PEGylation Quaternary (Triphenyl‐) Phosphonium Tosylate: A Class of Promising Carriers for Drug Delivery and Gene Delivery?

A new class of PEGylation quaternary (triphenyl‐) phosphonium tosylate (PQPT) was synthesized with different length of polyethylene glycol chain; the procedure is chromatography‐free and practical for large scale synthesis. All PQPTs are soluble in water and showed good anti‐bacterial activity. Particularly, cytotoxicity study on NIH 3T3 cell lines indicated PQPT with PEG750 does not inhibit cell proliferation even at relatively high concentration of 6 mg/ml. The observed excellent binding ability of quaternary (triphenyl‐) phosphonium centre with drug Fluorouracil and the low cytotoxicity in healthy cell lines make PQPTs promising candidates as carriers for drug/gene delivery targeting cells’ mitochondria. PEGylation quaternary (triphenyl‐) phosphonium tosylate (PQPT) with different length of polyethylene glycol chain was synthesized in a chromatography‐free manner. The observed excellent binding ability of quaternary (triphenyl‐) phosphonium centre with drug Fluorouracil and the low cytotoxicity to healthy cell lines make PQPTs promising candidates as carriers for drug/gene delivery.