
          carriers), and targeting ligands (including targeting folate receptor, targeting transferrin receptor, and exosomes). These inhalation
          nano-drug delivery systems comprehensively consider key factors such as particle size, surface charge, and hydrophobicity, which
          can prevent the drugs from being cleared by mucus, cilium and macrophages, thus exhibiting great potential for application.
          KEYWORDS     inhalation nano-drug delivery systems; active ingredients of traditional Chinese medicine; pulmonary diseases


                                                                                                  [1]
              近年来,肺部疾病的发病率呈上升趋势,严重降低                          药物的分解代谢,提高药物的生物利用度 。尽管槲皮
          了民众生活幸福感。肺部给药作为一种无创给药方式,                            素(quercetin,Qu)、紫杉醇(paclitaxel,PTX)等中药活性
          能直接将药物运送至肺部,以较低的给药剂量获得较高                            成分被证实对肺部疾病具有良好的治疗效果,但因其存
          的局部药物浓度,成为治疗肺部疾病的优选。相较于传                            在水溶性差和肺清除率高等问题,吸入给药的生物利用
          统给药途径,肺部给药可以避免肝脏的首过效应,减少                            度较低   [2―3] 。纳米载体的使用可有效增加药物水溶性和
                                                              稳定性,提高药物在肺部的渗透性和滞留性,为中药活
              Δ 基金项目 黑龙江省“头雁”计划(No.〔2019〕5 号);黑龙江省博           性成分在肺部给药的有效应用提供了一个良好的递送
          士后科研启动金项目(No.LBH-Q21189)                            载体 。基于此,本文综述了肺部疾病应用纳米给药系
                                                                  [4]
             *第一作者 硕士研究生。研究方向:新药研究与开发。E-mail:
                                                              统的机遇和挑战,概述了治疗肺部疾病的中药活性成分
          2108170706@qq.com
                                                              可吸入纳米给药系统的研究进展,以期为肺部疾病的治
              # 通信作者 教授,硕士生导师。研究方向:新药研究与开发。电
          话:0451-87266916。E-mail:lswa5599@hotmail.com         疗提供参考。

          · 2954 ·    China Pharmacy  2024 Vol. 35  No. 23                            中国药房  2024年第35卷第23期
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