Plasma protein binding

Plasma protein binding refers to the process by which drugs or other compounds in the bloodstream bind to proteins in the plasma, which can affect their metabolism and excretion. The affinity of a compound for plasma proteins can be measured through a Plasma Protein Binding assay, which determines the fraction of the compound that is unbound in pooled human plasma using equilibrium dialysis against an isotonic buffer.From: Sterile Drug Products [2019], Engineering Tools for Environmental Risk Management [2019]

Pharmacokinetics and Pharmacodynamics of Drugs Delivered to the Lung

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Published in Anthony J. Hickey, Sandro R.P. da Rocha, Pharmaceutical Inhalation Aerosol Technology, 2019

Stefanie K. Drescher, Mong-Jen Chen, Jürgen B. Bulitta, Günther Hochhaus

Another aspect of tissue and plasma protein binding should be discussed. More lipophilic drugs are currently in development, which show both increased tissue and plasma protein binding. These compounds consequently have small fu and fuT values. Yet there are no dramatic increases in the estimates of volume of distribution and half-life when compared to other drugs, because fu and fuT are both higher (see Figure 6.8 for relevant equation). With a decrease in the overall fraction of free drug, the effects (local and systemic) will be smaller than those of a similar drug with equivalent volume of distribution, but lower tissue and plasma protein binding. In this case, the drug with the higher degree of binding, but otherwise identical properties, will show reduced systemic side effects and reduced pulmonary effects at a given concentration.

Human serum albumin interaction studies of a new copper(II) complex containing ceftobiprole drug using molecular modeling and multispectroscopic methods

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Published in Journal of Coordination Chemistry, 2018

Nahid Shahabadi, Soraya Moradi Fili, Soheila Kashanian

To understand the potential of these compounds as drugs, studies on the binding of candidates to plasma proteins is a crucial step in assessing their bioavailability [11]. The report on plasma protein binding is now an FDA requirement in screening potential therapeutic agents. Therefore, understanding and characterizing the interaction of drugs with human serum albumin (HSA) are important to candidate drugs [12].

Plasma protein binding

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Pharmacokinetics and Pharmacodynamics of Drugs Delivered to the Lung

Human serum albumin interaction studies of a new copper(II) complex containing ceftobiprole drug using molecular modeling and multispectroscopic methods