scholarly journals Terpenoid Hydrazones as Biomembrane Penetration Enhancers: FT-IR Spectroscopy and Fluorescence Probe Studies

Molecules ◽  
2021 ◽  
Vol 27 (1) ◽  
pp. 206
Author(s):  
Mariia Nesterkina ◽  
Serhii Smola ◽  
Nataliya Rusakova ◽  
Iryna Kravchenko
Keyword(s):  
Fluorescence Probe ◽  
Fluorescence Analysis ◽  
Penetration Enhancers ◽  
Molecular Organization ◽  
Fluorescence Probes ◽  
Ultrasonic Dispersion ◽  
Major Mechanism ◽  
Polar Groups ◽  
Ft Ir

Hydrazones based on mono- and bicyclic terpenoids (verbenone, menthone and carvone) have been investigated in vitro as potential biomembrane penetration enhancers. In this regard, liposomes composed of lecithin or cardiolipin as phospholipid phase components with incorporated fluorescence probes have been prepared using the thin-film ultrasonic dispersion method. The mean particle size of the obtained liposomes, established using laser diffraction, was found to be 583 ± 0.95 nm, allowing us to categorize them as multilamellar vesicles (MLVs) according to their morphology. Pursuant to fluorescence analysis, we may assume a reduction in microviscosity and, consequently, a decrease in the packing density of lecithin and cardiolipin lipids to be the major mechanism of action for terpenoid hydrazones 1–15. In order to determine the molecular organization of the lipid matrix, lipids were isolated from rat strata cornea (SCs) and their interaction with tested compounds was studied by means of Fourier transform infrared spectroscopy. FT-IR examination suggested that these hydrazones fluidized the SC lipids via the disruption of the hydrogen-bonded network formed by polar groups of SC constituents. The relationship between the structure of terpenoid hydrazones and their ability to enhance biomembrane penetration is discussed.

A study of ultrasound/H2O2 combined surface modification on polyglycolic acid monofilaments for acupoint catgut embedding therapy application

2018 ◽  
Vol 89 (15) ◽  
pp. 3112-3126
Author(s):  
Shaoju Fu ◽  
Dongchao Yang ◽  
Cunyi Zhao ◽  
Peihua Zhang
Keyword(s):  
Surface Modification ◽  
Cell Attachment ◽  
Polyglycolic Acid ◽  
Contact Angles ◽  
Swelling Behavior ◽  
Polar Groups ◽  
Embedding Therapy ◽  
Ft Ir ◽  
Ir Analysis

Polyglycolic acid (PGA) monofilament has been regarded as an excellent acupoint catgut embedding therapy (ACET) material because it offers numerous advantages, including easy accessibility and good forming and degradable properties. However, the poor hydrophilicity and cytocompatibility are the main disadvantages preventing it from having wider applications. In this communication, two types of PGA monofilaments were first fabricated from their polymer chips, followed by ultrasound/H2O2 combined surface modification at 1:1 (V/V), and different ultrasound frequencies (45, 60 and 75 KHz) were explored. The modified PGA monofilaments were fully characterized with respect to structure characterizations (surface morphology, weights and diameters, Fourier transform infrared spectroscopy (FT-IR) analysis and hydrophilicity), mechanical properties (tensile property, swelling behavior and flexibility) and in vitro properties (cytotoxicity, cell attachment and cell morphology). The results showed that the PGA monofilaments after modification would become coarser, with larger weights and diameters. Samples 1-PGA 75 and 2-PGA 75 exhibited the smallest contact angles at 70.51° ± 3.27° and 62.84° ± 2.53°, respectively. The FT-IR analysis results confirmed that some polar groups emerged, promoting the hydrophilicity of PGA monofilaments. The swelling behavior of monofilaments was enhanced, while tensile and bending stiffness values slightly decreased. All the prepared samples presented no toxicity, and the cell attachment ratio (cultured for 48 h) of PGA monofilaments had been greatly improved after modification. These findings present important clinical implications in the ACET materials manufacturing process and warrant further study to develop new PGA embedding materials with outstanding clinical efficacy.

Characterization and Screening of a Novel Multiparticulate Pulsatile Delivery of Aceclofenac

2016 ◽  
Vol 9 (5) ◽  
pp. 3494-3501
Author(s):  
Bipul Nath ◽  
Santimoni Saikia
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Alginate Beads ◽  
In Vitro Drug Release ◽  
Dsc Studies ◽  
Ft Ir ◽  
Lag Period ◽  
Pulsatile Delivery ◽  
Ca Alginate

In the present investigation, sodium alginate based multiparticulate system overcoated with time and pH dependent polymer was studied in the form of oral pulsatile system to achieve pulsatile with sustained release of aceclofenac for chronotherapy of rheumatoid arthritis seven batches of micro beads with varying concentration of sodium alginate (2-5 %) were prepared by ionotropic-gelation method using CaCl2 as cross-linking agent. The prepared Ca-alginate beads were coated with 5% Eudragit L100 and filled into pulsatile capsule with varying proportion of plugging materials. Drug loaded microbeads were investigated for physicochemical properties and drug release characteristics. The mean particle sizes of drug-loaded microbeads were found to be in the range 596±1.1 to 860 ± 1.2 micron and %DEE in the range of 65-85%. FT-IR and DSC studies revealed the absence of drug polymer interactions. The release of aceclofenac from formulations F1 to F7 in buffer media (pH 6.8) at the end of 5h was 65.6, 60.7, 55.7, 41.2, 39.2, 27 and 25% respectively. Pulsatile system filled with eudragit coated Ca-alginate microbeads (F2) showed better drug content, particle size, surface topography, in-vitro drug release in a controlled manner. Different plugging materials like Sterculia gum, HPMC K4M and Carbopol were used in the design of pulsatile capsule. The pulsatile system remained intact in buffer pH 1.2 for 2 hours due to enteric coat of the system with HPMCP. The enteric coat dissolved when the pH of medium was changed to 7.4. The pulsatile system developed with Sterculia gum as plugging material showed satisfactory lag period when compared to HPMC and Carbopol.

Solubility Enhancement of Poorly Water-Soluble Antifungal Drug Acyclovir by Nanocrystal Formulation Approach

2018 ◽  
Vol 11 (2) ◽  
pp. 4036-4042
Author(s):  
Prakash Goudanavar ◽  
Ankit Acharya ◽  
Vinay C.H
Keyword(s):  
Chemical Interaction ◽  
Research Work ◽  
Antiviral Drug ◽  
In Vitro Release ◽  
Oral Route ◽  
Water Soluble ◽  
Precipitation Method ◽  
Dsc Studies ◽  
Ft Ir

Administration of an antiviral drug, acyclovir via the oral route leads to low and variable bioavailability (15-30%). Therefore, this research work was aimed to enhance bioavailability of acyclovir by nanocrystallization technique. The drug nanocrystals were prepared by anti-solvent precipitation method in which different stabilizers were used. The formed nanocrystals are subjected to biopharmaceutical characterization including solubility, particle size and in-vitro release. SEM studies showed nano-crystals were crystalline nature with sharp peaks. The formulated drug nanocrystals were found to be in the range of 600-900nm and formulations NC7 and NC8 showed marked improvement in dissolution velocity when compared to pure drug, thus providing greater bioavailability. FT-IR and DSC studies revealed the absence of any chemical interaction between drug and polymers used. 

The Development of Pemetrexed Diacid-Loaded Gelatin-Cloisite 30B (MMT) Nanocomposite for Improved Oral Efficacy Against Cancer: Characterization, In-Vitro and Ex-Vivo Assessment

2020 ◽  
Vol 17 (3) ◽  
pp. 246-256
Author(s):  
Kriti Soni ◽  
Ali Mujtaba ◽  
Md. Habban Akhter ◽  
Kanchan Kohli
Keyword(s):  
Drug Release ◽  
Oral Delivery ◽  
Ex Vivo ◽  
Confocal Laser ◽  
Release Mechanism ◽  
Scanning Calorimetry ◽  
Sem Images ◽  
Cloisite 30B ◽  
Ft Ir

Aim: The intention of this investigation was to develop Pemetrexed Diacid (PTX)-loaded gelatine-cloisite 30B (MMT) nanocomposite for the potential oral delivery of PTX and the in vitro, and ex vivo assessment. Background: Gelatin/Cloisite 30 B (MMT) nanocomposites were prepared by blending gelatin with MMT in aqueous solution. Methods: PTX was incorporated into the nanocomposite preparation. The nanocomposites were investigated by Fourier Transmission Infra Red Spectroscopy (FT-IR), Differential Scanning Calorimetry (DSC), Scanning Electron Microscope (SEM) X-Ray Diffraction (XRD) and Confocal Laser Microscopy (CLSM). FT-IR of nanocomposite showed the disappearance of all major peaks which corroborated the formation of nanocomposites. The nanocomposites were found to have a particle size of 121.9 ± 1.85 nm and zeta potential -12.1 ± 0.63 mV. DSC thermogram of drug loaded nanocomposites indicated peak at 117.165 oC and 205.816 oC, which clearly revealed that the drug has been incorporated into the nanocomposite because of cross-linking of cloisite 30 B and gelatin in the presence of glutaraldehyde. Results: SEM images of gelatin show a network like structure which disappears in the nanocomposite. The kinetics of the drug release was studied in order to ascertain the type of release mechanism. The drug release from nanocomposites was in a controlled manner, followed by first-order kinetics and the drug release mechanism was found to be of Fickian type. Conclusion: Ex vivo gut permeation studies revealed 4 times enhancement in the permeation of drug present in the nanocomposite as compared to plain drug solution and were further affirmed by CLSM. Thus, gelatin/(MMT) nanocomposite could be promising for the oral delivery of PTX in cancer therapy and future prospects for the industrial pharmacy.

In-vitro bactericidal activity of a novel plant source Plumeria pudica against some human and fish pathogenic bacteria

2020 ◽  
Vol 17 ◽  
Author(s):  
Shubhaisi Das ◽  
Sunanda Burman ◽  
Goutam Chandra
Keyword(s):  
Ethyl Acetate ◽  
Bioactive Compounds ◽  
Pathogenic Bacteria ◽  
Ethyl Acetate Extract ◽  
Positive Control ◽  
Leaf Extracts ◽  
Ms Analysis ◽  
Ft Ir ◽  
Aldehyde Groups

Background: The only remedy for up surging problem of antibiotic resistance is the discovery of antibacterial agents of natural origin. Objective: The present study was aimed at finding antibacterial potential of crude and solvent extracts of mature leaves of Plumeria pudica. Methods: Antibacterial activity of three different solvent extracts were evaluated in four human and four fish pathogenic bacteria by measuring the zone of inhibition and determining Minimum Inhibitory Concentration and Minimum Bactericidal Concentration values. Standard antibiotics were used as positive control. Preliminary phytochemical screening of most effective extract i.e., ethyl acetate extract, Fourier Transform Infra Red analysis and GC-MS analysis of the Thin Layer Chromatographic (TLC) fraction of ethyl acetate extract were done meticulously. All experiments were done thrice and analyzed statistically. Results: Crude leaf extracts and solvent extracts caused good inhibition of bacterial growth in all selected bacteria. Ethyl acetate extract showed highest inhibition zones in all tested strains with maximum inhibition (19.50±0.29 mm) in Escherichia coli (MTCC 739). MBC/MIC of the extracts indicated that all three solvent extracts were bactericidal. Preliminary phytochemical tests revealed the presence of tannins, steroids and alkaloids and FT-IR analysis revealed presence of many functional groups namely alcoholic, amide, amine salt and aldehyde groups. From the GC-MS analysis of TLC fraction of ethyl acetate extract five different bioactive compounds e.g., 2,4-ditert –butylphenyl 5-hydroxypentanoate, Oxalic acid; allyl nonyl ester, 7,9-Ditert-butyl-1-oxaspiro(4,5)deca-6,9-diene-2,8-dione, Dibutyl phthalate and 2,3,5,8-tetramethyl-decane were identified. Conclusion: Leaf extracts of P. pudica contain bioactive compounds that can be used as broad spectrum bactericidal agent.

Synthesis, SAR, In-Silico appraisal and Anti-Microbial Study of substituted 2-aminobenzothiazoles derivatives

2019 ◽  
Vol 15 ◽  
Author(s):  
Devidas G. Anuse ◽  
Suraj N. Mali ◽  
Bapu R. Thorat ◽  
Ramesh S. Yamgar ◽  
Hemchandra K. Chaudhari
Keyword(s):  
Antimicrobial Activity ◽  
In Silico ◽  
Docking Study ◽  
Moderate Activity ◽  
Molecular Docking Study ◽  
Mass Spectral ◽  
Gram Positive Bacteria ◽  
Ft Ir ◽  
In Silico Molecular Docking

Background: Antimicrobial resistance is major global health problem, which is being rapidly deteriorating the quality of human health. Series of substituted N-(benzo[d]thiazol-2-yl)-2-(4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl)acetamide (3a-j) were synthesized from substituted N-(benzo[d]thiazol-2-yl)-2-chloroacetamide/bromopropanamide (2a-j) and 6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole (2) and further evaluated for their docking properties and antimicrobial activity. Methods: All synthesized compounds were characterized by FT-IR, NMR and Mass spectral analysis. All compounds were allowed to dock against different antimicrobial targets having PDB ID: 1D7U and against common antifungal target having PDB ID: 1EA1. Results: The compounds 3d and 3h were showed good activity against Methicillin-resistant Staphylococcus aureus (MRSA, resistance Gram-positive bacteria). All synthesized compounds showed good to moderate activity against selected bacterial and fungal microbial strains. If we compared the actual in-vitro antimicrobial activity and in-silico molecular docking study, we found that molecules 3i and 3h were more potent than the others. Conclusion: Our current study would definitely pave the new way towards designing and synthesis of more potent 2-aminobenzothiazoles derivatives.

scholarly journals Microwave-Assisted Synthesis, Characterization, Antimicrobial and Antioxidant Activity of Some New Isatin Derivatives

2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
G. Kiran ◽  
T. Maneshwar ◽  
Y. Rajeshwar ◽  
M. Sarangapani
Keyword(s):  
Antioxidant Activity ◽  
Free Radical ◽  
Radical Scavenging ◽  
Microwave Assisted Synthesis ◽  
Stable Free Radical ◽  
Ft Ir ◽  
Antimicrobial And Antioxidant Activity ◽  
New Compounds ◽  
Isatin Derivatives

A series of β-Isatin aldehyde-N,N′-thiocarbohydrazone derivatives were synthesized and assayed for theirin vitroantimicrobial and antioxidant activity. The new compounds were characterized based on spectral (FT-IR, NMR, MS) analyses. All the test compounds possessed a broad spectrum of activity having MIC values rangeing from 12.5 to 400 μg/ml against the tested microorganisms. Among the compounds3e,3jand3nshow highest significant antimicrobial activity. The free radical scavenging effects of the test compounds against stable free radical DPPH (α,α-diphenyl-β-picryl hydrazyl) and H2O2were measured spectrophotometrically. Compounds3j,3n,3l, and3e, respectively, had the most effective antioxidant activity against DPPH and H2O2scavenging activity.

A study on using expanded perlite with hydroxyapatite: Reinforced bio-composites

2021 ◽  
pp. 095441192199656
Author(s):  
Erdoğan Karip ◽  
Mehtap Muratoğlu
Keyword(s):  
Body Fluid ◽  
Xrd Analysis ◽  
Cold Isostatic Pressing ◽  
Expanded Perlite ◽  
X Ray Diffraction ◽  
Pressing Method ◽  
X Ray ◽  
Infra Red ◽  
Ft Ir

People are exposed to different kinds of diseases or various accidents in life. Hydroxyapatite (HA) has been widely employed for bone treatment applications. In this study, HA was extracted from sheep bones. Bio-composites were doped with 1, 5, and 10 wt.% of expanded perlite and 5 wt.% of ZrO2–MgO-P2O5. The bio-composites were prepared by the cold isostatic pressing method (250 MPa) and sintered at 900°C for 1 h. In order to evaluate the characteristics of the bio-composites, microhardness, density, X-ray diffraction (XRD), Fourier transform infra-red spectroscopy (FT-IR), scanning electron microscopy (SEM), and energy dispersive spectroscopy (EDS) analyses were carried out on them. Additionally, the specimens whose characteristics were determined were kept in synthetic body fluid (SBF), and their in vitro behavior was examined. As a result, it was observed that microhardness increased as both the weight and the grain size of the expanded perlite were increased. Calcium silicate, tri-calcium phosphate, and hydroxyapatite were observed in the XRD analysis of all samples, and the formation of apatite structures was increased by addition of ZrO2–MgO–P2O5.

scholarly journals Design, Synthesis and Biological Evaluation of Novel Benzothiazole Based [1,2,4]Triazolo[4,3-c]quinazoline Derivatives

2020 ◽  
Vol 32 (3) ◽  
pp. 580-586
Author(s):  
Ranjit V. Gadhave ◽  
Bhanudas S. Kuchekar
Keyword(s):  
Biological Evaluation ◽  
Bacterial Strains ◽  
Active Compounds ◽  
Design Synthesis ◽  
Structural Modifications ◽  
E Coli ◽  
Chemical Structures ◽  
Ft Ir ◽  
Antioxidant Agent

A new series of N-(benzo[d]thiazol-2-yl)-[1,2,4]triazolo[4,3-c]quinazoline-5-carboxamide derivatives were synthesized by condensation of [1,2,4]triazolo[4,3-c]quinazoline-5-carboxylate derivatives with substituted benzothiazoles. The chemical structures of the synthesized compounds were confirmed by FT-IR, MS and 1H NMR spectra. Designed triazoloquinazoline derivatives were docked with oxido-reductase enzyme (PDB Code 4h1j) and DNA gyrase enzyme (PDB Code 3g75). Based on high binding affinity score, the best compound were selected for synthesis and subjected to in vitro antioxidant and antibacterial activity. Compounds 7a and 7d were found to be most active compounds as antioxidant agent among this series when compared with ascorbic acid. Compounds 7a, 7d and 7f were found to be most active compounds as an antibacterial agents among this series when compared with ciprofloxacin against bacterial strains such as S. aureus (ATCC 25923), E. coli (ATCC 25922) and P. aeruginosa (ATCC 27853). Study revealed that the most active compounds after structural modifications can be exploited as lead molecules for other pharmacological activities such as anti-inflammatory, anticancer and antidepressant activities.

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