This work is licensed under a Creative Commons Attribution 4.0 International License. The images
or other third party material in this article are included in the article’s Creative Commons license,
unless indicated otherwise in the credit line; if the material is not included under the Creative Commons license,
users will need to obtain permission from the license holder to reproduce the material. To view a copy of this
license, visit http://creativecommons.org/licenses/by/4.0/A modular p-phosphonated calix[4]arene vesicle (PCV) loaded with paclitaxel (PTX) and conjugated
with folic acid as a cancer targeting ligand has been prepared using a thin film-sonication method. It
has a pH-responsive capacity to trigger the release of the encapsulated PTX payload under mildly acidic
conditions. PTX-loaded PCV conjugated with alkyne-modified PEG-folic acid ligands prepared via click
ligation (fP-PCVPTX) has enhanced potency against folate receptor (FR)-positive SKOV-3 ovarian tumour
cells over FR-negative A549 lung tumour cells. Moreover, fP-PCVPTX is also four times more potent
than the non-targeting PCVPTX platform towards SKOV-3 cells. Overall, as a delivery platform the PCVs
have the potential to enhance efficacy of anticancer drugs by targeting a chemotherapeutic payload
specifically to tumours and triggering the release of the encapsulated drug in the vicinity of cancer cells
