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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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Mccoy, Clare
in Cooperation with on an Cooperation-Score of 37%
Topics
Publications (12/12 displayed)
- 2023A multipurpose ‘CZL’ vaginal ring for non-hormonal contraception and STI/HIV prevention
- 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
- 2009Development and evaluation of a vaginal ring device for sustained delivery of HIV microbicides to non-human primate
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article
Packing polymorphism of dapivirine and its impact on the performance of a dapivirine-releasing silicone elastomer vaginal ring
Abstract
A silicone elastomer vaginal ring providing sustained release over 28 days of the antiretroviral microbicide dapivirine has recently completed Phase III clinical testing and showed moderate protection against HIV acquisition. In support of the product licensure program, we report the impact of dapivirine packing polymorphism on the thermal and solubility characteristics of dapivirine and on the in vitro performance of the 25 mg dapivirine ring product. This is the first time that polymorphism has been reported for a drug-releasing vaginal ring product. Thermal, particle size, powder x-ray diffraction and thermodynamic solubility analyses of dapivirine polymorphic forms I and IV, both of which are persistent at room temperature and with form I being the thermodynamically stable form, were conducted for both micronized and non-micronized materials. No significant differences in solubility between DPV forms I and IV were observed in media commonly used for in vitro release testing. Matrix-type silicone elastomer vaginal rings were manufactured and the impact of dapivirine polymorphism on key in vitro parameters (compression and tensile behaviour; content assay; in vitro release; residual content assay) was investigated. The data demonstrate that dapivirine packing polymorphism has no significant impact on in vitro performance of the 25 mg dapivirine vaginal ring.