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Eur J Pharm Biopharm. 2016 Nov;108:32-40. doi: 10.1016/j.ejpb.2016.08.009. Epub 2016 Aug 20.

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

Author information

1
Institute of Pharmacy, Faculty of Biosciences, Martin Luther University Halle-Wittenberg, Wolfgang-Langenbeck-Str. 4, D-06120 Halle (Saale), Germany. Electronic address: anika.mante@medizin.uni-leipzig.de.
2
Institute of Pharmacy, Faculty of Biosciences, Martin Luther University Halle-Wittenberg, Wolfgang-Langenbeck-Str. 4, D-06120 Halle (Saale), Germany. Electronic address: martha.heider@pharmazie.uni-halle.de.
3
Institute of Pharmacy, Faculty of Biosciences, Martin Luther University Halle-Wittenberg, Wolfgang-Langenbeck-Str. 4, D-06120 Halle (Saale), Germany. Electronic address: christin.zlomke@pharmazie.uni-halle.de.
4
Institute of Pharmacy, Faculty of Biosciences, Martin Luther University Halle-Wittenberg, Wolfgang-Langenbeck-Str. 4, D-06120 Halle (Saale), Germany. Electronic address: http://pharmtech.pharmazie.uni-halle.de.

Abstract

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.

KEYWORDS:

Biodegradable polymers; Lipase; Nanoparticles; Oral delivery; PLGA; Pancreatic lipase; Pancreatin, digestion; Peroral; Poly(lactide-co-glycolide)

PMID:
27553262
DOI:
10.1016/j.ejpb.2016.08.009
[Indexed for MEDLINE]

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