scholarly journals Improvement of Chemical and Physical Properties and Antioxidant Evaluation of Eugenol – PEG Adduct

2017 ◽  
Vol 12 (3) ◽  
pp. 1934578X1701200 ◽  
Author(s):  
Marina Zacchigna ◽  
Francesca Cateni ◽  
Giuseppe Procida
Keyword(s):  
Physical Properties ◽  
Release Kinetics ◽  
Parent Drug ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Scavenging Activity ◽  
Buffer Solution ◽  
Antioxidant Evaluation ◽  
Phenolic Group

Eugenol (EU) – PEG adduct was synthesized to improve the chemical and physical properties of eugenol. The phenolic group was covalently bound to the carboxyl group of PEG and the release kinetics were studied in vitro in buffer solution at pH 7.4, in simulated gastric fluid and in mouse plasma. Studies in vitro on the release of the parent drug from the prodrug in various media indicate that the adduct may be sufficiently stable to pass intact into the gastrointestinal tract and release EU into the circulation. The antioxidant activity of PEG-EU adduct was also evaluated. Scavenging activity was absent in the original PEG-EU adduct but gradually increased on the basis of drug delivery.

scholarly journals Preparation, Characterization, and In Vitro Evaluation of Resveratrol-Loaded Cellulose Aerogel

Materials ◽  
2020 ◽  
Vol 13 (7) ◽  
pp. 1624
Author(s):  
Lili Qin ◽  
Xinyu Zhao ◽  
Yiwei He ◽  
Hongqiang Wang ◽  
Hanjing Wei ◽  
...  
Keyword(s):  
High Speed ◽  
Drug Carrier ◽  
Phosphate Buffer Solution ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Oxidized Cellulose ◽  
Buffer Solution ◽  
Aggregation State ◽  
Cellulose Aerogel

Resveratrol is a natural active ingredient found in plants, which is a polyphenolic compound and has a variety of pharmaceutical uses. Resveratrol-loaded TEMPO-oxidized cellulose aerogel (RLTA) was prepared using a freeze-drying method, employing high speed homogenization followed by rapid freezing with liquid nitrogen. RLTAs were designed at varying drug–cellulose aerogel ratios (1:2, 2:3, 3:2, and 2:1). It could be seen via scanning electron microscopy (SEM) that Res integrated into TEMPO-oxidized cellulose (TC) at different ratios, which changed its aggregation state and turned it into a short rod-like structure. Fourier transform infrared (FTIR) spectra confirmed that the RLTAs had the characteristic peaks of TC and Res. In addition, X-ray diffraction (XRD) demonstrated that the grain size of RLTA was obviously smaller than that of pure Res. RLTAs also had excellent stability in both simulated gastric fluid and phosphate buffer solution. The drug release rate was initially completed within 5 h under a loading rate of 30.7 wt%. The results of an MTT assay showed the low toxicity and good biocompatibility of the RLTAs. TC aerogel could be a promising drug carrier that may be widely used in designing and preparing novel biomedicine.

scholarly journals Formulation of Quaternized Aminated Chitosan Nanoparticles for Efficient Encapsulation and Slow Release of Curcumin

Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 449
Author(s):  
Ahmed M. Omer ◽  
Zyta M. Ziora ◽  
Tamer M. Tamer ◽  
Randa E. Khalifa ◽  
Mohamed A. Hassan ◽  
...  
Keyword(s):  
Slow Release ◽  
Sodium Tripolyphosphate ◽  
Chitosan Nanoparticles ◽  
Gastric Fluid ◽  
Release Profile ◽  
Simulated Gastric Fluid ◽  
Maximum Value ◽  
Structure Surface ◽  
Drug Encapsulation Efficiency

An effective drug nanocarrier was developed on the basis of a quaternized aminated chitosan (Q-AmCs) derivative for the efficient encapsulation and slow release of the curcumin (Cur)-drug. A simple ionic gelation method was conducted to formulate Q-AmCs nanoparticles (NPs), using different ratios of sodium tripolyphosphate (TPP) as an ionic crosslinker. Various characterization tools were employed to investigate the structure, surface morphology, and thermal properties of the formulated nanoparticles. The formulated Q-AmCs NPs displayed a smaller particle size of 162 ± 9.10 nm, and higher surface positive charges, with a maximum potential of +48.3 mV, compared to native aminated chitosan (AmCs) NPs (231 ± 7.14 nm, +32.8 mV). The Cur-drug encapsulation efficiency was greatly improved and reached a maximum value of 94.4 ± 0.91%, compared to 75.0 ± 1.13% for AmCs NPs. Moreover, the in vitro Cur-release profile was investigated under the conditions of simulated gastric fluid [SGF; pH 1.2] and simulated colon fluid [SCF; pH 7.4]. For Q-AmCs NPs, the Cur-release rate was meaningfully decreased, and recorded a cumulative release value of 54.0% at pH 7.4, compared to 73.0% for AmCs NPs. The formulated nanoparticles exhibited acceptable biocompatibility and biodegradability. These findings emphasize that Q-AmCs NPs have an outstanding potential for the delivery and slow release of anticancer drugs.

scholarly journals Safety Assessment of Nano-Hydroxyapatite as an Oral Care Ingredient according to the EU Cosmetics Regulation

Cosmetics ◽  
2018 ◽  
Vol 5 (3) ◽  
pp. 53 ◽  
Author(s):  
Joana Ramis ◽  
Catarina Coelho ◽  
Alba Córdoba ◽  
Paulo Quadros ◽  
Marta Monjo
Keyword(s):  
Oral Care ◽  
Gastric Fluid ◽  
Gingival Tissue ◽  
Simulated Gastric Fluid ◽  
Tem Analysis ◽  
Consumer Safety ◽  
Transmission Electron ◽  
Dissolution Behaviour ◽  
Gingival Epithelium

Hydroxyapatite nanoparticles (HAP-NP) are incorporated in oral care products such as toothpastes and mouthwashes to treat dental sensitivity or to promote enamel remineralisation. Despite the good performance of HAP-NP in this application, it is important to ensure its safety for consumers. For that reason, the Scientific Committee on Consumer Safety (SCCS) evaluated the safety of HAP-NP as an oral care ingredient, but the issued opinion was not completely conclusive and the SCCS recommended that additional tests should be performed. Here, we used a commercially available human gingival epithelium (HGE) as a non-animal alternative and MTT cell viability, LDH activity, and IL-1alpha production were evaluated after 3.1% HAP-NP treatment for 10 min, 1 h, and 3 h. Moreover, the absorption of HAP-NP in the gingival tissue was assessed by transmission electron microscopy (TEM) analysis. Finally, the dissolution behaviour of HAP-NP in simulated gastric fluid was also investigated. No deleterious effect was observed for HGE tissues incubated with HAP-NP for all time-points and parameters evaluated. Moreover, a complete dissolution of 3.1% HAP-NP in simulated gastric fluid was observed after 7.5 min at 37 °C. In conclusion, our results evidence the safety of HAP-NP for oral care products with the use of an in vitro replacement alternative for human gingival epithelium and a simulated gastric fluid assay.

scholarly journals Formulation of non-effervescent floating matrix tablets of metronidazole using Abelmoschus esculentus gum as binder and 2-camphanone as sublimating agent.

2020 ◽  
Vol 19 (1) ◽  
pp. 387-397
Author(s):  
Airemwen Collins Ovenseri ◽  
Uwumagbe Michael Uhumwangho ◽  
Aiwaguore Johnbull Obarisiagbon ◽  
Chioma Promise Umechukwu
Keyword(s):  
Patient Adherence ◽  
Release Kinetics ◽  
Lag Time ◽  
Matrix Tablets ◽  
Angle Of Repose ◽  
Abelmoschus Esculentus ◽  
Fickian Diffusion ◽  
Simulated Gastric Fluid ◽  
Compatibility Study

The aim of this study was to formulate non-effervescent floating drug delivery system of metronidazole tablets using Abelmoschus esculentus (Okra) (AE) gum as a binder and 2-camphanone (camphor®) as the sublimating agent. Granules were prepared by wet granulation technique using varying concentrations of AE gum (2, 4, 6 and 8% w/w) admixed with 1%w/w acrylate methacrylate copolymer. A 30 %w/w of 2-camphanone was used as the sublimating agent. The granules were characterized for micromeritic properties. And thereafter, compressed at a compression pressure of 25 N/m2 using a Manesty single punch tableting machine. The metronidazole tablet was then sintered at 70oC for 12 h. Drug-excipient compatibility study was done using Fourier Transform Infra-red Spectroscopy (FTIR). Tablets were evaluated for floating lag time, in-vitro buoyancy and release kinetics. FTIR studies showed that the excipients and the active pharmaceutical ingredient (API) i.e. metronidazole, were compatible. All the granules were free flowing, with Carr’s index ≤ 15 %, Hausner ratio ≤ 1.18 and angle of repose of ≤ 33.5o. The tablets had hardness and friability values of 5.0-9.5 N and 0.4-0.8% respectively. The floating lag time was 0 s showing that the tablets floated immediately after immersion in the simulated gastric fluid. The maximum % release (m∞) and time to achieve it (t∞) were ≥ 88 % and ≥ 10 h, respectively. Release exponent (n) for all the formulations had values >0.45, hence their release was by non-Fickian diffusion. Non-effervescent floating matrix tablets of metronidazole were formulated using AE gum as the binder and 2-camphanone as the sublimating agent. The formulated floating tablets had increased in-vitro retention time, which indicated potential for sustained release of the drug. If well developed, this may help reduce the oral dosing frequency and encourage patient adherence to the drug therapy. Keywords: Non-effervescent, Abelmoschus esculentus, 2-camphanone, floating

scholarly journals THE USE OF CLINOPTILOLITES AS CARRIER OF METFORMIN HYDROCHLORIDE IN DRUG DELIVERY SYSTEM: IN VITRO DRUG RELEASE STUDY

2018 ◽  
Vol 11 (11) ◽  
pp. 285
Author(s):  
Putra Imwa ◽  
Kusumawati Igaw
Keyword(s):  
Drug Release ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Metformin Hydrochloride ◽  
Simulated Intestinal Fluid ◽  
In Vitro Drug Release ◽  
Encapsulation Process ◽  
N2 Sorption ◽  
Metformin Hcl

Objective: As an antidiabetic drug, metformin hydrochloride (HCl) has been well known to possess low oral bioavailability and short half-life. In this study, we prepared the drug delivery system (DDS) of metformin HCl and clinoptilolite as its carrier. The in vitro drug release profile was further investigated.Methods: DDS was made by encapsulating metformin HCl on clinoptilolite using the wet impregnation method at various pH and initial concentration of metformin HCl. Fourier transform infrared spectrometer (FTIR), X-ray diffractometer (XRD), and N2 Sorption Analyzer were used to characterize the as-synthesized DDS. Drug release study was conducted by stirring the DDS in simulated gastric fluid and simulated intestinal fluid over 12 h.Results: The encapsulation process was achieved optimally at pH 7.0 and initial concentration of metformin HCl of 300 mg/l (CLI2-300 denoted DDS). The results of FTIR and N2 sorption analyzer confirmed the existence of metformin HCl on clinoptilolites. Meanwhile, the XRD result showed that the crystallinity of clinoptilolites remained unchanged after the encapsulation process. The cumulative drug release in the simulated gastric fluid was found to be higher than that in the simulated intestinal fluid, which indicated the potent influence of pH on the release properties of the drugs. The drug release kinetics of metformin HCl from clinoptilolite was best fitted into the Korsmeyer-Peppas model with non-Fickian transport mechanism.Conclusion: We found that clinoptilolite was suitable for DDS application, particularly as a carrier of metformin HCl.

scholarly journals Design, synthesis, hydrolysis kinetics and phamacodynamic profiles of histidine and alanine conjugates of aceclofenac

2010 ◽  
Vol 60 (1) ◽  
pp. 99-109 ◽  
Author(s):  
Arun Rasheed ◽  
C. Kumar
Keyword(s):  
Human Plasma ◽  
Methyl Esters ◽  
Physicochemical Characterization ◽  
Parent Drug ◽  
Hydrolysis Rate ◽  
Simulated Gastric Fluid ◽  
Hydrolysis Kinetics ◽  
Simulated Intestinal Fluid ◽  
Design Synthesis

Design, synthesis, hydrolysis kinetics and phamacodynamic profiles of histidine and alanine conjugates of aceclofenacThe gastrointestinal toxicity associated with aceclofenac can be reduced by condensing its carboxylic acid group with methyl esters of amino acids like histidine and alanine to give amide linkage by the Schotten-Baumann method. Physicochemical characterization of the conjugates was carried out by various analytical and spectral methods. The synthesized conjugates were also subjected toin vitrohydrolysis in simulated gastric fluid (SGF) at pH 1.2, simulated intestinal fluid (SIF) at pH 7.4 and SIF+ 80% human plasma at pH 7.4. The release of free aceclofenac from histidine and alanine conjugated aceclofenac showed negligible hydrolysis in SGF compared to SIF. This indicated that the conjugates do not break in stomach, but release aceclofenac in SIF. Both synthesized conjugates showed excellent pharmacological response and encouraging hydrolysis rate in SIF and SIF + 80% human plasma. Marked reduction of the ulcer index and comparable increase in analgesic and anti-inflammatory activities were obtained in both cases compared to aceclofenac alone. These findings suggest that the conjugates are better in action compared to the parent drug and have fewer gastrointestinal side-effects.

scholarly journals The Antioxidant Properties of Pectin Fractions Isolated from Vegetables Using a Simulated Gastric Fluid

2017 ◽  
Vol 2017 ◽  
pp. 1-10 ◽  
Author(s):  
Vasily V. Smirnov ◽  
Victoria V. Golovchenko ◽  
Fedor V. Vityazev ◽  
Olga A. Patova ◽  
Nikolay Yu. Selivanov ◽  
...  
Keyword(s):  
Xanthine Oxidase ◽  
Antioxidant Properties ◽  
Sweet Pepper ◽  
Structural Features ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Oxygen Species ◽  
Pectic Polysaccharides ◽  
White Cabbage

The antioxidant properties of vegetable pectin fractions against intraluminal reactive oxygen species were elucidated in vitro in conjunction with their structural features. The pectin fractions were isolated using a simulated gastric fluid (pH 1.5, pepsin 0.5 g/L, 37°C, 4 h) from fresh white cabbage, carrot, onion, and sweet pepper. The fraction from onion was found to inhibit the production of superoxide radicals by inhibiting the xanthine oxidase. The high molecular weight of onion pectin and a large number of galactose residues in its side chains appeared to participate in interaction with xanthine oxidase. All the isolated pectic polysaccharides were found to be associated with protein (2–9%) and phenolics (0.5–0.7%) as contaminants; these contaminants were shown to be responsible for the antioxidant effect of vegetable pectin fractions against the hydroxyl and 1,1-diphenyl-2-picrylhydrazyl radicals.

scholarly journals Stability of recombinant 2 S albumin allergens in vitro

2002 ◽  
Vol 30 (6) ◽  
pp. 913-915 ◽  
Author(s):  
G. J. Murtagh ◽  
M. Dumoulin ◽  
D. B. Archer ◽  
M. J. Alcocer
Keyword(s):  
Immune Response ◽  
Circulatory System ◽  
Gastric Fluid ◽  
Low Ph ◽  
Simulated Gastric Fluid ◽  
Brazil Nut

Two well known 2 S albumins, Ber e 1 from brazil nut and sunflower 2 S albumin 8 (SFA-8), have been expressed in a eukaryotic system and purified. Analysis of recombinant versions of Ber e 1 and SFA-8 revealed them to be significantly more resistant to digestion by pepsin than BSA, and to be stable for up to 30 min in simulated gastric fluid. Unfolding monitored by CD indicated that both proteins were also very resistant to denaturation induced by heat and low pH. These results suggest that, although the ability of 2 S albumins to reach the circulatory system may be a prerequisite for the allergenicity of this group of proteins, stability is just one of a number of characteristics that provoke a selective immune response.

scholarly journals In Vitro Evaluation of Eudragit Matrices for Oral Delivery of BCG Vaccine to Animals

2019 ◽  
Author(s):  
Imran Saleem ◽  
Allan Coombes ◽  
Mark Chambers
Keyword(s):  
Oral Delivery ◽  
Freeze Drying ◽  
Tween 80 ◽  
Gastric Fluid ◽  
Powder Compaction ◽  
Bcg Vaccine ◽  
Simulated Gastric Fluid ◽  
Physical Damage ◽  
Freeze Dried

Bacillus Calmette-Guérin (BCG) vaccine is the only licensed vaccine against tuberculosis (TB) in humans and animals. It is most commonly administered parenterally but oral delivery is highly advantageous for immunisation of cattle and wildlife hosts of TB in particular. Since BCG is susceptible to inactivation in the gut, vaccine formulations were prepared from suspensions of Eudragit L100 copolymer powder and BCG in PBS, containing Tween 80, with and without the addition of mannitol or trehalose. Samples were frozen at -20oC, freeze-dried and the lyophilised powders were compressed to produce BCG-Eudragit matrices. Production of the dried powders resulted in a reduction in BCG viability. Substantial losses in viability occurred at the initial formulation stage and at the stage of powder compaction. Data indicated that the Eudragit matrix protected BCG against simulated gastric fluid (SGF). The matrices remained intact in SGF and dissolved completely in SIF within three hours. The inclusion of mannitol or trehalose in the matrix provided additional protection to BCG during freeze-drying. Control needs to be exercised over BCG aggregation, freeze-drying and powder compaction conditions to minimise physical damage of the bacterial cell wall and maximise the viability of oral BCG vaccines prepared by dry powder compaction.

scholarly journals Gastrin and Nitric Oxide Production in Cultured Gastric Antral Mucosa Are Altered in Response to a Gastric Digest of a Dietary Supplement

2021 ◽  
Vol 8 ◽  
Author(s):  
Jennifer L. MacNicol ◽  
Wendy Pearson
Keyword(s):  
Nitric Oxide ◽  
Cell Viability ◽  
Dietary Supplement ◽  
Culture Media ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Antral Mucosa ◽  
The Impact

In vitro organ culture can provide insight into isolated mucosal responses to particular environmental stimuli. The objective of the present study was to investigate the impact of a prolonged culturing time as well as the addition of acidic gastric fluid into the in vitro environment of cultured gastric antral tissue to evaluate how altering the commonly used neutral environment impacted tissue. Furthermore, we aimed to investigate the impact of G's Formula, a dietary supplement for horses, on the secretion of gastrin, interleukin1-beta (IL-1β), and nitric oxide (NO). These biomarkers are of interest due to their effects on gastric motility and mucosal activity. Gastric mucosal tissue explants from porcine stomachs were cultured in the presence of a simulated gastric fluid (BL, n = 14), simulated gastric fluid containing the dietary supplement G's Formula (DF, n = 12), or an equal volume of phosphate buffered saline (CO, n = 14). At 48 and 60 h, 10−5 M carbachol was used to stimulate gastrin secretion. Cell viability was assessed at 72 h using calcein and ethidium-homodimer 1 staining. Media was analyzed for gastrin, IL-1β, and NO at 48, 60, and 72 h. There were no effects of treatment or carbachol stimulation on explant cell viability. Carbachol resulted in a significant increase in gastrin concentration in CO and DF treatments, but not in BL. NO was higher in CO than in BL, and NO increased in the CO and DF treatments but not in BL. In conclusion, the addition of carbachol and gastric digests to culture media did not impact cell viability. The use of an acidic gastric digest (BL) reduced the effect of cholinergic stimulation with carbachol at a concentration of 10−5 M and reduced NO secretion. The addition of the dietary supplement to the gastric digest (DF) appeared to mediate these effects within this model. Further research is required to evaluate the specific effects of this dietary supplement on direct markers of mucosal activity and the functional relevance of these results in vivo.

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