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PHARMASPIRE - Volume 13, Issue 2, April - June, 2021

Pages: 35-41

Date of Publication: 07-Jun-2022

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Role and application of protein binding in drug distribution process

Author: Lavisha Jindal, Gurmeet Singh

Category: Pharmaceutics


The amount of drug which binds to proteins is considered protein-drug binding. The binding of drugs to protein is reversible and irreversible. Reversible generally involves a weak chemical bond. Irreversible arises due to covalent bonding. Irreversible binding can also occur because of carcinogenicity or tissue toxicity of the drug. The plasma protein binding to a drug has a significant role in the pharmacokinetics and pharmacodynamics of a drug. The amount of free active fraction of drug is determined by how much drug is bound to plasma protein. Protein binding to the drug can enhance or detract the drug’s efficiency. Protein binding can enhance the distribution of drugs throughout the body. It may also alter the duration of the action of the drug. Protein binding to drug alters therapeutic effect by forming a drug-protein complex which is itself biologically active. This review focuses on what is protein dug binding, how the protein binds to a drug. A description of the different methods used for determining protein-drug binding is also given. Protein-drug binding influences biological barriers, and how they cross them is also discussed. A discussion is also included to help readers to know the different factors affecting protein-drug binding.

Keywords: Protein, plasma, DNA, metabolism, drug distribution


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