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Electrospray-Based Microencapsulation of Epigallocatechin 3-Gallate for Local Delivery into the Intervertebral Disc
Locally delivered anti-inflammatory compounds can restore the homeostasis of the degenerated intervertebral disc (IVD). With beneficial effects on IVD cells, epigallocatechin 3-gallate (EGCG) is a promising therapeutic candidate. However, EGCG is prone to rapid degradation and/or depletion. Therefor...
Autores principales: | , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2019
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6781552/ https://www.ncbi.nlm.nih.gov/pubmed/31480533 http://dx.doi.org/10.3390/pharmaceutics11090435 |
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author | Loepfe, Moira Duss, Anja Zafeiropoulou, Katerina-Alexandra Björgvinsdóttir, Oddny D’Este, Matteo Eglin, David Fortunato, Giuseppino Klasen, Juergen Ferguson, Stephen J. Wuertz-Kozak, Karin Krupkova, Olga |
author_facet | Loepfe, Moira Duss, Anja Zafeiropoulou, Katerina-Alexandra Björgvinsdóttir, Oddny D’Este, Matteo Eglin, David Fortunato, Giuseppino Klasen, Juergen Ferguson, Stephen J. Wuertz-Kozak, Karin Krupkova, Olga |
author_sort | Loepfe, Moira |
collection | PubMed |
description | Locally delivered anti-inflammatory compounds can restore the homeostasis of the degenerated intervertebral disc (IVD). With beneficial effects on IVD cells, epigallocatechin 3-gallate (EGCG) is a promising therapeutic candidate. However, EGCG is prone to rapid degradation and/or depletion. Therefore, the purpose of this study was to develop a method for controlled EGCG delivery in the degenerated IVD. Primary IVD cells were isolated from human donors undergoing IVD surgeries. EGCG was encapsulated into microparticles by electrospraying of glutaraldehyde-crosslinked gelatin. The resulting particles were characterized in terms of cytocompatibility and anti-inflammatory activity, and combined with a thermoresponsive carrier to produce an injectable EGCG delivery system. Subsequently, electrospraying was scaled up using the industrial NANOSPIDER™ technology. The produced EGCG microparticles reduced the expression of inflammatory (IL-6, IL-8, COX-2) and catabolic (MMP1, MMP3, MMP13) mediators in pro-inflammatory 3D cell cultures. Combining the EGCG microparticles with the carrier showed a trend towards modulating EGCG activity/release. Electrospray upscaling was achieved, leading to particles with homogenous spherical morphologies. In conclusion, electrospray-based encapsulation of EGCG resulted in cytocompatible microparticles that preserved the activity of EGCG and showed the potential to control EGCG release, thus favoring IVD health by downregulating local inflammation. Future studies will focus on further exploring the biological activity of the developed delivery system for potential clinical use. |
format | Online Article Text |
id | pubmed-6781552 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2019 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-67815522019-10-30 Electrospray-Based Microencapsulation of Epigallocatechin 3-Gallate for Local Delivery into the Intervertebral Disc Loepfe, Moira Duss, Anja Zafeiropoulou, Katerina-Alexandra Björgvinsdóttir, Oddny D’Este, Matteo Eglin, David Fortunato, Giuseppino Klasen, Juergen Ferguson, Stephen J. Wuertz-Kozak, Karin Krupkova, Olga Pharmaceutics Article Locally delivered anti-inflammatory compounds can restore the homeostasis of the degenerated intervertebral disc (IVD). With beneficial effects on IVD cells, epigallocatechin 3-gallate (EGCG) is a promising therapeutic candidate. However, EGCG is prone to rapid degradation and/or depletion. Therefore, the purpose of this study was to develop a method for controlled EGCG delivery in the degenerated IVD. Primary IVD cells were isolated from human donors undergoing IVD surgeries. EGCG was encapsulated into microparticles by electrospraying of glutaraldehyde-crosslinked gelatin. The resulting particles were characterized in terms of cytocompatibility and anti-inflammatory activity, and combined with a thermoresponsive carrier to produce an injectable EGCG delivery system. Subsequently, electrospraying was scaled up using the industrial NANOSPIDER™ technology. The produced EGCG microparticles reduced the expression of inflammatory (IL-6, IL-8, COX-2) and catabolic (MMP1, MMP3, MMP13) mediators in pro-inflammatory 3D cell cultures. Combining the EGCG microparticles with the carrier showed a trend towards modulating EGCG activity/release. Electrospray upscaling was achieved, leading to particles with homogenous spherical morphologies. In conclusion, electrospray-based encapsulation of EGCG resulted in cytocompatible microparticles that preserved the activity of EGCG and showed the potential to control EGCG release, thus favoring IVD health by downregulating local inflammation. Future studies will focus on further exploring the biological activity of the developed delivery system for potential clinical use. MDPI 2019-09-01 /pmc/articles/PMC6781552/ /pubmed/31480533 http://dx.doi.org/10.3390/pharmaceutics11090435 Text en © 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Loepfe, Moira Duss, Anja Zafeiropoulou, Katerina-Alexandra Björgvinsdóttir, Oddny D’Este, Matteo Eglin, David Fortunato, Giuseppino Klasen, Juergen Ferguson, Stephen J. Wuertz-Kozak, Karin Krupkova, Olga Electrospray-Based Microencapsulation of Epigallocatechin 3-Gallate for Local Delivery into the Intervertebral Disc |
title | Electrospray-Based Microencapsulation of Epigallocatechin 3-Gallate for Local Delivery into the Intervertebral Disc |
title_full | Electrospray-Based Microencapsulation of Epigallocatechin 3-Gallate for Local Delivery into the Intervertebral Disc |
title_fullStr | Electrospray-Based Microencapsulation of Epigallocatechin 3-Gallate for Local Delivery into the Intervertebral Disc |
title_full_unstemmed | Electrospray-Based Microencapsulation of Epigallocatechin 3-Gallate for Local Delivery into the Intervertebral Disc |
title_short | Electrospray-Based Microencapsulation of Epigallocatechin 3-Gallate for Local Delivery into the Intervertebral Disc |
title_sort | electrospray-based microencapsulation of epigallocatechin 3-gallate for local delivery into the intervertebral disc |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6781552/ https://www.ncbi.nlm.nih.gov/pubmed/31480533 http://dx.doi.org/10.3390/pharmaceutics11090435 |
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