Preparation and characterization of nintedanib nano-liposomes

Le RAO; Mengyu GUO; Guogang XU

doi:10.16016/j.2097-0927.202402025

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Preparation and characterization of nintedanib nano-liposomes

Pharmacy | 更新时间：2026-01-09

- Preparation and characterization of nintedanib nano-liposomes
- Journal of Army Medical University Vol. 46, Issue 14, Pages: 1695-封三(2024)
- 作者机构：
  
  1.100853 北京，解放军总医院第二医学中心健康医学科
  2.100190 北京，国家纳米科学中心，中国科学院纳米生物效应与安全性重点实验室
- 作者简介：
- 基金信息：
  
  the General Program of National Natural Science Foundation of China(82341089);the General Program of National Natural Science Foundation of China(82370083);the National Natural Science Foundation for Young Scholars of China(82200091)
- DOI：10.16016/j.2097-0927.202402025
  CLC： R944;R961;R977.3
- Received：05 February 2024，
  
  Revised：2024-03-14，
  
  Published：30 July 2024
- 稿件说明：
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Le RAO, Mengyu GUO, Guogang XU. Preparation and characterization of nintedanib nano-liposomes[J]. Journal of Army Medical University, 2024, 46(14): 1695-封三.
DOI：

Le RAO, Mengyu GUO, Guogang XU. Preparation and characterization of nintedanib nano-liposomes[J]. Journal of Army Medical University, 2024, 46(14): 1695-封三. DOI： 10.16016/j.2097-0927.202402025.

摘要

目的

探讨4种不同方法制备尼达尼布脂质体的关键理化特性，筛选出尼达尼布脂质体的最佳制备方法。

方法

采用薄膜分散法、逆向蒸发法、乙醇注入法和改良版乙醇注入法制备尼达尼布脂质体；利用透析法测定尼达尼布脂质体的包封率，并进行粒径大小、分散性、表面电位和形貌表征，在室温放置7 d后评估其稳定性。

结果

薄膜分散法、逆向蒸发法、乙醇注入法和改良版乙醇注入法均制备了类圆形尼达尼布脂质体，粒径大小分别为(285.1±12.3)、(271.4±5.9)、(226.3±14.8)、(197.2±11.2)nm；包封率分别为(15.82±1.26)%、(16.71±1.35)%、(25.12±3.21)%和(32.5±3.61)%；与其他3种方法相比，改良版乙醇注入法制备尼达尼布脂质体粒径大小显著减小，包封率显著增加(

＜0.05)。室温放置7 d后，薄膜分散法和逆向蒸发法粒径明显增大(

＜0.01)，乙醇注入法和改良版乙醇注入法粒径大小无明显差异(

0.05)。

结论

改良版乙醇注入法制备的尼达尼布脂质体关键理化特性表现优异，可作为制备尼达尼布脂质体的优选方法。

Abstract

Objective

To investigate the key physical and chemical properties of nintedanib liposomes prepared by 4 different methods in order to screen out the best preparation method of nintedanib liposomes.

Methods

Firstly

nintedanib liposomes were prepared by thin film dispersion

reverse evaporation

ethanol injection and modified ethanol injection

respectively. The entrapment efficiency of nintedanib liposomes was then determined by dialysis and characterized for particle size

dispersibility

surface potential

and morphology. Their stability was evaluated after being placed at room temperature for 7 d.

Results

Circular nintedanib liposomes were respectively prepared by thin film dispersion

reverse evaporation

ethanol injection and modified ethanol injection

with a particle size of (285.1±12.3)

(271.4±5.9)

(226.3±14.8) and (197.2±11.2) nm

an enca

psulation rate of (15.82±1.26)%

(16.71±1.35)%

(25.12±3.21)% and (32.5±3.61)%

respectively. The nintedanib liposomes prepared by modified ethanol injection had significantly smallest particle size and highest encapsulation efficiency than the liposomes by the other 3 methods (

0.05). In 7 d after being placed at room temperature

the particle sizes of the liposomes prepared by film dispersion and reverse evaporation were increased notably (

0.01)

but no such change was observed in the liposomes prepared by ethanol injection and modified ethanol injection (

0.05).

Conclusion

Nintedanib liposomes prepared by modified ethanol injection have excellent key physical and chemical properties

and this method is an optical one for preparing nintedanib liposomes.

关键词

Keywords

references

PELJTO A L, BLUMHAGEN R Z, WALTS A D, et al . Idiopathic pulmonary fibrosis is associated with common genetic variants and limited rare variants[J ] . Am J Respir Crit Care Med, 2023, 207(9): 1194-1202. DOI: 10.1164/rccm.202207-1331OC.

RAJAN S K, COTTIN V, DHAR R, et al . Progressive pulmonary fibrosis: an expert group consensus statement[J ] . Eur Respir J, 2023, 61(3): 2103187. DOI: 10.1183/13993003.03187-2021.

SPAGNOLO P, KROPSKI J A, JONESM G, et al . Idiopathic pulmonary fibrosis: Disease mechanisms and drug development[J ] . Pharmacol Ther, 2021, 222: 107798. DOI: 10.1016/j.pharmthera.2020.107798.

GHAZIPURA M, MAMMEN M J, HERMAN DD, et al . Nintedanib in progressive pulmonary fibrosis: a syste matic review and meta-analysis[J ] . Ann Am Thorac Soc, 2022, 19(6): 1040-1049. DOI: 10.1513/AnnalsATS.202103-343OC.

TOMIOKA H, IWABAYASHI M, YOKOTA M, et al . Weight loss in nintedanib-treated patients with idiopathic pulmonary fibrosis[J ] . Pulm Pharmacol Ther, 2023, 80: 102213. DOI: 10.1016/j.pupt.2023.102213.

BARTHOLD S, KUNSCHKE N, MURGIA X, et al . Overview of inhaled nanopharmaceuticals[J ] . J Aerosol Med Pulm Drug Deliv, 2023, 36(3): 144-151. DOI: 10.1089/jamp.2023.29089.sb.

FU L Y, ZHANG Y, FAROKHZAD R A, et al . 'Passive' nanoparticles for organ-selective systemic delivery: design, mechanism and perspective[J ] . Chem Soc Rev, 2023, 52(21): 7579-7601. DOI: 10.1039/d2cs00998f.

LI D J, ZHAO A, ZHU J F, et al . Inhaled lipid nanoparticles alleviate established pulmonary fibrosis[J ] . Small, 2023, 19(30): e2300545. DOI: 10.1002/smll.202300545.

ZHAO J, QIN L, SONG R X, et al . Elucidating inhaled liposome surface charge on its interaction with biological barriers in the lung[J ] . Eur J Pharm Biopharm, 2022, 172: 101-111. DOI: 10.1016/j.ejpb.2022.01.0 09.

WANG J, LI P Y, YU Y, et al . Pulmonary surfactant-biomimetic nanoparticles potentiate heterosubtypic influenza immunity[J ] . Science, 2020, 367(6480): eaau0810. DOI: 10.1126/science.aau0810.

PRAPHAWATVET T, PETERS J I, WILLIAMS R O 3rd. Inhaled nanoparticles-An updated review[J]. Int J Pharm, 2020, 587: 119671. DOI: 10.1016/j.ijpharm.2020.119671.

WANG Z, XIANG L, LIN F, et al . Inhaled ACE2-engineered microfluidic microsphere for intratracheal neutralization of COVID-19 and calming of the cytokine storm[J ] . Matter, 2022, 5(1): 336-362. DOI: 10.1016/j.matt.2021.09.022.

GANDHI S, SHASTRI D H. Lipid-based nanoparticulate drug delivery[J]. Pharm Nanotechnol, 2024, 12: 1-26. DOI: 10.2174/0122117385275514231127062730.

HE H S, LU Y, QI J P, et al . Adapting liposomes for oral drug delivery[J ] . Acta Pharm Sin B, 2019, 9(1): 36-48. DOI: 10.1016/j.apsb.2018.06.005.

GUIMARAES D, CAVACO-PAULO A, NOGUEIRA E. Design of liposomes as drug delivery system for therapeutic applications[J]. Int J Pharm, 2021, 601: 120571. DOI: 10.1016/j.ijpharm.2021.120571.

CHOUDHARY M, CHAURAWAL N, BARKAT M A, et al . Proliposome-based nanostrategies: challenges and development as drug delivery systems[J ] . AAPS Pharm Sci Tech, 2022, 23(8): 293. DOI: 10.1208/s12249-022-02443-1.

MARITIM S, BOULAS P, LIN Y Q. Comprehensive analysis of liposome formulation parameters and their influence on encapsulation, stability and drug release in glibenclamide liposomes[J]. Int J Pharm, 2021, 592: 120051. DOI: 10.1016/j.ijpharm.2020.120051.

DADPOUR S, MEHRABIAN A, ARABSALMANI M, et al . The role of size in PEGylated liposomal doxorubicin biodistribution and anti-tumour activity[J ] . IET Nanobiotechnol, 2022, 16(7/8): 259-272. DOI: 10.1049/nbt2.12094.

WANG X, LIU M, LUTZ H, et al . Exosomes decorated with a recombinant SARS-CoV-2 receptor-binding domain as an inhalable COVID-19 vaccine[J ] . Nat Biomed Eng., 2022, 6(7): 791-805. DOI: 10.1038/s41551-022-00902-5.

BIAN J, GIROTTI J, FAN Y C, et al . Fast and versatile analysis of liposome encapsulation efficiency by nanoParticle exclusion chromatography[J ] . J Chromatogr A, 2022, 1662: 462688. DOI: 10.1016/j.chroma.2021.462688.

WU Z, GUAN R, LYN F, et al . Optimization of preparation conditions for lysozyme nanoliposomes using response surface methodology and evaluation of their stability[J ] . Molecules, 2016, 21(6): 741. Doi: 10.3390/molecules21060741.

ZHANG X, WU Z, ZHANG W, et al . Surface modification by chitosan for improving stability and antioxidative activity of astaxanthin-loaded liposomes[J ] , LWT, 2024, 198: 116033, DOI: 10.1016/j.lwt.2024.116033.

SANKET S, VIVEK D, RENE H, et al . Liposomes: Advancements and innovation in the manufacturing process[J ] , Adv Drug Deliv Rev. 2020, 154-155: 102-122. DOI: 10.1016/j.addr.2020.07.002.

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