Non-invasive insight into the release mechanisms of a poorly soluble drug from amorphous solid dispersions by confocal Raman microscopy
| Autor: | Jaroslav Hanuš, Branko Vukosavljevic, František Štěpánek, Maike Windbergs, Josef Beranek, Kateřina Punčochová |
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| Rok vydání: | 2016 |
| Předmět: |
Recrystallization (geology)
Polymers Morpholines Confocal Pharmaceutical Science 02 engineering and technology Spectrum Analysis Raman 030226 pharmacology & pharmacy Polyethylene Glycols 03 medical and health sciences symbols.namesake 0302 clinical medicine Drug Stability Microscopy medicine Organic chemistry Dissolution chemistry.chemical_classification Drug Carriers Microscopy Confocal Polyvinylpyrrolidone Chemistry Povidone General Medicine Polymer 021001 nanoscience & nanotechnology Amorphous solid Drug Liberation Kinetics Solubility Chemical engineering symbols Polyvinyls Crystallization 0210 nano-technology Raman spectroscopy Hydrophobic and Hydrophilic Interactions Aprepitant Biotechnology medicine.drug |
| Zdroj: | European Journal of Pharmaceutics and Biopharmaceutics. 101:119-125 |
| ISSN: | 0939-6411 |
| DOI: | 10.1016/j.ejpb.2016.02.001 |
| Popis: | In this study, we investigated the release mechanism of the poorly water soluble drug aprepitant from different amorphous solid dispersions using confocal Raman microscopy (CRM). Solid dispersions were fabricated based on either Soluplus®, as an amphiphilic copolymer and solubilizer, or on polyvinylpyrrolidone, as a hydrophilic polymer, in order to elucidate the influence of the polymer characteristics on the drug form and dissolution mechanisms. Aprepitant exhibited its amorphous form in both solid dispersions. However, the release differed depending on the polymer. The high complexation effect of Soluplus was shown to be a crucial factor for stabilization of the amorphous drug, resulting in continuous release without any recrystallization of aprepitant. In contrast, solid dispersions based on polyvinylpyrrolidone showed a different mechanism of dissolution; due to the good affinity of PVP and water, the polymer is dissolving fast, leading to phase separation and local recrystallization of the drug. The study highlights the complexity of release processes from solid dispersions and elucidates the influence of the polymer on drug release kinetics. |
| Databáze: | OpenAIRE |
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