Abstract
The histamine H2-receptor antagonists cimetidine, famotidine and nizatidine are individually encapsulated by macrocyclic cucurbit[7]uril (CB[7]), with binding affinities of 6.57 (±0.19) × 103 M−1, 1.30 (±0.27) × 104 M−1 and 1.05 (±0.33) × 105 M−1, respectively. These 1:1 host-guest inclusion complexes have been experimentally examined by 1H-NMR, UV-visible spectroscopic titrations (including Job plots), electrospray ionization mass spectrometry (ESI-MS), and isothermal titration calorimetry (ITC), as well as theoretically by molecular dynamics (MD) computation. This study may provide important insights on the supramolecular formulation of H2-receptor antagonist drugs for potentially enhanced stability and controlled release based on different binding strengths of these host-guest complexes.
Highlights
Among various macrocyclic molecules, an emerging family of molecular capsules known as cucurbit[n]urils (CB[n]s, n = 5–8, 10, 14) have recently attracted increasing attention in the field of pharmaceutical sciences and biomedical research [1,2]
We have recently extended our study to several other histamine H2 -receptor antagonists (Figure 1), have recently extended our study to several other histamine H2-receptor antagonists (Figure 1), namely namely cimetidine (CT), famotidine (FT) and nizatidine (NT), for their molecular encapsulation by cimetidine (CT), famotidine (FT) and nizatidine (NT), for their molecular encapsulation by CB[7]
The most significant difference between Ka values derived from comparable with those recently observed on other drug-CB[7] complexes [14,16,20,22], attesting the isothermal titration calorimetry (ITC) and NMR/UV-Vis methods is for the NT@CB[7] complexes, where the Ka from UV-Vis titration potential of these complexations in biomedical sciences
Summary
Even before these of preliminary investigations of CB[7]′s safety profile had been they have demonstrated that the toxicity these agents was reduced upon molecular encapsulation performed, over a decade ago the Collins [8] and Kim [9] research groups independently pioneered by CB[7], presumably due to steric protection provided by the molecular capsule [8,9] Following these the use of CB[7] for encapsulation of platinum complex-based anti-cancer agents, and they have works, CB[7] has drawn increasing attention as a host for the encapsulation of drug molecules demonstrated that the toxicity of these agents was reduced upon molecular encapsulation by CB[7], in recent years.
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