PREPARATION AND CHARACTERIZATION OF GLYCYRRHETINIC ACID-MODIFIED POLOXAMER 188/CHITOSAN NANOPARTICLES

NANO ◽  
2013 ◽  
Vol 08 (04) ◽  
pp. 1350042 ◽  
Author(s):  
JING WANG ◽  
LI GUO ◽  
LI FANG MA
Keyword(s):  
High Performance ◽  
Drug Loading ◽  
Chitosan Nanoparticles ◽  
Spherical Shape ◽  
Glycyrrhetinic Acid ◽  
Poloxamer 188 ◽  
H Nmr ◽  
Ft Ir

In this paper, we firstly synthesized glycyrrhetinic acid-modified double amino-terminated poloxamer 188 (GA–NH–POLO–NH–GA). The structure of the synthesized compound was confirmed by 1H-NMR and Fourier transform infrared (FT-IR) spectroscopy. Then the nanoparticles composed of GA–NH–POLO–NH–GA/chitosan (GA–NH–POLO–NH–GA/CTS) were prepared by an ionic gelation process. The characterization of the nanoparticles was measured by dynamic light scattering (DLS) and scanning electron microscope (SEM). The results showed that the nanoparticles were well dispersed with a spherical shape and the particle size was distributed between 100 nm and 300 nm. The cytotoxicity based on MTT assay against cells (QGY-7703 cells and L929 cells) showed that the nanoparticles had low toxicity and good biocompatibility. The encapsulation efficiency and drug loading of 5-fluorouracil-loaded nanoparticles (5-FU nanoparticles) were measured by high-performance liquid chromatography (HPLC) and fluorescence spectroscopy, ultraviolet-visible (UV-vis) absorbance. The encapsulation of 5-Fu-loaded CTS nanoparticles was 12.8% and the drug loading was 2.9%, while the encapsulation of 5-Fu-loaded GA–NH–POLO–NH–GA/CTS nanoparticles was 20.9% and the drug loading was 3.36%. The release profile showed that the GA–NH–POLO–NH–GA/CTS nanoparticles were available for sustained release of 5-Fu. The GA–NH–POLO–NH–GA/CTS nanoparticles have a higher affinity to the QGY-7703 cells, so indicated that the GA–NH–POLO–NH–GA/CTS nanoparticles have the capacity of liver-targeting in vitro.

Synthesis and Characterization of Polyesters Containing 5-Fluorouracil in the Main Chain

2012 ◽  
Vol 499 ◽  
pp. 99-103
Author(s):  
Jun Chang ◽  
Cheng Wu Li ◽  
Gang Li
Keyword(s):  
Main Chain ◽  
Slow Release ◽  
Uv Spectroscopy ◽  
Release Profile ◽  
Drug Release Profile ◽  
H Nmr ◽  
Ft Ir ◽  
Potential Antitumor

A series of polyesters containing 5-fluorouracil in the main chain were prepared by reacting potassium salt of 5-fluorouracil with different molecular weight ω-chloroalkyl chloroacetyl esters.The copolymers were characterized by FT-IR, 1H-NMR, VPO and UV spectroscopy. The drug release profile in vitro of the copolymers were studied, the results showed prodrug could slow release 5-FU or 5-FU units in different solution, they may be likely to become potential antitumor prodrug.

scholarly journals Synthesis and Characterization of New Amino Acid-Schiff Bases and Studies their Effects on the Activity of ACP, PAP and NPA Enzymes (In Vitro)

2012 ◽  
Vol 9 (2) ◽  
pp. 962-969 ◽  
Author(s):  
Zahraa Salim M. Al-Garawi ◽  
Ivan Hameed R. Tomi ◽  
Ali Hussein R. Al-Daraji
Keyword(s):  
Schiff Base ◽  
Condensation Reaction ◽  
Synthesis And Characterization ◽  
Activation Effect ◽  
Inhibition Effect ◽  
H Nmr ◽  
Ft Ir ◽  
High Concentrations

In this study, two new Schiff base compounds derived from the condensation reaction ofL-glycine andL-tryptophan with 4-methylbenzal-dehyde have been synthesized. The Schiff base compounds were characterized by FT-IR, UV and1H NMR spectroscopy. Their effects on the activity of total (ACP), prostatic (PAP) and non prostatic (NPA) acid phosphatase enzymes were studied. The Schiff base derived fromL-glycine (A) demonstrated inhibition effect on the ACP and NPA activities and activation effect on PAP activity. The Schiff base derived fromL-tryptophan (B) demonstrated semi fixed inhibition effects on the ACP and NPA activities at high concentrations (5.5×10-2, 5.5×10-3and 5.5×10-4M) and activator effect at low concentration (5.5×10-5M) while it was exhibits as activator on PAP activity.

scholarly journals Microencapsulation of Erlotinib and Nanomagnetite Supported in Chitosan as Potential Oncologic Carrier

Polymers ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1244
Author(s):  
Galo Cárdenas-Triviño ◽  
Sebastián Monsalve-Rozas ◽  
Luis Vergara-González
Keyword(s):  
Infrared Spectra ◽  
Hplc Analysis ◽  
Spherical Shape ◽  
Microbiological Activity ◽  
Reference Drug ◽  
Ft Ir ◽  
Average Size ◽  
Optimum Working

Microcapsules (MC) based on chitosan (CH) and including nano-magnetite and erlotinib were synthesized. The microparticles were characterized by SEM, FT-IR and TGA. The percentage of encapsulation was determined, as well as its microbiological activity. Finally, the effectiveness of the formulation was evaluated in terms of cell viability and/or toxicity when compared with the reference drug. The formulation used to prepare the microcapsules showed some bacteriostatic properties. The characterization of microcapsules exhibited amorphous spherical shape and average size of 1.29, 1.58 and 1.62 mm for chitosan, chitosan + nanomagnetite and chitosan + nanomagnetite + erlotinib, respectively. The infrared spectra showed characteristic bands of the erlotinib and magnetite, confirming its internalization. The thermogravimetric analyzes indicated that the materials do not undergo changes at optimum working temperatures. The HPLC analysis showed a 52% of encapsulation. Finally, the formulation probed had lower effectiveness and less cytotoxicity, than the drug without encapsulating “in vitro” studies. For that reason several assays are in progress.

Synthesis and Characterization of Polyesteramides Containing 5-Fluorouracil in the Main Chain

2011 ◽  
Vol 284-286 ◽  
pp. 1728-1731
Author(s):  
Jun Chang ◽  
Cheng Wu Li ◽  
Gang Li
Keyword(s):  
Main Chain ◽  
Slow Release ◽  
Uv Spectroscopy ◽  
Release Profile ◽  
Drug Release Profile ◽  
H Nmr ◽  
Ft Ir ◽  
Potential Antitumor

A series of polyesteramide containing 5-fluorouracil in the main chain were prepared by reacting potassium salt of 5-fluorouracil with N-(2-chloroacetoxylalkyl)-chloroacetamide.The copolymers were characterized by FT-IR, 1H-NMR, VPO and UV spectroscopy. The drug release profile in vitro of the copolymers were studied, the results showed prodrug could slow release 5-FU or 5-FU units in different solution, they may be likely to become potential antitumor prodrug.

scholarly journals A novel effective therapeutic approach for treatment of Leishmania tropica through Miltefosine Loaded Chitosan Nanoparticles

2020 ◽  
Author(s):  
Momin Khan ◽  
Muhammad Adnan Shereen ◽  
Mehvish Khokhar ◽  
Atif Kamil ◽  
Hazir Rahman
Keyword(s):  
Cell Viability ◽  
Sodium Tripolyphosphate ◽  
Colorimetric Assay ◽  
Drug Loading ◽  
Chitosan Nanoparticles ◽  
Spherical Shape ◽  
Leishmania Tropica ◽  
Hemolysis Assay ◽  
Mean Size

Abstract Objectives The aim of the present study was to develop miltefosine loaded chitosan nanoparticles (MLCNPs) to enhance the therapeutic efficacy of conventional miltefosine drug and to compare the in vitro activities of both forms of the drug against Leishmania tropica. Methods MLCNPs were synthesized through ionic gelation with sodium tripolyphosphate (TPP). For the stabilization of nanoparticles, a controlled oxidation of MLCNPs was done with hydrogen peroxide (H2O2). The anti-leishmanial activities of MLCNP were determined by MTT cell viability colorimetric assay. The in vitro hemolysis assay was performed for assessment of toxicity in the human blood. Results The MLCNPS displayed spherical shape with irregular surface morphology, had a mean size of 200nm and a zeta potential of +10.9 ± 4 mV. A high encapsulation efficacy and drug loading capacity of miltefosine loaded chitosan nanoparticles was also observed. The anti-leishmanial activities of MLCNP were determined by MTT cell viability colorimetric assay. The IC50 value of MLCNPs against promastigote and amastigote were recorded as 0.85µg/ml and 0.92µg/ml respectively. MLCNPs proved to be more effective as compared to conventional miltefosine. In terms of toxicity the MLCNPs caused only 2.25% hemolysis. Conclusions The engineered MLCNPs could be potential alternative for the treatment of cutaneous leishmaniasis.

scholarly journals Development of Spanish Broom and Flax Dressings with Glycyrrhetinic Acid-Loaded Films for Wound Healing: Characterization and Evaluation of Biological Properties

Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1192
Author(s):  
Angela Abruzzo ◽  
Concettina Cappadone ◽  
Valentina Sallustio ◽  
Giovanna Picone ◽  
Martina Rossi ◽  
...  
Keyword(s):  
Wound Healing ◽  
Drug Loading ◽  
Healing Process ◽  
In Vitro Release ◽  
Sodium Hyaluronate ◽  
Biological Properties ◽  
Glycyrrhetinic Acid ◽  
Wound Dressings ◽  
Biological Studies

The selection of an appropriate dressing for each type of wound is a very important procedure for a faster and more accurate healing process. So, the aim of this study was to develop innovative Spanish Broom and flax wound dressings, as alternatives to cotton used as control, with polymeric films containing glycyrrhetinic acid (GA) to promote wound-exudate absorption and the healing process. The different wound dressings were prepared by a solvent casting method, and characterized in terms of drug loading, water uptake, and in vitro release. Moreover, biological studies were performed to evaluate their biocompatibility and wound-healing efficacy. Comparing the developed wound dressings, Spanish Broom dressings with GA-loaded sodium hyaluronate film had the best functional properties, in terms of hydration ability and GA release. Moreover, they showed a good biocompatibility, determining a moderate induction of cell proliferation and no cytotoxicity. In addition, the wound-healing test revealed that the Spanish Broom dressings promoted cell migration, further facilitating the closure of the wound.

scholarly journals Synthesis, Characterization, and Antimicrobial Activity of Methyl-2-aminopyridine-4-carboxylate Derivatives

2013 ◽  
Vol 2013 ◽  
pp. 1-5 ◽  
Author(s):  
S. Nagashree ◽  
P. Mallu ◽  
L. Mallesha ◽  
S. Bindya
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Studies ◽  
H Nmr ◽  
Chemical Structures ◽  
Elemental Analyses ◽  
Ft Ir

A series of methyl-2-aminopyridine-4-carboxylate derivatives,3a–f,were synthesized in order to determine theirin vitroantimicrobial activity. The chemical structures of the synthesized compounds were confirmed by elemental analyses, FT-IR, and1H NMR spectral studies. Among the synthesized compounds,3cand3dshowed good antimicrobial activity compared to other compounds in the series.

Synthesis of Eco-friendly Nano-Structured Biosurfactants from Vegetable Oil Sources and Characterization of Their Interfacial Properties for Cosmetic Applications

MRS Advances ◽  
2018 ◽  
Vol 4 (07) ◽  
pp. 377-384 ◽  
Author(s):  
DaNan Yea ◽  
SeonHui Jo ◽  
JongChoo Lim
Keyword(s):  
Raw Materials ◽  
Coconut Oil ◽  
Interfacial Properties ◽  
Interfacial Property ◽  
Solution Stability ◽  
H Nmr ◽  
Wetting Property ◽  
Potential Applicability ◽  
Ft Ir

ABSTRACTIn this study, 3 types of zwitterionic phospholipid biosurfactants LDP(S), CDP(S) and CTDP(S) were prepared from 3 different raw materials such as rapeseed oil, coconut oil and cottonseed oil respectively. The structure of the resulting phospholipid biosurfactants was elucidated by FT-IR, 1H NMR and 13C NMR spectroscopies and their interfacial properties have been examined such as CMC, static surface tension, wetting property, solution stability, and foam property. Interfacial property measurement and prescription test in cosmetic formulation prepared with the newly synthesized biosurfactants revealed that CDP(S) biosurfactant possesses excellent mildness and superior interfacial properties, indicating the potential applicability in cosmetic product formulations.

scholarly journals SYNTHESIS AND STRUCTURAL ELUCIDATION OF AMINO ACETYLENIC AND THIOCARBAMATES DERIVATIVES FOR 2-MERCAPTOBENZOTHIAZOLE AS ANTIMICROBIAL AGENTS

2017 ◽  
Vol 9 (2) ◽  
pp. 192
Author(s):  
Aseel Alsarahni ◽  
Zuhair Muhi Eldeen ◽  
Elham Al-kaissi ◽  
Ibrahim Al- Adham ◽  
Najah Al-muhtaseb
Keyword(s):  
Antimicrobial Activity ◽  
Elemental Analysis ◽  
Antimicrobial Agents ◽  
Diffusion Method ◽  
Benzothiazole Derivatives ◽  
H Nmr ◽  
Ft Ir ◽  
Potential Antimicrobial Activity ◽  
C Nmr

<p><strong>Objective: </strong>To design and synthesize amino acetylenic and thiocarbonate of 2-mercapto-1,3-benthiazoles as potential antimicrobial agents.</p><p><strong>Methods: </strong>A new series of 2-{[4-(t-amino-1-yl) but-2-yn-1-yl] sulfanyl}-1,3-benzothiazole derivatives (AZ1-AZ6), and S-1,3-benzothiazol-2-yl-O-alkyl carbonothioate derivatives were synthesised, with the aim that the target compounds show new and potential antimicrobial activity. The elemental analysis was indicated by the EuroEA elemental analyzer, and biological characterization was via IR, <sup>1</sup>H-NMR, [13]C-NMR, DSC were determined with the aid of Bruker FT-IR and Varian 300 MHz spectrometer using DMSO-d<sub>6</sub> as a solvent.<em> </em><em>In vitro </em>antimicrobial activity, evaluation was done for the synthesised compounds, by agar diffusion method and broth dilution test. The minimum inhibitory concentration (MIC) and the minimum bactericidal concentration (MBC) were determined. <em></em></p><p><strong>Results: </strong>The IR, <sup>1</sup>H-NMR, <sup>13</sup>C-NMR, DSC and elemental analysis were consistent with the assigned structures. Compound of 2-{[4-(4-methylpiperazin-1-yl)but-2-yn-1-yl] sulfanyl}-1,3-benzothiazole (AZ1), 2-{[4-(2-methylpiperidin-1-yl)but-2-yn-1-yl]sulfanyl}-1,3-benzothiazole (AZ2), 2-{[4-(piperidin-1-yl) but-2-yn-1-yl]sulfanyl}-1, 3-benzothiazole (AZ6), S-1,3-benzothiazol-2-yl-O-ethyl carbonothioate (AZ7), and S-1,3-benzothiazol-2-yl-O-(2-methylpropyl) carbonothioate (AZ9) showed the highest antimicrobial activity against <em>Pseudomonas aeruginosa </em>(<em>P. aeruginosa</em>), AZ-9 demonstrated the highest antifungal activity against <em>Candida albicans </em>(<em>C. albicans</em>), with MIC of 31.25 µg/ml.</p><p><strong>Conclusion: </strong>These promising results promoted our interest to investigate other structural analogues for their antimicrobial activity further.</p>

Electrochemically Synthesis and Characterization of Copolymers Based on 1, 4-Diethoxybenzene and 3, 4-Ethylenedioxythiophene

2011 ◽  
Vol 335-336 ◽  
pp. 989-993
Author(s):  
Mi Ouyang ◽  
Zhen Wei Yu ◽  
Yi Xu ◽  
Yu Jian Zhang ◽  
Cheng Zhang
Keyword(s):  
Cyclic Voltammetry ◽  
Ir Spectroscopy ◽  
Feed Ratio ◽  
Synthesis And Characterization ◽  
Monomer Mixture ◽  
Long Wavelength ◽  
H Nmr ◽  
Ft Ir ◽  
Ft Ir Spectroscopy

Copolymers based on 1, 4-diethoxybenzene (DEB) and 3, 4-ethylenedioxythiophene (EDOT) were electrochemically synthesized and characterized. The structures of the copolymers were established by 1H NMR and FT-IR spectroscopy. The results indicated the final product was a copolymer instead of a blend or a composite. The physical properties were systematically investigated by cyclic voltammetry, UV-vis absorption and fluorescence. The PL maximum of copolymers presented obviously red-shift to long wavelength as the feed ratio of EDOT in monomer mixture increased.

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