Mixed micelles of Pluronic F127 andD-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 evaluatedin vitroby 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 ( M) than the 10 : 0 combination ( 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.
The lysozyme (LZ)-entrapped mannosylated liposomes were prepared in this study by the use of N-octadecyl-D-mannopyranosylamine (SAMAN), which had been synthesized in-house and confirmed by characterization with FTIR and NMR. The reactant residues of synthesized SAMAN were found to be less than 1%. The mean sizes, zeta potentials, drug entrapment efficiencies, and loading capacities of all liposomal formulations were in the ranges of 234.7 to 431.0 nm, -10.97 to -25.80 mV, 7.52 to 14.10%, and 1.44 to 2.77%, respectively. The permeability of mannosylated LZ liposomes across Caco-2 cell monolayers was significantly enhanced to about 2.5- and 7-folds over those of conventional liposomes and solution, respectively, which might be due to the role of mannose receptor or mannose-binding protein on the intestinal enterocytes.
Abstract. the present study examined the antioxidant activity and protective effect of extracts from Asparagus racemosus roots against lipofectamine-induced apoptosis. Five fractions from a successive extraction process ranging from non-polar to more polar solvents were obtained. the total saponin content as a marker in terms of diosgenin equivalent value of the root extracts was found to be in the range of 240-420 µg/ mg extract, with higher values for the ethanol and aqueous fractions. the antioxidant activity measured using the dpph method in terms of mean effective concentration (Ec 50 ) of the aqueous fraction was found to be 600 µg/ml as compared to 1.5 µg/ml of ascorbic acid. it is proposed that Asparagus racemosus root extracts effectively inhibit lipofectamineinduced apoptosis by their protective effect, and may serve as an advantageous alternative option for gene delivery.
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