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Nano Research 2019, 12(2): 421-428 https://doi.org/10.1007/s12274-018-2233-3
Research Article | Issue | Published: 08 November 2018

Optimized in vivo performance of acid-liable micelles for the treatment of rheumatoid arthritis by one single injection

Show Author's Information Qin Wang§,  Yan Li§,  Xiaoyan Chen,  Hao Jiang,  Zhirong Zhang,  Xun Sun( )
Key Laboratory of Drug Targeting and Drug Delivery Systems,Ministry of Education, West China School of Pharmacy, Sichuan University,Chengdu,610041,China;

§ Qin Wang and Yan Li contributed equally to this work.

Keywords:
micelles, rheumatoid arthritis, pH-responsive, dexamethasone
Topics:
Controlled drug deliveryDiseasesTargeted drug delivery
Cite this article:
Wang Q, Li Y, Chen X, et al. Optimized in vivo performance of acid-liable micelles for the treatment of rheumatoid arthritis by one single injection. Nano Research, 2019, 12(2): 421-428. https://doi.org/10.1007/s12274-018-2233-3
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Abstract Full text Electronic supplementary material About this article

Current therapeutic limitations existed in effective treatment of rheumatoid arthritis (RA) have motivated numerous researches on finding new strategies. Regarding to the non-targeted distribution and uncontrollable in vivo performance which hinder the effective treatment for RA, we designed an acid-responsive polymeric micelle formulation by attaching the dexamethasone (Dex) to the side chains of a wheat-like polyethylene glycol (PEG) derivate via a hydrazone linker. The self-assembly micelles with the diameter around 50 nm could passively migrate to inflamed sites. The presence of hydrazone linkers avoided the drug leakage in circulation and ensured the preferential release in acidic arthritic joints. Here, we evaluated how the polymer-drug micelles with different density of drug payloads influenced the release pattern, pharmacokinetics and biodistribution, as well as the most importantly, the duration of the therapeutic efficacy. Our exploration would offer the chemical and structural basis for designing and optimizing the nanocarriers for enhanced therapeutic efficacy.


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Electronic supplementary material
About this article

Optimized in vivo performance of acid-liable micelles for the treatment of rheumatoid arthritis by one single injection

Show Author's information Qin Wang§, Yan Li§, Xiaoyan Chen, Hao Jiang, Zhirong Zhang, Xun Sun( )
Key Laboratory of Drug Targeting and Drug Delivery Systems,Ministry of Education, West China School of Pharmacy, Sichuan University,Chengdu,610041,China;

§ Qin Wang and Yan Li contributed equally to this work.

Abstract

Current therapeutic limitations existed in effective treatment of rheumatoid arthritis (RA) have motivated numerous researches on finding new strategies. Regarding to the non-targeted distribution and uncontrollable in vivo performance which hinder the effective treatment for RA, we designed an acid-responsive polymeric micelle formulation by attaching the dexamethasone (Dex) to the side chains of a wheat-like polyethylene glycol (PEG) derivate via a hydrazone linker. The self-assembly micelles with the diameter around 50 nm could passively migrate to inflamed sites. The presence of hydrazone linkers avoided the drug leakage in circulation and ensured the preferential release in acidic arthritic joints. Here, we evaluated how the polymer-drug micelles with different density of drug payloads influenced the release pattern, pharmacokinetics and biodistribution, as well as the most importantly, the duration of the therapeutic efficacy. Our exploration would offer the chemical and structural basis for designing and optimizing the nanocarriers for enhanced therapeutic efficacy.

Keywords: micelles, rheumatoid arthritis, pH-responsive, dexamethasone

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Publication history
Copyright
Acknowledgements

Publication history

Received: 07 July 2018
Revised: 09 October 2018
Accepted: 19 October 2018
Published: 08 November 2018
Issue date: February 2019

Copyright

© Tsinghua University Press and Springer-Verlag GmbH Germany, part of Springer Nature 2018

Acknowledgements

Acknowledgements

We acknowledge financial support from the National Natural Science Foundation of China (No. 81673362).

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