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Formulation and Characterization of Isradipine Nanoparticle for Dissolution Enhancement
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Isradipine belong to dihydropyridine (DHP) class of calcium channel blockers (CCBs). It is  used in the treatment of hypertension, angina pectoris, in addition to Parkinson disease. It goes under the BCS class II drug (low solubility-high permeability). The drug will experience extensive first-pass metabolism in liver, therefore, oral bio-availability will be approximately15 to 24 %.

 

 The aim of this study was to formulate and optimize a stable  nanoparticles of a highly hydrophobic drug, isradipine by anti-solvent microprecipitation Method to achieve the higher in vitro dissolution rate, so that it will be absorbed by intestinal lymphatic transport in order to avoid hepatic first-pass metabolism  and improve drug bioavailability.

 

Twenty one formulas of Isradipine nanoparticles were prepared by antisolvent precipitation method utilizing one of these polymers (Poloxamer 188, PVP-k30, HPMC E5, PVA, Poloxamer 407, and Soluplus) at different drugs: polymer ratios. The polymer type, the drug to polymer ratio, ultrasonication power and the effect of addition of co-stabilizer on the particle size, and polydispersity index (PDI)  were investigated.

 

Among all the prepared nanoparticles formulas, formula (F9) which contain Soluplus as a stabilizer at polymer: drug ratio of (1:0.75) and solvent: antisolvent ratio of (1:9) was considered as the optimum formula which shows good evaluation parameters in addition to the increment in the solubility to about 10 times than that of the pure drug. The investigations of the drug–excipients compatibility studies by FTIR and DSC, crystalline state by P-XRD, surface morphology by SEM were done. Moreover, the analysis by DSC and SEM of the nanoparticles of the selected formula (F12) indicate a reduction in the crystallinity and amorphization of the drug. It can be concluded that the dissolution rate of Isradipine was significantly increased through particle size reduction to nanosize.

 

 

 

 

 

 

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Publication Date
Fri Aug 02 2024
Journal Name
Farmacia
SOLUPLUS AND SOLUTOL HS-15 OLMESARTAN MEDOXOMIL NANOMICELLE BASED ORAL FAST DISSOLVING FILM: IN VITRO AND IN VIVO CHARACTERIZATION
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Olmesartan medoxomil (OM) has low bioavailability and limited solubility. To enhance bioavailability, fast dissolving films (FDF) with mixed micelles of soluplus (SPL) and solutol HS15 (STL H15) were developed using solvent casting. The optimised formula, FM2, used polyvinyl alcohol (PVA) and showed high entrapment efficiency, rapid disintegration, and significant improvement in OM bioavailability compared to the market tablet (Olmetec®). FM2 also demonstrated stability and potential for enhanced drug delivery.

Publication Date
Thu Aug 16 2012
Journal Name
Journal Of Chemical And Pharmaceutical Research
Synthesis, Characterization, Schiff Base Phenyl 2-(2-hydroxybenzylidenamino)benzoate and its complexes with LaIII,Cr III and Pr III
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The aim of the work is the synthesis and characterization of the tridentate Schiff base (HL) containing (N and O) as donor atoms type (ONO). The ligand is: (HL) phenyl 2-(2-hydroxybenzylidenamino)benzoate . This ligand was prepared by the reaction of (phenyl 2-aminobenzoate) with salicylaldehyde under reflux in ethanol and few drops of glacial acetic acid which gave the ligand (HL). The prepared ligand was characterized by (FT IR,UV–Vis) spectroscopy, Elemental analysis of carbon, hydrogen and nitrogen (C.H.N.) and melting point. The ligand was reacted with some metal ions under reflux in ethanol with (1 metal :2 ligand )mole ratio which gave complexes of the general formula: [M(L)2]Cl , M = Cr III La III and , Pr III Products were found

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Publication Date
Thu Jun 01 2023
Journal Name
Baghdad Science Journal
Mn(II),Fe(III),Co(II)and Rh(III) complexes with azo ligand: Synthesis, characterization, thermal analysis and bioactivity
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New series of metal ions complexes have been prepared from the new ligand [4-Amino-N-(5-methyl-isaxazol-3-yl)-benzenesulfonamide] derived from Sulfamethoxazole and 3-aminophenol. Accordingly, mono-nuclear Mn(II), Fe(III), Co (II), and Rh(III) complexes were prepared by the reaction of previous ligand with MnCl2.4H2O, CoCl2.6H2O, FeCl3.6H2O and RhCl3H2O, respectively. The compounds have been characterized by Fourier-transform infrared (FTIR), ultraviolet–visible (UV–vis), mass,  1H-, and 13C-nuclear magnetic resonance (NMR) spectra and thermo gravimetric analysis (TGA& DSC) curve, Bohr magnetic (B.M.), elemental microanal

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Publication Date
Tue Jan 12 2021
Journal Name
Systematic Review In Pharmacy
CUPPER(||)AND MERCURY (||)Complexes WITH SCHIFF BASE LIGAND FROM BENZIDIN WITH ISATIN AND BENZOIN:SYNTHESIS,SPECTRAL CHARACTERIZATION, THERMAL STUDIES AND BIOLOGICAL ACTIVITIES
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CUPPER(||)AND MERCURY (||)Complexes WITH SCHIFF BASE LIGAND FROM BENZIDIN WITH ISATIN AND BENZOIN:SYNTHESIS,SPECTRAL CHARACTERIZATION, THERMAL STUDIES AND BIOLOGICAL ACTIVITIES

Publication Date
Sun Jan 01 2023
Journal Name
Materials Today: Proceedings
Preparation, characterization and preliminary cytotoxic evaluation of 6-mercaptopurine-coated biotinylated carbon dots nanoparticles as a drug delivery system
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Publication Date
Sun Jan 01 2023
Journal Name
Materials Today: Proceedings
Preparation, characterization and preliminary cytotoxic evaluation of 6-mercaptopurine-coated biotinylated carbon dots nanoparticles as a drug delivery system
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Publication Date
Wed Jul 01 2020
Journal Name
International Journal Of Pharmaceutical Research
Synthesis, characterization of new Schiff base compounds contains 5H-thiazolo[3,4-b][1,3,4] thiadiazole and study its biological activity
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A new derivatives of Schiff bases connected with 5H-thiazolo[3,4-b][1,3,4]thiadiazole ring 5a-c were prepared via many reactions starting by treating 1,4-phenylene diamine 1 with chloroacetylchloride to prepared compound 2, then reaction with p-hydroxybenzaldehyde to synthesize compound 3 then, this was reacted with thioglycolic acid and thiosemicarazide to giveN,N-(1.4-phenylene)bis(2-(4-(2-amino-5Hthiazolo[4,3-b][1,3,4]thiadiazol-5-yl)phenoxy)acetamide) 4. Compound 4 was treated with different aromatic aldehydes to give a new derivatives of Schiff bases containing 5H-thiazolo[3,4-b][1,3,4]thiadiazole ring 5a-c. The synthesized compounds were characterized using FTIR spectrophotometer and 1H NMR spectroscopy and the biological activity of

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Publication Date
Sun Mar 04 2018
Journal Name
Baghdad Science Journal
Synthesis, Characterization and Biological Activates Studies of some New Derivatives From 2-aminoo-5-mercapto-1, 3, 4-thiadiazole
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In this work, thiadiazole derivatives were prepared by taking advantage of active sites in (2-amino-5-mercapto-1, 3, 4-thiadiazole) as a starting material base. The main heterocyclic compounds (1, 3, 4-thiadiazole, oxazole) etc, 2-amino-5-mercapto-1,3,4-thiadiazole compound (1) was prepared by cyclic closure of thiosemicarbazide compound with anhydrous sodium carbonate and carbon disulfide. Oxidation of (1) via hydrogen peroxide, to have (2) which was treated with chloro acetyl chloride to get (3). Preparation of thiazole ring (4) was from reacting of (3) with thiourea. Synthesis of diazonium salts (5) from compound (4) using sodium nitrite and HCl. Compound (5) reacted with different ester compounds to prepare a new azo compounds (6–8).C

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Publication Date
Sat May 20 2023
Journal Name
Baghdad Science Journal
Synthesis, Characterization and Anticancer Activity of Chitosan Schiff Base / PVP Gold Nano Composite in Treating Esophageal Cancer Cell Line
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In the present paper, chitosan Schiff base has been synthesized from chitosan’s reaction with the salicyldehyde. The AuNPs was manufacture by extract of onion peels as a reducing agent. The Au NPs that have been prepared were characterized through the UV-vis spectroscopy, XRD analyses and SEM microscopy. The polymer blends of the chitosan Schiff base / PVP has been prepared through using the approach of solution casting. Chitosan Schiff base / PVP Au nano-composites was prepared. Nano composites and polymer blends have been characterized by FTIR which confirm the formation of Schiff base by revealing a new band of absorption at 1651cm-1 as a result of the (C=N) imine group. SEM, DSC and TGA confirms the thermal stability of the pr

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Publication Date
Fri Feb 14 2014
Journal Name
Journal Of Basic Microbiology
Isolation and characterization of lytic vibriophage against <i>Vibrio cholerae</i> O1 from environmental water samples in Kelantan, Malaysia
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Water samples from a variety of sources in Kelantan, Malaysia (lakes, ponds, rivers, ditches, fish farms, and sewage) were screened for the presence of bacteriophages infecting Vibrio cholerae. Ten strains of V. cholerae that appeared to be free of inducible prophages were used as the host strains. Eleven bacteriophage isolates were obtained by plaque assay, three of which were lytic and further characterized. The morphologies of the three lytic phages were similar with each having an icosahedral head (ca. 50–60 nm in diameter), a neck, and a sheathed tail (ca. 90–100 nm in length) characteristic of the family Myoviridae.

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