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Int J Pharm. 2014 Oct 1;473(1-2):203-12. doi: 10.1016/j.ijpharm.2014.07.009. Epub 2014 Jul 8.

pH-sensitive nanoparticles for colonic delivery of curcumin in inflammatory bowel disease.

Author information

1
Université catholique de Louvain, Louvain Drug Research Institute, Advanced Drug Delivery and Biomaterials, 1200 Brussels, Belgium.
2
Université catholique de Louvain, Louvain Drug Research Institute, Advanced Drug Delivery and Biomaterials, 1200 Brussels, Belgium; University of Kinshasa, Faculty of Pharmaceutical Sciences, Laboratoire de Pharmacie galénique, BP 212 Kinshasa XI,Democratic Republic of the Congo.
3
Université catholique de Louvain, Louvain Drug Research Institute, Advanced Drug Delivery and Biomaterials, 1200 Brussels, Belgium. Electronic address: veronique.preat@uclouvain.be.

Abstract

Nano-scaled particles have been found to preferentially accumulate in inflamed regions. Local delivery of anti-inflammatory drugs loaded in nanoparticles to the inflamed colonic site is of great interest for inflammatory bowel disease (IBD) treatment. Curcumin (CC) is an anti-inflammatory local agent, which presents poor ADME properties. Hence, we evaluated, both in vitro and in vivo, the local delivery of CC using pH-sensitive polymeric nanoparticles (NPs) combining both poly(lactide-co-glycolide) acid (PLGA) and a polymethacrylate polymer (Eudragit(®) S100). CC-NPs significantly enhanced CC permeation across Caco-2 cell monolayers when compared to CC in suspension. CC-NPs significantly reduced TNF-α secretion by LPS-activated macrophages (J774 cells). In vivo, CC-NPs significantly decreased neutrophil infiltration and TNF-α secretion while maintaining the colonic structure similar to the control group in a murine DSS-induced colitis model. Our results support the use of nanoparticles made of PLGA and Eudragit(®) S100 combination for CC delivery in IBD treatment.

KEYWORDS:

Curcumin; Eudragit(®); Inflammatory bowel disease; Nanoparticles; PLGA; pH-sensitive

PMID:
25014369
DOI:
10.1016/j.ijpharm.2014.07.009
[Indexed for MEDLINE]

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