scholarly journals ATORVASTATIN ADSORPTION STUDIES ON CHITOSANS IN AN in vitro PHARMACEUTICAL MODEL

2018 ◽  
Vol XXIII ◽  
pp. 140-148
Author(s):  
Jan Meler ◽  
Bożena Grimling ◽  
Maria Szcześniak ◽  
Bożena Karolewicz ◽  
Paweł Biernat
Keyword(s):  
Binding Capacity ◽  
Chemical Properties ◽  
Drug Dose ◽  
Pharmacological Therapy ◽  
Swelling Properties ◽  
Average Percentage ◽  
Anticholinesterase Drug ◽  
Average Size ◽  
A Charge

During the pharmacological therapy of specific diseases, drugs are used which, with other preparations or foods, can create connections, in many cases changing or even blocking their action. On the other hand, the use of unsuitable polymers as excipients may result in drug-polymer incompatibilities. Interactions consisting mainly of the occurrence of the adsorption phenomenon and on the formation of complex bonds that reduce the effect of the drugs are of particular importance. The aim of the study was to investigate whether the active substance atorvastatin is incompatible with dietary supplements containing chitosan. The phenomenon of the adsorption of the drug was examined using a static model of a pharmaceutical gastrointestinal tract, in the concentration range generally ingested in a single dose. Measurement results of the amount of bound drug were used to determine the average percentage of adsorbed drug dose. The results of the study prove that the anticholinesterase drug is adsorbed on chitosan in the pH ranges used, and that the binding capacity depends on the chitosan variety, which indirectly affects the reaction of the environment. It was observed that the average size of sorption depending on the chitosan variety ranged from 38% to 86%. The fact that the lowest value of adsorption was at pH 6.4 can be explained by the chemical properties of chitosan, which shows a charge only at pH >6.7. Under such conditions, the phenomenon of electrostatic adsorption may occur in relation to the healing substances of weak acids. At a pH above 7.6, corresponding to the intestinal fluid-filled intestine, the mean sorption for the highest dose of chitosan was from 38–86%. The increase in the adsorbed amount of anticholinesterase drugs on the polymer along with the increase in pH from 7.6 to 8.0 can be explained by the chitosan swelling properties, which increase with an increase in the pH. As a result, the specific surface area of the polymer and its sorption capacity increase. Based on the above considerations, it can be concluded that there is an antagonistic interaction between the drug and the polymer studied, which involves the adsorption of a drug from this group on the polymer (chitosan) and a decrease in its bioavailability.

Boosting the Food Functionality (In Vivo and In Vitro) of Spirulina by Gamma Radiation: An Inspiring Approach

2015 ◽  
Vol 11 (4) ◽  
pp. 579-585 ◽  
Author(s):  
Jahid M. M. Islam ◽  
Md. Ismail ◽  
Md. Rakibul Islam ◽  
Md. Faruk Hossain ◽  
Hossain Uddin Shekhar
Keyword(s):  
Radiation Dose ◽  
Gamma Radiation ◽  
Binding Capacity ◽  
Chemical Properties ◽  
Maximum Level ◽  
Biologically Active ◽  
Optimum Dose ◽  
Radiation Doses

Abstract Foods (natural or processed) containing known biologically active compounds, which supplies clinically established and well-documented health benefits, are termed as functional food. Study objectives were to boost food functionality of spirulina, to optimize the required radiation dose, and to test functionality of spirulina both in vitro and in vivo. For this purpose fat binding capacity, sugar binding capacity, hydration property, antioxidative property, total polyphenol content were assessed at different radiation doses. A total of 30 rats were divided into three groups to carry out in vivo experiments to validate the outcomes of in vitro experiments. Targeted physico-chemical properties of spirulina were increased at their maximum level at 15 kGy radiation dose. In vivo experiments validated the outcomes of in vitro experiments. Though gamma radiation improves food functionality of spirulina at various radiation doses, but the optimum dose is recommended as 15 kGy.

scholarly journals Digestive and metabolic effects of potato and maize fibres in human subjects

1997 ◽  
Vol 77 (1) ◽  
pp. 33-46 ◽  
Author(s):  
C. Cherbut ◽  
A.-C. Aube ◽  
N. Mekki ◽  
C. Dubois ◽  
D. Lairon ◽  
...  
Keyword(s):  
Transit Time ◽  
Binding Capacity ◽  
Human Subjects ◽  
Chemical Properties ◽  
Basal Diet ◽  
Metabolic Effects ◽  
Healthy Human ◽  
Water Binding ◽  
Blood Concentrations

The physiological effects of dietary fibres in humans are due to their physico-chemical properties. However, it is difficult to predict these effects simply by measuring certain characteristicsin vitro. Studies in human subjects are still required to assess the effectiveness of new substrates. The aim of the present study in healthy human subjects was to evaluate the effects of two novel fibres, potato (PF) and maize (MF), on fasting and postprandial blood concentrations of carbohydrate and lipid metabolites as well as on stool ouput and transit time. The chemical composition, water-binding capacity (WBC) and fermentative properties of the fibres were also characterized in order to determine their possible involvement in digestive and metabolic effects. Stools, as well as breath and blood samples, were collected after consumption for 1 month of either a basal diet (control) or a basal diet supplemented with fibre (15 g/d). MF resisted fermentation better than PF and had lower digestibility. However, both fibres increased faecal output of dry matter, neutral sugars and water. There was an inverse relationship between stool weight and orofaecal transit time, although only MF significantly reduced transit time. Orocaecal transit was lengthened by PF, probably because of its high WBC. PF ingestion also decreased postprandial plasma levels of total and esterified cholesterol but had no effect on fasting concentrations. In contrast, MF lowered fasting cholesterolaemia and increased free:esterified cholesterol. These particular physiological and fermentative properties suggest that PF and MF would be suitable ingredients in a healthy diet.

A Proposed Role of Surfactant in Platelet Function and Treatment of Pulmonary Hemorrhage in Preterm and Term Infants

2018 ◽  
Vol 140 (4) ◽  
pp. 215-220
Author(s):  
Tal  Sadeh-Vered ◽  
Nurit  Rosenberg ◽  
Iris  Morag ◽  
Asaf A. Berg ◽  
Gili Kenet ◽  
...  
Keyword(s):  
Preterm Infants ◽  
Platelet Activation ◽  
Platelet Function ◽  
Complete Blood Count ◽  
Binding Capacity ◽  
Pulmonary Hemorrhage ◽  
Adenosine Diphosphate ◽  
Term Infants ◽  
Average Size

Background: We evaluated the effect of surfactant on platelet function as a potential contributing mechanism to the pathogenesis of pulmonary hemorrhage (PHEM) in term and preterm infants. Methods: Cord blood samples were collected from neonates following delivery. Complete blood count and platelet function were measured using a cone and platelet analyzer (CPA). Increasing surfactant concentrations were added to platelets in vitro, and the adhesion molecule P-selectin and the monoclonal antibody PAC-1 were evaluated following platelet activation by flow cytometry. Results: Forty-one infants (11 preterm and 30 term) were studied. CPA revealed a significant decrease in the average size of the aggregates and in platelet adhesion when surfactant was added. In term infants, the addition of surfactant to native platelets yielded an increased binding capacity of PAC-1 but did not affect P-selectin expression. In preterm infants, platelet activation with adenosine diphosphate in the presence of a high surfactant concentration (0.5 mg/mL) resulted in increased PAC-1 binding and no change in P-selectin expression. Conclusions: The platelets of preterm infants are less active (hyporesponsive) than those of term infants, both in their native state as well as after stimulation with various agonists. Surfactant may play an important role in treating PHEM in preterm infants.

Development of Gelatin-Thai Silk Fibroin Microspheres for Three Dimensional Cell Culture

2014 ◽  
Vol 931-932 ◽  
pp. 200-204
Author(s):  
S. Sinthop ◽  
S. Patumraj ◽  
S. Kanokpanont
Keyword(s):  
Silk Fibroin ◽  
High Surface ◽  
High Surface Area ◽  
Three Dimensional ◽  
Chemical Properties ◽  
Tissue Engineering Scaffolds ◽  
Gelatin Microspheres ◽  
Size And Morphology ◽  
Average Size

Microspheres have been widely used for tissue engineering scaffolds. Microspheres have many advantages over the macrostructure such as high surface area for cell adhesion and proliferation and low mass transfer limits. In this study, we fabricated microspheres from gelatin and silk fibroin using water-in-oil (w/o) emulsion technique and glutaraldehyde crosslinking. Gelatin (G) and silk fibroin (SF) were blended at different G/SF weight blending ratios of 100/0, 90/10, 70/30, and 50/50. Physical and chemical properties of the microspheres including size and morphology were characterized. The Average size of microspheres obtained were at 858.42±41.93, 832.97± 9.44 , 785.24±17.66 and 735.83 ±13.19 μm, respectively. Morphology of G/SF microspheres was observed under a scanning electron microscope. Blending of silk fibroin increased the crosslinking degrees and water absorption. It also reduced degradation rate, comparing to the gelatin microspheres. Thein vitroattachment and proliferation of rat bone marrow derived mesenchymal stem cells (MSC) cultured on G/SF microspheres were evaluated. G/SF 50/50 microspheres promoted the highest attachment of MSC on microspheres (46.0±5.8% of initial seeding at 6 hr). The G/SF 70/30 microspheres promoted the higher cell proliferation of MSC compared the others. Specific growth rate of the cells on the microspheres was at 9.85x10-3h-1.

scholarly journals Relationship between Chemical Properties of Alginate Extracted from Brown Algae and Sodium Ion Binding Capacity in vitro.

1996 ◽  
Vol 43 (5) ◽  
pp. 569-574 ◽  
Author(s):  
Hiroyuki UKEDA ◽  
Michiko IIDA ◽  
Masayoshi SAWAMURA ◽  
Hirozo KUSUNOSE
Keyword(s):  
Brown Algae ◽  
Binding Capacity ◽  
Chemical Properties ◽  
Sodium Ion ◽  
Ion Binding

Investigation of the Free and Total Thyroxine-binding Capacity of Plasma Proteins in Thyroid Disorders

1971 ◽  
Vol 10 (04) ◽  
pp. 299-304
Author(s):  
József Takó ◽  
János Fischer ◽  
Jusztina Juhász ◽  
Ilona Sztraka ◽  
István Kapus ◽  
...  
Keyword(s):  
Blood Cell ◽  
Thyroid Function ◽  
Oral Contraceptives ◽  
Red Blood Cell ◽  
Plasma Proteins ◽  
Binding Capacity ◽  
Thyroid Disorders ◽  
Thyroid Function Tests ◽  
Total Thyroxine

SummaryThe results of thyroid function tests have been compared with data on the thyroxine-binding capacity of plasma proteins in hyper-, hypo- and euthyroid cases, the latter including women taking oral contraceptives (Infecundin). It was found that there exists a significant correlation of exponential nature between the in vitro red blood cell 125I-triiodothyronine uptake (RCU) and the free thyroxine-binding capacity of the thyroxine-inding globulin (TBG).

In Vitro and in Vivo Comparison of Binding of 99m-Tc-Iabeled Anti-CEA MAb F33-104 with 99m-Tc-labeled Anti-CEA MAb BW431/26

1999 ◽  
Vol 38 (04) ◽  
pp. 115-119
Author(s):  
N. Oriuchi ◽  
S. Sugiyama ◽  
M. Kuroki ◽  
Y. Matsuoka ◽  
S. Tanada ◽  
...  
Keyword(s):  
Nude Mice ◽  
Binding Capacity ◽  
Colon Adenocarcinoma ◽  
Human Colon ◽  
Cell Binding ◽  
Vitro Binding ◽  
Labeling Method ◽  
Human Colon Adenocarcinoma

Summary Aim: The purpose of this study was to assess the potential for radioimmunodetection (RAID) of murine anti-carcinoembryonic antigen (CEA) monoclonal antibody (MAb) F33-104 labeled with technetium-99m (99m-Tc) by a reduction-mediated labeling method. Methods: The binding capacity of 99m-Tc-labeled anti-CEA MAb F33-104 with CEA by means of in vitro procedures such as immunoradiometric assay and cell binding assay and the biodistribution of 99m-Tc-labeled anti-CEA MAb F33-104 in normal nude mice and nude mice bearing human colon adenocarcinoma LS180 tumor were investigated and compared with 99m-Tc-labeled anti-CEA MAb BW431/26. Results: The in vitro binding rate of 99m-Tc-labeled anti-CEA MAb F33-104 with CEA in solution and attached to the cell membrane was significantly higher than 99m-Tclabeled anti-CEA MAb BW431/261 (31.4 ± 0.95% vs. 11.9 ± 0.55% at 100 ng/mL of soluble CEA, 83.5 ± 2.84% vs. 54.0 ± 2.54% at 107 of LS 180 cells). In vivo, accumulation of 99m-Tc-labeled anti-CEA MAb F33-104 was higher at 18 h postinjection than 99m-Tc-labeled anti-CEA MAb BW431/26 (20.1 ± 3.50% ID/g vs. 14.4 ± 3.30% ID/g). 99m-Tcactivity in the kidneys of nude mice bearing tumor was higher at 18 h postinjection than at 3 h (12.8 ± 2.10% ID/g vs. 8.01 ± 2.40% ID/g of 99m-Tc-labeled anti-CEA MAb F33-104, 10.7 ± 1.70% ID/g vs. 8.10 ± 1.75% ID/g of 99m-Tc-labeled anti-CEA MAb BW431/26). Conclusion: 99m-Tc-labeled anti-CEA MAb F33-104 is a potential novel agent for RAID of recurrent colorectal cancer.

Development and Ex-vivo Evaluation of Topiramate Mucoadhesive Nanoparticles for Intranasal Delivery

2020 ◽  
Vol 13 (6) ◽  
pp. 5250-5255
Author(s):  
Ashwin Kumar Tulasi ◽  
Anil Goud Kandhula ◽  
Ravi Krishna Velupula
Keyword(s):  
Particle Size ◽  
Nasal Mucosa ◽  
Intranasal Administration ◽  
Ex Vivo ◽  
Chemical Properties ◽  
Brain Targeting ◽  
Oral Tablet ◽  
Promising Alternative ◽  
Ex Vivo Permeation

Topiramate is a second-generation antiepileptic drug used in partial, generalized seizures as an oral tablet. Oral route of administration is most convenient but shows delayed absorption. Moreover, in emergency cases, parenteral administration is not possible as it requires medical assistance. Hence, the present study was aimed to develop topiramate mucoadhesive nanoparticles for intranasal administration using ionotropic gelation method. The developed nanoparticles were evaluated for physico-chemical properties like particle size, zeta potential, surface morphology, drug content, entrapment efficiency, in vitro drug release, mucoadhesive strength, and ex vivo permeation studies in excised porcine nasal mucosa. Optimized nanoparticle formulation (T9) was composed oil mucoadhesive agent (Chitosan 1% w/w), cross linking polymer (TPP) and topiramate 275mg, 100mg and 4% respectively. It showed particle size of 350nm, high encapsulation efficacy and strong mucoadhesive strength. In vitro drug diffusion of optimized formulation showed 95.12% release of drug after 180min. Ex-vivo permeation of drug across nasal mucosa was   88.05 % after 180min. Nasocilial toxicity studies showed optimized formulation did not damage the nasal mucosa. Thus, the intranasal administration of topiramate using chitosan can be a promising alternative for brain targeting and the treatment of epilepsy.

Quality-by-Design Enabled Chitosan Nanoparticles for Antitubercular Therapy: Formulation, Statistical Optimization, and In vitro Characterization

2020 ◽  
Vol 15 ◽  
Author(s):  
Manasi M. Chogale ◽  
Sujay S. Gaikwad ◽  
Savita P. Kulkarni ◽  
Vandana B. Patravale
Keyword(s):  
Side Effects ◽  
Treatment Regimen ◽  
Research Work ◽  
Chitosan Nanoparticles ◽  
In Vitro Release ◽  
Antitubercular Therapy ◽  
Prolonged Treatment ◽  
High Dose ◽  
Average Size

Background: Tuberculosis (TB) continues to be among the leading causes for high mortality among developing countries. Though a seemingly effective treatment regimen against TB is in place, there has been no significant improvement in the therapeutic rates. This is primarily owing to the high drug doses, their associated sideeffects, and prolonged treatment regimen. Discontinuation of therapy due to the severe side effects of the drugs results in the progression of the infection to the more severe drug-resistant TB. Objectives: Reformulation of the current existing anti TB drugs into more efficient dosage forms could be an ideal way out. Nanoformulations have been known to mitigate the side effects of toxic, high-dose drugs. Hence, the current research work involves the formulation of Isoniazid (INH; a first-line anti TB molecule) loaded chitosan nanoparticles for pulmonary administration. Methods: INH loaded chitosan nanoparticles were prepared by ionic gelation method using an anionic crosslinker. Drugexcipient compatibility was evaluated using DSC and FT-IR. The formulation was optimized on the principles of Qualityby-Design using a full factorial design. Results: The obtained nanoparticles were spherical in shape having an average size of 620±10.97 nm and zeta potential +16.87±0.79 mV. Solid state characterization revealed partial encapsulation and amorphization of INH into the nanoparticulate system. In vitro release study confirmed an extended release of INH from the system. In vitro cell line based safety and efficacy studies revealed satisfactory results. Conclusion: The developed nanosystem is thus an efficient approach for antitubercular therapy.

In Vitro Assessment of Hydroxyapatite Coating on the Surface of Additive Manufactured Ti6Al4V Scaffolds

2016 ◽  
Vol 879 ◽  
pp. 2444-2449 ◽  
Author(s):  
Ekaterina Chudinova ◽  
Maria Surmeneva ◽  
Andrey Koptioug ◽  
Irina V. Savintseva ◽  
Irina Selezneva ◽  
...  
Keyword(s):  
Stem Cells ◽  
Mesenchymal Stem Cells ◽  
Human Mesenchymal Stem Cells ◽  
Nanocrystalline Structure ◽  
X Ray Diffraction ◽  
Ha Coating ◽  
Magnetron Sputter Deposition ◽  
In Vitro Assessment ◽  
Average Size

Custom orthopedic and dental implants may be fabricated by additive manufacturing (AM), for example using electron beam melting technology. This study is focused on the modification of the surface of Ti6Al4V alloy coin-like scaffolds fabricated via AM technology (EBM®) by radio frequency (RF) magnetron sputter deposition of hydroxyapatite (HA) coating. The scaffolds with HA coating were characterized by Scanning Electron microscopy, X-ray diffraction. HA coating showed a nanocrystalline structure with the crystallites of an average size of 32±9 nm. The ability of the surface to support adhesion and the proliferation of human mesenchymal stem cells was studied using biological short-term tests in vitro. In according to in vitro assessment, thin HA coating stimulated the attachment and proliferation of cells. Human mesenchymal stem cells cultured on the HA-coated scaffold also formed mineralized nodules.

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