In vitro characterization of pluronic F127 and D-α-tocopheryl polyethylene glycol 1000 succinate mixed micelles as nanocarriers for targeted anticancer-drug delivery

Abstract

Mixed micelles of Pluronic F127 and d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) in different molar ratios (10: 0, 7: 3, 5: 5, and 3: 7) were prepared to characterize this system as nanocarriers for targeted delivery of chemotherapeutic agents. Their size, zeta potential, critical micelle concentration, drug loading content, entrapment efficiency, drug release, cytotoxicity, and stability in serum were evaluated in vitro by using doxorubicin as the model anticancer drug. The micellar sizes ranged from 25 to 35 nm. The 7: 3 and 5: 5 micellar combinations had lower critical micelle concentrations (5×10-5 M) than the 10: 0 combination (5×10-4 M). The entrapment efficiencies of the 7: 3, 5: 5, and 3: 7 micellar combinations were 72, 88, and 69, respectively. Doxorubicin release was greater at acidic tumour pH than at normal physiological pH. The doxorubicin-loaded mixed micelles showed greater percent inhibition and apoptosis activity in human breast adenocarcinoma (MCF-7) and acute monocytic leukaemia (THP-1) cell lines than free doxorubicin did. The mixed micelles were also stable against aggregation and precipitation in serum. These findings suggest that Pluronic F127-TPGS mixed micelles could be used as nanocarriers for targeted anticancer-drug delivery. © 2012 Adeel Masood Butt et al.