The controlled intravenous delivery of drugs using PEG-coated sterically stabilized nanospheres
Name
nihms582980.pdf
Description
Accepted version
Size
2 MB
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Unknown
Checksum (MD5)
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Author(s)
Gref, R
Domb, A
Quellec, P
Blunk, T
Müller, RH
Verbavatz, JM
Langer, Robert S
Date Issued
2012
Journal
Advanced Drug Delivery Reviews
Publisher
Elsevier BV
Citation
Gref, R., et al. "The Controlled Intravenous Delivery of Drugs Using Peg-Coated Sterically Stabilized Nanospheres." (2012).
Version
Author's final manuscript
Abstract
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.
MIT Department
Massachusetts Institute of Technology. Department of Chemical Engineering
Massachusetts Institute of Technology. Department of Biological Engineering
Terms of Use
Creative Commons Attribution-NonCommercial-NoDerivs License
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DOI of Published Version
https://doi.org/10.1016/j.addr.2012.09.008
