Release Of Active Substances Research Articles

Effects of Dendrobium officinale on the Quality of Rice Wine Fermented Separately by Saccharomyces cerevisiae and Wickerhamomyces anomalus: Physicochemical Indices, Volatile Compounds and Nonvolatile Metabolites

This study aims to investigate the difference in the quality of rice wine fermented with different yeasts (Saccharomyces cerevisiae FBKL2.8022 (Sc) and Wickerhamomyces anomalus FBKL2.8023 (Wa)) by adding Dendrobium officinale (D. officinale). The results showed that the addition of D. officinale improved the physicochemical indices and sensory scores in rice wine and promoted the release of active substances from D. officinale. The addition of D. officinale increased the types and contents of flavor substances in Wa-fermented rice wine and inhibited the generation of flavor substances in Sc-fermented rice wine. Untargeted metabolomics analysis showed that the number of differential metabolites was higher before and after fermentation with D. officinale. The main pathways causing the differences were phenylalanine metabolism and alanine, aspartate and glutamate metabolism (which belong to the amino acid metabolism pathways). This study provides a reference to explore the application value of D. officinale in the fermentation and food industry.

Characterisation, slow-release, and antibacterial properties of carboxymethyl chitosan/inulin hydrogel film loaded with novel antilisterial durancin GL

This paper reports the development of a hydrogel film with antibacterial activity and controlled release characteristics. Carboxymethyl chitosan (CMCS) is grafted onto durancin GL and inulin via a mediated reaction between N-hydroxysuccinimide and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride. Rheology tests, Fourier transform infrared (FTIR) spectroscopy, X-ray photoelectron spectroscopy, and lap shear tests confirmed the formation of a stable chemical cross-linking and excellent adhesion hydrogel with 4 % CMCS and 8 % inulin. The CMCS/inulin hydrogel film loaded with durancin GL appears transparent and uniform. FTIR spectroscopy results reveal the interaction mode among CMCS, inulin, durancin GL, and the hydrogel film structure. Cross-linking improved thermal stability and water-vapour barrier performance. The hydrophobicity of CMCS/inulin @Durancin GL increased under a durancin GL concentration of 0.036 g/30 mL, and the release of active substances is prolonged. In-vitro antibacterial capacity and salmon preservation experiments show that the addition of durancin GL enhanced the antibacterial activity of the hydrogel film. Therefore, CMCS/inulin@Durancin GL hydrogel films can be used as fresh-keeping packaging materials in practical applications.

A comprehensive review of intelligent controlled release antimicrobial packaging in food preservation.

Intelligent responsive packaging provides informative feedback or control the release of active substances like antimicrobial agents in response to stimuli in food or the environment to ensure food safety. This paper provides an overview of two types of intelligent packaging, information-responsive and intelligent controlled-release, focusing on the recent research progress of intelligent controlled-release antimicrobial packaging with enzyme, pH, relative humidity, temperature, and light as triggering factors. It also summarizes the current status of application in different food categories, as well as the challenges and future prospects. Intelligent controlled-release technology aims to optimize the antimicrobial effect and ensure the quality of food products by synchronizing the release of active substances with food preservation needs through sensing stimuli, which is an innovative and challenging packaging technology. The paper seeks to provide a reference for the research and industrial development of responsive intelligent packaging and controlled-release packaging applications in food.

Polymeric Based Hydrogel Membranes for Biomedical Applications.

The development of biomedical applications is a transdisciplinary field that in recent years has involved researchers from chemistry, pharmacy, medicine, biology, biophysics, and biomechanical engineering. The fabrication of biomedical devices requires the use of biocompatible materials that do not damage living tissues and have some biomechanical characteristics. The use of polymeric membranes, as materials meeting the above-mentioned requirements, has become increasingly popular in recent years, with outstanding results in tissue engineering, for regeneration and replenishment of tissues constituting internal organs, in wound healing dressings, and in the realization of systems for diagnosis and therapy, through the controlled release of active substances. The biomedical application of hydrogel membranes has had little uptake in the past due to the toxicity of cross-linking agents and to the existing limitations regarding gelation under physiological conditions, but now it is proving to be a very promising field This review presents the important technological innovations that the use of membrane hydrogels has promoted, enabling the resolution of recurrent clinical problems, such as post-transplant rejection crises, haemorrhagic crises due to the adhesion of proteins, bacteria, and platelets on biomedical devices in contact with blood, and poor compliance of patients undergoing long-term drug therapies.

Thymus mast cells as a component of neuro-endocrine-immune interactions under stress

Mast cells (MCs) are a required component of the thymus microenvironment. They affect intercellular interactions and permeability of the hematothymic barrier through cytokine production. There is speculation that the thymus is the site of MCs formation and deposition. MCs are under complex neuro-endocrine control and they can play an important role in the process of acute transformation of the thymus in the formation of a stress reaction, affecting the extrathymic migration of cells. The purpose of this study is to assess the functional involvement of MCs in the process of the thymus acute transformation at various hyper- and hypodynamic effects during the formation of stress response and without it.The study was conducted on male Wistar rats. The stress factors were physical activity (swimming) of different intensities and immobilization, which represent two opposite states of dynamic stress. MCs were classified on histological preparations; a degranulation coefficient and a mean histochemical coefficient (synthetic activity) were calculated.In groups with preserved adrenal glands after exposure a significant decrease in the thymus mass coefficient is noted, which indicates a weakening of its functional activity in response to the development of stress. At the same time, MCs of the thymus quickly respond to neuro-endocrine factors under stress. These cells are involved in a general reaction: their activity consists in a synchronous decrease of the synthesis of granules in the cytoplasm and an increased release of active substances accumulated earlier. The mass and structure of the thymus remain unchanged in groups with removed adrenal glands after immobilization. No changes in morphofunctional indicators of mast cells were detected either. Experiments with hypo- and hyperdinamic loading of animals with preserved and removed adrenal glands indicate that the MCs response is largely determined by the hypothalamic-pituitary-adrenal axis of the endocrine system. Removal of the adrenal glands (inability to release glucocorticoids) leads to a lack of functional response from the thymus MCs. The stimulating effect of adrenal glucocorticoids on MCs under stress is carried out in combination with other neuro-endocrine factors (catecholamines, corticotropin-releasing hormone, adrenocorticotropic hormone). When this axis is activated and a full-fledged stress reaction is formed by the body, MCs are actively involved in the process of acute transformation of the thymus through cytokine secretion. These is an important condition for the development of adaptation mechanisms by the immune system.

Emulgels: Promising Carrier Systems for Food Ingredients and Drugs.

Novel delivery systems for cosmetics, drugs, and food ingredients are of great scientific and industrial interest due to their ability to incorporate and protect active substances, thus improving their selectivity, bioavailability, and efficacy. Emulgels are emerging carrier systems that represent a mixture of emulsion and gel, which are particularly significant for the delivery of hydrophobic substances. However, the proper selection of main constituents determines the stability and efficacy of emulgels. Emulgels are dual-controlled release systems, where the oil phase is utilized as a carrier for hydrophobic substances and it determines the occlusive and sensory properties of the product. The emulsifiers are used to promote emulsification during production and to ensure emulsion stability. The choice of emulsifying agents is based on their capacity to emulsify, their toxicity, and their route of administration. Generally, gelling agents are used to increase the consistency of formulation and improve sensory properties by making these systems thixotropic. The gelling agents also impact the release of active substances from the formulation and stability of the system. Therefore, the aim of this review is to gain new insights into emulgel formulations, including the components selection, methods of preparation, and characterization, which are based on recent advances in research studies.

Clindamycin-Loaded Nanosized Calcium Phosphates Powders as a Carrier of Active Substances.

Bioactive calcium phosphate ceramics (CaPs) are one of the building components of the inorganic part of bones. Synthetic CaPs are frequently used as materials for filling bone defects in the form of pastes or composites; however, their porous structure allows modification with active substances and, thus, subsequent use as a drug carrier for the controlled release of active substances. In this study, four different ceramic powders were compared: commercial hydroxyapatite (HA), TCP, brushite, as well as HA obtained by wet precipitation methods. The ceramic powders were subjected to physicochemical analysis, including FTIR, XRD, and determination of Ca/P molar ratio or porosity. These techniques confirmed that the materials were phase-pure, and the molar ratios of calcium and phosphorus elements were in accordance with the literature. This confirmed the validity of the selected synthesis methods. CaPs were then modified with the antibiotic clindamycin. Drug release was determined on HPLC, and antimicrobial properties were tested against Staphylococcus aureus. The specific surface area of the ceramic has been demonstrated to be a factor in drug release efficiency.

Hyaluronic acid-based dual network hydrogel with sustained release of platelet-rich plasma as a diabetic wound dressing

In recent years, the incidence of diabetic skin ulcers has increased. Because of its extremely high disability and fatality rate, it brings a huge burden to patients and society. Platelet-rich plasma (PRP) contains a large number of biologically active substances and is of great clinical value in the treatment of various wounds. However, its weak mechanical properties and the consequent abrupt release of active substances greatly limit its clinical application and therapeutic efficacy. Here, we chose hyaluronic acid (HA) and ε-polylysine (ε-PLL) to prepare a hydrogel with the ability to prevent wound infection and promote tissue regeneration. At the same time, using the macropore barrier effect of the lyophilized hydrogel scaffold, platelets in PRP are activated with calcium gluconate in the macropores of the scaffold carrier, and fibrinogen from PRP is converted in a fibrin-packed network forming a gel that interpenetrates the hydrogel scaffold carrier, thus creating a double network hydrogel with slow-release of growth factors from degranulated platelets. The hydrogel not only showed better performance in functional assays in vitro, but also showed more superior therapeutic effects in reducing inflammatory response, promoting collagen deposition, facilitating re-epithelialization and angiogenesis in the treatment of full skin defects in diabetic rats.

Astaxanthin encapsulation in nanocapsule by high-pressure homogenization technology: a study on stability, antioxidant activity and in vitro release

The astaxanthin nanocapsules (ASX-LNC) was prepared by high-pressure homogenization technology, the microstructure, stability, antioxidant activity, and in vitro release characteristics of ASX-LNC were characterized and evaluated. The ASX-LNC comprised a core material and wall materials. The core material was composed of astaxanthin oil, and the wall materials were composed of β-cyclodextrin, decapolyglycerol monooleate, soybean lecithin (PC60), glycerol, and deionized water. The mean particle size of the ASX-LNC was 206.9 ± 2.8 nm, and the polydispersity index (PdI) value was 0.218 ± 0.026. The zeta potential of ASX-LNC was −26.16 ± 0.87 mV. The loading amount of ASX-LNC was 0.546%±0.032%, and the encapsulation efficiency was 99.65%±0.13%, indicating that the preparation process was feasible. The stability of ASX-LNC was determined under different conditions, indicating good stability of the ASX-LNC. In antioxidant research, the inhibition rate of free radicals of ASX-LNC was 91.03 ± 0.87% under 250 μg/mL for 30 min, and the inhibition rate of free radicals of astaxanthin ethanol solution was 90.83 ± 1.37%. The antioxidant capacity of astaxanthin was not affected by the encapsulation, which demonstrated the effect of prolonging the release of active ingredients due to the protection of the biological activity of astaxanthin by encapsulation. Compared with the astaxanthin ethanol solution, the ASX-LNC had a slow-release effect and could prolong the action time of active substances. Overall, ASX-LNC is a potential carrier for application in food and health products, which can control the release of active substances.

Co-delivery system based on multilayer structural nanoparticles for programmed sequential release of fucoxanthin and curcumin

Multilayer structural nanoparticles (MSNPs) fabricated by gliadin (Gli), carboxymethyl konjac glucomannan (CMK) and chitosan hydrochloride (CHC) were used to co-encapsulate fucoxanthin (FUC) and curcumin (Cur), and the effect of CHC level on the physiochemical properties of MSNPs (FUC-Gli-CMK-Cur-CHC) was evaluated. The prepared FUC-Gli-CMK-Cur-CHC had a particle size of about 628.1 nm and showed a spherical shape with high ζ potential (+27.1 mV) and maximal encapsulation efficiency of FUC (96.3%) and Cur (72.8%). Lyophilized FUC-Gli-CMK-Cur-CHC exhibited excellent water redispersibility after the addition of CHC. Furthermore, the physical stability, storage stability and thermal stability of MSNPs were dramatically improved by CHC coating. FUC-Gli-CMK-Cur-CHC were shown to be effective at retarding the photo- and thermal-degradation of the encapsulated FUC and Cur. In addition, in vitro release and in vivo gastrointestinal distribution studies demonstrated that the prepared MSNPs exhibited programmed sequential release properties, which enabled the delivery of Cur and FUC in the small intestine and colon, respectively. This research provides new insights for MSNPs in constructing co-delivery systems and programmed sequential release of active substances.

Influence of PEGDA Molecular Weight and Concentration on the In Vitro Release of the Model Protein BSA-FITC from Photo Crosslinked Systems.

Novel 3D printing techniques enable the development of medical devices with drug delivery systems that are tailored to the patient in terms of scaffold shape and the desired pharmaceutically active substance release. Gentle curing methods such as photopolymerization are also relevant for the incorporation of potent and sensitive drugs including proteins. However, retaining the pharmaceutical functions of proteins remains challenging due to the possible crosslinking between the functional groups of proteins, and the used photopolymers such as acrylates. In this work, the in vitro release of the model protein drug, albumin-fluorescein isothiocyanate conjugate (BSA-FITC) from differently composed, photopolymerized poly(ethylene) glycol diacrylate (PEGDA), an often employed, nontoxic, easily curable resin, was investigated. Different PEGDA concentrations in water (20, 30, and 40 wt %) and their different molecular masses (4000, 10,000, and 20,000 g/mol) were used to prepare a protein carrier with photopolymerization and molding. The viscosity measurements of photomonomer solutions revealed exponentially increasing values with increasing PEGDA concentration and molecular mass. Polymerized samples showed increasing medium uptake with an increasing molecular mass and decreasing uptake with increasing PEGDA content. Therefore, the modification of the inner network resulted in the most swollen samples (20 wt %) also releasing the highest amount of incorporated BSA-FITC for all PEGDA molecular masses.

Photodynamic Light-Triggered Release of Curcumin from Hierarchical FAU Zeolite

Photodynamic therapy (PDT) is a method used in the treatment of various diseases and represents a promising alternative to classical active substance release methods. According to the United States National Institute of Health, this therapy exploits the health-promoting potential of active substances, referred to as “photosensitizers”, and radiation of specific energy. Curcumin is a natural “photosensitizer” that exhibits anti-inflammatory, antioxidant, and anti-cancer effects. Despite the novelty and innovation of PDT, the method is limited by the difficulty of using “photosensitizers” such as curcumin because of its low solubility in water, which hinders the clinical application of this technique. The use of a “photosensitizer” along with suitable carriers such as hierarchical zeolites is a potential strategy to offset this difficulty. Therefore, the objective of this study was to develop the photodynamic release of curcumin from hierarchical zeolites using the classical open-circuit release method and a novel closed-circuit release technique involving light of different wavelengths. Based on the obtained data, it was possible to unequivocally state that the speed and efficiency of curcumin release from the zeolite carrier is influenced by light with a wavelength in the range of 430–525 nm (blue-cyan-green). As much as 53.24% of the active substance was released upon light exposure.

Characterization of citric acid crosslinked chitosan/gelatin composite film with enterocin CHQS and red cabbage pigment

A chitosan/gelatin composite packaging film with antioxidant activity, bacteriostatic activity and pH responsiveness was prepared. Red cabbage pigment (RC) and enterocin CHQS were added as actives. In addition, different concentrations of citric acid (CA) were selected as crosslinking agents. Before that, in order to improve the yield of enterocin CHQS and simplify the purification process, we cloned and expressed CHQS in E. coli BL21 (DE3), resulting in an approximately 10-fold increase in yield. The appearances of the films were uniform and transparent with some UV-blocking ability. The results of antioxidant experiments of the films showed that the antioxidant capacity of the films was significantly increased by the addition of RC. Ammonia sensitivity experiments showed that the films could respond to volatile ammonia. Cross-linking improved the thermal stability, water sensitivity and photosensitivity of the films. FTIR and XPS revealed the mode of interaction between CHQS, CA, RC and the composite film structure. FTIR, XPS and XRD confirmed the cross-linking effect of CA. Atomic force microscopy showed that the addition of CA significantly increased the roughness of the film surface. The release experiments of RC showed that the cross-linking of CA promoted the release of active substances from the film and avoided the excessive release due to the dissolution breakage of the film. In addition, bacteria inhibition experiments showed that the addition of CA increased the antimicrobial properties of the films The experiments demonstrated that CHQS was effectively released and the bacteriocins in the films were stably preserved. • Citric acid crosslinking improved smart packaging film properties. • Enterocin CHQS and red cabbage were added as active ingredients. • The water resistance of films containing citric acid improved significantly. • Enterocin CHQS might be kept stably in the films and released effectively.

Biodegradable film based on sodium alginate/flax seed mucilage modified with norbixin and WO3 nanoparticles: investigation of physicochemical properties and release of active substances

Biodegradable film based on sodium alginate/flax seed mucilage modified with norbixin and WO3 nanoparticles: investigation of physicochemical properties and release of active substances

Effect of Ionization Degree of Poly(amidoamine) Dendrimer and 5-Fluorouracil on the Efficiency of Complex Formation-A Theoretical and Experimental Approach.

Due to their unique structure, poly(amidoamine) (PAMAM) dendrimers can bind active ingredients in two ways: inside the structure or on their surface. The location of drug molecules significantly impacts the kinetics of active substance release and the mechanism of internalization into the cell. This study focuses on the effect of the protonation degree of the G4PAMAM dendrimer and the anticancer drug 5-fluorouracil (5FU) on the efficiency of complex formation. The most favorable conditions for constructing the G4PAMAM-5FU complex are a low degree of protonation of the dendrimer molecule with the drug simultaneously present in a deprotonated form. The fluorine components in the XPS spectra confirm the formation of the stable complex. Through SAXS and DLS methods, a decrease in the dendrimer's molecular size resulting from protonation changes at alkaline conditions was demonstrated. The gradual closure of the dendrimer structure observed at high pH values makes it difficult for the 5FU molecules to migrate to the interior of the support structure, thereby promoting drug immobilization on the surface. The 1H NMR and DOSY spectra indicate that electrostatic interactions determine the complex formation process. Through MD simulations, the localization profile and the number of 5FU molecules forming the complex were visualized on an atomic scale.

Каротиноиды в терапии возрастной макулярной дегенерации: система доставки имеет значение

Age-related macular degeneration (AMD) is one of the leading causes of low vision and blindness worldwide for people over age 60. By 2040, the number of people living with macular degeneration is expected to reach 288 million due to the exponential acceleration of population aging. A decline in visual functions caused by AMD has a significant economic impact in all countries. Besides aging, there are other multiple heterogenic risk factors associated with AMD: gender, environmental condition, lifestyle, genetic characteristics, chronic inflammatory processes in the human body, level of education, etc. It is important for the ophthalmologist to be aware of modifiable risk factors and thus to collect a comprehensive medical history, interact with patients using motivational interviewing and to involve promptly other healthcare specialists into the patient management strategy. Etiopathogenesis of AMD is still not entirely understood. However, it is known that the major pathways include age-related alterations of retinal pigment epithelium (RPE) cells, oxidative stress, dysregulated lipid metabolism, inflammation, hemodynamic changes, and neovascularization. Carotenoids lutein and zeaxanthin are natural compounds with a proven efficacy in reducing AMD progression, which have been demonstrated to act as medications for patients with early AMD stages. The micro- encapsulated formula offers such an advantage as gradual and controlled release of active substances. Keywords: age-related macular degeneration, risk factors, etiopathogenesis, carotenoids, lutein, zeaxanthin, microcapsules. For citation: Maksimov M.L., Oganezova J.G., Kanner I.D., Voznesenskaya A.A. Carotenoids in the treatment of age-related macular degeneration: a drug delivery system does matter. Russian Journal of Clinical Ophthalmology. 2023;23(1):60–65 (in Russ.). DOI: 10.32364/2311-7729-2023-23-1-60-65.

Improving the active food packaging function of poly(lactic acid) film coated by poly(vinyl alcohol) based on proanthocyanidin functionalized layered clay

In this paper, natural plant polyphenol-proanthocyanidin (PAC) and layered clay-layered double hydroxides (LDHs) were firstly introduced into poly(vinyl alcohol) (PVA) based coatings to construct PAC/PVA and PAC functionalized LDHs (LDHs@PAC-Cu)/PVA dual active coatings, and further successively coated on the surface of PLA base films to develop PLA active films. The results showed that PAC and copper ions were successfully loading on the LDHs surface through adsorption and complexation. After a certain amount (≥3 wt%) of LDHs@PAC-Cu was added, active packaging functions and gas barrier properties of PLA active films were improved markedly. When 5 wt% LDHs@PAC-Cu was added, antioxidant and antibacterial properties of PLA active films reached 84.31% and 95.5%, oxygen and water vapor transmission rate decreased by 99.4% and 62.6% compared with PLA base film, and the shelf life of pasteurized milk was extended from 60 h to 96 h. Active substances release test indicated that LDHs@PAC-Cu could not only delay the release of active substances in the early stage, but also supplement the release of active substances in the later stage, thus extending the shelf life of food more effectively. Therefore, PLA active films have good application potential in the field of active food packaging.

The Development of the Antibacterial Microcapsules of Citrus Essential Oil for the Cosmetotextile Application: A Review.

Essential oils (EOs) obtained from the Citrus genus were reported to exhibit good antimicrobial activity. Therefore, they can potentially be applied in daily necessities such as textile sectors as antibacterial functional fabric products. However, a packaging technique to retain such volatile and labile active substances is compulsory. In particular, microencapsulation was found to be a common coating technique employed to protect EOs from the effects of light, heat, humidity, stability, and controlled release of active substances. Various microencapsulation techniques have been introduced, but the most widely used method is complex coacervation, as it is simple, inexpensive, and capable of snaring high essential oils. Hence, this review focused on the microencapsulation of the most consumable citrus EOs with complex coacervation methods and their immobilization on commonly carried-out fabrics. In addition, it also discusses the isolation methods of the EOs, their chemical composition, and the mechanism of antibacterial action.

The Applications of Ferulic-Acid-Loaded Fibrous Films for Fruit Preservation.

The aim of this study was to develop a novel ultrathin fibrous membrane with a core-sheath structure as an antioxidant food packaging membrane. The core-sheath structure was prepared by coaxial electrospinning, and the release of active substances was regulated by its special structure. Ferulic acid (FA) was incorporated into the electrospun zein/polyethylene oxide ultrathin fibers to ensure their synergistic antioxidant properties. We found that the prepared ultrathin fibers had a good morphology and smooth surface. The internal structure of the fibers was stable, and the three materials that we used were compatible. For the different loading positions, it was observed that the core layer ferulic-acid-loaded fibers had a sustained action, while the sheath layer ferulic-acid-loaded fibers had a pre-burst action. Finally, apples were selected for packaging using fibrous membranes to simulate practical applications. The fibrous membrane was effective in reducing water loss and apple quality loss, as well as extending the shelf life. According to these experiments, the FA-loaded zein/PEO coaxial electrospinning fiber can be used as antioxidant food packaging and will also undergo more improvements in the future.

Simultaneous Determination of Glibenclamide and Silymarin Released from Chitosan Microparticles by HPLC-ESI-MS Technique: Method Development and Validation.

The study aim was to develop and validate a high-performance liquid chromatography–electrospray ionization mass spectrometry (HPLC-ESI-MS) method to simultaneously determine glibenclamide (Gli) and silymarin (Sil) released from chitosan (CS) microparticles in aqueous solutions. The CS microparticles were synthesized using an ionic gelation method, and their morphology, swelling degree, encapsulation efficiency and active substance release were investigated. Gli and Sil were loaded in different concentrations, and their identification and quantification were performed using the HPLC-ESI-MS method, which was further validated. The drugs’ characteristic m/z was found in the higher intensity of retention time (Rt) (Gli, 8.909 min; Sil A, 5.41 min; and Sil B, 5.66 min). The method selectivity and precision are very good, and the blank solution proved no interference. The linearity of the answer function is very good for Sil A (R2 = 1), Sil B (R2 = 0.9998) and Gli (R2 = 0.9991). For Gli, we obtained a limit of detection (LOD) = 0.038 mg/mL and limit of quantification (LOQ) = 1.275 mg/mL; for Sil A, a LOD = 0.285 mg/mL and LOQ = 0.95 mg/mL; and for Sil B, a LOD = 0.045 mg/mL and LOQ = 0.15 mg/mL. A high-resolution HPLC-ESI-MS method was developed and validated, which allowed the simultaneous determination of Gli and Sil loaded in CS microparticles, in a concentration range of 0.025–1 mg/mL.