# A novel nanochannel system for sustained delivery of Tenofovir Alafenamide Fumarate and Emtricitabine for HIV pre-exposure prophylaxis

> **NIH NIH R01** · METHODIST HOSPITAL RESEARCH INSTITUTE · 2020 · $761,083

## Abstract

Abstract
An implantable system capable of long-term sustained release of antiretroviral drugs is needed to overcome
patient adherence issues and achieve desired clinical outcomes in pre-exposure prophylaxis (PrEP) of HIV
infection. The goal of this proposal, leveraging the extensive experience from a team of accomplished
investigators with multidisciplinary backgrounds and based on encouraging preliminary findings, is to develop a
novel, nanotechnology-based, implantable drug delivery device, the nanochannel drug delivery system (nDS),
for sustained and constant release of antiretroviral drugs. The safety and efficacy of this implant, used for the
delivery of tenofovir alafenamide fumarate and emtricitabine (TAF/FTC), will be validated in vitro and in
established animal models. This broad objective will be achieved through the following specific aims: Aim 1) to
develop nDS implants capable of sustained and constant release of TAF/FTC in rats and NHP for 60 days.
Two nDS implants designed for small and large animal models, and incorporating a remotely controlled
deactivation mechanism, will be developed and tested with TAF/FTC to establish release rates in vitro. In vivo
analysis to evaluate safety of implant, test the deactivation mechanism, and determine the pharmacokinetics of
nDS-delivered TAF/FTC will be conducted in healthy rat models. Aim 2) to assess the pharmacokinetics of
constant delivery of TAF/FTC from nDS implants at target release rates for 60 days in non-human primates
(NHP). Aim 3) to evaluate prevention of simian-human immunodeficiency virus (SHIV) infection by release of
TAF/FTC from nDS implants through rectal challenge in NHP. This will be followed by pharmacometric
modeling for future clinical evaluation in humans. The proposed work focuses at developing a novel
implantable drug delivery device for the sustained delivery of antiretroviral drugs and the preclinical validation
of the drug-device combination for pre-exposure prophylaxis of HIV infection. The nDS-TAF/FTC combination
is expected to provide unique information about antiretroviral drugs’ efficacy in PrEP by eliminating issues
related to patient compliance, gut absorption, and bioavailability from oral administration. The successful
completion of this project will represent a significant step forward toward the clinical translation of the nDS
implant for HIV PrEP and an effective preventive strategy for individuals who are at substantial risk of acquiring
HIV infection.

## Key facts

- **NIH application ID:** 9932319
- **Project number:** 5R01AI120749-05
- **Recipient organization:** METHODIST HOSPITAL RESEARCH INSTITUTE
- **Principal Investigator:** Alessandro Grattoni
- **Activity code:** R01 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2020
- **Award amount:** $761,083
- **Award type:** 5
- **Project period:** 2016-06-20 → 2022-05-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/9932319

## Citation

> US National Institutes of Health, RePORTER application 9932319, A novel nanochannel system for sustained delivery of Tenofovir Alafenamide Fumarate and Emtricitabine for HIV pre-exposure prophylaxis (5R01AI120749-05). Retrieved via AI Analytics 2026-05-23 from https://api.ai-analytics.org/grant/nih/9932319. Licensed CC0.

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