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Combinatorial Chemistry & High Throughput Screening

Editor-in-Chief

ISSN (Print): 1386-2073
ISSN (Online): 1875-5402

Dendrimer-Based Prodrugs: Design, Synthesis, Screening and Biological Evaluation

Author(s): Yiyun Cheng, Yang Gao, Tingling Rao, Yiwen Li and Tongwen Xu

Volume 10, Issue 5, 2007

Page: [336 - 349] Pages: 14

DOI: 10.2174/138620707781662808

Price: $65

Abstract

Dendrimers are a new class of artificial macromolecules with well-defined hyperbranched structures which enable bio-active molecules such as drugs to be presented in a highly multi-valent fashion. Covalent conjugation of drugs to the surface of dendrimers can be easily achieved either by direct chemical reactions between dendrimers and drug molecules including esterification and amidation or through cleavable linkers, depending on the functional groups on the surface of dendrimers. The pharmacological properties of these dendrimer-based prodrugs such as biocompatibility, biodistribution, biostability, bioadhesion and biopermeability can be modulated by further modifying dendrimers with specific functional molecules to fit a specific medicinal purpose. In this mini-review, recent advances on the use of dendrimers as prodrug nano-scaffolds were briefly demonstrated. The design and synthesis of dendrimer-based prodrugs as well as screening their intrinsic properties in biological systems were fully discussed.

Keywords: Dendrimer, prodrug, multi-valent, scaffolds, polyamidoamine, spacer, nanodevices


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