التفاصيل البيبلوغرافية
العنوان: |
Sustained In-Vivo Release of Triptorelin Acetate from a Biodegradable Silica Depot: Comparison to Pamorelin® LA |
المؤلفون: |
Ari-Pekka Forsback, Panu Noppari, Jesse Viljanen, Jari Mikkola, Mika Jokinen, Lasse Leino, Simon Bjerregaard, Camilla Borglin, Janet Halliday |
المصدر: |
Nanomaterials; Volume 11; Issue 6; Pages: 1578 |
بيانات النشر: |
Multidisciplinary Digital Publishing Institute |
سنة النشر: |
2021 |
المجموعة: |
MDPI Open Access Publishing |
مصطلحات موضوعية: |
controlled release, silica hydrogel, silica microparticles, silica nanoparticles, triptorelin |
الوصف: |
Triptorelin acetate was encapsulated into silica microparticles by spray-drying a mixture of colloidal silica sol and triptorelin acetate solution. The resulting microparticles were then combined with another silica sol containing silica nanoparticles, which together formed an injectable silica-triptorelin acetate depot. The particle size and surface morphology of the silica-triptorelin acetate microparticles were characterized together with the in vitro release of triptorelin, injectability and rheology of the final injectable silica-triptorelin acetate depot. In vivo pharmacokinetics and pharmacodynamics of the silica-triptorelin acetate depot and Pamorelin® were evaluated and compared in Sprague-Dawley male rats after subcutaneous administration. Serum samples up to 91 days were collected and the plasma concentrations of triptorelin and testosterone were analyzed with ultraperformance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS). In vivo pharmacokinetics showed that injections of the silica-triptorelin acetate depot gave 5-fold lower Cmax values than the corresponding Pamorelin® injections. The depot also showed a comparable sustained triptorelin release and equivalent pharmacodynamic effect as the Pamorelin® injections. Detectable triptorelin plasma concentrations were seen with the depot after the 91-day study period and testosterone plasma concentrations remained below the human castration limit for the same period. |
نوع الوثيقة: |
text |
وصف الملف: |
application/pdf |
اللغة: |
English |
العلاقة: |
Biology and Medicines; https://dx.doi.org/10.3390/nano11061578Test |
DOI: |
10.3390/nano11061578 |
الإتاحة: |
https://doi.org/10.3390/nano11061578Test |
حقوق: |
https://creativecommons.org/licenses/by/4.0Test/ |
رقم الانضمام: |
edsbas.57C41F6C |
قاعدة البيانات: |
BASE |