Paclitaxel-loaded phosphonated calixarene nanovesicles as a modular drug delivery platform

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Mo, Jingxin
Eggers, Paul K
Yuan, Zhixiang
Raston, Colin L
Lim, Lee Yong
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Nature Publishing Group
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.
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Mo J, Eggers PK, Yuan ZX, Raston CL, Lim LY. Paclitaxel-loaded phosphonated calixarene nanovesicles as a modular drug delivery platform. Sci Rep. 2016 Mar 24;6:23489. doi: 10.1038/srep23489.