Light-triggered release of conventional local anesthetics from a macromolecular prodrug for on-demand local anesthesia

An on-demand anesthetic that would only take effect when needed and where the intensity of anesthesia could be easily adjustable according to patients’ needs would be highly desirable. Here, we design and synthesize a macromolecular prodrug (P407-CM-T) in which the local anesthetic tetracaine (T) is...

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Autores principales: Zhang, Wei, Ji, Tianjiao, Li, Yang, Zheng, Yueqin, Mehta, Manisha, Zhao, Chao, Liu, Andong, Kohane, Daniel S.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group UK 2020
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7210304/
https://www.ncbi.nlm.nih.gov/pubmed/32385252
http://dx.doi.org/10.1038/s41467-020-16177-w
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author Zhang, Wei
Ji, Tianjiao
Li, Yang
Zheng, Yueqin
Mehta, Manisha
Zhao, Chao
Liu, Andong
Kohane, Daniel S.
author_facet Zhang, Wei
Ji, Tianjiao
Li, Yang
Zheng, Yueqin
Mehta, Manisha
Zhao, Chao
Liu, Andong
Kohane, Daniel S.
author_sort Zhang, Wei
collection PubMed
description An on-demand anesthetic that would only take effect when needed and where the intensity of anesthesia could be easily adjustable according to patients’ needs would be highly desirable. Here, we design and synthesize a macromolecular prodrug (P407-CM-T) in which the local anesthetic tetracaine (T) is attached to the polymer poloxamer 407 (P407) via a photo-cleavable coumarin linkage (CM). P407-CM-T solution is an injectable liquid at room temperature and gels near body temperature. The macromolecular prodrug has no anesthetic effect itself unless irradiated with a low-power blue light emitting diode (LED), resulting in local anesthesia. By adjusting the intensity and duration of irradiation, the anesthetic effect can be modulated. Local anesthesia can be repeatedly triggered.
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spelling pubmed-72103042020-05-13 Light-triggered release of conventional local anesthetics from a macromolecular prodrug for on-demand local anesthesia Zhang, Wei Ji, Tianjiao Li, Yang Zheng, Yueqin Mehta, Manisha Zhao, Chao Liu, Andong Kohane, Daniel S. Nat Commun Article An on-demand anesthetic that would only take effect when needed and where the intensity of anesthesia could be easily adjustable according to patients’ needs would be highly desirable. Here, we design and synthesize a macromolecular prodrug (P407-CM-T) in which the local anesthetic tetracaine (T) is attached to the polymer poloxamer 407 (P407) via a photo-cleavable coumarin linkage (CM). P407-CM-T solution is an injectable liquid at room temperature and gels near body temperature. The macromolecular prodrug has no anesthetic effect itself unless irradiated with a low-power blue light emitting diode (LED), resulting in local anesthesia. By adjusting the intensity and duration of irradiation, the anesthetic effect can be modulated. Local anesthesia can be repeatedly triggered. Nature Publishing Group UK 2020-05-08 /pmc/articles/PMC7210304/ /pubmed/32385252 http://dx.doi.org/10.1038/s41467-020-16177-w Text en © The Author(s) 2020 Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/.
spellingShingle Article
Zhang, Wei
Ji, Tianjiao
Li, Yang
Zheng, Yueqin
Mehta, Manisha
Zhao, Chao
Liu, Andong
Kohane, Daniel S.
Light-triggered release of conventional local anesthetics from a macromolecular prodrug for on-demand local anesthesia
title Light-triggered release of conventional local anesthetics from a macromolecular prodrug for on-demand local anesthesia
title_full Light-triggered release of conventional local anesthetics from a macromolecular prodrug for on-demand local anesthesia
title_fullStr Light-triggered release of conventional local anesthetics from a macromolecular prodrug for on-demand local anesthesia
title_full_unstemmed Light-triggered release of conventional local anesthetics from a macromolecular prodrug for on-demand local anesthesia
title_short Light-triggered release of conventional local anesthetics from a macromolecular prodrug for on-demand local anesthesia
title_sort light-triggered release of conventional local anesthetics from a macromolecular prodrug for on-demand local anesthesia
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7210304/
https://www.ncbi.nlm.nih.gov/pubmed/32385252
http://dx.doi.org/10.1038/s41467-020-16177-w
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