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TAT-conjugated nanoparticles for the CNS delivery of anti-HIV drugs

Open access
Rao, Kavitha S., Reddy, Maram K., Horning, Jayme L., Labhasetwar, Vinod·2008·Biomaterials

Abstract

We have shown that nanoparticles (NPs) conjugated to trans-activating transcriptor (TAT) peptide bypass the efflux action of P-glycoprotein and increases the transport of the encapsulated ritonavir, a protease inhibitor (PI), across the blood-brain-barrier (BBB) to the central nervous system (CNS). A steady increase in the drug parenchyma/capillary ratio with time without disrupting the BBB integrity suggests that TAT-conjugated NPs are first immobilized in the brain vasculature prior to their transport into parenchyma. Localization of NPs in the brain parenchyma was further confirmed with histological analysis of the brain sections. The brain drug level with conjugated NPs was 800-fold higher than that with drug in solution at two weeks. Drug clearance was seen within four weeks. In conclusion, TAT-conjugated NPs enhance the CNS bioavailability of the encapsulated PI and maintained therapeutic drug level in the brain for a sustained period that could be effective in reducing the viral load in the CNS which acts as a reservoir for replicating HIV-1 virus.

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Metadata

Authors
Rao, K. S., Reddy, M. K., Horning, J. L., & Labhasetwar, V.
Venue
Biomaterials
Publisher
Elsevier BV
Published
2008-11
Volume
29
Issue
33
Pages
4429-4438
ISSN
0142-9612 (ISSN-L)
OpenAlex
W2074754374
Cited by
314
References
4
FWCI
7.84
Type
journal article
Language
en
Open access
green

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CoChat. (2026). Citation check: TAT-conjugated nanoparticles for the CNS delivery of anti-HIV drugs. https://app.cochat.ai/papers/10.1016/j.biomaterials.2008.08.004
The paper
Rao, K. S., Reddy, M. K., Horning, J. L., & Labhasetwar, V. (2008). TAT-conjugated nanoparticles for the CNS delivery of anti-HIV drugs. Biomaterials. https://doi.org/10.1016/j.biomaterials.2008.08.004

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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).

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