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Rapid Fluorescence-based Characterization of Single Extracellular Vesicles in Human Blood with Nanoparticle-tracking Analysis
Published on: January 7, 2019
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Rilpivirine-associated aggregation-induced emission enables cell-based nanoparticle tracking
Insiya Z Mukadam1, Jatin Machhi2, Jonathan Herskovitz3
1Department of Pharmaceutical Sciences, College of Pharmacy, University of Nebraska Medical Center, NE, 68198, USA.
Biomaterials
|December 23, 2019
Summary
New drug formulations using aggregation-induced emission (AIE) allow tracking of antiretroviral therapy (ART) drugs within HIV target cells. This advance aids in developing more potent HIV treatments by visualizing drug distribution.
Area of Science:
- Nanomedicine
- HIV Therapeutics
- Biophysical Chemistry
Background:
- Antiretroviral therapy (ART) has significantly improved outcomes for people with HIV.
- Current ART faces challenges including drug resistance, limited efficacy, and poor targeting of cellular reservoirs.
- Novel drug delivery systems are needed to enhance ART potency and therapeutic outcomes.
Purpose of the Study:
- To develop a method for tracking antiretroviral drugs within HIV cellular reservoirs.
- To utilize the aggregation-induced emission (AIE) property of rilpivirine (RPV) for drug visualization.
- To create a platform for monitoring drug biodistribution in target cells.
Main Methods:
- Harnessing the AIE property of the non-nucleoside reverse transcriptase inhibitor rilpivirine (RPV).
- Synthesizing RPV nanocrystals with inherent AIE characteristics.
- Visualizing intracellular RPV nanocrystals using cell and tissue-based assays.
- Detecting drug crystals in CD4+ T cells and macrophages via flow cytometry and LC-MS/MS.
Main Results:
- RPV nanocrystals exhibited endogenous AIE properties, enabling visualization.
- Intact RPV nanocrystals were successfully detected in CD4+ T cells and macrophages.
- The method allowed for monitoring of drug particles within natural HIV target cells.
Conclusions:
- Aggregation-induced emission (AIE) is a viable strategy for developing traceable antiretroviral drug formulations.
- This approach enables monitoring of drug cell and subcellular biodistribution.
- Harnessing AIE offers a promising pathway for optimizing ART delivery and efficacy.
Keywords:
Aggregation-induced emissionAntiretroviral therapyCD4(+) T cell trackingDrug biodistributionMonocyte-macrophageRilpivirineSingle-crystal x-ray diffraction
