期刊
ACS NANO
卷 12, 期 7, 页码 6389-6397出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsnano.8b00470
关键词
oral drug delivery; poorly water-soluble drug; M cells; intestinal lymphatic transport; pancreatitis
类别
资金
- Ministry of Science and Technology of Taiwan (ROC) [MOST 106-2119-M-007-007, 105-2314-B-038-089-MY2]
Increasing the intestinal dissolution of orally administered poorly water-soluble drugs that have poor oral bioavailability to a therapeutically effective level has long been an elusive goal. In this work, an approach that can greatly enhance the oral bioavailability of a poorly watersoluble drug such as curcumin (CUR) is developed, using a Transformers-like nanocarrier system (TLNS) that can self-emulsify the drug molecules in the intestinal lumen to form nanoemulsions. Owing to its known anti-inflammation activity, the use of CUR in treating pancreatitis is evaluated herein. Structural changes of the TLNS in the intestinal environment to form the CUR-laden nanoemulsions are confirmed in vitro. The therapeutic efficacy of this TLNS is evaluated in rats with experimentally induced acute pancreatitis (AP). Notably, the CUR-laden nanoemulsions that are obtained using the proposed TLNS can passively target intestinal M cells, in which they are transcytosed and then transported into the pancreatic tissues via the intestinal lymphatic system. The pancreases in rats that are treated with the TLNS yield approximately 12 times stronger CUR signals than their counterparts receiving free CUR, potentially improving the recovery of AP. These findings demonstrate that the proposed TLNS can markedly increase the intestinal drug dissolution, making oral delivery a favorable noninvasive means of administering poorly water-soluble drugs.
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