scholarly journals A Way to Increase the Bioaccesibility and Photostability of Roflumilast, a COPD Treatment, by Cyclodextrin Monomers

Polymers ◽  
2019 ◽  
Vol 11 (5) ◽  
pp. 801 ◽  
Author(s):  
Adrián Matencio ◽  
Samanta Hernández-García ◽  
Francisco García-Carmona ◽  
José Manuel López-Nicolás
Keyword(s):  
Adverse Effects ◽  
In Vitro Digestion ◽  
Chronic Obstructive ◽  
Fluorescence Signal ◽  
Complexation Constant ◽  
Chronic Obstructive Pulmonary Diseases ◽  
Increasing Temperature ◽  
First Time ◽  
Low Solubility

Roflumilast is an orally available inhibitor of phosphodiesterase (PDE) type 4, which is widely used in chronic obstructive pulmonary diseases. However, it has low solubility and adverse effects include diarrhea and nausea. Since its solubilization may improve treatment and, dismissing any adverse effects, its interaction with cyclodextrins (CDs) was studied. The Higuchi-Connors method was used to determine the complexation constant with different CDs, pH values and temperatures. Molecular docking was used to predict interaction between the complexes. An in vitro digestion experiment was carried out to test roflumilast protection. Finally, the photostability of the complex was evaluated. The complex formed with β-CD had the highest K11 value (646 ± 34 M−1), although this value decreased with increasing temperature. Similarly, K11 decreased as the pH increased. In vitro digestion showed that CDs protect the drug during digestion and even improve its bioaccessibility. Finally, CDs reduced the drug’s extreme photosensitivity, originating a fluorescence signal, which is described for first time. The kinetic parameters of the reaction were obtained. This study not only completes the complexation study of roflumilast-CD, but also points to the need to protect roflumilast from light, suggesting that tablets containing the drug might be reformulated.

scholarly journals Impact of Acetic Acid on the Survival ofL. plantarumupon Microencapsulation by Coaxial Electrospraying

2017 ◽  
Vol 2017 ◽  
pp. 1-6 ◽  
Author(s):  
Laura G. Gómez-Mascaraque ◽  
Jesús Ambrosio-Martín ◽  
Rocío Perez-Masiá ◽  
Amparo Lopez-Rubio
Keyword(s):  
Acetic Acid ◽  
Inner Core ◽  
In Vitro Digestion ◽  
Probiotic Bacteria ◽  
Whey Protein Concentrate ◽  
Protein Concentrate ◽  
Outer Solution ◽  
Protein Particles ◽  
First Time

In this work, coaxial electrospraying was used for the first time to microencapsulate probiotic bacteria, specificallyLactobacillus plantarum, within edible protein particles with the aim of improving their resistance to in vitro digestion. The developed structures, based on an inner core of whey protein concentrate and an outer layer of gelatin, were obtained in the presence of acetic acid in the outer solution as a requirement for the electrospraying of gelatin. Despite the limited contact of the inner suspension and outer solution during electrospraying, the combination of the high voltage used during electrospraying with the presence of acetic acid was found to have a severe impact on the lactobacilli, not only decreasing initial viability but also negatively affecting the survival of the bacteria during storage and their resistance to different stress conditions, including simulated in vitro digestion.

In vitro digestion of citric acid esters of mono- and diglycerides (CITREM) and CITREM-containing infant formula/emulsions

2014 ◽  
Vol 5 (7) ◽  
pp. 1409-1421 ◽  
Author(s):  
Sawsan Amara ◽  
Amaury Patin ◽  
Francesca Giuffrida ◽  
Tim J. Wooster ◽  
Sagar K. Thakkar ◽  
...  
Keyword(s):  
Citric Acid ◽  
Infant Formula ◽  
In Vitro Digestion ◽  
First Time ◽  
Digestive Lipases ◽  
Acid Esters

The GI lipolysis of CITREM is investigated for the first time using various digestive lipases and a two-stepin vitrodigestion model.

scholarly journals Characterization of Resveratrol, Oxyresveratrol, Piceatannol and Roflumilast as Modulators of Phosphodiesterase Activity. Study of Yeast Lifespan

2020 ◽  
Vol 13 (9) ◽  
pp. 225
Author(s):  
Adrián Matencio ◽  
Francisco García-Carmona ◽  
José Manuel López-Nicolás
Keyword(s):  
Pde4 Inhibitor ◽  
Chronic Obstructive ◽  
Phosphodiesterase Activity ◽  
Chronic Obstructive Pulmonary Diseases ◽  
Phosphodiesterase Type ◽  
Approved Drugs

Our desire to live longer has led to an ever-increasing number of novel antiaging products. However, few molecules have any real effect and new ones need to be studied before they can be used commercially. In this contribution, activation of the caloric restriction (CR) pathway was studied using different three (resveratrol, oxyresveratrol and piceatannol)—a family with demonstrated bioactivity on phosphodiesterase activity. The high-affinity phosphodiesterase type 2 (PDE2) of Saccharomyces cerevisiae was expressed in Escherichia coli, purified and characterized. The activity and the inhibitory activity of each stilbene was studied, and the findings were compared in vitro and in silico with those obtained with roflumilast—a human PDE4 inhibitor widely used in chronic obstructive pulmonary diseases. Finally, an in vivo chronological lifespan assay using WT S. cerevisiae and ΔPDE2 S. cerevisiae strains was carried out. It was demonstrated that stilbenes can modulate yPDE2 activity, increasing the lifespan of the yeast by 18% over a control (in combination with other pathways). In addition, roflumilast increased the lifespan in the WT strain. The findings as a whole would increase the range of lifespan products available and suggest novel uses for approved drugs.

Development of antioxidant gliadin particle stabilized Pickering high internal phase emulsions (HIPEs) as oral delivery systems and the in vitro digestion fate

2018 ◽  
Vol 9 (2) ◽  
pp. 959-970 ◽  
Author(s):  
F. Z. Zhou ◽  
T. Zeng ◽  
S. W. Yin ◽  
C. H. Tang ◽  
D. B. Yuan ◽  
...  
Keyword(s):  
Lipid Oxidation ◽  
Chemical Stability ◽  
Oral Delivery ◽  
In Vitro Digestion ◽  
Delivery Systems ◽  
Algal Oil ◽  
Internal Phase ◽  
First Time ◽  
Oral Delivery Systems

In this paper, we demonstrate for the first time the use of gliadin particles to structure algal oil (rich in DHA) and to exert chemical stability against lipid oxidation via the Pickering high internal phase emulsion (HIPE) strategy.

scholarly journals Moringa oleifera—Storage Stability, In Vitro-Simulated Digestion and Cytotoxicity Assessment of Microencapsulated Extract

Processes ◽  
2020 ◽  
Vol 8 (7) ◽  
pp. 770
Author(s):  
Cecilia Castro-López ◽  
Catarina Gonçalves ◽  
Janeth M. Ventura-Sobrevilla ◽  
Lorenzo M. Pastrana ◽  
Cristóbal N. Aguilar-González ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
In Vitro Digestion ◽  
Storage Conditions ◽  
Simulated Digestion ◽  
A Cell ◽  
Total Polyphenolic Content ◽  
Cytotoxicity Assessment ◽  
First Time ◽  
And Storage

Moringa extract was microencapsulated for the first time by spray-drying technique using tragacanth gum (MorTG) to improve its stability under gastrointestinal and storage conditions, assessing total polyphenolic content (TPC) and antioxidant activity. Additionally, cytotoxicity of the microencapsulated components was evaluated after contact with Caco-2 cells. Results showed that TPC was released as follows—oral (9.7%) < gastric (35.2%) < intestinal (57.6%). In addition, the antioxidant activity in in vitro digestion reached up to 16.76 ±0.15 mg GAE g−1, which was 300% higher than the initial value. Furthermore, microencapsulated moringa extract presented a half-life up to 45 days of storage, where the noticeably change was observed at 35 °C and 52.9% relative humidity. Finally, direct treatment with 0.125 mg mL−1 MorTG on Caco-2 cells showed a slight antiproliferative effect, with a cell viability of approx. 87%. Caco-2 cells’ viability demonstrated non-cytotoxicity, supporting the safety of the proposed formulation and potential use within the food field.

scholarly journals Toxoplasmicidal in vitro effect of dehydroepiandrosterone on Toxoplasma gondii extracellular tachizoytes

2020 ◽  
Author(s):  
Saé Muñiz-Hernández ◽  
Carmen T. Gómez de León ◽  
Angélica Luna Nophal ◽  
Lenin Domínguez-Ramírez ◽  
Olga-Araceli Patrón-Soberano ◽  
...  
Keyword(s):  
Toxoplasma Gondii ◽  
Adverse Effects ◽  
Molecular Level ◽  
Protozoan Parasite ◽  
New Drugs ◽  
Limited Effectiveness ◽  
Vitro Effect ◽  
First Time ◽  
In Vitro Treatment

AbstractToxoplasmosis is a zoonotic disease caused by the apicomplexa protozoan parasite Toxoplasma gondii. This disease is a health burden, mainly in pregnant women and immunocompromised individuals, in whom they can cause death. Despite advances in the medical area, nowadays there are no new drugs to treat toxoplasmosis. The standard therapy to toxoplasmosis has not had progress for last seven decades; it is a combination of sulfadiazine-pyrimethamine (S-P); which is co-administered with folic acid due to the adverse effects of the drug. Several studies have shown that the conventional treatment has limited effectiveness and severe adverse effects. Thus, the search of better treatments with greater efficacy and without the adverse effects becomes relevant. In the current work we demonstrate for the first time the parasiticidal effect of dehydroepiandrosterone (DHEA), a steroid hormone produced by many mammals, on extracellular tachyzoites (the infective stage of T. gondii). In vitro treatment with DHEA reduces the viability of extracellular tachyzoites, and both the active and passive invasion processes. The ultrastructural analysis of treated parasites showed that DHEA alters the cytoskeleton structures, leading in the lost of the organelle structure and organization, as well as, the lost of the cellular shape. On a molecular level, we observed an important reduction of the expression of several proteins that are essential for the motility and virulence of parasites when they were exposed to DHEA. These results suggest that DHEA could be used as an alternative treatment against toxoplasmosis.

An in vitro digestion method adapted for carotenoids and carotenoid esters: moving forward towards standardization

2016 ◽  
Vol 7 (12) ◽  
pp. 4992-5001 ◽  
Author(s):  
Daniele Bobrowski Rodrigues ◽  
Lilian Regina Barros Mariutti ◽  
Adriana Zerlotti Mercadante
Keyword(s):  
In Vitro Digestion ◽  
Digestion Method ◽  
Before And After ◽  
Systematic Identification ◽  
First Time

The consensus INFOGESTin vitrodigestion method was adapted for carotenoids. The systematic identification of carotenoid esters before and afterin vitrodigestion is presented for the first time.

Somatic Embryogenesis and In vitro Plant Regeneration in Vigna trilobata (L.) Verd. - A Potential Pasture Legume

1970 ◽  
Vol 19 (1) ◽  
pp. 89-99
Author(s):  
K. Choudhary ◽  
M. Singh ◽  
M. S. Rathore ◽  
N. S. Shekhawat
Keyword(s):  
Somatic Embryogenesis ◽  
Growth Regulators ◽  
Somatic Embryos ◽  
Basal Medium ◽  
Long Term Study ◽  
Continuous Application ◽  
First Time ◽  
Pasture Legume

This long term study demonstrates for the first time that it is possible to propagate embryogenic Vigna trilobata and to subsequently initiate the differentiation of embryos into complete plantlets. Initiation of callus was possible on 2,4-D. Somatic embryos differentiated on modified MS basal nutrient medium with 1.0 mg/l  of 2,4-D and 0.5 mg/l  of Kn. Sustained cell division resulted in globular and heart shape stages of somatic embryos. Transfer of embryos on to a fresh modified MS basal medium with 0.5 mg/l of Kn and 0.5 mg/l of GA3 helped them to attain maturation and germination. However, the propagation of cells, as well as the differentiation of embryos, were inhibited by a continuous application of these growth regulators. For this reason, a long period on medium lacking these growth regulators was necessary before the differentiation of embryos occurred again. The consequences for improving the propagation of embryogenic cultures in Vigna species are discussed. Key words: Pasture  legume, Vigna trilobata, Globular, Heart shape, somatic embryogenesis D.O.I. 10.3329/ptcb.v19i1.4990 Plant Tissue Cult. & Biotech. 19(1): 89-99, 2009 (June)

Dwindling status of Epimedium Elatum (Morren & Decne) and its geographical distribution in Kashmir Himalaya, India

2018 ◽  
pp. 47-52
Keyword(s):  
Medicinal Plant ◽  
Biological Activities ◽  
Conservation Status ◽  
Natural Populations ◽  
Culture Techniques ◽  
Kashmir Himalayas ◽  
Near Future ◽  
First Time ◽  
Tissue Culture Techniques

Epimedium elatum (Morren & Decne) of family Berberidaceace is a rare perennial medicinal plant, endemic to high altitude forests of Northwestern Himalayas in India. Ethnobotanically, it has been used as an ingredient for treatment of bone-joint disorders, impotence and kidney disorders in Kashmir Himalayas. Phytochemically, it is rich in Epimedin ABC and Icariin; all of these have been demonstrated to possess remarkable biological activities like PDE-5 inhibition (treatment of erectile dysfunction), anticancer, antiosteoporosis antioxidant and antiviral properties. The present investigation reports its traditional usage, comprehensive distribution and conservation status from twenty ecogeographical regions in Kashmir Himalayas, India. The species was reported from Gurez valley for the first time. Numerous threats like excessive grazing, deforestration, habitat fragmentation, tourism encroachment, landslides and excessive exploitation have decreased its natural populations in most of the surveyed habitats. Consequently, its existence may become threatened in near future if timely conservation steps are not taken immediately by concerned stakeholders involved in medicinal plant research. Moreover, use of plant tissue culture techniques is recommended for development of its in vitro propagation protocols. Therefore, introduction of this medicinal plant in botanical gardens, protected sites and development of monitoring programmes are needed for its immediate conservation in Northwestern Himalayas, India.

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