scholarly journals DESIGN, CHARACTERIZATION AND ENHANCED BIOAVAILABILITY OF HYDROXYPROPYLCELLULOSE-BASED NOVEL BIOCONJUGATES FOR INCLUSION OF A FLUOROQUINOLONE ANTIBIOTIC – GEMIFLOXACIN

2021 ◽  
Vol 55 (9-10) ◽  
pp. 1019-1027
Author(s):  
MUHAMMAD AJAZ HUSSAIN ◽  
◽  
IRAM MALIK ◽  
IQRA SHAD ◽  
FASIHA AMJAD ◽  
...  
Keyword(s):  
Drug Carriers ◽  
Pharmacokinetic Studies ◽  
High Efficacy ◽  
Drug Molecules ◽  
Tosyl Chloride ◽  
Inert Environment ◽  
Uv Visible ◽  
Macromolecular Prodrugs ◽  
High Degree ◽  
Hydrolysis Of

Polysaccharides are beneficially used as drug carriers via prodrug formation and offer a mechanism for better effectiveness and delivery of the drug. The unique geometry of hydroxypropylcellulose (HPC), a polysaccharide, allows the attachment of drug molecules with a higher degree of substitution. Therefore, HPC-gemifloxacin conjugates, i.e., macromolecular prodrugs, were synthesized using acylation reagents, i.e., tosyl chloride and carbonyldiimidazole using N,N-dimethylacetamide as a solvent. The reactions were carried out at 80 °C under stirring for 24 h in inert environment. This strategy of reaction appeared efficient to obtain a high degree of drug substitution (DS = 0.42-1.34) on the polymer parent chain, as calculated by UV-visible spectrophotometry after hydrolysis of the samples. The method provides high efficacy as product yields were high (71-76%). Macromolecular prodrugs with different DS of gemifloxacin (GEM) designed were found soluble in organic solvents. The pharmacokinetic studies showed that the t1/2 and tmax values of GEM from HPC-GEM conjugate were considerably higher, which indicates improved bioavailability of the drug after conjugate formation.

scholarly journals Refinement of Structural Leads for Centrally Acting Oxime Reactivators of Phosphylated Cholinesterases

2012 ◽  
Vol 287 (15) ◽  
pp. 11798-11809 ◽  
Author(s):  
Zoran Radić ◽  
Rakesh K. Sit ◽  
Zrinka Kovarik ◽  
Suzana Berend ◽  
Edzna Garcia ◽  
...  
Keyword(s):  
Ph Dependence ◽  
Pharmacokinetic Studies ◽  
Visible Spectroscopy ◽  
H Nmr ◽  
Pharmacokinetic Properties ◽  
Uv Visible ◽  
Cns Penetration ◽  
Intrinsic Reactivity ◽  
Hydrolysis Of

We present a systematic structural optimization of uncharged but ionizable N-substituted 2-hydroxyiminoacetamido alkylamine reactivators of phosphylated human acetylcholinesterase (hAChE) intended to catalyze the hydrolysis of organophosphate (OP)-inhibited hAChE in the CNS. Starting with the initial lead oxime RS41A identified in our earlier study and extending to the azepine analog RS194B, reactivation rates for OP-hAChE conjugates formed by sarin, cyclosarin, VX, paraoxon, and tabun are enhanced severalfold in vitro. To analyze the mechanism of intrinsic reactivation of the OP-AChE conjugate and penetration of the blood-brain barrier, the pH dependence of the oxime and amine ionizing groups of the compounds and their nucleophilic potential were examined by UV-visible spectroscopy, 1H NMR, and oximolysis rates for acetylthiocholine and phosphoester hydrolysis. Oximolysis rates were compared in solution and on AChE conjugates and analyzed in terms of the ionization states for reactivation of the OP-conjugated AChE. In addition, toxicity and pharmacokinetic studies in mice show significantly improved CNS penetration and retention for RS194B when compared with RS41A. The enhanced intrinsic reactivity against the OP-AChE target combined with favorable pharmacokinetic properties resulted in great improvement of antidotal properties of RS194B compared with RS41A and the standard peripherally active oxime, 2-pyridinealdoxime methiodide. Improvement was particularly noticeable when pretreatment of mice with RS194B before OP exposure was combined with RS194B reactivation therapy after the OP insult.

scholarly journals Drug Carriers Based on Graphene Oxide and Hydrogel: Opportunities and Challenges in Infection Control Tested by Amoxicillin Release

Materials ◽  
2021 ◽  
Vol 14 (12) ◽  
pp. 3182
Author(s):  
Anna Trusek ◽  
Edward Kijak
Keyword(s):  
Graphene Oxide ◽  
Enzymatic Hydrolysis ◽  
Infection Control ◽  
Bacterial Species ◽  
Drug Carriers ◽  
Peptide Bond ◽  
Drug Molecules ◽  
Model Drug ◽  
Hydrolysis Of ◽  
Plant Enzyme

Graphene oxide (GO) was proposed as an efficient carrier of antibiotics. The model drug, amoxicillin (AMOX), was attached to GO using a peptide linker (Leu-Leu-Gly). GO-AMOX was dispersed in a hydrogel to which the enzyme responsible for releasing AMOX from GO was also added. The drug molecules were released by enzymatic hydrolysis of the peptide bond in the linker. As the selected enzyme, bromelain, a plant enzyme, was used. The antibacterial nature of the carrier was determined by its ability to inhibit the growth of the Enterococcus faecalis strain, which is one of the bacterial species responsible for periodontal and root canal diseases. The prepared carrier contained only biocompatible substances, and the confirmation of its lack of cytotoxicity was verified based on the mouse fibrosarcoma cell line WEHI 164. The proposed type of preparation, as a universal carrier of many different antibiotic molecules, can be considered as a suitable solution in the treatment of inflammation in dentistry.

Effect of Trypsin on Antioxidant Activity and Gel-Rheology of Flaxseed Protein

2017 ◽  
Vol 13 (3) ◽  
Author(s):  
Yuan-yuan Chang ◽  
Chong-hao Bi ◽  
Li-jun Wang ◽  
Dong Li ◽  
Benu Adhikari ◽  
...  
Keyword(s):  
Gel Strength ◽  
Protein Hydrolysates ◽  
Hydrodynamic Diameter ◽  
Considerable Decrease ◽  
Antioxidative Properties ◽  
Trypsin Hydrolysis ◽  
Gelling Property ◽  
High Degree ◽  
Hydrolysis Of ◽  
Antioxidative Property

Abstract Enzymatic hydrolysis of flaxseed protein (FP) was carried out using trypsin in order to obtain flaxseed protein hydrolysates possessing better antioxidative property and modified rheological properties. The antioxidative properties of hydrolysates were much higher than the unhydrolyzed flaxseed protein. The hydrolysis also significantly reduced the hydrodynamic diameter of the magnitude of zeta potential of the dispersions. The gelling point of the hydrolysates occurred earlier than the unhydrolyzed sample while the duration of hydrolysis (30–120 min) did not affect gelling point of the hydrolysates. Considerable decrease in the gel strength and the frequency dependence of gel strength were observed in gels produced using hydrolyzed flaxseed protein. The above findings indicate that hydrolysates possessing high degree of antioxidative properties. The gels produces from these hydrolysates will have fast gelling property and will produce gels with reasonable strength. Thus, flaxseed protein hydrolysates obtained from trypsin hydrolysis can be used in applications that require proteins with higher antioxidative properties but softer texture.

scholarly journals Non-Lamellar Liquid Crystalline Nanocarriers for Thymoquinone Encapsulation

Molecules ◽  
2019 ◽  
Vol 25 (1) ◽  
pp. 16 ◽  
Author(s):  
Anan Yaghmur ◽  
Boi Vi Tran ◽  
Seyed Moein Moghimi
Keyword(s):  
Liquid Crystalline ◽  
Drug Carriers ◽  
Structural Features ◽  
Drug Induced ◽  
Guest Molecules ◽  
Drug Molecules ◽  
Liquid Crystalline Nanoparticles ◽  
The Mean ◽  
Biological Performance ◽  
Glycerol Monooleate

Owing to their unique structural features, non-lamellar liquid crystalline nanoparticles comprising cubosomes and hexosomes are attracting increasing attention as versatile investigative drug carriers. Background: Depending on their physiochemical characteristics, drug molecules on entrapment can modulate and reorganize structural features of cubosomes and hexosomes. Therefore, it is important to assess the effect of guest molecules on broader biophysical characteristics of non-lamellar liquid crystalline nanoparticles, since drug-induced architectural, morphological, and size modifications can affect the biological performance of cubosomes and hexosomes. Methods: We report on alterations in morphological, structural, and size characteristics of nanodispersions composed from binary mixtures of glycerol monooleate and vitamin E on thymoquinone (a molecule with wide therapeutic potentials) loading. Results: Thymoquinone loading was associated with a slight increase in the mean hydrodynamic nanoparticle size and led to structural transitions from an internal biphasic feature of coexisting inverse cubic Fd3m and hexagonal (H2) phases to an internal inverse cubic Fd3m phase (micellar cubosomes) or an internal inverse micellar (L2) phase (emulsified microemulsions, EMEs). We further report on the presence of “flower-like” vesicular populations in both native and drug-loaded nanodispersions. Conclusions: These nanodispersions have the potential to accommodate thymoquinone and may be considered as promising platforms for the development of thymoquinone nanomedicines.

SOME ASPECTS OF THE ENZYMIC HYDROLYSIS OF URINARY 17-KETOSTEROID CONJUGATES

1960 ◽  
Vol 38 (1) ◽  
pp. 769-776
Author(s):  
R. Hobkirk ◽  
J. J. Cohen
Keyword(s):  
Liver Enzymes ◽  
Striking Difference ◽  
Degree Of Hydrolysis ◽  
Enzyme Preparations ◽  
Bacterial Preparation ◽  
Bacterial Enzyme ◽  
The Difference ◽  
Normal Urine ◽  
High Degree ◽  
Hydrolysis Of

Four enzyme preparations containing β-glucuronidase, of bacterial, mammalian, and molluscan origin, have been shown to be equally effective in liberating 17-ketosteroids (17-KS) of the 5β-(etiocholane) configuration in normal urine. The bacterial preparation releases steroids of the 5α-(androstane) configuration more rapidly than do the molluscan enzymes and with much greater ease than does the liver enzyme. In view of the data obtained it seems unlikely that the striking difference between the bacterial and liver enzymes can be due to the hydrolysis of some labile conjugate, such as sulphate, by the former and not by the latter. Possibilities that the difference is due to the hydrolysis of an unknown type of urinary conjugate by the bacterial preparation, or to the low specificity of the bacterial β-glucuronidase, are discussed. The high degree of hydrolysis of 17-KS conjugates by the bacterial enzyme followed by solvolysis suggests this as a most useful hydrolytic procedure.

SOME ASPECTS OF THE ENZYMIC HYDROLYSIS OF URINARY 17-KETOSTEROID CONJUGATES

1960 ◽  
Vol 38 (7) ◽  
pp. 769-776 ◽  
Author(s):  
R. Hobkirk ◽  
J. J. Cohen
Keyword(s):  
Liver Enzymes ◽  
Striking Difference ◽  
Degree Of Hydrolysis ◽  
Enzyme Preparations ◽  
Bacterial Preparation ◽  
Bacterial Enzyme ◽  
The Difference ◽  
Normal Urine ◽  
High Degree ◽  
Hydrolysis Of

Four enzyme preparations containing β-glucuronidase, of bacterial, mammalian, and molluscan origin, have been shown to be equally effective in liberating 17-ketosteroids (17-KS) of the 5β-(etiocholane) configuration in normal urine. The bacterial preparation releases steroids of the 5α-(androstane) configuration more rapidly than do the molluscan enzymes and with much greater ease than does the liver enzyme. In view of the data obtained it seems unlikely that the striking difference between the bacterial and liver enzymes can be due to the hydrolysis of some labile conjugate, such as sulphate, by the former and not by the latter. Possibilities that the difference is due to the hydrolysis of an unknown type of urinary conjugate by the bacterial preparation, or to the low specificity of the bacterial β-glucuronidase, are discussed. The high degree of hydrolysis of 17-KS conjugates by the bacterial enzyme followed by solvolysis suggests this as a most useful hydrolytic procedure.

scholarly journals Poly(Vinyl Alcohol) Recent Contributions to Engineering and Medicine

2020 ◽  
Vol 4 (4) ◽  
pp. 175
Author(s):  
Dorel Feldman
Keyword(s):  
Vinyl Alcohol ◽  
Dye Removal ◽  
Chemical Separation ◽  
Drug Carriers ◽  
Synthetic Polymers ◽  
Synthetic Polymer ◽  
Poly Vinyl Alcohol ◽  
Numerous Application ◽  
Separation Element ◽  
Hydrolysis Of

Poly(vinyl alcohol) (PVA) is a thermoplastic synthetic polymer, which, unlike many synthetic polymers, is not obtained by polymerization, but by hydrolysis of poly(vinyl acetate) (PVAc). Due to the presence of hydroxylic groups, hydrophilic polymers such as PVA and its composites made mainly with biopolymers are used for producing hydrogels that possess interesting morphological and physico-mechanical features. PVA hydrogels and other PVA composites are studied in light of their numerous application for electrical film membranes for chemical separation, element and dye removal, adsorption of metal ions, fuel cells, and packaging. Aside from applications in the engineering field, PVA, like other synthetic polymers, has applications in medicine and biological areas and has become one of the principal objectives of the researchers in the polymer domain. The review presents a few recent applications of PVA composites and contributions related to tissue engineering (repair and regeneration), drug carriers, and wound healing.

Direct Interaction of Colloidal Nanostructured ZnO and SnO2 with NO and SO2

2008 ◽  
Vol 8 (12) ◽  
pp. 6389-6397 ◽  
Author(s):  
D. Velasco-Arias ◽  
D. Díaz ◽  
P. Santiago-Jacinto ◽  
G. Rodríguez-Gattorno ◽  
A. Vázquez-Olmos ◽  
...  
Keyword(s):  
Electronic Absorption ◽  
Room Temperature ◽  
Emission Spectra ◽  
Direct Interaction ◽  
X Ray Diffraction ◽  
Wurtzite Phase ◽  
X Ray ◽  
Spontaneous Hydrolysis ◽  
Uv Visible ◽  
Hydrolysis Of

A novel and easy synthesis pathway of small SnO2 nanoparticles is reported. The method consists of the spontaneous hydrolysis of SnCl4·5H2O in dimethyl sulfoxide (DMSO), containing 3% water, at room temperature. The structure of the SnO2 nanocrystals corresponds to that of the cassiterite phase, as shown by powder X-ray diffraction and HR-TEM. The UV-visible electronic absorption and emission spectra of the SnO2 colloids are discussed. The reactions of NO(g) and SO2(g) with ZnO (wurtzite phase) and SnO2 nanocolloids are studied. The interaction of NO with ZnO nanoparticles generates the dissolution of the particles and it is quite probable that NO−13, NO−12, N2O and N2 are formed; while its contact with SO2 probably yields SO−24, SO−23 and also the dissolution of the particles is observed. When these gases are reacted with SnO2, then NO−13, NO−12, SO−23 and SO−24, were respectively obtained.

scholarly journals Coal Fly Ash Ceramics: Preparation, Characterization, and Use in the Hydrolysis of Sucrose

2014 ◽  
Vol 2014 ◽  
pp. 1-7 ◽  
Author(s):  
Ricardo Pires dos Santos ◽  
Jorge Martins ◽  
Carlos Gadelha ◽  
Benildo Cavada ◽  
Alessandro Victor Albertini ◽  
...  
Keyword(s):  
Fly Ash ◽  
Surface Area ◽  
Power Plants ◽  
Coal Fly Ash ◽  
Thermal Power ◽  
Coal Ash ◽  
Mineralogical Composition ◽  
Degree Of Hydrolysis ◽  
High Degree ◽  
Hydrolysis Of

Coal ash is a byproduct of mineral coal combustion in thermal power plants. This residue is responsible for many environmental problems because it pollutes soil, water, and air. Thus, it is important to find ways to reuse it. In this study, coal fly ash, obtained from the Presidente Médici Thermal Power Plant, was utilized in the preparation of ceramic supports for the immobilization of the enzyme invertase and subsequent hydrolysis of sucrose. Coal fly ash supports were prepared at several compaction pressures (63.66–318.30 MPa) and sintered at 1200°C for 4 h. Mineralogical composition (by X-ray diffraction) and surface area were studied. The ceramic prepared with 318.30 MPa presented the highest surface area (35 m2/g) and amount of immobilized enzyme per g of support (76.6 mg/g). In assays involving sucrose inversion, it showed a high degree of hydrolysis (around 81%) even after nine reuses and 30 days’ storage. Therefore, coal fly ash ceramics were demonstrated to be a promising biotechnological alternative as an immobilization support for the hydrolysis of sucrose.

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