APTES monolayer coverage on self-assembled magnetic nanospheres for controlled release of anticancer drug Nintedanib

Abstract The use of an appropriate delivery system capable of protecting, translocating, and selectively releasing therapeutic moieties to desired sites can promote the efficacy of an active compound. In this work, we have developed a nanoformulation which preserves its magnetization to load a model...

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Autores principales:	V. C. Karade, A. Sharma, R. P. Dhavale, S. R. Shingte, P. S. Patil, J. H. Kim, D. R. T. Zahn, A. D. Chougale, G. Salvan, P. B. Patil
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2021
Materias:	Medicine R Science Q
Acceso en línea:	https://doaj.org/article/2086fb8197de4b1cb8a435b01ed131ce
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spelling	oai:doaj.org-article:2086fb8197de4b1cb8a435b01ed131ce2021-12-02T13:33:44ZAPTES monolayer coverage on self-assembled magnetic nanospheres for controlled release of anticancer drug Nintedanib10.1038/s41598-021-84770-02045-2322https://doaj.org/article/2086fb8197de4b1cb8a435b01ed131ce2021-03-01T00:00:00Zhttps://doi.org/10.1038/s41598-021-84770-0https://doaj.org/toc/2045-2322Abstract The use of an appropriate delivery system capable of protecting, translocating, and selectively releasing therapeutic moieties to desired sites can promote the efficacy of an active compound. In this work, we have developed a nanoformulation which preserves its magnetization to load a model anticancerous drug and to explore the controlled release of the drug in a cancerous environment. For the preparation of the nanoformulation, self-assembled magnetic nanospheres (MNS) made of superparamagnetic iron oxide nanoparticles were grafted with a monolayer of (3-aminopropyl)triethoxysilane (APTES). A direct functionalization strategy was used to avoid the loss of the MNS magnetization. The successful preparation of the nanoformulation was validated by structural, microstructural, and magnetic investigations. X-ray photoelectron spectroscopy (XPS) and Fourier transform infrared spectroscopy (FTIR) were used to establish the presence of APTES on the MNS surface. The amine content quantified by a ninhydrin assay revealed the monolayer coverage of APTES over MNS. The monolayer coverage of APTES reduced only negligibly the saturation magnetization from 77 emu/g (for MNS) to 74 emu/g (for MNS-APTES). Detailed investigations of the thermoremanent magnetization were carried out to assess the superparamagnetism in the MNS. To make the nanoformulation pH-responsive, the anticancerous drug Nintedanib (NTD) was conjugated with MNS-APTES through the acid liable imine bond. At pH 5.5, which mimics a cancerous environment, a controlled release of 85% in 48 h was observed. On the other hand, prolonged release of NTD was found at physiological conditions (i.e., pH 7.4). In vitro cytotoxicity study showed dose-dependent activity of MNS-APTES-NTD for human lung cancer cells L-132. About 75% reduction in cellular viability for a 100 μg/mL concentration of nanoformulation was observed. The nanoformulation designed using MNS and monolayer coverage of APTES has potential in cancer therapy as well as in other nanobiological applications.V. C. KaradeA. SharmaR. P. DhavaleR. P. DhavaleS. R. ShingteP. S. PatilJ. H. KimD. R. T. ZahnA. D. ChougaleG. SalvanP. B. PatilNature PortfolioarticleMedicineRScienceQENScientific Reports, Vol 11, Iss 1, Pp 1-12 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine R Science Q
spellingShingle	Medicine R Science Q V. C. Karade A. Sharma R. P. Dhavale R. P. Dhavale S. R. Shingte P. S. Patil J. H. Kim D. R. T. Zahn A. D. Chougale G. Salvan P. B. Patil APTES monolayer coverage on self-assembled magnetic nanospheres for controlled release of anticancer drug Nintedanib
description	Abstract The use of an appropriate delivery system capable of protecting, translocating, and selectively releasing therapeutic moieties to desired sites can promote the efficacy of an active compound. In this work, we have developed a nanoformulation which preserves its magnetization to load a model anticancerous drug and to explore the controlled release of the drug in a cancerous environment. For the preparation of the nanoformulation, self-assembled magnetic nanospheres (MNS) made of superparamagnetic iron oxide nanoparticles were grafted with a monolayer of (3-aminopropyl)triethoxysilane (APTES). A direct functionalization strategy was used to avoid the loss of the MNS magnetization. The successful preparation of the nanoformulation was validated by structural, microstructural, and magnetic investigations. X-ray photoelectron spectroscopy (XPS) and Fourier transform infrared spectroscopy (FTIR) were used to establish the presence of APTES on the MNS surface. The amine content quantified by a ninhydrin assay revealed the monolayer coverage of APTES over MNS. The monolayer coverage of APTES reduced only negligibly the saturation magnetization from 77 emu/g (for MNS) to 74 emu/g (for MNS-APTES). Detailed investigations of the thermoremanent magnetization were carried out to assess the superparamagnetism in the MNS. To make the nanoformulation pH-responsive, the anticancerous drug Nintedanib (NTD) was conjugated with MNS-APTES through the acid liable imine bond. At pH 5.5, which mimics a cancerous environment, a controlled release of 85% in 48 h was observed. On the other hand, prolonged release of NTD was found at physiological conditions (i.e., pH 7.4). In vitro cytotoxicity study showed dose-dependent activity of MNS-APTES-NTD for human lung cancer cells L-132. About 75% reduction in cellular viability for a 100 μg/mL concentration of nanoformulation was observed. The nanoformulation designed using MNS and monolayer coverage of APTES has potential in cancer therapy as well as in other nanobiological applications.
format	article
author	V. C. Karade A. Sharma R. P. Dhavale R. P. Dhavale S. R. Shingte P. S. Patil J. H. Kim D. R. T. Zahn A. D. Chougale G. Salvan P. B. Patil
author_facet	V. C. Karade A. Sharma R. P. Dhavale R. P. Dhavale S. R. Shingte P. S. Patil J. H. Kim D. R. T. Zahn A. D. Chougale G. Salvan P. B. Patil
author_sort	V. C. Karade
title	APTES monolayer coverage on self-assembled magnetic nanospheres for controlled release of anticancer drug Nintedanib
title_short	APTES monolayer coverage on self-assembled magnetic nanospheres for controlled release of anticancer drug Nintedanib
title_full	APTES monolayer coverage on self-assembled magnetic nanospheres for controlled release of anticancer drug Nintedanib
title_fullStr	APTES monolayer coverage on self-assembled magnetic nanospheres for controlled release of anticancer drug Nintedanib
title_full_unstemmed	APTES monolayer coverage on self-assembled magnetic nanospheres for controlled release of anticancer drug Nintedanib
title_sort	aptes monolayer coverage on self-assembled magnetic nanospheres for controlled release of anticancer drug nintedanib
publisher	Nature Portfolio
publishDate	2021
url	https://doaj.org/article/2086fb8197de4b1cb8a435b01ed131ce
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APTES monolayer coverage on self-assembled magnetic nanospheres for controlled release of anticancer drug Nintedanib

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