Delivery of Islatravir via High Drug‐Load, Long‐acting Microarray Patches for the Prevention or Treatment of Human Immunodeficiency Virus

Islatravir-loaded dissolving microarray patches (MAPs) provide a minimally invasive, long-acting solution for HIV-1 prevention and treatment. In rats, sustained islatravir delivery lasts up to three months, while in minipigs, efficacious plasma levels are detected for six days. Scaled-up projections indicate monthly dosing in humans, showcasing the potential of MAPs for sustained antiretroviral therapy.

Abstract

This research focuses on developing and characterizing islatravir-loaded dissolving microarray patches (MAPs) to provide an effective, minimally invasive treatment option for human immunodeficiency virus (HIV-1) prevention and treatment. The research involves manufacturing these MAPs using a double-casting approach, and conducting in vitro and in vivo evaluations. Results show that the MAPs have excellent needle fidelity, structural integrity, and mechanical strength. in vitro studies demonstrate that the MAPs can penetrate skin up to 580 µm and dissolve within 2 hours. Permeation studies reveal that the delivery efficiency of islatravir across the skin is around 40%. In rodent models, these dissolving MAPs sustain islatravir delivery for up to 3 months. Scaling up the MAPs and increasing drug loading produced detectable levels in minipig. Projections from animal data suggest that these dissolving MAPs can achieve effective islatravir levels for a month after a single application in humans. These findings indicate dissolving MAPs as a minimally invasive approach to sustained release of islatravir.