Systemic delivery of tenofovir alafenamide using dissolving and implantable microneedle patches

The human immunodeficiency virus (HIV) remains a global health concern, with 37.7 million people currently living with the infection and 1.5 million new cases every year. Current antiretroviral (ARV) therapies are administered through the oral route daily, often in lifelong treatments, leading to pill fatigue and poor treatment adherence. Therefore, the development of novel formulations for the administration ARV drugs using alternative routes is actively sought out.

Highlights

HIV is still a global concern, with 38 million people currently living with the infection.

ARV therapy can prevent HIV spread and extend life expectancy in infected people.

MAPs constitute an attractive platform for the delivery of antiretroviral drugs including TAF.

Dissolving and implantable TAF MAPs were obtained and characterised in vitro and ex vivo.

Both MAPs were able to deliver TAF systemically in rats.

In this sense, microneedle array patches (MAPs) offer a unique user-centric platform that can be painlessly self-applied to the skin and deliver drugs to the systemic circulation. In this work, dissolving and implantable MAPs loaded with the tenofovir alafenamide (TAF) were developed with the aim of releasing the drug systemically. Both MAPs were sufficiently strong to pierce excised neonatal full-thickness porcine skin and form drug depots. In vitro release experiments performed in dialysis membrane models, demonstrated a relatively fast delivery of the drug in all cases.

Franz cells experiments revealed that dissolving and implantable MAPs deposited 47.87 ​± ​16.33 ​μg and 1208.04 ​± ​417.9 ​μg of TAF in the skin after 24 ​h. Pharmacokinetic experiments in rats demonstrated a fast metabolization of TAF into tenofovir, with a rapid elimination of the metabolite from the plasma. The MAPs described in this work could be used as an alternative to current oral treatments for HIV management.

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Article information: Alejandro J. Paredes, Fabiana Volpe-Zanutto, Lalitkumar K. Vora, Ismaiel A. Tekko, Andi Dian Permana, Camila J. Picco, Helen O. McCarthy, Ryan F. Donnelly, Systemic delivery of tenofovir alafenamide using dissolving and implantable microneedle patches, Materials Today Bio, Volume 13, 2022. https://doi.org/10.1016/j.mtbio.2022.100217.