Small molecules drug conjugate mutual prodrug design (SMDC) composed of folate and lethal agent conjugate, rigidly bonded via hydrophilic bridge and self immolative disulfide bond ; represent new interesting approaches for cancer treatment , the component of SMDC intended for targeting folate receptor , along with greater conservation of component until reaching the target tumor tissue . The designing and synthesis of compound VI and VIII derived from 6-Mercaptopurine (6-MP) and Methotrexate ( MTX) conjugate altogether as mutual prodrugs were processed forward successfully by multistep reaction procedures , and by Thin Layer Chromatography (TLC) for
... Show MoreBackground: The treatment of schizophrenia typically involves the use of olanzapine (OLZ), a typical antipsychotic drug that has poor oral bioavailability due to its low solubility and first-pass effect. Objective: To prepare and optimize OLZ as nanoparticles for transdermal delivery to avoid problems with oral administration. Methods: The nanoprecipitation technique was applied for the preparation of eight OLZ nanoparticles by using different polymers with various ratios. Nanoparticles were evaluated using different methods, including particle size, polydispersity index (PDI), entrapment efficiency (EE%), zeta potential and an in vitro release study. The morphology was evaluated by a field emission scanning electron microscope (F
... Show MoreThis study aims to encapsulate atenolol within floating alginate-ethylcellulose beads as an oral controlled-release delivery system using aqueous colloidal polymer dispersion (ACPD) method.To optimize drug entrapment efficiency and dissolution behavior of the prepared beads, different parameters of drug: polymer ratio, polymer mixture ratio, and gelling agent concentration were involved.The prepared beads were investigated with respect to their buoyancy, encapsulation efficiency, and dissolution behavior in the media: 0.1 N HCl (pH 1.2), acetate buffer (pH 4.6) and phosphate buffer (pH 6.8). The release kinetics and mechanism of the drug from the prepared beads was investigated.All prepare
... Show MoreThis study aims to encapsulate atenolol within floating alginate-ethylcellulose beads as an oral controlled-release delivery system using aqueous colloidal polymer dispersion (ACPD) method.To optimize drug entrapment efficiency and dissolution behavior of the prepared beads, different parameters of drug: polymer ratio, polymer mixture ratio, and gelling agent concentration were involved.The prepared beads were investigated with respect to their buoyancy, encapsulation efficiency, and dissolution behavior in the media: 0.1 N HCl (pH 1.2), acetate buffer (pH 4.6) and phosphate buffer (pH 6.8). The release kinetics and mechanism of the drug from the prepared beads was investigated.All prepared atenolol beads remained f
... Show MorePulsatile drug delivery systems are time-controlled dosage forms which are designed to release the active pharmaceutical ingredient after a predetermined lag time to synchronize the disease circadian rhythm. A migraine shows circadian rhythm with a marked increase in attacks between 6 a.m. and 8 a.m.
Sumatriptan is a selective agonist at serotonin (5-Hydroxy tryptamine1 (5-HT1))receptors, is an effective treatment for acute migraine attacks.
The aim of this work is to prepare time-controlled press-coated tablet with a lag time of 5.45 hrs.
Six formulas of fast dissolving core tablets and three formulas of press-coated tablets were prepared by using direct compression method using different variables to prepa
... Show MoreMesoporous silica (MPS) nanoparticle was prepared as carriers for drug delivery systems by sol–gel method from sodium silicate as inexpensive precursor of silica and Cocamidopropyl betaine (CABP) as template. The silica particles were characterized by SEM, TEM, AFM, XRD, and N2adsorption–desorption isotherms. The results show that the MPS particle in the nanorange (40-80 nm ) with average diameter equal to 62.15 nm has rods particle morphology, specific surface area is 1096.122 m2/g, pore volume 0.900 cm3/g, with average pore diameter 2.902 nm, which can serve as efficient carriers for drugs. The adsorption kinetic of Ciprofloxacin (CIP) drug was studied and the data were analyzed and found to match well with
... Show MoreThe aim of present study was to develop gel formulation of microsponges of poorly soluble drug meloxicam (MLX) in order to enhance the release and dissolution of MLX which is the limitation for preparation in topical forms. Also skin delivery is an alternative administration for MLX that can minimize gastrointestinal (GI) side effects and improve patient compliance. The microsponges of MLX were prepared by quasi-emulsion solvent diffusion method. The effects of drug:polymer ratio, stirring time and Eudragit polymer type on the physical characteristics of microsponges were investigated and characterized for production yield, loading efficiency, particle size, surface morphology, and in vitro drug release from microsponges. The selec
... Show MoreThe aim of present study was to develop solid and liquid self-microemulsifying drug delivery system of poorly water soluble drug mebendazole using Aerosil 200 as solid carrier. Microemulsions are clear, stable, isotropic liquid mixtures of oil, water and surfactant, frequently in combination with a co-surfactant having droplet size range usually in the range of 20-250 nm. Oleic acid, tween 80 and polypropylene glycol were selected as oil, surfactant and co-surfactant respectively and for preparation of stable SMEDDS, micro emulsion region was identified by constructing pseudo ternary phase diagram containing different proportion of surfactant: co-surfactant (1:1, 2:1 and 3:1), oil and water. In brief S/ CoS mix means su
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