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Issue 7, 2011
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Covalently cross-linked amphiphilic block copolymer micelles

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Polymeric micelles constitute an important class of nanomaterials that are highly attractive for pharmaceutical applications. The hydrophobic core of the micelles can be loaded with poorly water soluble drugs, while the shell of the micelles provides colloidal stability in vitro and in vivo. In recent years, covalent cross-linking of micelles is attracting increasing attention, because in vitro data show that it can prevent the self-assembled micelles from dissociation, can modulate drug release and may provide tools for triggered release. This paper reviews the methods used to cross-link either the core or the shell of the micelles, and focuses on drug delivery applications of cross-linked micelles. Whereas non-cross-linked micelles generally do not improve pharmacokinetics of encapsulated drugs when compared to common drug formulations, recent in vivo data show that cross-linking provides dramatic improvements in both pharmacokinetics and biodistribution of the micelles, and that drugs can fully benefit from that when they are covalently linked to the micelles. Although the field is still in its infancy, the latest results promise a bright future of cross-linked micelles for drug delivery and/or diagnostic applications.

Graphical abstract: Covalently cross-linked amphiphilic block copolymer micelles

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Publication details

The article was received on 15 Sep 2010, accepted on 30 Nov 2010 and first published on 12 Jan 2011

Article type: Review Article
DOI: 10.1039/C0SM00999G
Citation: Soft Matter, 2011,7, 3246-3259
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    Covalently cross-linked amphiphilic block copolymer micelles

    C. F. van Nostrum, Soft Matter, 2011, 7, 3246
    DOI: 10.1039/C0SM00999G

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