Abstract

To construct a water-soluble and bone-targeting non-steroidal anti-inflammatory dendritic drug carrier, a series of Asp oligopeptides and naproxen based poly amido-ester Janus dendrimers were synthesized using a conventional method and their water solubility was preliminary evaluated. The corresponding small dendritic linkers contain two or three drug moieties on the surface and two or three oligopeptides groups at the focal terminus. This design provided an effective entry for the synthesis of multiple drug carriers with water-soluble and bone-targeting.

Highlights

  • IntroductionThe art of designing dendritic macromolecules progresses toward the synthesis of more and more sophisticated compounds, including those with several types of terminal groups, precisely placed on different areas of the surface

  • The features of dendrimers such as monodisperse, highly branched macromolecules with well-defined three dimensional structures, made them have many properties that significantly differ from those of corresponding linear polymers.[1,2,3] Due to the ability to control the synthesis, the large globular structure and functionality of dendrimers, they have been found to use in applications such as light-harvesting systems, catalysis and drug delivery.[4,5,6]The art of designing dendritic macromolecules progresses toward the synthesis of more and more sophisticated compounds, including those with several types of terminal groups, precisely placed on different areas of the surface

  • It has been demonstrated that ester bond linkage to non-steroidal anti-inflammatory drugs (NSAIDs) does not impair its anti-inflammatory activity.[22,23]

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Summary

Introduction

The art of designing dendritic macromolecules progresses toward the synthesis of more and more sophisticated compounds, including those with several types of terminal groups, precisely placed on different areas of the surface Such compounds can be called “Janus” or surface-block codendrimers.[7] The synthesis of part of these compounds have already been described, often using them for self-assembly or as liquid crystals.[8,9,10] Frechet et al designed and prepared such kind of Janus dendrimer which consisted of two covalently attached dendrons for drug delivery and related therapeutic applications.[19] These new carriers were useful for improving the effect of polymer on pharmacokinetic properties.[20,21]

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