The controlled intravenous delivery of drugs using PEG-coated sterically stabilized nanospheres

Injectable blood persistent particulate carriers have important therapeutic application in site-specific drug delivery or medical imaging. However, injected particles are generally eliminated by the reticulo-endothelial system within minutes after administration and accumulate in the liver and splee...

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Main Authors: Gref, R, Domb, A, Quellec, P, Blunk, T, Müller, RH, Verbavatz, JM, Langer, R
Format: Article
Language:English
Published: Elsevier BV 2021
Online Access:https://hdl.handle.net/1721.1/134465
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author Gref, R
Domb, A
Quellec, P
Blunk, T
Müller, RH
Verbavatz, JM
Langer, R
author_facet Gref, R
Domb, A
Quellec, P
Blunk, T
Müller, RH
Verbavatz, JM
Langer, R
author_sort Gref, R
collection MIT
description Injectable blood persistent particulate carriers have important therapeutic application in site-specific drug delivery or medical imaging. However, injected particles are generally eliminated by the reticulo-endothelial system within minutes after administration and accumulate in the liver and spleen. To obtain a coating that might prevent opsonization and subsequent recognition by the macrophages, sterically stabilized nanospheres were developed using amphiphilic diblock or multiblock copolymers. The nanospheres are composed of a hydrophilic polyethylene glycol coating and a biodegradable core in which various drugs were encapsulated. Hydrophobic drugs, such as lidocaine, were entrapped up to 45. wt% and the release kinetics were governed by the polymer physico-chemical characteristics. Plasma protein adsorption was drastically reduced on PEG-coated particles compared to non-coated ones. Relative protein amounts were time-dependent. The nanospheres exhibited increased blood circulation times and reduced liver accumulation, depending on the coating polyethylene glycol molecular weight and surface density. They could be freeze-dried and redispersed in aqueous solutions and possess good shelf stability. It may be possible to tailor "optimal" polymers for given therapeutic applications. © 2012.
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spelling mit-1721.1/1344652022-03-30T14:46:45Z The controlled intravenous delivery of drugs using PEG-coated sterically stabilized nanospheres Gref, R Domb, A Quellec, P Blunk, T Müller, RH Verbavatz, JM Langer, R Injectable blood persistent particulate carriers have important therapeutic application in site-specific drug delivery or medical imaging. However, injected particles are generally eliminated by the reticulo-endothelial system within minutes after administration and accumulate in the liver and spleen. To obtain a coating that might prevent opsonization and subsequent recognition by the macrophages, sterically stabilized nanospheres were developed using amphiphilic diblock or multiblock copolymers. The nanospheres are composed of a hydrophilic polyethylene glycol coating and a biodegradable core in which various drugs were encapsulated. Hydrophobic drugs, such as lidocaine, were entrapped up to 45. wt% and the release kinetics were governed by the polymer physico-chemical characteristics. Plasma protein adsorption was drastically reduced on PEG-coated particles compared to non-coated ones. Relative protein amounts were time-dependent. The nanospheres exhibited increased blood circulation times and reduced liver accumulation, depending on the coating polyethylene glycol molecular weight and surface density. They could be freeze-dried and redispersed in aqueous solutions and possess good shelf stability. It may be possible to tailor "optimal" polymers for given therapeutic applications. © 2012. 2021-10-27T20:05:07Z 2021-10-27T20:05:07Z 2012 2019-09-04T17:46:09Z Article http://purl.org/eprint/type/JournalArticle https://hdl.handle.net/1721.1/134465 Gref, R., et al. "The Controlled Intravenous Delivery of Drugs Using Peg-Coated Sterically Stabilized Nanospheres." (2012). en 10.1016/j.addr.2012.09.008 Advanced Drug Delivery Reviews Creative Commons Attribution-NonCommercial-NoDerivs License http://creativecommons.org/licenses/by-nc-nd/4.0/ application/pdf Elsevier BV PMC
spellingShingle Gref, R
Domb, A
Quellec, P
Blunk, T
Müller, RH
Verbavatz, JM
Langer, R
The controlled intravenous delivery of drugs using PEG-coated sterically stabilized nanospheres
title The controlled intravenous delivery of drugs using PEG-coated sterically stabilized nanospheres
title_full The controlled intravenous delivery of drugs using PEG-coated sterically stabilized nanospheres
title_fullStr The controlled intravenous delivery of drugs using PEG-coated sterically stabilized nanospheres
title_full_unstemmed The controlled intravenous delivery of drugs using PEG-coated sterically stabilized nanospheres
title_short The controlled intravenous delivery of drugs using PEG-coated sterically stabilized nanospheres
title_sort controlled intravenous delivery of drugs using peg coated sterically stabilized nanospheres
url https://hdl.handle.net/1721.1/134465
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