叶酸靶向多西紫杉醇纳米肺吸入粉雾剂的制备及评价

中国临床药理学与治疗学 ›› 2017, Vol. 22 ›› Issue (5): 495-500.

叶酸靶向多西紫杉醇纳米肺吸入粉雾剂的制备及评价

朱晓婕，孔颖，刘琦，卢杨，赵娣，李宁，陈西敬

中国药科大学基础医学与临床药学院，南京 211198，江苏

收稿日期:2017-03-17 修回日期:2017-04-18 出版日期:2017-05-26 发布日期:2017-05-27
通讯作者: 陈西敬，男，博士，教授，博士生导师，研究方向：药物代谢动力学。 Tel: 025-86185379 E-mail: chenxj-lab@hotmail.com
作者简介:朱晓婕，女，硕士研究生，研究方向：药物代谢动力学。 E-mail:njzhuxiaojie@163.com
基金资助:
国家自然科学基金项目（81473272；81503148）

Preparation and evaluation of inhaled dry powders based on folic acid-conjugated Docetaxel nanoparticles

ZHU Xiaojie, KONG Ying, LIU Qi, LU Yang, ZHAO Di, LI Ning, CHEN Xijing

School of Basic Medicine and Clinical Pharmacy, China Pharmaceutical University, Nanjing 211198，Jiangsu，China

Received:2017-03-17 Revised:2017-04-18 Online:2017-05-26 Published:2017-05-27

摘要/Abstract

摘要：

目的: 制备基于叶酸靶向多西紫杉醇纳米粒的肺吸入粉雾剂，用于肺癌的治疗。方法: 采用有机溶剂挥发法制备叶酸靶向纳米粒，考察纳米粒理化性质，溴化噻唑蓝四氮唑（MTT）实验法研究纳米粒的体外细胞毒性和肿瘤细胞叶酸靶向性，使用喷雾干燥技术进一步制备基于纳米粒的肺吸入粉雾剂，并考察其理化性质。结果: 本实验制备的叶酸靶向纳米粒粒径为（100.1±1.0） nm，普通纳米粒组IC50为（2.09±0.82） μmol/L，叶酸靶向纳米粒组IC50为（0.80±0.32） μmol/L。肺吸入粉雾剂体外沉积率和休止角分别为（21.10±0.18）%和（36.75±0.52）°。结论: 成功制备了基于叶酸靶向纳米粒的肺吸入粉雾剂，肺部吸入抗癌药物直达病灶部位，主动靶向肺癌细胞，提高靶器官药物浓度，降低毒副作用，提高患者的顺应性，满足临床肺癌治疗所需。

关键词: 多西紫杉醇, 纳米粒, 肺吸入粉雾剂

Abstract:

AIM: To prepare docetaxel-loaded folic acid-conjugated nanoparticles (NPs-DTX-FA) for the treatment of lung cancer. METHODS: The NPs-DTX-FA were prepared by the solvent evaporation method and the nanoparticles (NPs) were then co-spray dried with excipients to obtain inhaled dry powders. The physiochemical properties of NPs and inhaled dry powders were evaluated. MTT assay was employed to study the cytotoxicity and tumor-targeting property of the NPs. RESULTS:The diameter of LPs-DTX-FA was （100.1±1.0） nm, the IC50for NPs-DTX and NPs-DTX-FA were （2.09±0.82） μmol/L and （0.80±0.32） μmol/L, respectively. The fine particle fraction (FPF) and angle of repose (θ) of the inhaled dry powders were （21.10±0.18）% and （36.75±0.52）°, respectively. CONCLUSION: The preparation of NPs-DTX-FA based inhaled dry powders was successful and this formulation represented a possibility of clinical application by achieving higher anti-cancer activity in tumor site and lower damage to healthy organs.

Key words: docetaxel, nanoparticle, dry powder inhalation

中图分类号:

R965.2

朱晓婕，孔颖，刘琦，卢杨，赵娣，李宁，陈西敬. 叶酸靶向多西紫杉醇纳米肺吸入粉雾剂的制备及评价[J]. 中国临床药理学与治疗学, 2017, 22(5): 495-500.

ZHU Xiaojie, KONG Ying, LIU Qi, LU Yang, ZHAO Di, LI Ning, CHEN Xijing . Preparation and evaluation of inhaled dry powders based on folic acid-conjugated Docetaxel nanoparticles[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2017, 22(5): 495-500.

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