# pH-Responsive supramolecular vesicles for imaging-guided drug delivery: Harnessing aggregation-induced emission

**Authors:** Xin-Rui Wang, Wei-Xiu Lin, Yi-Long Lu, Dietmar Kuck, Wen-Rong Xu

PMC · DOI: 10.1098/rsos.240664 · Royal Society Open Science · 2024-09-25

## TL;DR

This paper introduces pH-responsive fluorescent vesicles that enable real-time monitoring of drug release and enhance cancer treatment effectiveness.

## Contribution

The study presents a novel supramolecular vesicle system that combines aggregation-induced emission with pH-responsive drug delivery.

## Key findings

- The vesicles self-assemble from host–guest complexes and exhibit pH-responsive fluorescence.
- Encapsulation of doxorubicin allows for dual-fluorescence deactivation and recovery during drug release.
- DOX-loaded vesicles show enhanced anticancer activity with low toxicity to normal cells.

## Abstract

The water-soluble tribenzotriquinacene-based hexacarboxylic acid ammonium salt, TBTQ-C

6
, acts as the host component (H) forming host–guest complexes with tetraphenylethylene (TPE)-functionalized monotopic and tetratopic quaternary ammonium derivatives, G1 and G2, to yield supra-amphiphiles. These supra-amphiphiles self-assemble to form pH-responsive fluorescent vesicles, which have allowed us to capitalize on the aggregation-induced emission (AIE) effect for imaging-guided drug delivery systems. These systems exhibit efficient drug loading and pH-responsive delivery capabilities. Upon encapsulation of the anticancer drug doxorubicin (DOX), both the TPE and DOX chromophores undergo dual-fluorescence deactivation due to the energy transfer relay (ETR) effect. Under acidic conditions, the release of DOX interrupts the ETR effect, resulting in the fluorescence recovery of TPE fluorogens and DOX, allowing for real-time visual monitoring of the drug release process. Cytotoxicity experiments confirmed the low toxicity of the unloaded vectors to normal cells, while the DOX-loaded vectors were found to significantly enhance the anticancer activity of DOX against cancer cells in vitro. The AIE-featured supramolecular vesicles presented in this research hold great potential for imaging-guided drug delivery systems.

## Linked entities

- **Chemicals:** doxorubicin (PubChem CID 31703), tetraphenylethylene (PubChem CID 69437)

## Full-text entities

- **Diseases:** cancer (MESH:D009369), Cytotoxicity (MESH:D064420)
- **Chemicals:** TPE (MESH:C000617116), water (MESH:D014867), TBTQ-C 6 (-), DOX (MESH:D004317)

## Full text

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## Figures

7 figures with captions in the complete paper: https://tomesphere.com/paper/PMC11421929/full.md

## References

65 references — full list in the complete paper: https://tomesphere.com/paper/PMC11421929/full.md

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Source: https://tomesphere.com/paper/PMC11421929