Synthesis and Preliminary Kinetic Study of 5-fluorouracil Derivatives for Targeting Colon Tumor

5-Fluorouracil (5-FU) is used widely as an anticancer drug to treat solid cancers, such as colon, breast, rectal, and pancreatic cancers; although it’s clinical application is greatly limited by its short plasma half-life, poor tumor affinity, myelosuppression, and gastrointestinal toxicity. To tackle these problems, numerous modifications of the 5- Fu structure have been performed.Thus, 5-Fu as possible colon specific prodrugs were synthesized in which 5-Fu is attached to amino acids (alanine & phenylalanine) using succinate group as a spacer via amide or ester bond. An approach to improve the properties of 5-fluorouracil is the chemical transformation into bioreversible derivatives (prodrugs) which are converted to the parent drug by enzymatic and / or chemical hydrolysis. The synthesis of the target compounds were accomplished following multistep reaction procedures, the chemical reaction followed up and the purity of the products were checked by TLC.   The structures of the final compounds were confirmed by their melting points, infrared spectroscopy and 1H-NMR spectra. The hydrolysis of compounds III, IV, V, and VI in aqueous buffer solutions of pH 1.2 and pH 7.4 were studied.   Compounds III, IV, V and VI had enough stability at pH 1.2 (t = 429.874min, t =429.874min, t=334.336min and t =376.139min respectively) and at pH 7.4 (t=601.823min, t=601.823min, t=429.874min and t=501.519min respectively); expecting that hydrolysis of these compounds by microbial enzymes in the colon will deliver 5-fluorouracil spontaneously

Formulation and In Vitro Evaluation of Mucoadhesive Antimicrobial Vaginal Tablets of Ciprofloxacin Hydrochloride

Ciprofloxacin is a broad spectrum fluoroquinolone, effective in the treatment of a wide range of infections, including genitourinary tract infections. In this study, bioadhesive vaginal tablets of ciprofloxacin hydrochloride were prepared by direct compression method using a combination of bioadhesive polymers carbopol 934P(Cp), carboxymethylcellulose (CMC) and sodium alginate (SA) in different ratios. The prepared tablet formulations were characterized by measuring their swelling capacity, surface pH, bioadhesive properties, and in-vitro drug dissolution. It was found that the bioadhesive force was directly proportional to carbopol 934P content in different formulae and was further enhanced by the inclusion of carboxymethylcellulose. Swelling studies indicated that formulae containing a combination of carbopol 934P and sodium alginate or carboxymethylcellulose had greater swelling index than those containing carbopol 934P alone. Formulations containing Carbopol 934P and carboxymethylcellulose were found to swell to a greater extent than those composed of similar ratios of carbopol and sodium alginate. In vitro drug release study showed that the release of ciprofloxacin hydrochloride from formulae containing carboxymethylcellulose was faster than from those containing sodium alginate. Formula F5 composed of CP/CMC in a ratio of 2:1 showed moderate swelling, suitable bioadhesion and retardation of drug release. Thus, it may be considered a good candidate as a base for bioadhesive vaginal table

Preparation and evaluation of lipid matrix microencapsulation for drug delivery of azilsartan kamedoxomil

The aim of the work is to consolidate azilsartan-kamedoxomil (AZM) into lipid matrix controlled-release microparticles to enhance its permeability because AZM belongs to Biopharmaceutical classification (BCS) IV which characterized by poor permeability and to protect AZM from light and humidity and execute a prolonged release profile. Materials and methods. A reversed-phase HPLC method was created and validated to estimate the drug. AZM microparticles formulations were invented using melt dispersion technique and waxy materials such as carnuba wax, beeswax, stearic acid in the ratio of waxy-substance: drug ranging from 0.25: 1 to 1:1 and stabilizer namely; tween 80 and Poloxamer 407 in ratio of stabilizer: drug ranging from 0.5:1 to 1:1. Azilsartan formulations were assessed for azilsartan-medoxomil content, loading, entrapment efficiency, the zeta potential,the particle size, the morphology by scanning electronic microscopy (SEM), and in-vitro release profile. Results. Zeta potential results for microparticle formulations using beeswax and carnuba range from -21.1 mV to -26.6 mV and -20.6 mV to -26.7 mV, respectively. This difference indicates that the azilsartan microparticles containing stearic acid are better stabilized with zeta potential of 25.3 - 29.7 mV. Furthermore, the release from azilsartan microparticle formulations containing stearic acid exceeded 80 % after 8 h and remained for 24 h while release from beeswax did not exceed 65 % after the same period and less than 60 % in case of carnuba formulations Conclusions. The formulation (AZSP4) exhibited the highest zeta potential and released exceeding 80 % of AZM over the course of 8 hours and remained over a day. AZSP4 microparticles formulation containing, poloxamer 407, in a 0.8:0.8:1 drug: stearic acid: poloxamer ratio proved the ability of stearic acid microencapsulation employing poloxamer as stabilizer in a certain ratio can prolong the release of AZ

Formulation, characterization and evaluation of vildagliptin and metformin combined tablets

The current study was conducted to formulate and assess combined vildagliptin (VD) and metformin hydrochloride (MET) tablets. The formulations were developed by wet granulation to overwhelm the reduced compressibility of MET powder. Polymers like Kollidon K30 and K90 were used to prepare formulations. Micromeritics characteristics of blends were assessed. Subsequently, the tablets that had been manufactured were assessed for post-compression characteristics. The composition formula F7 was optimal due to having the best hardness, friability and good dissolution

Formulation, characterization and evaluation of vildagliptin and metformin combined tablets

The current study was conducted to formulate and assess combined vildagliptin (VD) and metformin hydrochloride (MET) tablets. The formulations were developed by wet granulation to overwhelm the reduced compressibility of MET powder. Polymers like Kollidon K30 and K90 were used to prepare formulations. Micromeritics characteristics of blends were assessed. Subsequently, the tablets that had been manufactured were assessed for post-compression characteristics. The composition formula F7 was optimal due to having the best hardness, friability and good dissolution

Preparation and evaluation of lipid matrix microencapsulation for drug delivery of azilsartan kamedoxomil

The aim of the work is to consolidate azilsartan-kamedoxomil (AZM) into lipid matrix controlled-release microparticles to enhance its permeability because AZM belongs to Biopharmaceutical classification (BCS) IV which characterized by poor permeability and to protect AZM from light and humidity and execute a prolonged release profile. Materials and methods. A reversed-phase HPLC method was created and validated to estimate the drug. AZM microparticles formulations were invented using melt dispersion technique and waxy materials such as carnuba wax, beeswax, stearic acid in the ratio of waxy-substance: drug ranging from 0.25: 1 to 1:1 and stabilizer namely; tween 80 and Poloxamer 407 in ratio of stabilizer: drug ranging from 0.5:1 to 1:1. Azilsartan formulations were assessed for azilsartan-medoxomil content, loading, entrapment efficiency, the zeta potential,the particle size, the morphology by scanning electronic microscopy (SEM), and in-vitro release profile. Results. Zeta potential results for microparticle formulations using beeswax and carnuba range from -21.1 mV to -26.6 mV and -20.6 mV to -26.7 mV, respectively. This difference indicates that the azilsartan microparticles containing stearic acid are better stabilized with zeta potential of 25.3 - 29.7 mV. Furthermore, the release from azilsartan microparticle formulations containing stearic acid exceeded 80 % after 8 h and remained for 24 h while release from beeswax did not exceed 65 % after the same period and less than 60 % in case of carnuba formulations Conclusions. The formulation (AZSP4) exhibited the highest zeta potential and released exceeding 80 % of AZM over the course of 8 hours and remained over a day. AZSP4 microparticles formulation containing, poloxamer 407, in a 0.8:0.8:1 drug: stearic acid: poloxamer ratio proved the ability of stearic acid microencapsulation employing poloxamer as stabilizer in a certain ratio can prolong the release of AZ

Extraction, characterization and evaluation of the plant extract of Tamarix as an antibiotic to treat types of burns bacteria

Background : Tamarixaphylla (L.) is included in our common and large species, The genus Tamarix L. belongs to the Tamaricaceae family.Tamarix species are employed in traditional medicine as astringent, aperitif, stimulus of perspiration and diuretic.leaves are considered as a source for curing different infectious diseases.. (Marwat et al 2003, Panhwar et al 2007), The good antimicrobial activities of medicinal plants are due to the presence of secondary metabolites., Aim of study To find out the antimicrobial activity of the aqueous and alcoholic extracts of tamex in the bacterial species S. epidermidis, s. mutanss, s. aureas, E. coli and burns infections, Material and methods: Chemical detection of active compounds were investigated The presence of active compounds and used agar diffusion method is used to test the effectiveness of the extracts as antibacterial, Results and discussion :The presence of these compounds in extracts of the Tamex plant, which are compounds that have an effective effect in inhibiting the growth of various microorganisms, is important because most of the therapeutic effects are attributed to them

Evaluation of Eruca Sativa and Capsicum annuum alcoholic extracts as pesticide against aphid and whitefly pests

The aphid (Aphidoidea family) and the whitefly (Aleyrodidae family) are closely related, quickly breeding insects that, when infected, render plants susceptible to diseases since they suck the juices of these plants. They damage the aerial parts of plants and even their roots. Their control is of high concern to limit the damage and minimize the loss of the crops with the use of the safest pesticides. The present study was conducted to assess the perished effect of the Eruca sativa (local name: arugula) leaves and the Capsicum annuum (local name: hot pepper) fruits on aphids and on the eggs and nymphs of whitefly by spraying their alcoholic extracts on tested species. Three pesticide concentrations (0.5, 1 and 1.5%) of either extract were prepared and tested. Adhesives, propellants and other materials were added to the extracts to enhance their effectiveness. The results indicated that the pesticide prepared from these extracts has a concentration- and time-dependent impact on the growth of all tested species; the highest mortality rate was achieved at 1.5% concentrations. The time required for that highest effect was 72 hours for Eruca sativa leaf extract on aphids (100%); and on the eggs (89%) and nymphs (94.1%) of whiteflies. Meanwhile, the highest mortality rates achieved by 1.5% Capsicum annuum fruit extract were after 48 hours on aphids (100%), on the nymphs of whiteflies (100%), and 72 hours on whitefly eggs (96.4%). These effects may be related to the presence of many bioactive substances that were detected in the extracts of these two plants, including tannins, glycosides, phenols, resins, flavonoids, saponins, alkaloids, coumarin, steroids and terpenes