Development of a Transdermal Delivery System for Tenofovir Alafenamide, a Prodrug of Tenofovir with Potent Antiviral Activity Against HIV and HBV
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 resis...
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| Format: | Article |
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MDPI AG
2019-04-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/11/4/173 |
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| author | Ashana Puri Sonalika A. Bhattaccharjee Wei Zhang Meredith Clark Onkar N. Singh Gustavo F. Doncel Ajay K. Banga |
| author_facet | Ashana Puri Sonalika A. Bhattaccharjee Wei Zhang Meredith Clark Onkar N. Singh Gustavo F. Doncel Ajay K. Banga |
| author_sort | Ashana Puri |
| collection | DOAJ |
| description | 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/cm<sup>2</sup>/h. However, the silicone-based patch comprising of 15% w/w TAF showed the highest permeation (7.24 ± 0.47 μg/cm<sup>2</sup>/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. |
| first_indexed | 2024-12-10T06:23:24Z |
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| id | doaj.art-a7f6c30526864f21bf4d52a12f733f71 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-12-10T06:23:24Z |
| publishDate | 2019-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-a7f6c30526864f21bf4d52a12f733f712022-12-22T01:59:17ZengMDPI AGPharmaceutics1999-49232019-04-0111417310.3390/pharmaceutics11040173pharmaceutics11040173Development of a Transdermal Delivery System for Tenofovir Alafenamide, a Prodrug of Tenofovir with Potent Antiviral Activity Against HIV and HBVAshana Puri0Sonalika A. Bhattaccharjee1Wei Zhang2Meredith Clark3Onkar N. Singh4Gustavo F. Doncel5Ajay K. Banga6Center for Drug Delivery Research, Department of Pharmaceutical Sciences, College of Pharmacy, Mercer University, Atlanta, GA 30341, USACenter for Drug Delivery Research, Department of Pharmaceutical Sciences, College of Pharmacy, Mercer University, Atlanta, GA 30341, USACONRAD, Department of Obstetrics and Gynecology, Eastern Virginia Medical School, Arlington, VA 22209, USACONRAD, Department of Obstetrics and Gynecology, Eastern Virginia Medical School, Arlington, VA 22209, USACONRAD, Department of Obstetrics and Gynecology, Eastern Virginia Medical School, Arlington, VA 22209, USACONRAD, Department of Obstetrics and Gynecology, Eastern Virginia Medical School, Arlington, VA 22209, USACenter for Drug Delivery Research, Department of Pharmaceutical Sciences, College of Pharmacy, Mercer University, Atlanta, GA 30341, USATenofovir 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/cm<sup>2</sup>/h. However, the silicone-based patch comprising of 15% w/w TAF showed the highest permeation (7.24 ± 0.47 μg/cm<sup>2</sup>/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.https://www.mdpi.com/1999-4923/11/4/173transdermal patchtenofovir alafenamideacrylate adhesivein vitro permeationsilicone adhesivesuspension patch |
| spellingShingle | Ashana Puri Sonalika A. Bhattaccharjee Wei Zhang Meredith Clark Onkar N. Singh Gustavo F. Doncel Ajay K. Banga Development of a Transdermal Delivery System for Tenofovir Alafenamide, a Prodrug of Tenofovir with Potent Antiviral Activity Against HIV and HBV Pharmaceutics transdermal patch tenofovir alafenamide acrylate adhesive in vitro permeation silicone adhesive suspension patch |
| title | Development of a Transdermal Delivery System for Tenofovir Alafenamide, a Prodrug of Tenofovir with Potent Antiviral Activity Against HIV and HBV |
| title_full | Development of a Transdermal Delivery System for Tenofovir Alafenamide, a Prodrug of Tenofovir with Potent Antiviral Activity Against HIV and HBV |
| title_fullStr | Development of a Transdermal Delivery System for Tenofovir Alafenamide, a Prodrug of Tenofovir with Potent Antiviral Activity Against HIV and HBV |
| title_full_unstemmed | Development of a Transdermal Delivery System for Tenofovir Alafenamide, a Prodrug of Tenofovir with Potent Antiviral Activity Against HIV and HBV |
| title_short | Development of a Transdermal Delivery System for Tenofovir Alafenamide, a Prodrug of Tenofovir with Potent Antiviral Activity Against HIV and HBV |
| title_sort | development of a transdermal delivery system for tenofovir alafenamide a prodrug of tenofovir with potent antiviral activity against hiv and hbv |
| topic | transdermal patch tenofovir alafenamide acrylate adhesive in vitro permeation silicone adhesive suspension patch |
| url | https://www.mdpi.com/1999-4923/11/4/173 |
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