Exploring the translocation behaviours in vivo of herpetrione amorphous nanoparticles via oral delivery

Abstract

Nanotechnology has been a primary strategy to enhance oral bioavailability of poorly water soluble drugs. However, the limited information in vivo fate of impedes the development of nanoparticles via the oral delivery, especially the amorphous nanoparticles with high energy states are rarely reported. This study is to track the translocation of oral herpetrione amorphous nanoparticles (HPE-ANPs). We prepare amorphous particles (ANPs) of various sizes (200 nm and 450 nm), which are embedded with an aggregation-caused quenching (ACQ) dyes for tracking the intact nanoparticles. Nanoparticles remain in the gastrointestinal tract (GIT) for 8 h following oral administration, suggesting that most ANPs was mainly degraded or absorbed in the small intestine. Ex vivo imaging shows that the fluorescent signals are observed in the GIT and liver but not in other organs, which attributed to low absorption of integral nanoparticles. Besides, HPE-ANPs may be directly interact with GIT epithelia, and ileum provides better absorption than the jejunum. Cellular studies prove that integral HPE-ANPs can be taken up by enterocyte, while it penetrates cell monolayers only small amounts. In conclusion, we speculate that the drug in the form of integral nanoparticles and small molecules may be co-absorbed to improve bioavailability in vivo.

Keywords:

• Amorphous nanoparticles
• oral
• drug delivery
• herpetrione
• particle size

Disclosure statement

No potential conflict of interest was reported by the authors.

Correction Statement

This article has been republished with minor changes. These changes do not impact the academic content of the article.

Additional information

Funding

This work was supported by the National Natural Science Foundation of China (Nos. 81873092, 82174074, 81573697, 81803741).