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Development of a Transdermal Delivery System for Tenofovir Alafenamide, a Prodrug of Tenofovir with Potent Antiviral Activity Against HIV and HBV

1
Center for Drug Delivery Research, Department of Pharmaceutical Sciences, College of Pharmacy, Mercer University, Atlanta, GA 30341, USA
2
CONRAD, Department of Obstetrics and Gynecology, Eastern Virginia Medical School, Arlington, VA 22209, USA
*
Author to whom correspondence should be addressed.
Pharmaceutics 2019, 11(4), 173; https://doi.org/10.3390/pharmaceutics11040173
Received: 27 February 2019 / Revised: 2 April 2019 / Accepted: 3 April 2019 / Published: 9 April 2019
(This article belongs to the Special Issue Novel Approaches for Delivery of Anti-HIV Drugs)
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Abstract

Tenofovir alafenamide (TAF) is an effective nucleotide reverse transcriptase inhibitor that is used in the treatment of HIV-1 and HBV. Currently, it is being investigated for HIV prophylaxis. Oral TAF regimens require daily intake, which hampers adherence and increases the possibility of viral resistance. Long-acting formulations would significantly reduce this problem. Therefore, the aim of this study was to develop a transdermal patch containing TAF and investigate its performance in vitro through human epidermis. Two types of TAF patches were manufactured. Transparent patches were prepared using acrylate adhesive (DURO-TAK 87-2516), and suspension patches were prepared using silicone (BIO-PSA 7-4301) and polyisobutylene (DURO-TAK 87-6908) adhesives. In vitro permeation studies were performed while using vertical Franz diffusion cells for seven days. An optimized silicone-based patch was characterized for its adhesive properties and tested for skin irritation. The acrylate-based patches, comprising 2% w/w TAF and a combination of chemical enhancers, showed a maximum flux of 0.60 ± 0.09 µg/cm2/h. However, the silicone-based patch comprising of 15% w/w TAF showed the highest permeation (7.24 ± 0.47 μg/cm2/h). This study demonstrates the feasibility of developing silicone-based transdermal patches that can deliver a therapeutically relevant dose of TAF for the control of HIV and HBV infections. View Full-Text
Keywords: transdermal patch; tenofovir alafenamide; acrylate adhesive; in vitro permeation; silicone adhesive; suspension patch transdermal patch; tenofovir alafenamide; acrylate adhesive; in vitro permeation; silicone adhesive; suspension patch
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
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Puri, A.; Bhattaccharjee, S.A.; Zhang, W.; Clark, M.; Singh, O.N.; Doncel, G.F.; Banga, A.K. Development of a Transdermal Delivery System for Tenofovir Alafenamide, a Prodrug of Tenofovir with Potent Antiviral Activity Against HIV and HBV. Pharmaceutics 2019, 11, 173.

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