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Methods Development for Blood Borne Macrophage Carriage of Nanoformulated Antiretroviral Drugs
Published on: December 9, 2010
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Short Communication: Specimen Processing Impacts Tissue Tenofovir Pharmacokinetic Measurements
Rahul P Bakshi1, Jennifer Breakey1, Madhuri Manohar1
11 Division of Clinical Pharmacology, Department of Medicine, Johns Hopkins University School of Medicine , Baltimore, Maryland.
AIDS Research and Human Retroviruses
|December 21, 2017
Summary
Accurate antiretroviral drug measurements in colonic biopsies are crucial for HIV prevention strategies. Collection method significantly impacts tenofovir (TFV) concentrations, but not tenofovir diphosphate (TFV-DP) levels, influencing assay interpretation.
Area of Science:
- Pharmacology
- HIV/AIDS Research
- Biomedical Science
Background:
- Antiretroviral drug concentrations at HIV exposure sites are critical for pre-exposure chemoprophylaxis (PrEP) strategies.
- Understanding how biopsy collection methods affect drug levels is essential for accurate pharmacokinetic assessments.
Purpose of the Study:
- To evaluate the impact of tissue culture medium on tenofovir (TFV) and tenofovir diphosphate (TFV-DP) concentrations in colonic biopsies.
- To determine the implications of these changes for HIV PrEP assay development and interpretation.
Main Methods:
- Colonic biopsies were collected and analyzed for TFV and TFV-DP concentrations.
- Biopsies were incubated with and without tissue culture medium to assess changes in drug concentrations over time.
- Tissue weight changes and drug concentrations were measured and compared between conditions.
Main Results:
- Significant baseline interbiopsy variation was observed for both TFV (38% CV) and TFV-DP (33% CV).
- Incubation in medium increased tissue weight twofold, decreasing weight-adjusted TFV concentrations by 75%.
- Adjusted TFV-DP concentrations decreased by only 25% in medium, a change that was not statistically significant.
Conclusions:
- Colonic biopsies should be collected without medium to ensure accurate TFV concentration measurements.
- The presence of medium does not significantly affect TFV-DP levels, suggesting minimal impact on TFV-DP-dependent assays.
- Accurate assessment of tissue drug concentrations requires consideration of biopsy collection methods and drug-specific mechanisms of action.

