scholarly journals Cornea-PAMPA as an Orthogonal in Vitro Physicochemical Model of Corneal Permeability

2020 ◽  
Vol 64 (3) ◽  
pp. 384-390
Author(s):  
Anna Vincze ◽  
Gergő Dargó ◽  
György Tibor Balogh
Keyword(s):  
Physicochemical Properties ◽  
Passive Diffusion ◽  
Gastrointestinal Absorption ◽  
Absorption Model ◽  
Physicochemical Model ◽  
Corneal Permeability ◽  
Cellular Permeability ◽  
Permeability Assay ◽  
Permeability Data

The present study was aimed to investigate the relationships between permeability and membrane retention values (logPe and MR) of the in vitro non-cellular permeability assay, corneal-PAMPA in comparison with experimental Caco-2 permeability data and calculated physicochemical properties (MW, clogP, clogD7.4 , TPSA). For the investigation, 50 structurally and physicochemically diverse drugs were selected and measured in PAMPA model optimized for corneal permeability. The results showed corneal-PAMPA model's orthogonality in terms of passive diffusion to the FDA approved Caco-2 as a gastrointestinal absorption model, while the comparison with physicochemical properties revealed trends between logPe , MR and the lipophilicity descriptors and TPSA.

Biopharmaceutical and pharmacokinetic activities of oxymatrine determined by a sensitive UHPLC-MS/MS method

2021 ◽  
Vol 22 ◽  
Author(s):  
Hai-Qiao Wang ◽  
Feng-Hua Chen ◽  
Liang Wang ◽  
Li-Qun Chi ◽  
Guang-Hua Wang
Keyword(s):  
Rat Liver ◽  
Liver Microsomes ◽  
Passive Diffusion ◽  
Pharmacokinetic Parameters ◽  
Rat Liver Microsomes ◽  
Absorption Model ◽  
Absolute Oral Bioavailability ◽  
Rat Liver Microsome

Background: Oxymatrine is one of the most promising alkaloids from Sophora flavescens for its excellent pharmacological effects. Objective: The aim of this research is to assess the biopharmaceutical and pharmacokinetic activities of oxymatrine, and clarify its mechanisms of absorption and metabolism. Methods: The biological characteristics of oxymatrine were systematically investigated by UHPLC-MS/MS. The mechanisms of absorption and metabolism of oxymatrine were further clarified through incubation in rat liver microsomes and transport across Caco-2 monolayer cell absorption model. Results: It was found that the absolute oral bioavailability of oxymatrine was 26.43% and the pharmacokinetic parameters Cmax, Tmax, and t1/2 were 605.5 ng/mL, 0.75 h, and 4.181 h after oral administration, indicating that oxymatrine can be absorbed quickly. The tissue distribution tests showed that oxymatrine distributed throughout all the organs, with the small intestine accumulating the highest level followed by kidney, stomach and spleen. The Papp in Caco-2 cell line absorption model was over 1 × 10-5 and PDR 1.064, t1/2 of oxymatrine in rat liver microsome in vitro was 1.042 h, indicating that oxymatrine can be absorbed easily through passive diffusion and CYP450 enzymes could be involved in its metabolism. The plasma protein binding rate of oxymatrine was 2.78 ± 0.85%. Conclusion: Oxymatrine can be absorbed into blood easily through passive diffusion, mainly distributed in the intestine, stomach, liver and spleen in vivo, and CYP450 enzymes in liver could be involved in its metabolism.

PREPARATION AND CHARACTERISATION OF ACETYLATED WHEAT STARCH SUPPORTING FOR DIABETES TREATMENT

2018 ◽  
Vol 8 (5) ◽  
pp. 78-84
Author(s):  
Uyen Tran Thi Ngoc ◽  
Nam Nguyen Khac ◽  
Dung Tran Huu
Keyword(s):  
Physicochemical Properties ◽  
Resistant Starch ◽  
Starch Content ◽  
Degree Of Substitution ◽  
Wheat Starch ◽  
Diabetes Treatment ◽  
Glucose Response ◽  
Swelling Capacity ◽  
Wheat Starches

Background: The purpose of the study was to prepare acetylated wheat starches which have amylase hydrolysis resistant capacity to use as functional food supporting for diabetes treatment. Method: Acetate wheat starches were prepared by acetylation reaction of native wheat starch with different mole ratios of acetic anhydride. These starches were determined for the physicochemical properties by 1H-NMR, SEM, X-ray, DSC, solubility and swelling capacity, the resistant capacity by amylase hydrolysis in-vitro. Results: Acetate wheat starches were prepared successfully with the increase in acetyl content and degree of substitution corresponding with the increase of anhydride acetic, which resulted in the change of physicochemical properties of the wheat starches, including constitution, solubility, swelling capacity and contributed to the increase in resistant starch content in the acetate wheat starches. The AC150-9 containing 2.42% acetyl with degree of substitution 0,094 and resistant starch 32,11% is acceptable by FDA guideline about food safety. Conclusion: Acetate wheat starches contain low rate of digestive starch, while containing a higher proportion of resistant starch than natural wheat starch, possessing a high resistance to amylase activities. Thus, it is hope that this kind of starch to control the rapid increase of postprandual blood glucose response for diabetes treatments effectively. Key words: Acetate wheat starch, substitution, DS, RS, amylase

High-Pressure Homogenization Alters Physicochemical Properties and In Vitro Digestibility of Chinese Yam (Dioscorea Opposita Thunb.) Starch

2018 ◽  
Vol 18 (1) ◽  
pp. 10-15
Author(s):  
Wang Yi-Wei ◽  
He Yong-Zhao ◽  
An Feng-Ping ◽  
Huang Qun ◽  
Zeng Feng ◽  
...  
Keyword(s):  
High Pressure ◽  
Physicochemical Properties ◽  
Starch Content ◽  
In Vitro Digestibility ◽  
High Pressure Homogenization ◽  
Starch Granules ◽  
Cross Polarization ◽  
Chinese Yam ◽  
Crystal Type

In this study, Chinese yam starch-water suspension (8%) were subjected to high-pressure homogenization (HPH) at 100 MPa for increasing cycle numbers, and its effect of on the physicochemical properties of the starch was investigated. Results of the polarizing microscope observations showed that the starch granules were disrupted (i.e. greater breakdown value) after HPH treatment, followed by a decrease in cross polarization. After three HPH cycles, the crystallinity of starch decreased, while the crystal type remained unaltered. Meanwhile, the contents of rapidly digestible starch and slowly digestible starch were increased. On the contrary, resistant starch content was decreased. Our results indicate that HPH treatment resulted in reduction of starch crystallinity and increase of starch digestibility.

Moxifloxacin Hydrochloride-Loaded Eudragit® RL 100 and Kollidon® SR Based Nanoparticles: Formulation, In vitro Characterization and Cytotoxicity.

2020 ◽  
Vol 23 ◽  
Author(s):  
Gülsel Yurtdaş Kırımlıoğlu ◽  
Sinan Özer ◽  
Gülay Büyükköroğlu ◽  
Yasemin Yazan
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Spray Drying ◽  
Prolonged Release ◽  
Ocular Delivery ◽  
Corneal Permeability ◽  
Release Pattern ◽  
In Vitro Characterization ◽  
Ocular Bioavailability

Background: Considering the low ocular bioavailability of conventional formulations used for ocular bacterial infection treatment, there’s a need for designing efficient novel drug delivery systems that may enhance of precorneal retention time and corneal permeability. Aim and Objective: The current research focuses on developing nanosized and non-toxic Eudragit® RL 100 and Kollidon® SR nanoparticles loaded with moxifloxacin hydrochloride (MOX) for its prolonged release to be promising for effective ocular delivery. Methods: In this study, MOX was incorporation was carried out by spray drying method aiming ocular delivery. In vitro characteristics were evaluated in detail with different methods. Results: MOX was successfully incorporated into Eudragit® RL 100 and Kollidon® SR polymeric nanoparticles by spray-drying process. Particle size, zeta potential, entrapment efficiency, particle morphology, thermal, FTIR, XRD and NMR analyses and MOX quantification using HPLC method were carried out to evaluate the nanoparticles prepared. MOX loaded nanoparticles demonstrated nanosized and spherical shape while in vitro release studies demonstrated modified release pattern which followed Korsmeyer-Peppas kinetic model. Following successful incorporation of MOX into the nanoparticles, the formulation (MOX: Eudragit® RL 100, 1:5) (ERL-MOX 2) was selected for further studies by the reason of its better characteristics like cationic zeta potential, smaller particle size, narrow size distribution and more uniform prolonged release pattern. Moreover, ERL-MOX 2 formulation remained stable for 3 months and demonstrated higher cell viability values for MOX. Conclusion: In vitro characterization analyses showed that non-toxic, nano-sized and cationic ERLMOX 2 formulation has the potential of enhancing ocular bioavailability.

scholarly journals Development and physicochemical characterization of novel porous phosphate glass bone graft substitute and in vitro comparison with xenograft

2021 ◽  
Vol 32 (6) ◽  
Author(s):  
Niketa Chauhan ◽  
Nilay Lakhkar ◽  
Amol Chaudhari
Keyword(s):  
Cell Proliferation ◽  
Physicochemical Properties ◽  
Bone Graft ◽  
Phosphate Glass ◽  
Physicochemical Characterization ◽  
Bone Graft Substitute ◽  
Organic Content ◽  
In Vitro Cytotoxicity ◽  
Porous Phosphate

AbstractThe process of bone regeneration in bone grafting procedures is greatly influenced by the physicochemical properties of the bone graft substitute. In this study, porous phosphate glass (PPG) morsels were developed and their physicochemical properties such as degradation, crystallinity, organic content, surface topography, particle size and porosity were evaluated using various analytical methods. The in vitro cytotoxicity of the PPG morsels was assessed and the interaction of the PPG morsels with Dental Pulp Stem Cells (DPSCs) was studied by measuring cell proliferation and cell penetration depth. The cell-material interactions between PPG morsels and a commercially available xenograft (XG) were compared. The PPG morsels were observed to be amorphous, biocompatible and highly porous (porosity = 58.45%). From in vitro experiments, PPG morsels were observed to be non-cytotoxic and showed better cell proliferation. The internal surface of PPG was easily accessible to the cells compared to XG.

Physicochemical Properties and In Vitro Digestibility of Dual‐Modified Starch by Cross‐Linking and Annealing

2021 ◽  
pp. 2100102
Author(s):  
Shuyu Jia ◽  
Bin Yu ◽  
Haibo Zhao ◽  
Haiteng Tao ◽  
Pengfei Liu ◽  
...  
Keyword(s):  
Physicochemical Properties ◽  
Cross Linking ◽  
In Vitro Digestibility ◽  
Modified Starch

Co-extrusion of proanthocyanins from Chinese bayberry leaves modifies the physicochemical properties as well as the in vitro digestion of restructured rice

2021 ◽  
Vol 27 ◽  
pp. 100182
Author(s):  
Yuxue Zheng ◽  
Jinhu Tian ◽  
Yukiharu Ogawa ◽  
Xiuxiu Yin ◽  
Enbo Xu ◽  
...  
Keyword(s):  
Physicochemical Properties ◽  
In Vitro Digestion ◽  
Chinese Bayberry
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