Lipid nanocapsules maintain full integrity after crossing a human intestinal epithelium model

JOURNAL OF CONTROLLED RELEASE

卷:253

Article

Roger, Emilie¹  Gimel, Jean-Christophe¹  Bensley, Conor¹  Klymchenko, Andrey S.²  Benoit, Jean-Pierre¹ 

[1] Univ Bretagne Loire, Univ Angers, CNRS 6021, MINT,INSERM 1066,IBS CHU, 4 Rue Larrey, F-49933 Angers, France

[2] Univ Strasbourg, CNRS, UMR7213, Lab Biophoton & Pharmacol, 74 Route Rhin, F-67401 Illkirch Graffenstaden, France

关键词: Nanocapsules;    Caco-2;    Intestinal transport;    FRET;    Integrity;   

DOI  :  10.1016/j.jconrel.2017.03.005

来源: Elsevier

【 摘 要 】

Lipid nanocapsules (LNCs) have demonstrated great potential for the oral delivery of drugs having very limited oral bioavailability (BCS class II, III and IV molecules). It has been shown previously that orally-administered LNCs can permeate through mucus, increase drug absorption by the epithelial tissue, and finally, increase drug bioavailability. However, even if transport mechanisms through mucus and the intestinal barrier have already been clarified, the preservation of particle integrity is still not known. The aim of the present work is to study in vitro the fate of LNCs after their transportation across an intestinal epithelium model (Caco-2 cell model). For this, two complementary techniques were employed: Forster Resonance Energy Transfer (FRET) and Nano-particle Tracking Analysis (NTA). Results showed, after 2 h, the presence of nanoparticles in the basolateral side of the cell layer and a measurable FRET signal. This provides very good evidence for the transcellular intact crossing of the nanocarriers. (C) 2017 Elsevier B.V. All rights reserved.

【 授权许可】

Free