Interactions between PAMAM-NH2 and 6-mercaptopurine: qualitative and quantitative NMR studies
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Despite being used as an anti-leukemic drug, the poor solubility of 6-mercaptopurine (6-MP) limits its use in topical and parenteral applications. Dendrimers are commonly used as drug carriers to improve their solubility in aqueous solution. In this work, the interactions between 6-MP and the amine-terminated poly(amidoamine) dendrimers (PAMAM-NH2 ) were investigated by various NMR technology. The chemical shift titrations disclosed that the 6-MP interacted with the surface of PAMAM-NH2 mainly through electrostatics. The determination of diffusion coefficient and relaxation measurements further confirmed the presence of interactions in 6-MP/PAMAM-NH2 complexes. In addition, the encapsulation of 6-MP within the cavity of PAMAM-NH2 was revealed through nuclear Overhauser effect spectroscopy and Saturation Transfer Double Difference analysis. Finally, the binding strength (H-8 is 1002 is 70 of 6-MP to PAMAM-NH2 was quantitatively expressed using epitope maps. This study provides a systematic methodology for qualitative and quantitative studies of the interactions between dendrimers and drug molecules in general.
Originalsprog | Engelsk |
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Tidsskrift | Chemistry - An Asian Journal |
Vol/bind | n/a |
Udgave nummer | n/a |
Sider (fra-til) | 3658-3663 |
Antal sider | 6 |
ISSN | 1861-471X |
DOI | |
Status | Udgivet - 8 sep. 2021 |
- Det Natur- og Biovidenskabelige Fakultet - 6-MP, binding strength, interaction, NMR, PAMAM-NH2
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