Interactions between PAMAM-NH2 and 6-mercaptopurine: qualitative and quantitative NMR studies
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Interactions between PAMAM-NH2 and 6-mercaptopurine: qualitative and quantitative NMR studies. / Gao, Xueke; Ma, Minjun; Pedersen, Christian Marcus; Liu, Rui; Zhang, Zhenzhou; Chang, Honghong; Qiao, Yan; Wang, Yingxiong.
I: Chemistry - An Asian Journal, Bind n/a, Nr. n/a, 08.09.2021, s. 3658-3663.Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt
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TY - JOUR
T1 - Interactions between PAMAM-NH2 and 6-mercaptopurine: qualitative and quantitative NMR studies
AU - Gao, Xueke
AU - Ma, Minjun
AU - Pedersen, Christian Marcus
AU - Liu, Rui
AU - Zhang, Zhenzhou
AU - Chang, Honghong
AU - Qiao, Yan
AU - Wang, Yingxiong
PY - 2021/9/8
Y1 - 2021/9/8
N2 - 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.
AB - 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.
KW - Faculty of Science
KW - 6-MP
KW - binding strength
KW - interaction
KW - NMR
KW - PAMAM-NH2
U2 - 10.1002/asia.202100771
DO - 10.1002/asia.202100771
M3 - Journal article
C2 - 34494362
VL - n/a
SP - 3658
EP - 3663
JO - Chemistry - An Asian Journal
JF - Chemistry - An Asian Journal
SN - 1861-4728
IS - n/a
ER -
ID: 279782632