Concentration Of Active Substance Research Articles

Comparative evaluation of florfenicol and polymeric nanopar-ticles loaded with florfenicol against bacterial strains isolated from chickens: insights into antimicrobial resistance

Antimicrobial resistance (AMR) poses a significant threat to both human and animal health, necessitating the search for alternative antimicrobial agents and strategies. In this study, we aimed to identify and isolate clinical bacterial strains from chickens and evaluate their sensitivity to florfenicol, a common antimicrobial agent that is used exclusively in veterinary medicine, along with polymeric nanoparticles loaded with florfenicol at various concentrations. Three clinical bacterial strains were successfully isolated and identified from chicken presenting clinical signs. In order to assess their susceptibility, the isolated strains were subjected to a standard disc diffusion assay using florfenicol. Subsequently, polymeric nanoparticles loaded with florfenicol were tested at six different concentrations and compared their efficacy against the bacterial strains. Our results demonstrated that all three clinical bacterial strains exhibited varying degrees of resistance to florfenicol. Interestingly, the use of polymeric nanoparticles loaded with florfenicol did not display enhanced antimicrobial activity compared to the free drug. Notably, the efficacy of the loaded nanoparticles did not significantly vary with different concentrations of active substance. This study highlights the importance of exploring novel therapeutic approaches to combat antimicrobial resistance. The use of polymeric nanoparticles loaded with florfenicol presents a promising avenue for overcoming resistance mechanisms and improving the efficacy of antimicrobial treatments both in human and veterinary medicine. Further investigations are needed to elucidate the underlying mechanisms and optimize the formulation of polymer nanoparticles for enhanced therapeutic outcomes in combating AMR.

Major Active Metabolite Characteristics of Dendrobium officinale Rice Wine Fermented by Saccharomyces cerevisiae and Wickerhamomyces anomalus Cofermentation.

Rice, supplemented with Dendrobium officinale, was subjected to cofermentation using Saccharomyces cerevisiae FBKL2.8022 (Sc) and Wickerhamomyces anomalus FBKL2.8023 (Wa). The alcohol content was determined with a biosensor, total sugars with the phenol-sulfuric acid method, reducing sugars with the DNS method, total acids and total phenols with the colorimetric method, and metabolites were analyzed using LC-MS/MS combined with multivariate statistics, while metabolic pathways were constructed using metaboAnalyst 5.0. It was found that the quality of rice wine was higher with the addition of D. officinale. A total of 127 major active substances, mainly phenols, flavonoids, terpenoids, alkaloids, and phenylpropanoids, were identified. Among them, 26 substances might have been mainly metabolized by the mixed-yeasts fermentation itself, and 10 substances might have originated either from D. officinale itself or from microbial metabolism on the newly supplemented substrate. In addition, significant differences in metabolite could be attributed to amino acid metabolic pathways, such as phenylalanine metabolism and alanine, aspartate, and glutamate metabolism. The characteristic microbial metabolism of D. officinale produces metabolites, which are α-dihydroartemisinin, alantolactone, neohesperidin dihydrochalcone, and occidentoside. This study showed that mixed-yeasts cofermentation and fermentation with D. officinale both could increase the content of active substances in rice wine and significantly improve the quality of rice wine. The results of this study provide a reference for the mixed fermentation of brewer's yeast and non-yeast yeasts in rice wine brewing.

Using of the chemography method for assessing the homogenizati on of graphene nanotubes in the aqueous environment

The problem of effective homogenization of graphene nanotubes in an aqueous environment is considered. Usually, the high activity of nanotubes leads to the formation of various conglomerates in the solution, and with further application of the aqueous solution, such conglomerates can be transferred to the composite materials being created. Currently, there are no effective fast control tools, and therefore in engineering practice, various fairly complex methods that require specific equipment are often used. Chemography as a method of recording oxidative reactions with ultra-low concentrations of active substances can be successfully used as a means of quick and effective control of the homogeneity of graphene solutions (mainly water-based). Recommendations for the application of the method are given, models are proposed for determining the dispersion of the expected concentration on the controlled surface. A conclusion is made regarding the expediency of monitoring the state and activity of graphene nanotubes.

Widely targeted metabolomic analysis revealed the effects of alkaline stress on nonvolatile and volatile metabolites in broomcorn millet grains

Broomcorn millet (BM) is a future smart food. However, no information is available on the metabolism of BM grains under alkaline stress. In this study, the effects of alkaline stress on nonvolatile and volatile metabolites in the BM grains of two varieties (S223 and T289) were investigated through metabolomics approaches. All 933 nonvolatile metabolites and 313 volatile metabolites were identified, with 114 and 89 nonvolatile metabolites and 16 and 20 volatile metabolites accumulating differentially under normal vs. alkaline stresses of S223 and T289, respectively. The results indicated that alkaline stress altered phenylpropanoids, flavonoids, flavone and flavonol, valine, leucine, and isoleucine biosynthesis, as well as arginine, proline, tryptophan, and ascorbate metabolism. The effects of alkaline stress were not identical between the two varieties, which could lead to variations in active substance content. These results provide valuable information for further studies on food chemistry and the functional food development of BM grains.

Quality Evaluation of Hainan Robusta Coffee Bean Oil Produced by Ultrasound Coupled with Coconut Oil Extraction.

This study investigates the treatment of coconut oil using thermosonic treatment in combination with green coffee beans. Under a defined ratio of coconut oil to green coffee beans, the effect of different thermosonic time on the quality parameters, active substance content, antioxidant capacity, and thermal oxidative stability of coconut oil were investigated as a strategy to potentially improve the quality of oil. Results showed that the β-sitosterol content of CCO (coconut coffee oil) treated with the thermal method combined with green coffee bean treatment reached up to 393.80 ± 11.13 mg/kg without affecting the lipid structure. In addition, DPPH clearance equivalents increased from 5.31 ± 1.30 mg EGCG/g to 71.34 ± 0.98 mg EGCG/g, and the ABTS clearance equivalent was 45.38 ± 0.87 mg EGCG/g versus 0 for the untreated sample. The improvement in thermal oxidation stability of treated coconut oil is also significant. The TG (Thermogravimetry) onset temperature was elevated from 277.97 °C to 335.08 °C and the induction time was elevated up to 24.73 ± 0.41 h from 5.17 ± 0.21 h. Thermosonic treatment in combination with green coffee beans is an ideal option to improve the quality of coconut oil. The results of this article provide new ideas for the development of plant-blended oil products and the new utilization of coconut oil and coffee beans.

Dynamic changes of active substances of rice, Pueraria and yam fermentation by Monascus ruber

Monascus spp., a fungus of medicine food homology, produces various beneficial secondary metabolites such as monacolin K (MK) during fermentation. In this study, the mixed fermentation of Monascus with rice, Pueraria, and yam has been systematically investigated. Single-factor and response surface methodology (RSM) were carried out to maximize MK content, and the optimized fermentation results showed that the content of MK reached 1.40 ± 0.04 mg/g. The optimal fermentation process determined the ratio of 8: 1: 1 for rice, Pueraria, and yam, respectively, the inoculation amount was 106 spores/mL, fermentation time was 15 days. Further analysis of the content of active substance in the fermentation process revealed that the β-glycosidase activity increased, the amylase enzyme activity decreased, the dioscin content decreased by 19.5%, and the diosgenin content increased by 175%, suggesting that there was a dynamic equilibrium relationship among the changes of active substances. This study aims at provide a basis and reference for the research of Monascus fermented foods by medicine food homology raw materials.

Local antibacterial therapy in patients with diseases of the nasal cavity and paranasal sinuses, including against the background of cystic fibrosis

Acute respiratory viral infection is one of the most common infectious diseases. Clinical manifestations vary from time to time and from person to person and, as a rule, include intoxication and catarrhal syndromes. ARVI is more often caused by such causative agents as pneumoviruses, human metapneumovirus, coronaviruses, rhinoviruses, adenoviruses and bocaviruses. Among diseases of the ENT organs, ARVI can cause rhinosinusitis and pharyngitis. The inflammation that occurs in the mucosa causes its dystrophy and necrosis, which leads to the dysfunction of mucociliary clearance. As a result, an optimal environment for the development of bacterial flora is created. Bacterial rhinosinusitis needs antibiotic therapy. These drugs can act locally and systemically. It is well known that topical drugs have fewer side effects and result in a greater active substance concentration directly at a site of inflammation. Currently, a nasal framycetin spray is used as a topical antibacterial therapy to treat bacterial rhinosinusitis and in the early postoperative period. Topical drugs have a good evidence base, fewer side effects, and are safe, even for patients with cystic fibrosis. Given the significant antibiotics load in patients with cystic fibrosis, any opportunity to delay re-administration of antibiotics is a positive thing. In this aspect, topical antibiotics that have no systemic adverse events, including negative effects on the normal human microbiome, and can be used to overcome the resistance of microorganisms in a varying degree due to the achievement of high active substance concentration directly in a focus of infection may have a certain therapeutic value. The article addresses issues of epidemiology, pathogenesis, clinical manifestations of acute respiratory viral infection, i. e. acute rhinosinusitis. In addition, the article describes the use of topical antibiotic therapy for the treatment of diseases of the nasal cavities and paranasal sinuses.

ОПТИМИЗАЦИЯ МЕТОДА ОПРЕДЕЛЕНИЯ ТАРГЕТНЫХ МОЛЕКУЛ В ОРГАНОИДНЫХ СИСТЕМАХ

The study optimized the analytical method for determining the active components of targeted drugs for the treatment of low-grade gliomas dabrafenib and trametinib, in a model organoid system. Third generation organoids were incubated for 24 hours in the presence of 100 μg/ml dabrafenib and trametinib (substance, SIGMA-Aldrich, Germany) (3 cultures in each series). The method for determining dabrafenib and trametinib in organoid tissue included sequential washing of tumor-like structures from the incubation medium, homogenization and centrifugation, followed by determination of the concentration of active substances in the supernatant by HPLC on a Shimadzu LCMS-8030 mass spectrometer (Japan) using a Phenomenex Luna® C18 column (2) 250 * 4.6 mm, with an internal diameter of 5 μm and a sorbent pore diameter of 100 Å. The release time (RT) of dabrafenib in these conditions was 7.405 minutes, the RT of trametinib was 8.356 minutes, the selectivity factor (α) was 1.19, which satisfied the requirements (α > 1). The chromatographic system resolution (Rs) was 2.13, indicating complete separation (Rs > 1.5). Thus, the developed method may be used to determine molecularly targeted drugs - dabrafenib and trametinib in model tumor systems.

TRANSFERSOMES AS NOVEL DRUG DELIVERY SYSTEM

Transdermal drug delivery appears to be most vital drug delivery system because of its merit over conventional systems. Transferosomes & the fundamental concept of transfersomes were launched by Gregor Cevc in the year 1991. The name means carrying body and is derived from the Latin word transferre, meaning to carry across and the Greek word soma, meaning a body. Novel drug delivery system aims to deliver the drug at a rate directed by need of body during the period of treatment and channel the active entity to the site of action. Transferosome is one of the novel vesicular drug delivery system which consists of phospholipids, surfactant and water for enhanced transdermal delivery. Transferosomes are able to reach intact deeper regions of the skin after topical drug administration while delivering higher concentrations of active substances making them a successful carrier for transdermal applications. These vesicular systems can deliver low as well as high molecular weight compounds. Targeted and controlled release formulations can also be prepared by transferosomes as it can accommodate drug molecules with wide range of solubility. Various strategies can be used to augment the transdermal delivery which includes iontophoresis, electrophoresis, sonophoresis, chemical permeation enhancers, microneedles, & vesicular system (liposomes, niosomes, elastic liposomes such as ethosomes & transfersomes). It exists as an ultra-deformable complex having a hydrated core surrounded by a complex layer of lipid. It penetrates the stratum corneum by either intracellular route or the transcellular route by the generation of osmotic gradient. Advantages of Transferosomes are wide range of solubilities, better penetration, biocompatible and biodegradable etc. Disadvantages of Transferosomes are oxidative degradation, expensive, etc. The transfersomes were formulated by the conventional rotary evaporation sonication method. Transferosomes can be applied in controlled release, transportation of large molecular weight compounds, target delivery to peripheral subcutaneous tissues, transdermal immunization etc.

Pharmacological justification of the composition of active ingredients in the composition of «Molozol» gel

Today, in connection with the rapid increase in the number of skin diseases complicated by secondary microbial and fungal infection, the creation of new drugs with a complex dermatomycosis effect for their local use is gaining particular relevance. In modern dermatological practice, mostly soft dosage forms are used. The wide use of soft medicinal forms is due to the presence of some advantages: high local concentration in the skin, relative economy and manufacturability of these means. However, on the modern Ukrainian pharmaceutical market, the range of drugs with a complex dermatomycosis effect is limited. This makes it necessary to find new means for local application in dermatitis with complicated fungal pathology.
 The aim of our research is an experimental ground of rational composition of operating substances in a gael under the conditional name «Molozol» for treatment of dermatomycoses. Gel was prepared on general rules by preparations of soft medical forms. Taking into account physical and chemical properties of operating substances, in particular their solubility, sucking, salicylic and sorbic acid was entered as a solution in propylene glycol and entered in the basis procured in advance for gel. With the aim of ground of rational concentration milk, salicylic and sorbic acid in the combined gel of «Molozol», and also study of his biological activity were conducted microbiological and toxicological.
 Determination of the antibacterial properties of the gel was carried out by diffusion in agar using reference strains of microorganisms Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853, Candida albicans ATCC 885/653.
 The rational composition of the active substances of the gel under the conventional name «Molosol» for the treatment of dermatomycosis was experimentally substantiated. Based on the data of microbiological studies, the concentration of active substances – lactic acid, salicylic acid and sorbic acid in the composition of the gel «Molosol» was justified. With the combination of active substances salicylic acid 8%, lactic acid 10%, for sorbic acid concentration 0.5%, «Molosol» gel shows the most pronounced antimicrobial and fungicidal activity against the tested strains of microorganisms.
 The index of acute toxicity when applied to the skin of animals was determined, which proved that the developed soft drug «Molosol» in the form of a gel belongs to the IV class of low-toxic substances.
 The combined gel «Molosol» is promising for further research as an antimicrobial and antifungal agent with keratolytic properties.

АНАЛИЗ ГЕРБИЦИДНОЙ АКТИВНОСТИ ПРЕПАРАТИВНЫХ ФОРМ ПРОТРАВИТЕЛЕЙ НА ОСНОВЕ БЕНТАЗОНА

The study is devoted to the analysis of the herbicidal activity of preparative forms of disinfectants based on the sodium salt of bentazone, as well as the oxy-forms of bentazone in comparison with the commercial herbicide Octapon Extra, CE. It was found that all studied samples exhibit high herbicidal activity against the dicotyledonous weeds field mustard (Sinapis arvensis L.) and blue cornflower (Centauréa cyánus L.). It was revealed that all samples based on the sodium salt of bentazone were 5% more effective than the commercial herbicide. Of the studied oxy-forms of bentazone, the drug with an active substance concentration of 480 g/l showed the maximum effectiveness, while its effectiveness was 3% higher than that of a commercial herbicide. It was shown that all tested samples did not exhibit herbicidal activity against spring wheat (Triticum aestivum L.). Based on the data obtained, it was concluded that the studied formulations are promising for the development of herbicides for use for guard of cereal crops.

The effectiveness of the use of analogue preparations with the active substance rimsulfuron on potatoes in the conditions of the Tyumen region

Relevance. The study of the effectiveness of protection methods, herbicides with different content and composition of active substances, their influence on the crop, weed component, yield and related factors is important for clarifying the regulations for use, production decisions in the manufacture of preparations and their use.Methods. The study of the effect of various analogues of herbicides with the active ingredient rimsulfuron on weed suppression and crop development was carried out on the experimental field of the Research Institute of Agriculture of the Northern Trans-Urals, the northern forest-steppe of the Tyumen region under the conditions of 2021. The object of research was 4 preparations of herbicidal action from different manufacturers with the main active ingredient rimsulfuron 250 g/kg for use on potato crops to suppress weeds of perennial and annual cereal type and annual dicotyledonous type.Results. The initial study of the clogging of experimental plots before treatment with the studied herbicides showed the presence of an average number of processing showed the presence of a total number of weeds according to the variants of the experiment 60–70 pcs/m2 with a quantitative advantage of 4 types of weeds еchinochloa crus-galli, Elymus repens, Thlaspi arvense, Chenopódium álbum. On the variants of herbicide application, the mass of weeds was 8–20 times less and amounted to 20–55 g/m2. As a result of the use of the studied herbicides against weeds, a stable and high efficiency of 86–97% during the entire growing season on options Herbicide 3, 4.

Effect of Urban Environment on Ecological and Phytochemical Features of <i>Crataegus fallacina</i> (Rosaceae) Flowers (the Case of the Donbass)

Abstract—The article presents the results of a study of the effect of urban environment in the Donbass on the content of biologically active substances, heavy metals and antioxidant activity of the flowers of Crataegus fallacina Klok., a poorly studied non-pharmacopoeial species of the genus Crataegus L. Under technogenic pollution, in the flowers of C. fallacina a decrease in the concentration of carotenoids and an increase in the content of phenolic compounds (flavonoids, procyanidins, oxycinnamic acids, tannins, anthocyanins), ascorbic and free organic acids was detected. The hermetic response of the content of anthocyanins and procyanidins to the pollution level was observed. The flowers of C. fallacina have a high total antioxidant activity, which increases under technogenic load, indicating plants sufficient adaptation to the urbanized environment. The ability of C. fallacina plants to limit flow of cadmium and lead to generative organs was revealed. The concentration of mercury in flowers exceeds its concentration in soil. C. fallacina flowers harvested in the Donbass meet the regulations on the content of active substances and comply with the requirements with regard to the heavy metals content. The obtained results prove the practicability of using C. fallacina for pharmaceutical purposes along with pharmacopoeial species of the genus Crataegus, and the possibility of their harvesting for medicinal use in the Donbass.

Validation of a Spectrophotometric Method of Some Antidepressant Drugs

Abstract Although the causes of depression include a wide range of conditions, from neurodegenerative to thyroid, they all have one common denominator, changes in the brain. Depression can be located in multiple brain regions simultaneously, which may be derived from a common molecular abnormality found in neurons in many brain regions. Abnormalities of receptors or impulse transmission could be the answer. In this work, a simple and accurate spectrophotometric method was developed for the analysis of escitalopram oxalate in various pharmaceutical formulations. In this method, absorbance was measured at 238 nm for escitalopram oxalate. Method validation parameters were studied. The method can be used for quality control of pharmaceutical forms containing escitalopram. Also, by the same method, the actual active substance concentrations compared to those listed on the package, the standard deviations and the relative standard deviations.

Investigation on optical and electrical properties of soil discharge under pulse voltage

Many researchers have studied the application of low temperature plasma in soil remediation, but most focus on the degradation efficiency of a specific pollutant, and less attention is paid to the development and evolution process of plasma behind the soil remediation. In this paper, the possible mechanism behind soil discharge under pulse voltage is studied from the perspectives of electricity and optics. The electrical and optical analyses show that the soil discharge under pulse voltage mainly exists at the rising stage of pulse voltage, and the existence time is related with the pulse voltage amplitude. At the same time, the relative intensity of active substances (•OH, H, O Ⅱ and N Ⅰ), vibration temperature and rotational temperature are obtained by using the emission spectrum, which demonstrate that high pulse voltage can increase the concentration of active substances, vibration temperature and rotational temperature.

Comprehensive transcriptional and metabolomic analysis reveals the neuroprotective mechanism of dietary gamma-aminobutyric acid response to hypoxic stress in the Chinese mitten crab (Eriocheir sinensis)

Hypoxia is one of the serious stress challenges that aquatic animals face throughout their life. Our previous study found that hypoxia stress could induce neural excitotoxicity and neuronal apoptosis in Eriocheir sinensis, and observed that gamma-aminobutyric acid (GABA) has a positive neuroprotective effect on juvenile crabs under hypoxia. To reveal the neuroprotective pathway and metabolic regulatory mechanism of GABA in E. sinensis exposed to hypoxia stress, an 8-week feeding trial and acute hypoxia challenge were performed. Subsequently, we performed a comprehensive transcriptomic and metabolomic analysis of the thoracic ganglia of juvenile crabs. Differential genes and differential metabolites were co-annotated to 11 KEGG pathways, and further significant analysis showed that only the sphingolipid signaling pathway and the arachidonic acid metabolism pathway were significantly enriched. In the sphingolipid signaling pathway, GABA treatment significantly increased long-chain ceramide content in thoracic ganglia, which exerted neuroprotective effects by activating downstream signals to inhibit hypoxia-induced apoptosis. Moreover, in the arachidonic acid metabolism pathway, GABA could increase the content of neuroprotective active substances and reduce the content of harmful metabolites by regulating the metabolism of arachidonic acid for inflammatory regulation and neuroprotection. Furthermore, the decrease of glucose and lactate levels in the hemolymph suggests the positive role of GABA in metabolic regulation. This study reveals the neuroprotective pathways and possible mechanisms of GABA in juvenile E. sinensis exposed to hypoxia stress and inspires the discovery of new targets for improving hypoxia tolerance in aquatic animals.

Quality control of Hugan capsule based on four-wavelength fusion profiling and electrochemical fingerprint combined with antioxidant activity and chemometric analysis

Improving the quality standard system of herbal preparations (HPs) is an arduous task for the development of traditional Chinese medicine (TCM). At present, an urgent task is to establish a comprehensive, scientific and effective evaluation method for improving the safety, effectiveness and quality consistency of HPs. In this study, Hu Gan capsules (HGCs) were used as an example. Firstly, the three quality markers (Q-markers) in 21 batches of HGCs from 4 manufacturers were determined by HPLC and great difference in content of each sample was found. Furthermore, four-wavelength fusion profiling (FWFP) was established and evaluated by systematically quantified fingerprint method (SQFM). Principal component analysis (PCA) was employed to make a preliminary analysis of the FWFP and distinguish the fluctuation of differences in chemical composition and content. Then, 9 characteristic parameters were recorded through the B-Z oscillating system, and the electrochemical fingerprint (ECFP) was constructed for jointing evaluation with the FWFP, using the equal weight of SQFM results to comprehensively evaluate the sample quality. The 21 batches of samples were divided into four groups and six grades, which indicated that there were significant differences in the content of indicator components and electrochemical active substances in samples. Finally, taking vitamin C as a positive control, 2, 2′-azino-bis (3 - ethyl -benzthiazoline - 6 - sulfonic acid) (ABTS) scavenging assay was applied to study the antioxidant activity of samples. Partial Least Squares (PLS) and bivariate correlation analysis (BCA) were used to analyze the fingerprint-efficacy relationships of FWFP-ABTS and FWFP-ECFP. Consequently, it was found that there were similar antioxidant capacities in electrochemistry and ABTS tests, and 31 of the 40 HPLC fingerprint peaks of HGCs were discovered to have antioxidant activity. The two methods supported each other, to effectively and corporately reflect the antioxidant components in HGCs. In this research, the FWFP and ECFP established could realize the quality detection of HGCs, and provide a novel direction for the improvement of the quality standard of HPs and the research of the quality standard method of TCM.

Plasma-Activated Tap Water Production and Its Application in Atomization Disinfection

Plasma-activated tap water (PATW) is a new technology for obtaining a high concentration of active aqueous plasma substances by discharging underwater. Commonly plasma-activated water (PAW) is realized by activating deionized water or distilled water, which has problems such as high cost, a small discharge area, and insufficient dissolution of active substances. This paper reports the development of a dielectric barrier discharge array to generate a high concentration of active aqueous plasma substances. The device can realize a uniform, stable, and large-area discharge in a large volume of tap water, and it has the advantages of low cost, high integration, and reusability. Using the device to treat 1000 mL of tap water for 1 h can reduce the pH of the tap water from 8.10 to 2.54, and the logarithmic value of killing E. coli is greater than 5.0. We sprayed PATW onto clothes to sterilize the bacteria when people were through the disinfection door and verified that the PATW had a good sterilization effect. The short-lived substances, singlet oxygen, and superoxide anion radicals played a key role in the sterilization process by PATW.

3D-Printed, Liquid-Filled Capsules of Concentrated and Stabilized Polyphenol Epigallocatechin Gallate, Developed in a Clinical Trial

In vitro studies have shown that epigallocatechin gallate (EGCG), the most potent antioxidant of the green tea polyphenol catechins, is able to effectively prevent the formation of amyloid plaques and induce their clearance. However, its high chemical reactivity promotes high chemical instability, which represents a major obstacle for the development of pharmaceutical forms containing solubilized EGCG, an essential condition for a better systemic passage via the oral route. After discovering that EGCG forms a deep eutectic with choline chloride, we exploited this property to formulate and patent liquid-filled capsules containing 200-800 mg of soluble EGCG in easy-to-administer sizes. The gelatin envelopes used are of the conventional type and their filling has been achieved using 3D printing technology. Not only did the EGCG-choline complex allow the formulation of hydrophilic solutions with a high concentration of active substance but it also contributed significantly to its chemical stability, since after at least 18 months of storage at 25 °C/60% RH and one year at 40 °C/75% RH, the capsules show unchanged hardness, chromatographic profiles and antioxidant activity compared to T0. Preclinical studies in monkeys showed that bioavailability was increased by a factor of 10 compared to marketed capsules comprising EGCG powder. This pharmaceutical development was conducted in the context of upcoming clinical trials to evaluate EGCG alone or in combination when treating transthyretin and light-chain cardiac amyloidosis.

Comparison of the In Vitro Drug Release Methods for the Selection of Test Conditions to Characterize Solid Lipid Microparticles

The release profiles of active substances from microspheres are one of the most important features in solid lipid microparticles (SLM) characterization. Unfortunately, the results of the dissolution tests are largely dependent on the chosen method and test conditions, which in relation to novel dosage forms, such as dispersions of lipid microspheres, are not clearly defined in international compendiums and guidelines. This makes it impossible to compare the results of different studies. The aim of the research was to identify the factors most influencing the variability of the obtained results. An attempt was also made to select the most appropriate method for testing drug substance release from SLM. Various dissolution methods were employed (method I: without a membrane, method II: in a dialysis bag, and method III: in a Side-Bi-Side chamber), and the obtained release profiles of cyclosporine and indomethacin from SLM dispersions were compared. In addition to the effect of membranes, the types of acceptor fluids were also investigated. Significant differences were observed when testing the SLM formulations under various test conditions. The results were significantly influenced by the selected membrane, the acceptor fluid, or the difference in the concentrations of active substance between the donor and acceptor compartments. The burst effect observed in some experimental methods was not noticed in other conditions. At this stage, the method with a dialysis bag has been selected as the most suitable, while the methods without the membrane can only play a complementary role.