title: Paclitaxel-loaded phosphonated calixarene nanovesicles as a modular drug delivery platform.
abstract: 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.
authors.affiliation: Pharmacy, School of Medicine and Pharmacology, The University of Western Australia, 35 Stirling Highway, Crawley, WA, 6009, Australia.|Key Laboratory for Stem Cells and Tissue Engineering (Sun Yat-sen University), Ministry of Education, Guangzhou, Guangdong, 510080, China.
authors.forename: Jingxin
authors.initials: J
authors.lastname: Mo
authors.affiliation: School of Chemistry and Biochemistry, The University of Western Australia, 35 Stirling Highway, Crawley, WA, 6009, Australia.
authors.forename: Paul K
authors.initials: PK
authors.lastname: Eggers
authors.affiliation: Department of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, Sichuan, 611130, China.
authors.forename: Zhi-xiang
authors.initials: ZX
authors.lastname: Yuan
authors.affiliation: Centre for NanoScale Science and Technology, School of Chemical and Physical Sciences, Flinders University, Bedford Park, SA, 5042, Australia.
authors.forename: Colin L
authors.initials: CL
authors.lastname: Raston
authors.affiliation: Pharmacy, School of Medicine and Pharmacology, The University of Western Australia, 35 Stirling Highway, Crawley, WA, 6009, Australia.
authors.forename: Lee Yong
authors.initials: LY
authors.lastname: Lim
mesh_terms: D000072283:A549 Cells; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D047250:Calixarenes / Q000737:chemistry*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D005492:Folic Acid / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D006863:Hydrogen-Ion Concentration; D049329:Nanostructures / Q000737:chemistry*; D009369:Neoplasms / Q000188:drug therapy; D017239:Paclitaxel / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D047250:Calixarenes; D005492:Folic Acid; D017239:Paclitaxel