An Intestinal "transformers"-like Nanocarrier System for Enhancing the Oral Bioavailability of Poorly Water-Soluble Drugs

Er Yuan Chuang, Kun Ju Lin, Tring Yo Huang, Hsin Lung Chen, Yang Bao Miao, Po Yen Lin, Chiung Tong Chen, Jyuhn Huarng Juang, Hsing Wen Sung

Research output: Contribution to journalArticle

5 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)6389-6397
Number of pages9
JournalACS Nano
Volume12
Issue number7
DOIs
Publication statusPublished - Jul 24 2018

Keywords

  • intestinal lymphatic transport
  • M cells
  • oral drug delivery
  • pancreatitis
  • poorly water-soluble drug

ASJC Scopus subject areas

  • Materials Science(all)
  • Engineering(all)
  • Physics and Astronomy(all)

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  • Cite this

    Chuang, E. Y., Lin, K. J., Huang, T. Y., Chen, H. L., Miao, Y. B., Lin, P. Y., Chen, C. T., Juang, J. H., & Sung, H. W. (2018). An Intestinal "transformers"-like Nanocarrier System for Enhancing the Oral Bioavailability of Poorly Water-Soluble Drugs. ACS Nano, 12(7), 6389-6397. https://doi.org/10.1021/acsnano.8b00470