Carbamazepine (CBZ) is used in the treatment of generalized tonic clonic and partial seizures. In seizure disorder the focal point of treatment is brain. At present no commercial parenteral formulation of CBZ is available. We developed o/w nanoemulsions of CBZ stabilized by 1-O-alkylglycerol/lecithin for intravenous administration and evaluated the brain targeting potential of these formulations. The nanoemulsions were characterized for globule size, zeta potential (ZP), CBZ content and in vivo tissue distribution in mice. The in vivo data revealed a significant uptake of CBZ in all tissues. Among the nanoemulsions, 1-O-decylglycerol stabilized system showed significantly higher tissue levels and availability of CBZ. Particularly for this system 2.37 times higher brain availability and a brain/serum concentration ratio of 3.0 at 30 min is an important finding. This indicates the brain targeting potential. A systematic formulation development of CBZ nanoemulsions employing 1-O-alkylglycerols might pave way to achieve selective brain delivery of this important antiepileptic drug.
Ciprofloxacin is routinely prescribed to treat a variety of infections, including those of the urinary tract. To achieve optimum therapeutic benefits of the drug, all of the factors which influence its pharmacokinetics and effectiveness need to be determined. This study investigated the urinary excretion kinetics of ciprofloxacin upon oral administration of a single dose of 250 mg at 1000 or 2200 h in 12 healthy human subjects in a crossover design. The urine samples were analyzed for unchanged ciprofloxacin by a sensitive high-performance liquid chromatography method. A significant decrease in the rate and extent of ciprofloxacin excretion following 2200 h (109.59 versus 53.8 mg [P < 0.05]) administration was observed. This result may be due to circadian changes in the factors affecting renal excretion and also probably metabolism of ciprofloxacin.
Various fractions of the alcoholic extract of the roots of SALACIA MACROSPERMA were evaluated for their antidiabetic activity in alloxan-diabetic rats by estimating various biochemical parameters in blood, viz. glucose, proteins, lipids, cholesterol, and free fatty acids, after oral administration for 8 days. From the data obtained, it is concluded that the methanolic fraction followed by the residual fraction of the alcoholic extract exhibited significant antidiabetic activity. These biofractions were able to correct the metabolic abberations in diabetic rats. This activity may be due to their insulin-like properties.
The aim of this study is to develop ascorbyl palmitate (ASP) loaded doxorubicin (DOX) pegylated liposomes and to evaluate their targeting potential to tumor. We have prepared conventional (DL), pegylated DOX liposomes with (SDL) and without ascorbyl palmitate (SDL-A). The vesicle size in all the formulations was within the range 105-120 nm and in vitro release studies in serum confirmed the stability of the liposomes. Biodistribution studies carried out in Ehrlich ascites tumor bearing mice indicate higher area under the curve for SDL and SDL-A liposomes compared to DL and plain drug solution. Drug targeting index assessed from tumor-to-serum concentration ratio and therapeutic availability of DOX in tumor tissue was also significantly higher for pegylated liposomes. In conclusion, biodistribution study reveals that the presence of ascorbyl palmitate alters the distribution pattern of liposomes and paves way for better drug targeting.
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