Magnesium Aluminometasilicate Research Articles

Antimicrobial, Probiotic, and Immunomodulatory Potential of Cannabis sativa Extract and Delivery Systems.

The compounds present in hemp show multidirectional biological activity. It is related to the presence of secondary metabolites, mainly cannabinoids, terpenes, and flavonoids, and the synergy of their biological activity. The aim of this study was to assess the activity of the Henola Cannabis sativae extract and its combinations with selected carriers (polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer, magnesium aluminometasilicate, and hydroxypropyl-β-cyclodextrin) in terms of antimicrobial, probiotic, and immunobiological effects. As a result of the conducted research, the antimicrobial activity of the extract was confirmed in relation to the following microorganisms: Clostridium difficile, Listeria monocytogenes, Enterococcus faecalis, Staphylococcus aureus, Staphylococcus pyrogenes, Escherichia coli, Klebsiella pneumoniae, Salmonella typhimurium, Pseudomonas aereuginosa, and Candida albicans (microorganism count was reduced from ~102 CFU mL-1 to <10 CFU mL-1 in most cases). Additionally, for the system with hydroxypropyl-β-cyclodextrin, a significant probiotic potential against bacterial strains was established for strains Lactobacillus acidophilus, Lactobacillus casei, Lactobacillus plantarum, Lactobacillus brevis, Lactobacillus rhamnosus, Lactobacillus reuteri, Pediococcus pentosaceus, Lactococcus lactis, Lactobacillus fermentum, and Streptococcus thermophilus (microorganism count was increased from ~102 to 104-107). In terms of immunomodulatory properties, it was determined that the tested extract and the systems caused changes in IL-6, IL-8, and TNF-α levels.

Innovative high fat diet establishes a novel zebrafish model for the study of visceral obesity

Obesity is a complex chronic condition associated with multiple health risks, including visceral obesity, which is particularly detrimental. To gain insight into the mechanisms underlying obesity and its associated pathologies, a novel zebrafish model was established using an innovative high-fat diet (HFD). The primary goal was to induce visceral obesity in zebrafish and study the associated structural changes. To achieve this, a unique HFD consisting of 40% beef fat (HFD40) was developed and supplemented with magnesium aluminometasilicate to improve stability in a high humidity environment. Feeding regimens were initiated for both juvenile (starting at 2 weeks post-fertilization, lasting 18 weeks) and adult zebrafish (3 months post-fertilization, 8 weeks feeding duration). The innovative dietary approach successfully induced visceral obesity in both juvenile and adult zebrafish. This new model provides a valuable tool to study obesity-related pathologies, metabolic syndrome, and potential therapeutic interventions. Most importantly, the low-cost and easy-to-prepare composition of HFD40 was seamlessly incorporated into the water without the need for separation, was readily absorbed by the fish and induced rapid weight gain in the zebrafish population. In conclusion, this study presents a novel HFD40 composition enriched with a high beef fat concentration (40%), which represents a significant advance in the development of an experimental zebrafish model for the study of visceral obesity and associated metabolic changes.

Comparison of the liquisolid technique and co-milling for loading of a poorly soluble drug in inorganic porous excipients

Drug loading into mesoporous carriers may help to improve the dissolution of poorly aqueous-soluble drugs. However, both preparation method and carrier properties influence loading efficiency and drug release. Accordingly, this study aimed to compare two preparation methods: formulation into liquisolid systems (LSS) and co-milling for their efficiency in loading the poorly soluble model drug cyclosporine A (CyA) into mesoporous magnesium aluminometasilicate Neusilin® US2 (NEU) or functionalized calcium carbonate (FCC). Scanning electron microscopy was used to visualize the morphology of the samples and evaluate the changes that occurred during the drug loading process. The solid-state characteristics and physical stability of the formulations, prepared at different drug concentrations, were determined using X-ray powder diffraction. In vitro release of the drug was evaluated in biorelevant media simulating intestinal fluid. The obtained results revealed improved drug release profiles of the formulations when compared to the milled (amorphous) CyA alone. The dissolution of CyA from LSS was faster in comparison to the co-milled formulations. Higher drug release was achieved from NEU than FCC formulations presumably due to the higher pore volume and larger surface area of NEU.

Febuxostat solubilization and stabilization approach using solid dispersion method: Synergistic effect of dicalcium phosphate dehydrate and chitosan

Drug solubilization studies are continuously being conducted. Febuxostat (FBX) has a low solubility in water. This study aims to develop a stable FBX-solid dispersion (SD) formulation using a solvent evaporation method. The solubilization strategy of FBX is to develope an optimal FBX-SD formulation by selecting a solubilizer and carrier through the screening method. The final selected solubilizer, macrogol 15 hydroxystearate and polyoxyl 15 hydroxystearate (Kolliphor® HS-15), is widely used in the pharmaceutical industry as a nonionic solubilizing and emulsifying agent and has low toxicity. Especially when commonly used in developing lipophilic drug formulations, it dissolves well in water and ethyl alcohol. The optimal composition ratio of the formulation (SD4) was FBX:HS-15®:granular dicalcium phosphate dehydrate (DCP-D): A synthetic magnesium aluminometasilicate (Neusilin®UFL2):chitosan = 1:3:3:1:1 (w/w) and showed 3.0-, 2.3-, and 1.1-fold higher dissolution (%) of FBX compared to that of the Feburic tab® in pH 1.2 media, distilled water (DW), and pH 6.8 buffer, respectively. Also, in vitro release and in vitro permeability in SD4 formulation showed higher than that of Feburic tab®. Based on its stability over 6 months, it was confirmed that chitosan acted as a stabilizer. Moreover, due to weak intermolecular interactions, FBX in the SD4 formulation was considered to exist in a mixed state of amorphous and crystalline FBX. In conclusion, the improved dissolution (%) and stability of FBX in SD4 formulation were secured through the synergistic effect of excipients.

Hop Flower Supercritical Carbon Dioxide Extracts Coupled with Carriers with Solubilizing Properties-Antioxidant Activity and Neuroprotective Potential.

Lupuli flos shows many biological activities like antioxidant potential, extended by a targeted effect on selected enzymes, the expression of which is characteristic for neurodegenerative changes within the nervous system. Lupuli flos extracts (LFE) were prepared by supercritical carbon dioxide (scCO2) extraction with various pressure and temperature parameters. The antioxidant, chelating activity, and inhibition of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and tyrosinase by extracts were studied. The extracts containing ethanol were used as references. The most beneficial neuroprotective effects were shown by the extract obtained under 5000 PSI and 50 °C. The neuroprotective effect of active compounds is limited by poor solubility; therefore, carriers with solubilizing properties were used for scCO2 extracts, combined with post-scCO2 ethanol extract. Hydroxypropyl-β-cyclodextrin (HP-β-CD) in combination with magnesium aluminometasilicate (Neusilin US2) in the ratio 1:0.5 improved dissolution profiles to the greatest extent, while the apparent permeability coefficients of these compounds determined using the parallel artificial membrane permeability assay in the gastrointestinal (PAMPA GIT) model were increased the most by only HP-β-CD.

Co-Dispersion Delivery Systems with Solubilizing Carriers Improving the Solubility and Permeability of Cannabinoids (Cannabidiol, Cannabidiolic Acid, and Cannabichromene) from Cannabis sativa (Henola Variety) Inflorescences.

Cannabinoids: cannabidiol (CBD), cannabidiolic acid (CBDA), and cannabichromene (CBC) are lipophilic compounds with limited water solubility, resulting in challenges related to their bioavailability and therapeutic efficacy upon oral administration. To overcome these limitations, we developed co-dispersion cannabinoid delivery systems with the biopolymer polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol (Soluplus) and magnesium aluminometasilicate (Neusilin US2) to improve solubility and permeability. Recognizing the potential therapeutic benefits arising from the entourage effect, we decided to work with an extract instead of isolated cannabinoids. Cannabis sativa inflorescences (Henola variety) with a confirming neuroprotective activity were subjected to dynamic supercritical CO2 (scCO2) extraction and next they were combined with carriers (1:1 mass ratio) to prepare the co-dispersion cannabinoid delivery systems (HiE). In vitro dissolution studies were conducted to evaluate the solubility of CBD, CBDA, and CBC in various media (pH 1.2, 6.8, fasted, and fed state simulated intestinal fluid). The HiE-Soluplus delivery systems consistently demonstrated the highest dissolution rate of cannabinoids. Additionally, HiE-Soluplus exhibited the highest permeability coefficients for cannabinoids in gastrointestinal tract conditions than it was during the permeability studies using model PAMPA GIT. All three cannabinoids exhibited promising blood-brain barrier (BBB) permeability (Papp higher than 4.0 × 10-6 cm/s), suggesting their potential to effectively cross into the central nervous system. The improved solubility and permeability of cannabinoids from the HiE-Soluplus delivery system hold promise for enhancement in their bioavailability.

Screening of the Anti-Neurodegenerative Activity of Caffeic Acid after Introduction into Inorganic Metal Delivery Systems to Increase Its Solubility as the Result of a Mechanosynthetic Approach.

The proven anti-neurodegenerative properties of caffeic acid in vivo are limited due to its poor solubility, which limits bioavailability. Therefore, caffeic acid delivery systems have been developed to improve caffeic acid solubility. Solid dispersions of caffeic acid and magnesium aluminometasilicate (Neusilin US2-Neu) were prepared using the ball milling and freeze-drying techniques. The solid dispersions of caffeic acid:Neu obtained by ball milling in a 1:1 mass ratio turned out to be the most effective. The identity of the studied system in comparison to the physical mixture was confirmed using the X-Ray Powder Diffractionand Fourier-transform infrared spectroscopy techniques. For caffeic acid with improved solubility, screening tests were carried out to assess its anti-neurodegenerative effect. The obtained results on the inhibition of acetylcholinesterase, butyrylcholinesterase, tyrosinase, and antioxidant potential provide evidence for improvement of caffeic acid's anti-neurodegenerative activity. As a result of in silico studies, we estimated which caffeic acid domains were involved in interactions with enzymes showing expression relevant to the neuroprotective activity. Importantly, the confirmed improvement in permeability of the soluble version of caffeic acid through membranes simulating the walls of the gastrointestinal tract and blood-brain barrier further strengthen the credibility of the results of in vivo anti-neurodegenerative screening tests.

Study of the Technological Methods Effect on Dissolution of the X-ray Amorphous Efavirenz-mesoporous Carrier System

Introduction. The low solubility of active pharmaceutical ingredients (APIs) in the physiological pH range of the intestinal tract can adversely affect their absorption and bioavailability. Various methods of increasing the solubility of APIs have been proposed in recent decades. Among them there are preparation of solid dispersions, micronization, solubilization and other methods, including ones based on the amorphization of the crystalline substances, such as, spray drying, hot melt extrusion, absorption on mesoporous carriers such as magnesium aluminosilicate, silica, etc.Aim. Study the technological methods effect on dissolution at physiological temperature and pH range of practically insoluble API efavirenz amorphized by absorption on mesoporous carriers.Materials and methods. Efavirenz form І (EFA) (LLC "AMEDART", Russia, batch 010520). Efavirenz reference standard (USP № R09740). Mesoporous carriers (MC): Silica – Syloid® 244FP (244), Syloid® XDP 3150 (3150) (W.R. Grace&amp;Co.-Conn, USA); FujiSil™ (FSL) (Fuji Chemical Industries Co., Ltd., Japan); Aeroperl® 300 (APL) (Evonik, Germany); Parteck® SLC (SLC) (Merck Millipore, USA); Synthetic magnesium aluminometasilicate – Neusilin® US2 (US2), Neusilin® UFL (UFL) (Fuji Chemical Industry Co., Ltd., Japan). The API absorption on MC was performed via solvent wetting and hot melt extrusion methods.Results and discussion. The dissolution increases in the MC series as the following: SLC &gt; FSL &gt; UFL = US2 &gt; 244 = 3150. The data are consistent with an increase in the surface area and a decrease in the pore size of MC. The crystalline state of the system API efavirenz-Aeroperl® is caused by the largest pore size. It is obvious according to the data that the solvent wetting method gives better results in comparison with the hot melt extrusion as the method of obtaining X-ray amorphous systems API efavirenz-MC.Conclusion. Solvent wetting technology is recommended for increasing the dissolution of practically insoluble APIs. The preferable mesoporous carriers are silica Parteck® SLC or synthetic magnesium aluminometasilicate Neusilin® US2.

Complex dispersions of poloxamers and mesoporous carriers with ibrutinib

Ibrutinib is an anticancer drug, a Bruton's tyrosine kinase inhibitor with poor solubility in aqueous media. This study reports on the study of the effectiveness of mesoporous carriers based on magnesium aluminometasilicate and poloxamers to improve the solubility and bioavailability of ibrutinib in the form of amorphous solid dispersions. The choice of the most effective composition was made on a parallel study of (a) a physical mixture of ibrutinib with a mesoporous carrier, (b) a solid dispersion with a poloxamer on a non-porous carrier, (c) a dispersion with a poloxamer deposited on a mesoporous carrier. Sample mixtures and dispersions with ibrutinib were tested to establish amorphism by various methods and to determine the solubility in aqueous media. The composition of ibrutinib-poloxamer P407-mesoporous carrier showed the best results in three standard media regarding the solubility of ibrutinib (increase in solubility at pH 1.2 - 129.6%, pH 4.5 - 300.2%, pH 6.8 - 363.3%). This composition became the basis for the tablet formulation and showed the best results in the Dissolution test (the dosage was dissolved in only 10 min of the test in pH 1.2 medium by 98.3%, pH 4.5 - 95.4%, pH 6.8 – 57.3%). These results were superior to those of the original Imbruvica capsules at all points in the study. In conclusion, the resulting formulation was stable under accelerated conditions according to the ICH Q1 Quality Guideline (40 °C, 75% relative humidity, 6 months).

Optimization of Naringin and Naringenin Extraction from Citrus × paradisi L. Using Hydrolysis and Excipients as Adsorbent.

While flavanones exist in a variety of chemical forms, their favorable health effects are most prominent in their free form—aglycones. Their concentrations in grapefruit (Citrus × paradisi L.) extracts vary according to the extraction and hydrolysis methods used. The primary aim of this work was to maximize the yields of naringin and naringenin from various parts of fresh grapefruit fruits (flavedo, albedo, and segmental) using different extraction and hydrolysis methods. In addition, we aimed to evaluate the excipient—magnesium aluminometasilicate—and determine its influence on the qualitative composition of grapefruit extracts. Extracts were obtained by heat reflux extraction (HRE), ultrasound-assisted extraction with an ultrasonic homogenizer (UAE*), and ultrasound-assisted extraction with a bath (UAE). Ultrasound-assisted extraction using a bath (UAE) was modulated using acidic, thermal, and alkaline hydrolysis. The highest yield of naringin 8A (17.45 ± 0.872 mg/g) was obtained from an albedo sample under optimal conditions using ultrasound-assisted extraction; a high yield of naringenin 23-SHR (35.80 ± 1.79 µg/g) was produced using the heat reflux method from the segmental part. Meanwhile, ultrasonic combined with thermal hydrolysis significantly increased flavanone extraction from the albedo and segmental parts: naringin from sample 9-A (from 17.45 ± 0.872 mg/g to 25.05 ± 1.25 mg/g) and naringenin from sample 15-S (from 0 to 4.21 ± 0.55 µg/g). Additionally, magnesium aluminometasilicate demonstrated significant increases of naringenin from all treated grapefruit parts. To our knowledge, this is the first report of magnesium aluminometasilicate used as an adsorbent in flavanone extractions.

Technology of Processing Plant Extracts Using an Aluminometasilicate Porous Carrier into a Solid Dosage Form.

A method of preparing tablets called liquisolid technique is currently emerging. In these formulations, an important role is played by porous carriers, which are the basic building blocks of liquisolid systems (LSSs). The most common are microcrystalline cellulose (MCC), magnesium aluminometasilicates, silica aerogels, mesoporous silicates, clays, etc. In this study, magnesium aluminometasilicate is used to prepare modified LSS formulations with plant extracts as model drugs dissolved in water (W) or ethanol (E). The modification involves drying tablets in a microwave (MW) and hot air dryer (HA) for a specified period. Powder blends and tablets were evaluated for physical properties, and their antioxidant activity (AA) was measured in a modified dissolution by ferric reducing antioxidant power assay (FRAP). PLS and ANOVA were used to compare tablets properties depending on the composition and technology. The experiment is based on a previous one, in which the plant extracts were processed into tablets using a similar method. Therefore, extending the study to include more plants and the robust statistical evaluation and comparison of the products was a procedure to justify the suitability of the presented method for a wide range of liquid plant extracts. As a result, we obtained tablets with excellent physical properties, including a short disintegration and dissolution, which is problematic in tableted extracts.

Exploration of Neusilin® US2 as an Acceptable Filler in HPMC Matrix Systems-Comparison of Pharmacopoeial and Dynamic Biorelevant Dissolution Study.

Modern pharmaceutical technology still seeks new excipients and investigates the further use in already known ones. An example is magnesium aluminometasilicate Neusilin® US2 (NEU), a commonly used inert filler with unique properties that are usable in various pharmaceutical fields of interest. We aimed to explore its application in hypromellose matrix systems (HPMC content 10–30%) compared to the traditionally used microcrystalline cellulose (MCC) PH 102. The properties of powder mixtures and directly compressed tablets containing individual fillers NEU or MCC, or their blend with ratios of 1.5:1, 1:1, and 0.5:1 were investigated. Besides the routine pharmaceutical testing, we have enriched the matrices’ evaluation with a biorelevant dynamic dissolution study and advanced statistical analysis. Under the USP apparatus 2 dissolution test, NEU, individually, did not provide advantages compared to MCC. The primary limitations were the burst effect increase followed by faster drug release at the 10–20% HPMC concentrations. However, the biorelevant dynamic dissolution study did not confirm these findings and showed similarities in dissolution profiles. It indicates the limitations of pharmacopoeial methods in matrix tablet development. Surprisingly, the NEU/MCC blend matrices at the same HPMC concentration showed technologically advantageous properties. Besides improved flowability, tablet hardness, and a positive impact on the in vitro drug dissolution profile toward zero-order kinetics, the USP 2 dissolution data of the samples N75M50 and N50M50 showed a similarity to those obtained from the dynamic biorelevant apparatus with multi-compartment structure. This finding demonstrates the more predictable in vivo behaviour of the developed matrix systems in human organisms.

Development and Evaluation of Extended Release Tacrolimus Tablets by Melt Granulation in Combination with Magnesium Alumino Metasilicate

To increase the effectiveness of tacrolimus, the present study sought to develop extended-release tablets. It is used to treat mild to severe atopic dermatitis as well as to prevent organ rejection after organ transplantation. Tacrolimus, on the other hand, has a poor bioavailability and a short half-life. The current research aims to create extended-release tacrolimus tablets by melting and granulating utilizing lipid and adsorbent materials to ensure excellent flow and a hypromellose matrix system to regulate release for 12 hr. Tacrolimus granules were prepared by melting with glyceryl behenate in rapid mixer granulator in the presence of polyethylene glycol followed by magnesium alumino metasilicate for adsorption purposes. Adsorbed granules were milled, sifted, and mixed with extra granular material such as hypromellose, lactose monohydrate and magnesium stearate. Granules were compressed to tablets using oval-shaped plain tooling. In vitro dissolution profile of solid dispersion and extended release tablets were investigated. Release profile of tablets and solid dispersion were improved by melt granulation due to the polymorphic form conversion of drug substance from crystalline to amorphous.Release kinetics of tacrolimus extended release tablets were fitted with zero order release with R2 value of 0.964, which designate constant release for 12 hr. Therefore, the present findings from the study revealed that the formulation was successfully prepared and showed extended release pattern over 12 hr.

Utilization of Pharmaceutical Technology Methods for the Development of Innovative Porous Metasilicate Pellets with a Very High Specific Surface Area for Chemical Warfare Agents Detection.

Pharmaceutical technology offers various dosage forms that can be applied interdisciplinary. One of them are spherical pellets which could be utilized as a carrier in emerging second-generation detection tubes. This detection system requires carriers with high specific surface area (SSA), which should allow better adsorption of toxic substances and detection reagents. In this study, a magnesium aluminometasilicate with high SSA was utilized along with various concentrations of volatile substances (menthol, camphor and ammonium bicarbonate) to increase further the carrier SSA after their sublimation. The samples were evaluated in terms of physicochemical parameters, their morphology was assessed by scanning electron microscopy, and the Brunauer–Emmett–Teller (BET) method was utilized to measure SSA. The samples were then impregnated with a detection reagent o-phenylenediamine-pyronine and tested with diphosgene. Only samples prepared using menthol or camphor were found to show red fluorescence under the UV light in addition to the eye-visible red-violet color. This allowed the detection of diphosgene/phosgene at a concentration of only 0.1 mg/m3 in the air for samples M20.0 and C20.0 with their SSA higher than 115 m2/g, thus exceeding the sensitivity of the first-generation DT-12 detection tube.

The importance of the coating material type and amount in the preparation of liquisolid systems based on magnesium aluminometasilicate carrier

Albeit the preparation of liquisolid systems represents an innovative approach to enhance the dissolution of poorly soluble drugs, their broader utilization is still limited mainly due to the problematic conversion of the liquid into freely flowing and readily compressible powder. Accordingly, the presented study aims to determine the optimal carrier/coating material ratio (R value) for formulations based on magnesium aluminometasilicate (NUS2) loaded with polyethylene glycol 400. Four commercially available colloidal silica were used as coating materials in nine different R values (range of 5 – 100). The obtained results suggested that the higher R value leads to the superior properties of powder mixtures, such as better flowability, as well as compacts with higher tensile strength and lower friability. Moreover, it was observed that the type of coating material impacts the properties of liquisolid systems due to the different arrangement of particles in the liquisolid mixture. To confirm the noted dependency of R value and coating material type, the one- and two-way ANOVA, linear regression and principal component analysis (PCA) techniques were performed. In addition, a comparison of results with the properties of loaded NUS2 itself revealed that LSS with sufficient properties may be prepared even without the coating material.

Novel Extraction Method Using Excipients to Enhance Yield of Genistein and Daidzein in Trifolium pratensis L.

Isoflavones can be found in different chemical forms, but the health beneficial effects mainly appear in their free forms—aglycones. Their yield in red clover (Trifolium pratensis L.) extracts differs due to different extraction and hydrolysis methodologies. The main aim of this study was to obtain the highest yields of daidzein and genistein from red clover blossoms through the various extraction and hydrolysis methods and to increase their quantities using additional excipients. Extracts were obtained by ultrasound-assisted, heat-reflux and maceration methods combining them with acidic, alkaline, and thermal hydrolysis. Using ultrasound-assisted extraction with optimal conditions and heat-reflux method highest yields of isoflavones were obtained in UTE510 (393.23 ± 19.66 µg/g daidzein and 171.57 ± 8.58 µg/g genistein); UTE530 (415.07 ± 20.75 µg/g daidzein and 150.57 ± 7.53 µg/g genistein) and HNE5 (432.30 ± 21.61 µg/g daidzein and 154.50 ± 7.72 µg/g genistein) samples. These conditions were used with excipients: magnesium aluminometasilicate, croscarmellose sodium, sodium carboxymethyl starch and vinylpyrrolidone-vinyl acetate copolymer. This is the first study reporting the ability of the vinylpyrrolidone-vinyl acetate copolymer to promote solubilization and availability of active compounds from a herbal extract, resulting in enhanced isoflavones yield. The results of the present study showing increased solubility and availability provided by the vinylpyrrolidone-vinyl acetate copolymer suggest that this preparation could in principle also reduce variability due to limited water solubility of isoflavones.

The method of random balance for studying the influence of excipients quantities on technological parameters of tablets based on Origanum vulgare L. dry extract

The aim. The aim of the research was to study the influence of excipients amount on the technological parameters of the compression mixture and tablets based on dry extract of Origanum vulgare L. herb using the method of random balance.&#x0D; Materials and methods. Objects of the study – Origanum vulgare L. herb dry extract, 8 excipients that have been studied at two quantitative levels. The tablets were prepared by direct compression method. The formulations were designed according to the method of random balance. The technological parameters of the compression mixture and tablets based on Origanum vulgare L. herb dry extract have been studied as a function of quantitative factors: silicon, magnesium carbonate basic, dioxide magnesium aluminometasilicate (Neusilin S1®), isomalt (GalenIQ™720), F-melt® Type C (co-spray dried excipients), sucralose, berry flavor and citric acid.&#x0D; Results and discussion. The increase in the amount of Neusilin S1®, GalenIQ™720 and F-melt®, and the decrease in the amount of magnesium carbonate basic and silicon dioxide improved the flowability expressed by the Hausner ratio. Results of bulk density and tapped density of the compression mixture depended on the quantities of GalenIQ™720 and F-melt®. All formulations of the prepared tablets had the rapid disintegration and ranging from 6 to 15 minutes. Resistance for crushing and friability tablets’ were improved with a decrease in the amount of silicon dioxide and increase in the amount of Neusilin S1®, F-melt® and sucralose. Higher resistance to moisture of tablets based on Origanum vulgare L. dry extract was obtained by using Neusilin S1®, F-melt® and sucralose on the upper levels.&#x0D; Conclusions. The tablets based on Origanum vulgare L. herb dry extract were successfully manufactured by direct compression method. The random balance method enabled us to identify the most significant quantitative factors to optimize their composition in the tablets based on the dry extract of Origanum vulgare L. herb.

Stress-Dependent Particle Interactions of Magnesium Aluminometasilicates as Their Performance Factor in Powder Flow and Compaction Applications.

In the pharmaceutical industry, silicates are commonly used excipients with different application possibilities. They are especially utilized as glidants in low concentrations, but they can be used in high concentrations as porous carriers and coating materials in oral solid drug delivery systems. The desirable formulations of such systems must exhibit good powder flow but also good compactibility, which brings opposing requirements on inter-particle interactions. Since magnesium aluminometasilicates (MAS) are known for their interesting flow behavior reported as “negative cohesivity” yet they can be used as binders for tablet compression, the objective of this experimental study was to investigate their particle interactions within a broad range of mechanical stress from several kPa to hundreds of MPa. Magnesium aluminometasilicate (Neusilin® US2 and Neusilin® S2)-microcrystalline cellulose (Avicel® PH102) physical powder mixtures with varying silicate concentrations were prepared and examined during their exposure to different pressures using powder rheology and compaction analysis. The results revealed that MAS particles retain their repulsive character and small contact surface area under normal conditions. If threshold pressure is applied, the destruction of MAS particles and formation of new surfaces leading to particle interactions are observed. The ability of MAS particles to form interactions intensifies with increasing pressure and their amount in a mixture. This “function switching” makes MAS suitable for use as multifunctional excipients since they can act as a glidant or a binder depending on the applied pressure.

Design and in vitro evaluation of solid SEDDS for breast cancer therapy

Lipid-based drug delivery systems have been used as a useful tool for the formulation of hydrophobic drugs giving us the opportunity to enhance permeation from biological membranes, protecting active ingredients from harsh in vivo environment, thus enhancing the bioavailability. Self-emulsifying drug delivery systems could be classified as one of lipid-based formulation strategies and their ability to provide a key solution to the solubility problems faced with most of the anticancer drugs, and ease of production, make them a popular choice. The use of SEDDS for the formulation of peptide-protein drugs to overcome in vivo stability problems comes from the protective effect of these formulations over enzymes in gastrointestinal tract and give us the opportunity to design an oral application platform. In this study, we used an anticancer peptide, LyP-1, with lymphatic targeting properties as model molecule for the solidification of SEDDS preconcentrates. As lyophilization and spray-drying techniques were used for the production of solid SEDDS, characterization studies were conducted to optimize the formulation parameters and evaluate the permeation enhancing effect of these novel formulations. The cell culture studies were utilized for the assessment of biocompatibility using Caco-2 cell line and anticancer properties were evaluated using MDA-MB-231 cell line. Solid SEDDS with droplet size under 250 nm were obtained with lyophilization and spray-drying method using mannitol and magnesium aluminometasilicate as adsorbents. The anticancer activity of solid SEDDS formulations containing LyP-1 peptide prepared with two different solidification method was shown using MDA-MB-231 cell line. The permeability enhancing effect of excipients used in SEDDS were observed in Caco-2 cell monolayer indicating the absorption enhancing potential of prepared formulations, especially for spray-dried powders.

The Solution Improvement of Quercetin Using Spontaneous Emulsification Systems

Quercetin has been used for health promotion for instance anti-bacterial, anti-inflammatory, anti-coagulative, antineoplastic and antioxidant. The poorly water-soluble quercetin has been a significant problem of bioavailability for oral administration. The objective of this study was to improve the quercetin solubility by spontaneous emulsion formulation (SEF). SEF was fabricated by dissolved quercetin in mixture of polyoxyl 35 castor oil, diethylene glycol monoethy ether, caprylic/capric glyceride. The solid-SEF was obtained by incorporation with solid carrier adsorbent (magnesium aluminometasilicate). The photon correlation spectroscopy was used to determine the emulsion size of diluted SEF and solid-SEF. The power X-ray diffraction and differential scanning calorimetry were also employed to elucidate the powder of solid-SEF compared with unmodified quercetin. The dissolution profiled at 120 min of unmodified quercetin, SEF and solid-SEF was about 2%, 77% and 89%, respectively.