Release mechanism between sarcoplasmic protein–bound and free heterocyclic amines and the effects of dietary additives using an in-vitro digestion model

Rebamipide, an amino acid derivative of 2-(1H)-quinolinone, is used for mucosal protection, healing of gastroduodenal ulcers, and treatment of gastritis. The current research study aimed to develop novel gastro-retentive mucoadhesive microspheres of rebamipide using ionotropic gelation technique. Studies of micromeritic properties confirmed that microspheres were free flowing with good packability. The in vitro drug release showed the sustained release of rebamipide up to 99.23 ± 0.13% within 12 h whereas marketed product displayed the drug release of 95.15 ± 0.23% within 1 h. The release mechanism from microspheres followed the zero-order and Korsmeyer-Peppas (R2 = 0.915, 0.969), respectively. The optimized M12 formulation displayed optimum features, such as entrapment efficiency 97%, particle size 61.94 ± 0.11 µm, percentage yield 98%, swelling index 95% and mucoadhesiveness was 97%. FTIR studies revealed no major incompatibility between drug and excipients. SEM confirmed the particles were of spherical in shape. Optimized formulation (M12) were stable at 40°C ± 2°C/75% RH ± 5% RH for 6 months. In vivo studies were performed and kinetic parameters like Cmax, Tmax, AUC0-t, AUC0-∞, t1/2, and Kel were calculated. The marketed product Cmax (3.15 ± 0.05 ng/mL) was higher than optimized formulation (2.58 ± 0.03 ng/mL). The optimized formulation AUC0-t (15.25 ± 1.14 ng.hr/mL), AUC0-∞ (19.42 ± 1.24 ng.hr/mL) was significantly higher than that of marketed product AUC0-t (10.21 ± 1.26 ng.hr/mL) and AUC0-∞ (13.15 ± 0.05 ng.hr/mL). These results indicate an optimized formulation bioavailability of 2.5-fold greater than marketed product.

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In Vivo Nylon Bag vs. Two‐Stage In Vitro Digestion: Comparison of Two Techniques for Estimating Dry‐Matter Digestibility of Forages 1

Agronomy Journal ◽

10.2134/agronj1969.00021962006100040032x ◽

1969 ◽

Vol 61 (4) ◽

pp. 587-589 ◽

Cited By ~ 30

Author(s):

W. G. Manson ◽

R. S. Lowrey ◽

Ian Forbes

Keyword(s):

Dry Matter ◽

In Vitro Digestion ◽

Two Stage ◽

Dry Matter Digestibility

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

Current Drug Delivery ◽

10.2174/1567201817666200210120231 ◽

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.

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Differential impact of Holder and High Temperature Short Time pasteurization on the dynamic in vitro digestion of human milk in a preterm newborn model

Food Chemistry ◽

10.1016/j.foodchem.2020.127126 ◽

2020 ◽

Vol 328 ◽

pp. 127126 ◽

Cited By ~ 2

Author(s):

Stefano Nebbia ◽

Marzia Giribaldi ◽

Laura Cavallarin ◽

Enrico Bertino ◽

Alessandra Coscia ◽

...

Keyword(s):

High Temperature ◽

Human Milk ◽

In Vitro Digestion ◽

Preterm Newborn ◽

Differential Impact ◽

High Temperature Short Time ◽

Short Time

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Interaction between barley β-glucan and corn starch and its effects on the in vitro digestion of starch

International Journal of Biological Macromolecules ◽

10.1016/j.ijbiomac.2019.08.268 ◽

2019 ◽

Vol 141 ◽

pp. 240-246 ◽

Cited By ~ 3

Author(s):

Hui Zhang ◽

Zhi Li ◽

Yanjun Tian ◽

Zibo Song ◽

Lianzhong Ai

Keyword(s):

Corn Starch ◽

In Vitro Digestion

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Bovine Milk-Derived Emulsifiers Increase Triglyceride Absorption in Newborn Formula-Fed Pigs

Nutrients ◽

10.3390/nu13020410 ◽

2021 ◽

Vol 13 (2) ◽

pp. 410 ◽

Cited By ~ 1

Author(s):

Kristine Bach Korsholm Knudsen ◽

Christine Heerup ◽

Tine Røngaard Stange Jensen ◽

Xiaolu Geng ◽

Nikolaj Drachmann ◽

...

Keyword(s):

Milk Fat ◽

Bovine Milk ◽

In Vitro Digestion ◽

Lipid Absorption ◽

Lipid Digestion ◽

Soy Lecithin ◽

Neonatal Piglets ◽

Milk Fat Globule Membranes

Efficient lipid digestion in formula-fed infants is required to ensure the availability of fatty acids for normal organ development. Previous studies suggest that the efficiency of lipid digestion may depend on whether lipids are emulsified with soy lecithin or fractions derived from bovine milk. This study, therefore, aimed to determine whether emulsification with bovine milk-derived emulsifiers or soy lecithin (SL) influenced lipid digestion in vitro and in vivo. Lipid digestibility was determined in vitro in oil-in-water emulsions using four different milk-derived emulsifiers or SL, and the ultrastructural appearance of the emulsions was assessed using electron microscopy. Subsequently, selected emulsions were added to a base diet and fed to preterm neonatal piglets. Initially, preterm pigs equipped with an ileostomy were fed experimental formulas for seven days and stoma output was collected quantitatively. Next, lipid absorption kinetics was studied in preterm pigs given pure emulsions. Finally, complete formulas with different emulsions were fed for four days, and the post-bolus plasma triglyceride level was determined. Milk-derived emulsifiers (containing protein and phospholipids from milk fat globule membranes and extracellular vesicles) showed increased effects on fat digestion compared to SL in an in vitro digestion model. Further, milk-derived emulsifiers significantly increased the digestion of triglyceride in the preterm piglet model compared with SL. Ultra-structural images indicated a more regular and smooth surface of fat droplets emulsified with milk-derived emulsifiers relative to SL. We conclude that, relative to SL, milk-derived emulsifiers lead to a different surface ultrastructure on the lipid droplets, and increase lipid digestion.

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