%0 Journal Article
%T Development of a Transdermal Delivery System for Tenofovir Alafenamide, a Prodrug of Tenofovir with Potent Antiviral Activity Against HIV and HBV
%A Ajay K. Banga
%A Ashana Puri
%A Gustavo F. Doncel
%A Meredith Clark
%A Onkar N. Singh
%A Sonalika A. Bhattaccharjee
%A Wei Zhang
%J Archive of "Pharmaceutics".
%D 2019
%R 10.3390/pharmaceutics11040173
%X 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 ¡À 0.09 ¦Ìg/cm2/h. However, the silicone-based patch comprising of 15% w/w TAF showed the highest permeation (7.24 ¡À 0.47 ¦Ìg/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
%K transdermal patch
%K tenofovir alafenamide
%K acrylate adhesive
%K in vitro permeation
%K silicone adhesive
%K suspension patch
%U https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6523937/