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In vitro protein binding and tissue distribution of D(+) usnic acid
D R Krishna1, D V Ramana, N V Mamidi
1University College of Pharmaceutical Sciences, Kakatiya University, Warangal, India.
Drug Metabolism and Drug Interactions
|January 1, 1995
Summary
D(+) usnic acid exhibits high protein binding (99.2%) in plasma, with potential therapeutic applications for pulmonary tuberculosis due to its distribution into lung tissues.
Area of Science:
- Pharmacokinetics
- Biochemistry
Background:
- D(+) usnic acid is a natural compound with potential medicinal properties.
- Understanding its protein binding and tissue distribution is crucial for therapeutic development.
Purpose of the Study:
- To investigate the in vitro protein binding of D(+) usnic acid.
- To determine the tissue distribution of D(+) usnic acid in rats.
Main Methods:
- Equilibrium dialysis was used to assess protein binding in rabbit plasma and bovine serum albumin.
- Scatchard plot analysis was employed to identify binding sites.
- Tissue distribution was studied in rats following intraperitoneal administration.
Main Results:
- D(+) usnic acid showed high protein binding (approximately 99.2%) at concentrations of 1-5 µg/ml.
- Binding decreased at low albumin concentrations and high drug concentrations.
- Scatchard analysis revealed two classes of binding sites.
- Usnic acid distributed well into well-perfused organs, with a high lung tissue/plasma ratio.
Conclusions:
- D(+) usnic acid demonstrates significant protein binding, suggesting favorable pharmacokinetic properties.
- The high concentration in lung tissue indicates potential efficacy for treating pulmonary tuberculosis.