Micelles based on HPMA copolymers

Polymeric micelles have been under extensive investigation during the past years as drug delivery systems, particularly for anticancer drugs. They are formed by the self-assembly of amphiphilic block copolymers in aqueous solutions and have a spherical shape and a size in the nano-range (< 200 nm...

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Bibliographic Details
Published in:Advanced drug delivery reviews 2010-02, Vol.62 (2), p.231-239
Main Authors: Talelli, M., Rijcken, C.J.F., van Nostrum, C.F., Storm, G., Hennink, W.E.
Format: Article
Language:English
Subjects:
Acrylamides - chemistry
Animals
Drug delivery
Drug Delivery Systems - methods
Drug Delivery Systems - trends
Drug targeting
EPR effect
HEMAm
HPMA
Humans
Micelle core
Micelle corona
Micelles
N-(2-hydroxylpropyl) methacrylamide
Nanomedicine - methods
Nanomedicine - trends
Polymeric micelles
Polymers - chemistry
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Summary:Polymeric micelles have been under extensive investigation during the past years as drug delivery systems, particularly for anticancer drugs. They are formed by the self-assembly of amphiphilic block copolymers in aqueous solutions and have a spherical shape and a size in the nano-range (< 200 nm). Tumor accumulation of polymeric micelles upon intravenous administration can occur as a result of the leaky vasculature of tumor tissue (called the enhanced permeation and retention (EPR) effect).To benefit from the EPR effect, polymeric micelles need to have prolonged circulation times as well as high and stable drug loadings. Poly[N-(2-hydroxypropyl) methacrylamide] (pHPMA) is a hydrophilic polymer currently under investigation for its use in polymer–drug conjugates. Its biocompatibility, non-immunogenicity and the possibility for functionalization are properties that resulted in broad pharmaceutical and biomedical applications, also in the micelle technology research. Being hydrophilic, it can serve as a micellar stealth corona, while it can also be modified with hydrophobic moieties to serve as a micellar core in which hydrophobic drugs can be solubilized and retained. HPMA-based polymeric micelles have been showing very promising in vitro and in vivo results. This review summarizes the applications of pHPMA in the field of polymeric micelles, either serving as a micellar stealth corona, or, if hydrophobically rendered by derivatization, as a micellar core.
ISSN:0169-409X
1872-8294
DOI:10.1016/j.addr.2009.11.029