| People | Locations | Statistics |
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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
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document
Thermal properties and eutectic behaviour of dapivirine in combination with steroid hormones and other antiretrovirals
Abstract
Background: Combination drug products can display thermal behaviour that is more complex than for the corresponding single drug products. For example, the contraceptive vaginal ring (VR) Nuvaring contains a eutectic (lowest melting) composition of etonogestrel (ETN) and ethinyl estradiol. Here we report the predisposition of dapivirine (DPV) to form reduced melting/eutectic mixtures when combined with other contraceptive hormones and antiretrovirals, and discuss the implications for development of combination microbicide and multipurpose prevention technology (MPT) products.<br/>Methods: Binary mixtures of DPV with darunavir (DRV), levonorgestrel (LNG), ETN or maraviroc (MVC) were prepared either by physical mixing or by solvent evaporation. Selected binary mixtures were also incorporated into silicone elastomer (SE) VR devices. Thermal behavior of the mixtures was analyzed using differential scanning calorimetry (DSC) operating in standard heating ramp mode (10 °C/min). DSC data were used to construct two component phase diagrams for each binary system.<br/>Results: Drug mixtures typically showed reduced melting transitions for both drug components, with clear evidence for a eutectic mixture at a well-defined intermediate composition. Eutectic temperatures and compositions for the various mixtures were: 40% DPV / 60% ETN - 170°C; 25% DPV / 75% MVC - 172°C; 65% DPV / 35% LNG - 192°C. In each case, the eutectic composition was also detected when the drug mixtures were incorporated into SE VRs. For the DPV/DRV system, the thermal behaviour is complicated by desolvation from the darunavir ethanolate polymorph.<br/>Conclusions: When DPV is combined with small molecular weight hydrophobic drugs, the melting temperature for both drugs is typically reduced to a degree dependent on the composition of the mixture. At specified compositions, a low melting eutectic system results. The formation of eutectic behavior in binary drug systems needs to be carefully characterised in order to define product performance and drug release.