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PLGA nanoparticles for peroral delivery: How important is pancreatic digestion and can we control it?

European Journal of Pharmaceutics and Biopharmaceutics, ISSN: 0939-6411, Vol: 108, Page: 32-40
2016
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Ausgezeichnet: Hallesche Pharmazeuten erhalten „Best Paper Award“ für Studie zu Nanopartikeln

Für ihre Forschung an Nanopartikeln als Medikamententräger haben Pharmazeuten der Martin-Luther-Universität Halle-Wittenberg (MLU) den "Best Paper Award" des Jahrs 2016 der renommierten Fachzeitschrift "European Journal of Pharmaceutics and Biopharmaceutics" (EJPB) gewonnen. Die Wissenschaftler konnten zeigen, wie die Partikel während der Verdauung zersetzt werden und wie sich dieser Prozess block

Article Description

Biodegradable nanoparticles made of Poly(lactide- co -glycolide) are increasingly proposed for the improvement of oral drug absorption, but also as carriers for the treatment of colonic diseases. Unfortunately, our knowledge of the digestibility of PLGA-NPs is rather limited. Therefore, we investigated the impact of pancreatin on the digestibility of PLGA-NPs stabilized with different emulsifiers. The pancreatin induced degradation was monitored by the pH-stat method and an enzymatic l-lactic acid assay. A high digestibility was found for poloxamer 188 and polysorbate 80 stabilized PLGA-NPs. The digestion could be blocked by Orlistat, indicating a major role of pancreatic lipase. PLGA-NPs stabilized with Poly(vinyl alcohol) (=PVA) were not digested at comparable surfactant concentrations (0.6%). However, PLGA-NPs stabilized with very low amounts of PVA (0.1%) were digestible. In conclusion, PLGA-NPs are substrates for the pancreatic lipase. The digestibility can be enhanced or blocked by the proper selection of the surfactant composition and concentration.

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