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bijps-413
Synthesis of new Conjugates of some NSAIDs with Sulfonamide as Possible Mutual Prodrugs using Tyrosine Spacer for Colon Targeted Drug Delivery
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The purpose of this research work is to synthesize conjugates of some NSAIDs with sulfamethoxazole as possible mutual prodrugs to overcome the local gastric irritation of NSAID with free carboxyl group by formation of ester linkage that supposed to remain intact in stomach and may hydrolyze in intestine chemically or enzymatically; in addition to that attempting to target the synthesized derivative to the colon by formation of azo group that undergo reduction only by colonic bacterial azo reductaze enzyme to liberate the parent compound to act locally (treatment of  inflammation and infections in colon).

Key words: Mutual prodrug, Ester linkage, Azo bond, Colon targeting

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Publication Date
Fri Jul 01 2022
Journal Name
Journal Of Molecular Structure
Interaction behavior of curcumin encapsulated onto functionalized SBA-15 as an efficient carrier and release in drug delivery
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In this work, mesoporous silica SBA-15 was prepared and functionalized with amine groups (i.e., NH2) to form NH2/SBA-15. The curcumin (CUR) was encapsulated into the surface and pore of NH2/SBA-15 to create CUR@NH2/SBA-15 as an efficient carrier in drug delivery systems (DDSs). The three samples (i.e., SBA-15, NH2/SBA-15, and CUR@NH2/SBA-15) were characterized. The study investigated the effect of the carrier dose, initial CUR concentration, pH, and contact time on the CUR loading efficiency (DLE%) via adsorption. The best DLE% for the SBA-15 and NH2/SBA-15 were found to be 45% and 89.7%, respectively. The Langmuir isotherm had a greater correlation coefficient (R2) of 0.998 for SBA-15. A pseudo-secondorder kinetic model seemed to fit well

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Publication Date
Tue Oct 22 2019
Journal Name
Scientia Pharmaceutica
Design, Synthesis, and Docking Study of Acyl Thiourea Derivatives as Possible Histone Deacetylase Inhibitors with a Novel Zinc Binding Group
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Histone deacetylase inhibitors with zinc binding groups often exhibit drawbacks like non-selectivity or toxic effects. Thus, there are continuous efforts to modify the currently available inhibitors or to discover new derivatives to overcome these problems. One approach is to synthesize new compounds with novel zinc binding groups. The present study describes the utilization of acyl thiourea functionality, known to possess the ability to complex with metals, to be a novel zinc binding group incorporated into the designed histone deacetylase inhibitors. N-adipoyl monoanilide thiourea (4) and N-pimeloyl monoanilide thiourea (5) have been synthesized and characterized successfully. They showed inhibition of growth of human colon adenoc

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Publication Date
Sat Jun 08 2024
Journal Name
Karbala International Journal Of Modern Science
Designing of Human Serum Albumin Nanoparticles for Drug Delivery: a Potential Use of Anticancer Treatment
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Human serum albumin (HSA) nanoparticles have been widely used as versatile drug delivery systems for improving the efficiency and pharmaceutical properties of drugs. The present study aimed to design HSA nanoparticle encapsulated with the hydrophobic anticancer pyridine derivative (2-((2-([1,1'-biphenyl]-4-yl)imidazo[1,2-a]pyrimidin-3-yl)methylene)hydrazine-1-carbothioamide (BIPHC)). The synthesis of HSA-BIPHC nanoparticles was achieved using a desolvation process. Atomic force microscopy (AFM) analysis showed the average size of HSA-BIPHC nanoparticles was 80.21 nm. The percentages of entrapment efficacy, loading capacity and production yield were 98.11%, 9.77% and 91.29%, respectively. An In vitro release study revealed that HSA-BIPHC nan

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Publication Date
Sun Oct 31 2021
Journal Name
Research Journal Of Pharmacy And Technology
A Review on Film Forming Drug Delivery Systems
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Conventional dosage forms for topical and transdermal drug delivery have several disadvantages related mainly to its poor skin permeation and patient compliance. Many approaches have been developed to improve these dosage forms. Film forming drug delivery systems represents a recent advancement in this field. It provides improved patient compliance with enhanced skin permeation of drugs. In its simplest form, these consist of a polymeric solution, usually in a supersaturated state, in a suitable solvent. A plasticizer is usually added to improve the flexibility and enhance the tensile strength to the film. It is also possible to control and sustain the drug release from the films by controlling the polymeric content, concentration o

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Publication Date
Wed Jul 07 2021
Journal Name
International Journal Of Applied Pharmaceutics
APPLICATION OF 3D PRINTING IN INNOVATED DRUG DELIVERY: A REVIEW
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Increasing requests for modified and personalized pharmaceutics and medical materials makes the implementation of additive manufacturing increased rapidly in recent years. 3D printing has been involved numerous advantages in case of reduction in waste, flexibility in the design, and minimizing the high cost of intended products for bulk production of. Several of 3D printing technologies have been developed to fabricate novel solid dosage forms, including selective laser sintering, binder deposition, stereolithography, inkjet printing, extrusion-based printing, and fused deposition modeling. The selection of 3D printing techniques depends on their compatibility with the printed drug products. This review intent to provide a perspecti

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Publication Date
Sun Jun 05 2016
Journal Name
Baghdad Science Journal
Synthesis, Characterization of Derivatives Tetrazoles for Trimethoprim Drug
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The present work involved synthesis of serval new substituted tetrazole via Schiff bases for trimethoprim drug by two steps. The first step involved direct reaction of different ketones and aldehydes with trimethoprim producing the corresponding Schiff bases (1-10), whereas the second step, involved preparation new tetrazoles derivatives (11-20) through reaction of the ready Schiff bases (in the first step) with sodium azidein in dioxin. The prepared compounds were characterized by UV, FT-IR, and some of them by 13C-NMR, 1H-NMR spectroscopy and physical properties.

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Publication Date
Sat Nov 01 2025
Journal Name
Bulletin Of The Chemical Society Of Ethiopia
SYNTHESIS, CHARACTERIZATION, THERMAL ANALYSIS AND ANTIOXIDANT DETERMINATION FOR SOME METAL IONS COMPLEXES WITH NEW LIGAND
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The research includes the preparation of a new Schiff base(4-methyl-2-((2-phenyl hydrazineylidene)methyl)naphthalen-1-ol), which was subsequently, used to prepare a series of complexes using chlorides of Mn2+, Co2+, Cu2+, Cr3+, and Fe3+ ions. The synthesized compounds were characterized using various techniques such as elemental microanalysis (C.H.N), chloride content determination using Mohr’s method, FT-IR spectroscopy, UV-Visible, mass spectra, conductivity, DSC (Differential Scanning Calorimetry), and thermogravimetric analysis. Overall, the decay of the ligand and its metal complexes was recorded to determine their thermal stability and weight-loss profiles. The results indicated that ligand acts as a bidentate doner, coordinating wi

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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
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 Dec 25 2022
Journal Name
International Journal Of Drug Delivery Technology
Design and Evaluation of Solid Lipid Nanoparticle Eye Drops Containing VRN for Ocular Drug Delivery
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As a well-known oral and intravenous antifungal, voriconazole (VRN) has an extensive history of usage in the medical field. Solid lipid nanoparticles (SLNs) have been produced to treat ocular fungal keratitis in the eye. A 32Box-behnken design was used to produce a variety of new formulas for hot-melt extrusion. The SLNs were evaluated by entrapment efficiency (EE percent), particle size (PS), polydispersity index (PDI), and zeta potential (ZP). A series of in-vitro and in-vivo studies were carried out on the new formula. The produced vesicles’ EE, PS, PDI, and ZP values were all good. SLNs eye drops were numerically adjusted to include carbopol, a stabilizer, lipids, and a surfactant, among other substances. ZP of -36.5 ± 0.20 m

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