A single binding site was observed in the BSA rivaroxaban complex and the binding constants indicated that their binding is quite strong to be highly bound in plasma.
As said before, both are highly bound to albumin, i.e. more than 90%, and distribution of the two drugs in the body after parenteral administration is similar.
Considering that oxa- and cloxacillin are highly bound to albumin (up to 90%) [24], we assumed that the unbound fraction increased in hypoproteinemic patients.
Finally, the PPB prediction denotes that all the designed molecules have binding ≤90%% clearly revealing that the molecules have good bioavailability and are not likely to be highly bound to carrier proteins in the blood [25].
Considering that oxa- and cloxacillin are highly bound to albumin and that their unbound fraction i.e. the available fraction for antibiotic efficacy in healthy patients is known to be 10%, we defined a target range of total antibiotic concentration of 20 50 mg/L to reach the 100% T > MIC.
We focus on drugs that are highly bound as this will restrict their potential to move freely into the skin but which are lipophilic so that, in the unbound form, they would demonstrate an affinity to the outer layers of the skin.
Ritonavir but also lopinavir are highly bound in plasma to albumin and α1-acid glycoprotein [32].
Tazarotenic acid is highly bound to proteins.
Acidic NSAIDs are highly bound to plasma proteins, mainly albumin.
Seliciclib is highly bound to plasma proteins (90%), primarily albumin (Vita et al, 2005).
