Synthesis of novel dendrimers having aspartate grafts and their ability to enhance the aqueous solubility of model drugs

In this study, a series of aspartate based dendrimers with different cores were synthesized in a convergent approach and well characterized by NMR and MS techniques. The aqueous solubility of the model drugs (L-Histidine, Naproxen, Methotrexate) was measured in the presence of this kind of dendrimers at room temperature in PBS buffers at pH 6, 7 and 8. Results clearly confirmed that the solubility enhancement was due to presence of dendrimers at different pH compared to their corresponding aqueous solubility at different pH. The results indicated that the aspartate based dendrimers could be considered as an effective supplement of PAMAM dendrimers in solubility enhancement and drug delivery. The surface groups played an important role in dendrimer-mediated solubility enhancement.

Graphical abstractA series of peptide dendrimers bearing aspartate grafts in periphery as macromolecules for solubility enhancer of drug delivery were synthesized.Figure optionsDownload full-size imageDownload as PowerPoint slide