Journal
ADVANCED FUNCTIONAL MATERIALS
Volume 29, Issue 13, Pages -Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/adfm.201809015
Keywords
fatty acid; intestinal lymphatic transport; nanoemulsion; oral drug delivery; phase change material
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Funding
- Ministry of Science and Technology [MOST 107-2119-M-007-016, MOST 107-3017-F-007-002]
- Ministry of Educationof Taiwan, ROC [MOE 107QR001I5]
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The oral absorption of a therapeutic peptide (such as exenatide; EXT) that can improve glycemic control in the treatment of type 2 diabetes is limited by multiple barriers of the intestinal epithelium. This work presents an oil-structured nanoemulsion system that consists of a phase-changeable fatty acid that allows EXT (EXT@PC/NEMs) to be delivered orally and absorbed efficiently in the small intestine. To construct an appropriate vehicle to encapsulate EXT, an oil-in-water single emulsion is generated at 37 degrees C, which is well above the melting point of the fatty acid but below the denaturation temperature of the peptide drug. The as-prepared EXT@PC/NEMs are physically stable when stored at 4 degrees C, as they form a solid core, which prevents drug leakage. Upon their oral delivery at body temperature, the deformable liquid EXT@PC/NEMs may undergo effective cellular uptake, enhancing their permeability across the intestinal epithelium. The orally administered PC/NEMs significantly improve the bioavailability of EXT via intestinal lymphatic transport, ultimately accumulating in the pancreas, suggesting the possibility of orally delivering labile peptide drugs. The delivered EXT may act on pancreatic beta- and alpha-cells to stimulate insulin release and suppress glucagon secretion, respectively, reducing the blood glucose level, eventually having antidiabetic effects.
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