%0 Online Multimedia
%A Chuang, Er-Yuan
%A Lin, Kun-Ju
%A Huang, Tring-Yo
%A Chen, Hsin-Lung
%A Miao, Yang-Bao
%A Lin, Po-Yen
%A Chen, Chiung-Tong
%A Juang, Jyuhn-Huarng
%A Sung, Hsing-Wen
%D 2018
%T An
Intestinal “Transformers”-like Nanocarrier
System for Enhancing the Oral Bioavailability of Poorly Water-Soluble
Drugs
%U https://acs.figshare.com/articles/media/An_Intestinal_Transformers_-like_Nanocarrier_System_for_Enhancing_the_Oral_Bioavailability_of_Poorly_Water-Soluble_Drugs/6450257
%R 10.1021/acsnano.8b00470.s001
%2 https://acs.figshare.com/ndownloader/files/11864135
%K CUR-laden nanoemulsions
%K TLNS
%K AP
%K Poorly Water-Soluble Drugs
%X 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 water-soluble
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.
%I ACS Publications