Acid-Labile Acyclic Cucurbit[n]uril Molecular Containers for Controlled Release

Caps off for targeted drug delivery

28 February 2018

Nanoscopic molecular containers featuring a cap that pops off in mildly acidic conditions could selectively deliver drugs to diseased tissues.

While healthy parts of the body are typical pH-neutral, inflamed tissues and tumours tend to be mildly acidic. For targeted drug delivery to these sites, researchers have been trying to develop a molecular capsule that retains its therapeutic cargo at neutral pH, but rapidly releases it as the pH drops slightly. 

Such a container has been developed by a team co-led by Jia Liu at ShanghaiTech University. For the container, the team used a C-shaped molecule called an acyclic cucurbit[n]urils. These molecules feature amine functional groups at each tip of their structure, which served as anchor points for attaching the acid-sensitive molecular cap.

Tests with dye molecules as a cargo confirmed the containers selectively released their payload at mildly acidic pH, between pH 5.5 and 6.5. The released dye molecules were quickly taken up by surrounding cells. The team is now testing the containers’ ability to deliver anticancer drugs to a tumour in vivo.

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References

1. Angewandte Chemie International Edition 56, 12614–12618 (2017). doi: 10.1002/anie.201707164