No abstract

No abstract

Thus it can be said that CSA coating can improve drug-loading capacity, control and sustain the release of CQ from such carriers, and can suitably act as safer and effective carriers for intravenous CQ administration.

This investigation is part of our ongoing effort to develop effective drug delivery systems for the treatment of Helicobacter pylori infection using polycarbonate (PC) floating microspheres as drug carriers. In an effort to augment the anti-H. pylori effect of acetohydroxamic acid (AHA), floating PC microspheres, which have the ability to reside in the gastrointestinal (GI) tract for an extended period, were prepared by emulsion (O/W) solvent evaporation technique. The effect of PC concentration on the morphology, particle size, entrapment efficiency and drug release rate was studied. In-vitro studies confirmed the excellent floating properties of PC microspheres. In-vitro and in-vivo growth inhibition studies were performed on developed system(s) taking isolated cultures of H. pylori and H. pylori-infected Mongolian gerbils, respectively. The drug and PC microspheres both showed anti-H. pylori activity in vivo, but the required dose of AHA was effectively reduced by a factor of 10 in the case of PC microspheres. In conclusion, the floating microspheres more effectively cleared H. pylori from the GI tract than the drug because of the prolonged gastric residence time resulting from the excellent buoyancy of the PC.

No abstract

The aim of the present study was to prepare and characterize novel vesicular carrier elastic liposomes, of most commonly used non-steroidal anti-inflammatory agent diclofenac for its sustained and targeted delivery. Elastic liposomes of diclofenac were prepared and characterized in vitro and in vivo. The effect of different formulation variables like type of surfactant, concentration of surfactant and dose of drug on transdermal flux, amount of drug deposited into the skin, muscle and plasma concentration was investigated. The biological activity of optimized formulation was evaluated using carrageenan induced rat paw edema model and results were compared with commercial hydrogel formulation. The elastic liposomal formulations achieved muscle drug concentration between 2.2+/-0.14 to 5.3+/-0.22 microg/g at 12 hr. The same dose of commercial hydrogel formulation produced drug levels between 0.41+/-0.07 to 1.1+/-0.09 microg/g in the muscle. Plasma concentration study showed regiospecificity of elastic liposomal formulation. The results of in vivo study revealed that incorporation of diclofenac in elastic liposomes increased its biological activity two fold as compared to commercial hydrogel formulation. The results of the present study demonstrated greater effectiveness of dermaly applied diclofenac elastic liposomal formulation in comparison to conventional delivery system. The optimized elastic liposomal formulation offers a promising means for the non-invasive treatment of local pain and inflammation by topical application.

Context:Bioavailability of conventional tablet of erythromycin stearate is low as it is unstable at acidic pH and also shows a low dissolution rate.Objective:It was proposed to protect it from the acidic condition of the stomach along with an increase in dissolution rate by formulating pH sensitive nanoparticles.Materials and Methods:The nanoparticles were prepared by the solvent evaporation technique using different quantities of Eudragit L100-55 and polyvinyl alcohol (PVA). Size reduction was achieved by high speed homogenization technique using Digital Ultra Turrax homogenizer. The formulation was optimized using 32 factorial design, keeping drug polymer ratio and surfactant concentration as independent variables. Particle size, entrapment efficiency, and drug-release (DR) were studied as dependent variables.Results:Optimized batch containing 1:0.3 erythromycin stearate: Eudragit L100-55 ratio and 1.0% PVA showed 8.24 ± 0.71% DR in pH 1.2 in 1-h and 90.38 ± 5.97% in pH 5.5 and pH 6.8 within 2-h, respectively.Discussion:The optimized batch exhibited lower release in acidic pH and faster release in higher pH compared to the marketed preparation.Conclusion:Thus the present study concludes that pH sensitive nanoparticles of erythromycin stearate increases the dissolution of the drug in intestinal pH and also protect it from acidic pH, which may help in improving the bioavailability of erythromycin.

No abstract