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
Combinatorial Chemistry & High Throughput Screening
Title: Dendrimer-Based Prodrugs: Design, Synthesis, Screening and Biological Evaluation
Volume: 10 Issue: 5
Author(s): Yiyun Cheng, Yang Gao, Tingling Rao, Yiwen Li and Tongwen Xu
Affiliation:
Keywords: Dendrimer, prodrug, multi-valent, scaffolds, polyamidoamine, spacer, nanodevices
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.
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Cite this article as:
Cheng Yiyun, Gao Yang, Rao Tingling, Li Yiwen and Xu Tongwen, Dendrimer-Based Prodrugs: Design, Synthesis, Screening and Biological Evaluation, Combinatorial Chemistry & High Throughput Screening 2007; 10 (5) . https://dx.doi.org/10.2174/138620707781662808
DOI https://dx.doi.org/10.2174/138620707781662808 |
Print ISSN 1386-2073 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5402 |
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