green-synthesis-characterization-encapsulation-measurement-release

Green Synthesis, Characterization, Encapsulation, and Measurement of the Release Potential of Novel Alkali Lignin Micro-/Submicron Particles

The applicability of biopolymer micro-/nano- technology in human, veterinary medicine, pharmaceutical, and food technology is rapidly growing due to the ...

Trakia University

This study was undertaken to determine the dietary supplements of Zn containing diet on the antioxidant status in chickens experimentally infected with Eimeria acervulina. The antioxidant status was monitored via determination of MDA concentrations and erythrocyte SOD and CAT activities, as well as vitamin E, vitamin C, Cu, and Zn in liver, muscle, and serum. The results showed increased MDA (P < .05), CAT (P < .001), and decreased SOD (P < .001) in the infected birds. Significant changes in Cu and Zn concentrations and dramatically reduction of vitamin C and E concentrations in the infected chickens were found. The observed deviations in the studied enzymes and nonenzymatic parameters evidence the occurrence of oxidative stress following the infection and impaired antioxidant status of chickens, infected with Eimeria acervulina. Our results proved the ameliorating role of CuZn(OH)(3)Cl (0.170 g per kg food) against Eimeria acervulina-induced oxidative damage in infected chickens.

Zinc Supplementation against Eimeria acervulina-Induced Oxidative Damage in Broiler Chickens.

The aim of the present study was to develop cresyl violet (CV)/bentonite composite system, to investigate the equilibrium sorption of the fluorescent dye on bentonite, to determine the characteristic equilibrium and thermodynamic parameters of the system by appropriate empirical isotherm models and to assess its pH-indicator properties. The absorption characteristics of CV solutions were investigated by UV/VIS spectrophotometer. Equilibrium experiments were conducted and the experimental data were modelled by six mathematical isotherm models. The analyses of the experimental data showed that bentonite exhibited significantly high capacity - 169.92 mg/g, towards CV. The encapsulation efficiency was 85%. The Langmuir, Flory-Huggins and El-Awady models best represented the experimental results. The free Gibbs energy of adsorption (ΔG) was calculated on the basis of the values of the equilibrium coefficients determined by the proposed models. The values of ΔG determined by the Langmuir, Temkin and Flory-Huggins models are within the range -20 to -40 kJ/mol, which indicates that the adsorption process is spontaneous and chemisorption takes place due to charge sharing or transfer from the dye molecules to the sorbent surface as a coordinate type of bond. The investigations of the obtained CV/bentonite hybrid systems for application as pH-markers showed satisfactory results.

Sorption equilibrium, thermodynamics and pH-indicator properties of cresyl violet dye/bentonite composite system.

Many studies have shown that mitochondrial metabolism has a fundamental role in induction of carcinogenesis due to the influence of increased levels of reactive oxygen species (ROS) generation in all steps of oncogene transformation and cancer progression. It is widely accepted that the anticancer effect of conventional anticancer drugs is due to induction of oxidative stress and elevated intracellular levels of ROS, which alter the redox homeostasis of cancer cells. On the other hand, the harmful side effects of conventional anticancer chemotherapeutics are also due to increased production of ROS and disruption of redox homeostasis of normal cells and tissues. Therefore, there is a growing interest toward the development of natural antioxidant compounds from various sources, which could impact the redox state of cancer and normal cells by different pathways and could prevent damage from oxidant-mediated reactions. It is known that chitosan exhibits versatile biological properties, including biodegradability, biocompatibility, and a less toxic nature. Because of its antioxidant, antibacterial, anticancer, anti-inflammatory, and immunostimulatory activities, the biopolymer has been used in a wide variety of pharmaceutical, biomedical, food industry, health, and agricultural applications and has been classified as a new physiologically bioactive material.

Antioxidant Properties and Redox-Modulating Activity of Chitosan and Its Derivatives: Biomaterials with Application in Cancer Therapy.

Epidemiological studies and clinical investigations proposed that catechins extracts alone may not provide a sufficient level of bioactivities and promising therapeutic effects to achieve health benefits due to a number of constraints related to poor oral absorption, limited bioavailability, sensitivity to oxidation, etc. Modern scientific studies have reported numerous techniques for the design of micro- and nano-bio-delivery systems as novel and promising strategies to overcome these obstacles and to enhance catechins' therapeutic activity. The objective assessment of their benefits, however, requires a critical comparative estimation of the advantages and disadvantages of the designed catechins-biocarrier systems, their biological activities and safety administration aspects. In this respect, the present review objectively outlines, compares and assesses the recent advances related to newly developed design concepts of catechins' encapsulation into various biopolymer carriers and their release behaviour, with a special emphasis on the specific physiological biofunctionalities of the innovative bioflavonoid/biopolymer delivery systems.

Catechins within the Biopolymer Matrix-Design Concepts and Bioactivity Prospects.

The main goal of the present study was to investigate the microencapsulation, in vitro release capacity and efficiency of catechin-rich  extract by Clinosorbent-5 (CLS-5) microparticles by in-depth detailed analyses and mathematical modelling of the encapsulation and in vitro release kinetics behaviour of the polyphenol-mineral composite system. The bioflavanol encapsulation and release efficiency on/from the mineral matrix were assessed by sorption experiments and interpretative modelling of the experimental data. The surface and spectral characteristics of the natural bioactive substance and the inorganic microcarrier were determined by Fourier Transform Infrared Spectroscopy (FTIR) and Ultraviolet/Visible (UV/Vis) spectrophotometric analyses. The maximum extent of catechin microencapsulation in acidic medium was 32%. The in vitro release kinetics study in simulated enzyme-free gastric medium (pH = 1.2) approved 88% maximum release efficiency achieved after 24 h. The in vitro release profile displayed that the developed bioflavanol/clinoptilolite microcarrier system provided sustained catechin in vitro release behaviour without an initial burst effect. Thus, the results from the present study are essential for the design and development of innovative catechin-CLS-5 microcarrier systems for application in human and veterinary medicine.

Clinoptilolite Microparticles as Carriers of Catechin-Rich  Extracts: Microencapsulation and In Vitro Release Study.

This study analysed the effect of α-tocopheryl succinate (α-TS) on the redox-state of leukemia and normal lymphocytes, as well as their sensitization to fifteen anticancer drugs.

Effect of Alpha-tocopheryl Succinate on the Cytotoxicity of Anticancer Drugs Towards Leukemia Lymphocytes.

The aim of the present study was to investigate the radioprotective activity of silymarin, a plant substance with hepatoprotective activity, of four newly synthesized structural derivatives of anthranilic acid azomethines, and alkyl-2-styrylquinolinic acid, as well as to establish and assess the influence of the solvent type and bioactive compound dose on the in vivo radioprotective potential of the natural and novel synthetic compounds. Male Wistar strain rats weighing 110-120 g were used for the in vivo experiments. Fifteen minutes after i.p. injection of the compounds, the experimental animals were irradiated by 8 Gy. Results indicate that the compound 2-{[(3,5-dihydro-2-hydroxyphenyl)methylen] amino}-benzoic acid in a dose of 60 mg/kg body weight exhibited the highest radioprotective effect, whereas the natural extract silymarin did not manifest radioprotective potential, even in high doses.

In Vivo Radioprotective Potential of Newly Synthesized Azomethine and Styrylquinoline Derivatives and a Natural Polyphenol: A Preliminary Study.

As natural biopolymers, chitosan and lignin are characterized by their good biocompatibility, high biodegradability and satisfactory biosafety. The active polymers’ functional groups are responsible for the potential of these biomaterials for use as carrier matrices in the construction of polymer−drug conjugates with prospective applicability in the fields of medicine, food and agriculture—subjects that have attracted attention in recent years. Hence, the aim of this research was to place substantial emphasis on the antimicrobial potential of flavonoid−biopolymer complex systems by assessment of the probable synergetic, additive or antagonistic effects arising as a function of systemic complexity. The joint implementation of morin, chitosan and lignin in conjugated two- and three-component systems provoked species-dependent antimicrobial synergistic and/or potentiation effects against the activity of the tested bacterial strains Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853 and the clinical isolate Bacillus cereus. The double combinations of morin−chitosan and morin−lignin resulted in a 100% increase in their inhibitory activity against S. aureus as compared to the pure biocompounds. The inhibitory effects of the three-component system, in decreasing order, were: S. aureus (IZ = 15.7 mm) > P. aeruginosa (IZ = 15 mm) > B. cereus and E. coli (IZ = 14 mm). All tested morin-containing two- and three-component systems exhibited clear and significant potentiation effects, especially against S. aureus and B. cereus. The results obtained are a prerequisite for the potential use of the studied conjugated lignin−morin−chitosan combinations in the construction of novel drug-carrier formulations with improved bioactivities.

Antimicrobial Potential of Conjugated Lignin/Morin/Chitosan Combinations as a Function of System Complexity.

Orally administered tetracycline antibiotics interact with feed, which may impact their bioavailability and efficacy. Therefore, the pH-dependent adsorption of doxycycline and its interaction with feed for ruminants was studied in vitro. Adsorption experiments on animal feed (135 and 270 mg) with initial doxycycline concentrations of 35, 75, and 150 µg/mL were performed. Desorption experiments were conducted by agitation of a predetermined mass of doxycycline-loaded animal feed in PBS, at pH = 3.0, 6.0, and 7.4, to simulate changes in the gastrointestinal tract. Antibiotic concentrations were determined by LC-MS/MS analysis. The adsorption/desorption of doxycycline was described by mathematical models. Chemisorption with strong intermolecular interactions between the active functional groups of doxycycline and the organic biomass was found. The experimental release curve comprised three sections: initial prolonged 27-30% release (pH = 6.0), followed by moderate 56-59% release (pH = 3.0), and final 63-74% release (pH = 7.4). The sigmoidal model showed a considerable role of diffusion with an initial prevalence of desorption and a decreased desorption rate thereafter. The Weibull equation revealed an initial release stage followed by a lag time section and sustained release. The study of doxycycline adsorption by the animal feed proved a maximum 80% encapsulation efficiency and revealed initial diffusion followed by chemisorption. The highest release efficiency of 74% suggests high bioavailability of doxycycline after oral administration in ruminants.

Investigation of the Effect of pH on the Adsorption-Desorption of Doxycycline in Feed for Small Ruminants.

Mitochondria-targeted anticancer drugs ("mitocans") of natural origin are attractive candidates as adjuvants in cancer therapy. The redox couple menadione/ascorbate (M/A), which belongs to the "mitocans" family, induces selective oxidative stress in cancerous mitochondria and cells, respectively. DHA has also been found to regulate the mevalonate pathway, which is closely related to the prenylation of the cytotoxic menadione to the non-cytotoxic menaquinone. The aim of this study was to elucidate the ability of docosahexaenoic acid (DHA) to potentiate the anticancer effect of M/A by increasing ROS production, as well as affecting steady-state ATP levels in cancer cells.

Docosahexaenoic Acid Potentiates the Anticancer Effect of the Menadione/Ascorbate Redox Couple by Increasing Mitochondrial Superoxide and Accelerating ATP Depletion.

The aim of the present study was to synthesize lignin microparticles, to evaluate their physicochemical, spectral, morphological and structural characteristics, to examine their encapsulation and in vitro release potential and behaviour towards the flavonoid morin in simulated physiological medium and to assess the in vitro radical-scavenging potential of the morin-loaded lignin microcarrier systems. The physicochemical, structural and morphological characteristics of alkali lignin, lignin particles (LP) and morin-encapsulated lignin microparticles (LMP) were determined based on particle size distribution, SEM, UV/Vis spectrophotometric, FTIR and potentiometric titration analyses. The encapsulation efficiency of LMP was 98.1%. The FTIR analyses proved that morin was successfully encapsulated in the LP without unexpected chemical reactions between the flavonoid and the heteropolymer. The in vitro release performance of the microcarrier system was successfully mathematically described by Korsmeyer-Peppas and the sigmoidal models outlining the general role of diffusion during the initial stages of the in vitro release process in simulated gastric fluid (SGF), and the predominant contribution of biopolymer relaxation and erosion was determined in simulated intestinal medium (SIF). The higher radical-scavenging potential of LMP, as compared to that of LP, was proven via DPPH and ABTS assays. The synthesis of lignin microcarriers not only provides a facile approach for the utilization of the heteropolymer but also determines its potential for the design of drug-delivery matrices.

Newly Synthesized Lignin Microparticles as Bioinspired Oral Drug-Delivery Vehicles: Flavonoid-Carrier Potential and In Vitro Radical-Scavenging Activity.

Several phytochemicals, which display antioxidant activity and inhibit cancer cell phenotypes, could be used for cancer treatment and prevention. Lignin, as a part of plant biomass, is the second most abundant natural biopolymer worldwide, and represents approximately 30% of the total organic carbon content of the biosphere. Historically, lignin-based products have been viewed as waste materials of limited industrial usefulness, but modern technologies highlight the applicability of lignin in a variety of industrial branches, including biomedicine. The aims of our preliminary study were to compare the antioxidant properties of water-soluble alkali lignin solutions, before and after UV-B irradiation, as well as to clarify their effect on colon cancer cell viability (Colon 26), applied at low (tolerable) concentrations. The results showed a high antioxidant capacity of lignin solutions, compared to a water-soluble control antioxidant standard (Trolox) and remarkable radical scavenging activity was observed after their UV-B irradiation. Diminishment of cell viability as well as inhibition of the proliferative activity of the colon cancer cell line with an increase in alkali lignin concentrations were observed. Our results confirmed that, due to its biodegradable and biocompatible nature, lignin could be a potential agent for cancer therapy, especially in nanomedicine as a drug delivery system.

Water-Soluble Alkali Lignin as a Natural Radical Scavenger and Anticancer Alternative.

Vitamin K (menadione), classified as a pro-vitamin, is a synthetic form of the fat-soluble family of vitamin K compounds. The combination of the vitamin with other molecules sharing structural and/or functional similarities, such as naturally occurring polyphenols, vitamins, or biopolymers, could potentiate mutual improvement of their antioxidant activity. The aim of the present study was to evaluate the role and contribution of vitamin K to the in vitro radical scavenging capacity of double and triple combinations with the phytochemicals naringenin and lignin, as well as assess possible intermolecular interactions between the bioactive compounds. Comparative analyses of the DPPH and ABTS radical scavenging activity of the pure substances vitamin K, naringenin, and lignin; the two-component systems lignin/vitamin K and vitamin K/naringenin; and the triple combination vitamin K/flavonoid/lignin were carried out. The experimental results demonstrated increased DPPH and ABTS activities of the vitamin in combination with lignin compared to those of the two pure substances, i.e., a synergistic effect was observed. The registered significant increases in the radical scavenging activity of the triple combination determined via both methods are indicative of a remarkable potentiation effect, i.e., higher antioxidant potential exceeding the additive activity of the three pure substances.

Menadione Contribution to the In Vitro Radical Scavenging Potential of Phytochemicals Naringenin and Lignin.

Consumers associate the color of food with its freshness and quality. More and more attention is being paid to natural colorants that bring additional health benefits to humans. Such natural substances are the carotenoids (yellow to orange), the anthocyanins (red to blue), and the betalains (red and yellow), which are very sensitive to exposure to light, air, high temperatures, and chemicals. Stability and diversity in terms of color can be optimized by using environmentally friendly and selective extraction processes that provide a balance between efficacy, safety, and stability of the resulting extracts. Green solvents like water, supercritical fluids, natural deep eutectic solvents, and ionic liquids are the most proper green solvents when combined with different extraction techniques like maceration, supercritical extraction, and ultrasound-assisted or microwave-assisted extraction. The choice of the right extracting agent is crucial for the selectivity of the extraction method and the stability of the prepared colorant. The present work reviews the green solvents used for the extraction of natural food colorants from plants and focuses on the issues related to the selectivity and stability of the products extracted.

Article	Year
Zinc Supplementation against Eimeria acervulina-Induced Oxidative Damage in Broiler Chickens. Veterinary medicine international\| PubMed ID: 21461390	2011
Sorption equilibrium, thermodynamics and pH-indicator properties of cresyl violet dye/bentonite composite system. Water science and technology : a journal of the International Association on Water Pollution Research\| PubMed ID: 28876248	2017
Antioxidant Properties and Redox-Modulating Activity of Chitosan and Its Derivatives: Biomaterials with Application in Cancer Therapy. BioResearch open access\| PubMed ID: 32219012	2020
Catechins within the Biopolymer Matrix-Design Concepts and Bioactivity Prospects. Antioxidants (Basel, Switzerland)\| PubMed ID: 33256098	2020
Clinoptilolite Microparticles as Carriers of Catechin-Rich Extracts: Microencapsulation and In Vitro Release Study. Molecules (Basel, Switzerland)\| PubMed ID: 33809751	2021
Effect of Alpha-tocopheryl Succinate on the Cytotoxicity of Anticancer Drugs Towards Leukemia Lymphocytes. Anticancer research\| PubMed ID: 34969764	2022
In Vivo Radioprotective Potential of Newly Synthesized Azomethine and Styrylquinoline Derivatives and a Natural Polyphenol: A Preliminary Study. Life (Basel, Switzerland)\| PubMed ID: 35330097	2022
Antimicrobial Potential of Conjugated Lignin/Morin/Chitosan Combinations as a Function of System Complexity. Antibiotics (Basel, Switzerland)\| PubMed ID: 35625293	2022
Investigation of the Effect of pH on the Adsorption-Desorption of Doxycycline in Feed for Small Ruminants. Antibiotics (Basel, Switzerland)\| PubMed ID: 36830179	2023
Docosahexaenoic Acid Potentiates the Anticancer Effect of the Menadione/Ascorbate Redox Couple by Increasing Mitochondrial Superoxide and Accelerating ATP Depletion. Anticancer research\| PubMed ID: 36854499	2023
Newly Synthesized Lignin Microparticles as Bioinspired Oral Drug-Delivery Vehicles: Flavonoid-Carrier Potential and In Vitro Radical-Scavenging Activity. Pharmaceutics\| PubMed ID: 37111553	2023
Water-Soluble Alkali Lignin as a Natural Radical Scavenger and Anticancer Alternative. International journal of molecular sciences\| PubMed ID: 37628882	2023
Menadione Contribution to the In Vitro Radical Scavenging Potential of Phytochemicals Naringenin and Lignin. International journal of molecular sciences\| PubMed ID: 38003457	2023
Green Solvents for Extraction of Natural Food Colorants from Plants: Selectivity and Stability Issues. Foods (Basel, Switzerland)\| PubMed ID: 38397582	2024

Zvezdelina Yaneva

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