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Naji, M. |
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Motta, Antonella |
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Aletan, Dirar |
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Mohamed, Tarek |
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Ertürk, Emre |
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Taccardi, Nicola |
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Kononenko, Denys |
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Petrov, R. H. | Madrid |
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Alshaaer, Mazen | Brussels |
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Bih, L. |
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Casati, R. |
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Muller, Hermance |
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Kočí, Jan | Prague |
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Šuljagić, Marija |
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Kalteremidou, Kalliopi-Artemi | Brussels |
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Azam, Siraj |
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Ospanova, Alyiya |
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Blanpain, Bart |
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Ali, M. A. |
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Popa, V. |
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Rančić, M. |
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Ollier, Nadège |
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Azevedo, Nuno Monteiro |
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Landes, Michael |
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Rignanese, Gian-Marco |
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Murphy, Diarmaid
in Cooperation with on an Cooperation-Score of 37%
Topics
Publications (10/10 displayed)
- 2021Custom silicone elastomers for improved mechanical performance and reduced hormone binding in a dapivirine/levonorgestrel vaginal ring
- 2021Formulation development of an ethylene vinyl acetate ring for sustained release of the experimental entry inhibitor DS003
- 2021Silicone elastomer formulations for improved performance of a multipurpose vaginal ring releasing dapivirine and levonorgestrelcitations
- 2019Post-use ring weight, residual drug content and drug depletion zone thickness as objective measures of user adherence to a contraceptive progesterone vaginal ringcitations
- 2019Towards a dapivirine and levonorgestrel multipurpose vaginal ring: Investigations into the reaction between levonorgestrel and addition-cure silicone elastomerscitations
- 2019Mechanical testing methods for drug-releasing vaginal ringscitations
- 2019In vitro release testing methods for drug-releasing vaginal ringscitations
- 2018Density Mediated Drug Release From Dapivirine Vaginal Rings Produced by Additive Manufacturing
- 2017Packing polymorphism of dapivirine and its impact on the performance of a dapivirine-releasing silicone elastomer vaginal ringcitations
- 2014Thermal properties and eutectic behaviour of dapivirine in combination with steroid hormones and other antiretrovirals
Places of action
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article
Silicone elastomer formulations for improved performance of a multipurpose vaginal ring releasing dapivirine and levonorgestrel
Abstract
A dapivirine-releasing silicone elastomer vaginal ring for reducing women’s risk of HIV acquisition has recently been approved. A next-generation multipurpose vaginal ring releasing dapivirine and levonorgestrel is currently in development, offering hormonal contraception and HIV prevention from a single device. Previously, we reported challenges with incorporating levonorgestrel into rings manufactured from addition-cure silicone elastomers due to an irreversible chemical reaction between the levonorgestrel molecule and the hydride-functionalised crosslinker component of the silicone elastomer formulation, leading to low drug content assay, cure inhibition, and reduced ring mechanical properties (which may account for the increased incidence of ring expulsion in vivo). Here, we report on the development and testing of various custom silicone elastomer materials specifically formulated to circumvent these issues. After extensive testing of the custom silicones and subsequent manufacture and testing (Shore M hardness, pot life, content assay, oscillatory rheology, mechanical testing) of rings containing both dapivirine and levonorgestrel, a lead candidate formulation was selected that was amenable to practical ring manufacture via injection molding, exhibited no substantial levonorgestrel binding, and offered suitable mechanical properties.