Abstract
Objective:In-vitro red blood cell (RBC) partitioning of doxycycline was studied to determine whether doxycycline penetrates RBC and its concentration was assayed keeping in view its high lipophilicity.Materials and Methods:Standardization of doxycycline was performed in whole blood and plasma of cattle by microbiological assay using Bacillus subtillis ATCC 6633 as indicator organizm. Actual concentration of the drug was obtained by comparing zone inhibition with standard graph and the extent of partitioning was mathematically calculated.Results:The R2 value of standard graph for doxycycline was 0.9934 and 0.9727 for plasma and whole blood, respectively. Overall, RBC partitioning of doxycycline was found to be 18.40 ± 1.70%.Conclusions:Overall RBC partitioning of doxycycline indicated low penetration into RBC. Plasma is the fluid suggested for pharmacokinetic evaluation of doxycycline.
Highlights
High lipophilicity of certain drugs may increase the extent of red blood cell (RBC) penetration and act as temporary storage of a drug and eventually affect the drug’s in-vivo behavior
This study is an effort to determine the extent of penetration of Doxycycline in RBCs
Red blood cell partitioning To study RBC partitioning, serial dilutions (10, 5, 2.5 μg/ml) of doxycycline were performed in whole blood (6 ml) of which PCV was measured after collection and incubated for 24 hours at 37°C allowing sufficient time for drug to penetrate RBCs
Summary
High lipophilicity of certain drugs may increase the extent of RBC penetration and act as temporary storage of a drug and eventually affect the drug’s in-vivo behavior. It cannot be over-ruled that plasma drug concentration may get affected due to high penetration into RBCs. it would be interesting to study the in-plasma profile of drugs such as doxycycline having high plasma protein binding as well as high lipophilicity. Tetracyclines supersede other antibiotics, spectrum wise, by virtue of action against haemoprotozoan infections like Anaplasma, Theileria, Eherlichia and Malaria These protozoa, in due course of their life cycle, enter RBCs and such infected RBCs are the main source of infection to other animals via intermediate host.[2] In case of Theileria, micromerozoites enter RBC via ticks of Rhipicephalus and Hyaloma spp. This study is an effort to determine the extent of penetration of Doxycycline in RBCs
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