A comparative study of curcumin-loaded lipid-based nanocarriers in the treatment of inflammatory bowel disease

作者：Beloqui Ana; Memvanga Patrick B; Coco Regis; Reimondez Troitino Sonia; Alhouayek Mireille; Muccioli Giulio G; Alonso Maria Jose; Csaba Noemi; de la Fuente Maria; Preat Veronique^*

来源：Colloids and Surfaces B: Biointerfaces , 2016, 143: 327-335.

DOI：10.1016/j.colsurfb.2016.03.038

• IBD
• NLC
• SNEDDS
• Nanocapsules
• Lipids
• Curcumin

Selective drug delivery to inflamed tissues is of widespread interest for the treatment of inflammatory bowel disease (IBD). Because a lack of physiological lipids has been described in patients suffering IBD, and some lipids present immunomodulatory properties, we hypothesize that the combination of lipids and anti-inflammatory drugs together within a nanocarrier may be a valuable strategy for overcoming IBD. In the present study, we investigated and compared the in vitro and in vivo efficacy of three lipid-based nanocarriers containing curcumin (CC) as an anti-inflammatory drug for treating IBD in a murine DSS-induced colitis model. These nanocarriers included self-nanoemulsifying drug delivery systems (SNEDDS), nanostructured lipid carriers (NLC) and lipid core-shell protamine nanocapsules (NC). In vitro, a 30-fold higher CC permeability across Caco-2 cell monolayers was obtained using NC compared to SNEDDS (NC > SNEDDS > NLC and CC suspension). The CC SNEDDS and CC NLC but not the CC NC or CC suspension significantly reduced TNF-alpha secretion by LPS-activated macrophages (J774 cells). In vivo, only CC NLC were able to significantly decrease neutrophil infiltration and TNF-a secretion and, thus, colonic inflammation. Our results show that a higher CC permeability does not correlate with a higher efficacy in IBD treatment, which suggests that lipidic nanocarriers exhibiting increased CC retention at the intestinal site, rather than increased CC permeability are efficient treatments of IBD.

• 出版日期2016-7-1