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Open AccessArticle

Controlled-Release from High-Loaded Reservoir-Type Systems—A Case Study of Ethylene-Vinyl Acetate and Progesterone

1
Research Center Pharmaceutical Engineering GmbH, Inffeldgasse 13, 8010 Graz, Austria
2
Institute of Pharmaceutical Sciences, Department Pharmaceutical Technology and Biopharmacy, University of Graz, Universitaetsplatz 1, 8010 Graz, Austria
3
Institute of Process and Particle Engineering, Graz University of Technology, Inffeldgasse 13, 8010 Graz, Austria
4
Evestra Inc., 6410 Tri County Parkway, Schertz, TX 78154, USA
*
Authors to whom correspondence should be addressed.
Pharmaceutics 2020, 12(2), 103; https://doi.org/10.3390/pharmaceutics12020103
Received: 19 December 2019 / Revised: 14 January 2020 / Accepted: 26 January 2020 / Published: 28 January 2020
(This article belongs to the Special Issue Coating Design: From Nanoparticle to Solid Dosage)
Reservoir systems (drug-loaded core surrounded by drug-free membrane) provide long-term controlled drug release. This is especially beneficial for drug delivery to specific body regions including the vagina. In this study, we investigated the potential of reservoir systems to provide high drug release rates over several weeks. The considered model system was an intra-vaginal ring (IVR) delivering progesterone (P4) in the mg/day range using ethylene-vinyl acetate (EVA) as release rate-controlling polymers. To circumvent the high material needs associated with IVR manufacturing, we implemented a small-scale screening procedure that predicts the drug release from IVRs. Formulations were designed based on the solubility and diffusivity of P4 in EVAs with varying vinyl acetate content. High in-vitro P4 release was achieved by (i) high P4 solubility in the core polymer; (ii) high P4 partition coefficient between the membrane and the core; and/or (iii) low membrane thicknesses. It was challenging for systems designed to release comparatively high fractions of P4 at early times to retain a constant drug release over a long time. P4 crystal dissolution in the core could not counterbalance drug diffusion through the membrane and drug crystal dissolution was found to be the rate-limiting step. Overall, high P4 release rates can be achieved from EVA-based reservoir systems View Full-Text
Keywords: vaginal drug delivery; controlled release; thermoplastic polymer; hot-melt extrusion; drug diffusivity vaginal drug delivery; controlled release; thermoplastic polymer; hot-melt extrusion; drug diffusivity
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MDPI and ACS Style

Koutsamanis, I.; Paudel, A.; Nickisch, K.; Eggenreich, K.; Roblegg, E.; Eder, S. Controlled-Release from High-Loaded Reservoir-Type Systems—A Case Study of Ethylene-Vinyl Acetate and Progesterone. Pharmaceutics 2020, 12, 103. https://doi.org/10.3390/pharmaceutics12020103

AMA Style

Koutsamanis I, Paudel A, Nickisch K, Eggenreich K, Roblegg E, Eder S. Controlled-Release from High-Loaded Reservoir-Type Systems—A Case Study of Ethylene-Vinyl Acetate and Progesterone. Pharmaceutics. 2020; 12(2):103. https://doi.org/10.3390/pharmaceutics12020103

Chicago/Turabian Style

Koutsamanis, Ioannis; Paudel, Amrit; Nickisch, Klaus; Eggenreich, Karin; Roblegg, Eva; Eder, Simone. 2020. "Controlled-Release from High-Loaded Reservoir-Type Systems—A Case Study of Ethylene-Vinyl Acetate and Progesterone" Pharmaceutics 12, no. 2: 103. https://doi.org/10.3390/pharmaceutics12020103

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