Structural Deformation of MTX Induced by Nanodrug Conjugation Dictate Intracellular Drug Transport and Drug Efficacy

Jun-Young Park,1 Ja-Shil Hyun,2 Jun-Goo Jee,3 Sung Jean Park,2 Dongwoo Khang1,4 1Lee Gil Ya Cancer and Diabetes Institute, Gachon University, Incheon, 21999, Republic of Korea; 2College of Pharmacy and Gachon Institute of Pharmaceutical Sciences, Gachon University, Incheon, 21936, Republic of Korea;...

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Autores principales:	Park JY, Hyun JS, Jee JG, Park SJ, Khang D
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2021
Materias:	structural deformation methotrexate covalent conjugation rheumatoid arthritis carbon nanotube Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/0c83161aa49d4c5587dbdb1b64497218
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spelling	oai:doaj.org-article:0c83161aa49d4c5587dbdb1b644972182021-12-02T14:47:59ZStructural Deformation of MTX Induced by Nanodrug Conjugation Dictate Intracellular Drug Transport and Drug Efficacy1178-2013https://doaj.org/article/0c83161aa49d4c5587dbdb1b644972182021-07-01T00:00:00Zhttps://www.dovepress.com/structural-deformation-of-mtx-induced-by-nanodrug-conjugation-dictate--peer-reviewed-fulltext-article-IJNhttps://doaj.org/toc/1178-2013Jun-Young Park,1 Ja-Shil Hyun,2 Jun-Goo Jee,3 Sung Jean Park,2 Dongwoo Khang1,4 1Lee Gil Ya Cancer and Diabetes Institute, Gachon University, Incheon, 21999, Republic of Korea; 2College of Pharmacy and Gachon Institute of Pharmaceutical Sciences, Gachon University, Incheon, 21936, Republic of Korea; 3Research Institute of Pharmaceutical Sciences, College of Pharmacy, Kyungpook National University, Daegu, 41566, Republic of Korea; 4Department of Physiology, College of Medicine, Gachon University, Incheon, 21999, Republic of KoreaCorrespondence: Dongwoo KhangDepartment of Physiology, College of Medicine, Gachon University, Incheon, 21999, South KoreaTel +82-32-899-6515Email dkhang@gachon.ac.krSung Jean ParkCollege of Pharmacy and Gachon Institute of Pharmaceutical Sciences, Gachon University, Incheon, 21936, Republic of KoreaTel +82-32-899-6113Email psjnmr@gachon.ac.krBackground: Understanding structural interactions between the active drug and conjugated nanoparticles is critical for optimizing intracellular drug transport and for increasing nano drug efficacy. In this regard, analyzing the conformational deformation of conjugated drugs surrounding nanoparticles is essential to understand the corresponding nanodrug efficacy.Purpose: The objective of this study is to present an optimal synthesis method for efficient drug delivery through a clear structural analysis of nanodrugs according to the type of conjugation.Methods and Results: In this study, the structural variation of methotrexate (MTX) surrounding carbon nanotubes, depending on the type of conjugation style, such as covalent and non-covalent (PEGylation) bonds, was investigated. Specifically, covalent bonds of MTX surrounding CNTs induced greater structural deformation compared to non-covalent bonds (ie, PEGylated CNT).Conclusion: Greater changes in the structural variations of MTX analyzed by nuclear magnetic resonance (NMR) significantly improved the anti-inflammatory drug efficacy of human fibroblast-like synovial cells (FLS) via stable drug release in the extracellular environment and burst drug release under intracellular conditions.Keywords: structural deformation, methotrexate, covalent conjugation, rheumatoid arthritis, carbon nanotubePark JYHyun JSJee JGPark SJKhang DDove Medical Pressarticlestructural deformationmethotrexatecovalent conjugationrheumatoid arthritiscarbon nanotubeMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 16, Pp 4943-4957 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	structural deformation methotrexate covalent conjugation rheumatoid arthritis carbon nanotube Medicine (General) R5-920
spellingShingle	structural deformation methotrexate covalent conjugation rheumatoid arthritis carbon nanotube Medicine (General) R5-920 Park JY Hyun JS Jee JG Park SJ Khang D Structural Deformation of MTX Induced by Nanodrug Conjugation Dictate Intracellular Drug Transport and Drug Efficacy
description	Jun-Young Park,1 Ja-Shil Hyun,2 Jun-Goo Jee,3 Sung Jean Park,2 Dongwoo Khang1,4 1Lee Gil Ya Cancer and Diabetes Institute, Gachon University, Incheon, 21999, Republic of Korea; 2College of Pharmacy and Gachon Institute of Pharmaceutical Sciences, Gachon University, Incheon, 21936, Republic of Korea; 3Research Institute of Pharmaceutical Sciences, College of Pharmacy, Kyungpook National University, Daegu, 41566, Republic of Korea; 4Department of Physiology, College of Medicine, Gachon University, Incheon, 21999, Republic of KoreaCorrespondence: Dongwoo KhangDepartment of Physiology, College of Medicine, Gachon University, Incheon, 21999, South KoreaTel +82-32-899-6515Email dkhang@gachon.ac.krSung Jean ParkCollege of Pharmacy and Gachon Institute of Pharmaceutical Sciences, Gachon University, Incheon, 21936, Republic of KoreaTel +82-32-899-6113Email psjnmr@gachon.ac.krBackground: Understanding structural interactions between the active drug and conjugated nanoparticles is critical for optimizing intracellular drug transport and for increasing nano drug efficacy. In this regard, analyzing the conformational deformation of conjugated drugs surrounding nanoparticles is essential to understand the corresponding nanodrug efficacy.Purpose: The objective of this study is to present an optimal synthesis method for efficient drug delivery through a clear structural analysis of nanodrugs according to the type of conjugation.Methods and Results: In this study, the structural variation of methotrexate (MTX) surrounding carbon nanotubes, depending on the type of conjugation style, such as covalent and non-covalent (PEGylation) bonds, was investigated. Specifically, covalent bonds of MTX surrounding CNTs induced greater structural deformation compared to non-covalent bonds (ie, PEGylated CNT).Conclusion: Greater changes in the structural variations of MTX analyzed by nuclear magnetic resonance (NMR) significantly improved the anti-inflammatory drug efficacy of human fibroblast-like synovial cells (FLS) via stable drug release in the extracellular environment and burst drug release under intracellular conditions.Keywords: structural deformation, methotrexate, covalent conjugation, rheumatoid arthritis, carbon nanotube
format	article
author	Park JY Hyun JS Jee JG Park SJ Khang D
author_facet	Park JY Hyun JS Jee JG Park SJ Khang D
author_sort	Park JY
title	Structural Deformation of MTX Induced by Nanodrug Conjugation Dictate Intracellular Drug Transport and Drug Efficacy
title_short	Structural Deformation of MTX Induced by Nanodrug Conjugation Dictate Intracellular Drug Transport and Drug Efficacy
title_full	Structural Deformation of MTX Induced by Nanodrug Conjugation Dictate Intracellular Drug Transport and Drug Efficacy
title_fullStr	Structural Deformation of MTX Induced by Nanodrug Conjugation Dictate Intracellular Drug Transport and Drug Efficacy
title_full_unstemmed	Structural Deformation of MTX Induced by Nanodrug Conjugation Dictate Intracellular Drug Transport and Drug Efficacy
title_sort	structural deformation of mtx induced by nanodrug conjugation dictate intracellular drug transport and drug efficacy
publisher	Dove Medical Press
publishDate	2021
url	https://doaj.org/article/0c83161aa49d4c5587dbdb1b64497218
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_version_	1718389491627982848

Structural Deformation of MTX Induced by Nanodrug Conjugation Dictate Intracellular Drug Transport and Drug Efficacy

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