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Abstract Many pharmaceutical agents possess low solubility and dissolution behavior. This drawback limited their applications in the pharmaceutical field. The aim of this study is to apply nanotechnology to improve the physicochemical properties of pharmaceutical agents so as to improve its bioavailability and, hence, its therapeutic and clinical activity. Nanoprecipitation technique was optimized in order to obtain nanoparticles of Quercetin with enhanced solubility and dissolution rate. In order to attain this target, the thesis is classified into two chapters: Chapter I: (Preparation and physicochemical characterization of Quercetin nanoparticles) In this chapter nanoprecipitation method was applied to prepare the nanoparticles and different parameters were studied to obtain optimum nanoparticles of the drug including, 1. Effect of polymer type 2. Effect of polymer concentration 3. Effect of homogenization time 4. Effect of homogenization intensity Results showed that the nanoparticles are greatly affected by the type of polymer; in addition, increasing the polymer concentrations resulted in decreasing the particle size of the nanoparticles. In addition, increasing the homogenization intensity and the homogenization time resulted in further decrease in the size of the nanoparticles. This is followed by characterization of the prepared nanoparticles that include the following: 1. Particles size analysis 2. Zeta potential 3. Differential scanning calorimetry 4. FT-Infra Red spectrophotometry 5. X-Ray diffraction pattern Results showed that preparing nanoparticles by nanoprecipitation technique resulted in varied physicochemical changes of the drug including Nanosizing the particles with accepted surface charge (zeta potential) that ranged between 30.4:36.6 mV , change in the crystalline structure and formation of hydrogen bonding between the drug and the used polymer. Chapter II (Pharmacokinetic evaluation of the prepared Quercetin Nanoparticles) In this chapter the optimum drug nanoparticles, as well as, the untreated drug was given to rabbits orally in a dose equivalent to 10 mg/kg. Different parameters were studied including, 1. The maximum concentration (Cmax) 2. The time of maximum concentration (Tmax) 3. The area under plasma concentration-time curve( AUC) 4. The area under first moment curve (AUMC) 5. The elimination rate constant 6. The half-life elimination 7. The absorption rate constant 8. The half-life absorption Results showed that the prepared nanoparticles produced significant increase in the AUC0- (from 113.4 to 341.2 ng.hr/ml) suggesting increasing the bioavailability of the drug. This is accompanied with increasing Cmax from (25.2 to 60.4 ng/ml) and slight decrease in the Tmax value to 1.6 hr. |