European Pharmaceutical Journal Feed

Chemical Diversity and Chemotypic Variation of Mentha spicata Essential Oils from Different Regions of Iran

Mon, 12 Jan 2026 00:00:00 GMT

Aim This study investigated the chemical diversity of essential oils (EOs) extracted from eight Mentha spicata samples collected across different regions of Iran. Material and Methods Essential oils obtained by hydrodistillation were analyzed using gas chromatography mass spectrometry (GC-MS), and their compositional patterns were examined through principal component analysis (PCA). Results Essential oil yields ranged from 0.3% to 1.6% (v/w), consistent with previously reported values for Iranian mints. Oxygenated monoterpenes were the dominant constituents, with carvone, D-limonene, and 1,8-cineole as major compounds. PCA explained 94.47% of the total variance and revealed clear clustering of samples, indicating significant chemical differentiation among populations. Three chemotypic patterns were identified: (1) a carvone-limonene (spearmint-type) profile found in most samples, (2) a mixed carvone/carvone oxide type, and (3) a 1,8-cineole-rich type. Conclusion The chemical variation observed among Iranian M. spicata populations may result from both genetic diversity and environmental influences on essential oil biosynthesis. These findings expand the understanding of Iranian M. spicata chemotypic diversity and provide a basis for selecting desirable chemotypes for pharmaceutical, aromatic, and flavor applications.

40th Technology Days 11th and 12th September 2025 Bratislava: Book of abstracts

Mon, 24 Nov 2025 00:00:00 GMT

Preliminary in vitro investigation of docetaxel nanomedicines based on cetyl palmitate for inhibition of prostate cancer cells' growth

Fri, 07 Nov 2025 00:00:00 GMT

AimProstate cancer is a disease characterized by unusual uncontrolled growth and proliferation of prostate cells. Docetaxel (DTX) has been associated with reduction in tumor growth, progression, and metastasis. The purpose of this research is to develop nanomedicines of DTX and rubone with effective antitumor activity against prostate cancer cells. Materials and MethodsDTX solid lipid nanoparticles were formulated by solvent emulsification evaporation method with melting and injection using cetyl palmitate, phosphatidylcholine, Soluplus, Brij O10, and rubone while applying computer-aided techniques to validate the use of selected lipid matrix. DTX nanoparticles were evaluated for particle size and shape, zeta potential, stability, drug loading, entrapment efficiency, in vitro drug release, and permeation properties. The prostate cancer cells' viability and drug cytotoxicity were assessed using the 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide assay. ResultsThe formulated spherical drug-loaded nanoparticles had sizes and zeta potential as low as 125.77 ± 3.0 nm and −7.35 ± 2.2 mV, respectively. The in vitro drug released from the solid lipid nanoparticles showed up to 80% DTX released after drug entrapment and loading of around 80% and 10%, respectively. The optimized DTX nanomedicines increased the cytotoxicity of DTX since it limited the viability of the DU145 prostate cancer cell lines to less than 30%, which represents a 50% increase in cytotoxicity of DTX. ConclusionDTX entrapped in stable lipid-based matrices provided effective in vitro activities against prostate cancer cells.

Physicochemical Properties and Release Profiles of Lidocaine Hydrochloride in Microemulsion Gels

Fri, 07 Nov 2025 00:00:00 GMT

This study focuses on the development and characterization of microemulsion gel systems incorporating the model drug lidocaine. Microemulsions were prepared via the standard phase titration method using various oil phases, surfactants, and co-surfactants, with demineralized water as the aqueous component. The primary objective was to assess the physical properties of the resulting gels and compare their drug release profiles to conventional gel formulations. The study examined the impact of varying surfactant and co-surfactant types, as well as the presence of the active pharmaceutical ingredient, on gel characteristics. Physical properties were evaluated through texture analysis and rheological measurements, while drug release was determined using Franz diffusion cells. Results showed that while the physical properties of microemulsion gels remained largely consistent across formulations, significant differences were observed in lidocaine liberation, highlighting the potential of microemulsion gels to modulate drug release behavior.

Development of carboxymethyl tamarind gum-based composite hydrogel films for wound dressing applications

Fri, 07 Nov 2025 00:00:00 GMT

Carboxymethyl tamarind gum (CMTG) is an anionic polymer gaining attention for its potential in drug delivery applications. In the present study, composite hydrogel films composed of CMTG and flaxseed mucilage (FSM) were developed for wound dressing applications. According to previous reports, hydrogel films prepared using CMTG alone exhibited poor matrix integrity and limited swelling capacity. To overcome these limitations, FSM was incorporated due to its highly hydrophilic nature, excellent water-holding capacity, and superior swelling characteristics, which are expected to enhance the overall performance of the composite hydrogel films. The composite hydrogel films were prepared by using solvent casting method. The developed hydrogel films were evaluated for weight loss, thickness, carboxyl content, contact angle, and swelling. The hydrogel films were characterized by attenuated total reflectance–Fourier transform infrared (ATR–FTIR) and thermal analysis. The drug loading was initiated by using diffusion mechanism. The drug release was studied in Tris HCl buffer pH 7.4. The physicochemical properties of the hydrogel films, including weight loss, thickness, carboxyl content, and contact angle, were influenced by the concentrations of citric acid and FSM. The optimized films showed enhanced swelling capacity (up to 37.83 g/g), superior to CMTG-alone films. The films were hemocompatible and exhibited minimal protein adsorption (<0.5 %). In addition, they demonstrated favorable water vapor permeability and effectively resisted microbial penetration. Drug release studies with metronidazole revealed a non-Fickian diffusion mechanism. ATR–FTIR and thermogravimetric analyses confirmed crosslinking between CMTG and citric acid, along with entanglement of FSM polymeric chains within the hydrogel matrix. The CMTG–FSM composite hydrogel films offer enhanced performance and biocompatibility, making them promising candidates for wound dressing applications.

Formulation of stimuli-responsive gels containing silver complex with nicotinamide

Sun, 31 Aug 2025 00:00:00 GMT

The use of stimuli-responsive gels is increasingly widespread and includes almost all routes of administration. Their main property is the phase transition from sol to gel under the influence of physiological stimuli such as temperature, pH, ion presence, or enzymes. The aim of this formulation study was to prepare oral in situ gel containing silver complex with nicotinamide. We prepared formulations based on the thermosensitive polymer Pluronic® F-127 (15% w/w), methylcellulose (0.25% w/w), and various concentrations of the ion-sensitive polymer sodium alginate (0.2%–4% w/w). Various properties were evaluated, such as pH, injectability, critical sol–gel transition temperature of sols, gelation capacity, as well as dissolution profile and antimicrobial activity. We found that sodium alginate affects the critical sol–gel transition temperature of sols, and with higher concentrations, the sol–gel transition temperature decreases. At a 4% w/w sodium alginate concentration, the presence of calcium cations was necessary for gel formation. Sodium alginate also significantly influenced the viscosity of sols; higher concentrations led to more viscous sols. The most suitable formulation contained 4% sodium alginate and was used to incorporate silver complex with nicotinamide, a new potential antimicrobial agent. The drug release kinetics most closely correlated with the first-order kinetics, and the drug was released via Fickian diffusion. During antimicrobial activity testing, the formulation demonstrated higher efficacy against Pseudomonas aeruginosa compared to a commercial dental gel containing chlorhexidine gluconate, although this difference was not statistically significant. Overall, the chlorhexidine gel showed greater efficacy against most of the tested bacteria, while the antimicrobial in situ gel maintained a consistent moderate level of antimicrobial activity.

Antioxidant and Antibacterial Properties of Leaf and Root Extracts of Dipsacus fullonum

Sat, 16 Aug 2025 00:00:00 GMT

Dipsacus fullonum L. (teasel) is a traditional medicinal plant, known to be a supplement in the treatment of Lyme disease. However, its scientific evaluation remains limited. This study investigates the phytochemical composition, antioxidant capacity and antibacterial properties of D. fullonum leaf and root ethanolic extracts. Ultrasound-assisted extraction with 70% ethanol was performed, and the extracts were analysed for total polyphenols, tannins and hydroxycinnamic acids. Antioxidant activity was assessed using the DPPH radical scavenging method, while antibacterial activity was evaluated via the broth microdilution method against various bacterial reference strains. Results indicate that leaf extract contains higher levels of bioactive compounds and exhibits stronger antioxidant activity than root extract. A combination of both extracts showed an additive effect. The leaf extract displayed weak antibacterial activity against selected Gram-positive and Gram-negative bacteria, whereas the root extract demonstrated no antibacterial effects.

A comprehensive study of ground-roasted coffee beans from Coffea liberica as dipeptidyl peptidase IV inhibitors

Fri, 15 Aug 2025 00:00:00 GMT

Type 2 diabetes mellitus (T2DM), a degenerative disease characterized by insulin resistance, has been reported as a serious healthcare problem, especially in low-to-middle-income countries. Dipeptidyl peptidase IV (DPP4) inhibition is a potential solution to overcome T2DM-related problems. Liberica coffee (Coffea liberica) was reported to have several health benefits due to the bioactive compounds it contains, such as phenolics, flavonoids, and alkaloids. This study aimed to provide a comprehensive evaluation of ground-roasted coffee beans (GRCB) from C. liberica, including in vitro evaluation, metabolite fingerprinting using LC-HRMS, and authentication analysis using Fourier transform infrared (FTIR) spectroscopy combined with chemometric techniques. In vitro evaluation proved the inhibitory activity of GRCB solution (with a percentage inhibition of 92.09%), which was comparable to sitagliptin used as a positive control. Metabolite identification revealed the presence of caffeine and chlorogenic acid isomers, namely cryptochlorogenic acid and isochlorogenic acid, as potential markers for further investigation. Chemometric techniques, namely principal component analysis (PCA) and partial least squares-discriminant analysis (PLS-DA), were used to perform exploratory data analysis and authentication study, respectively. The PCA results generated the plot observation, capturing 99.4% of the total variance within the first two components. It also facilitated the functional group identification by evaluating wavenumbers as the variables in the model construction. An authentication study using PLS-DA was also carried out, and it successfully differentiated GRCB with the presence of starch as an adulterant with the area under the curve-receiver operating characteristic (AUC-ROC) outcome of 1.

Abstract Collection From the Second Conference of Therapeutic Drug Monitoring – TDM 2025

Mon, 09 Jun 2025 00:00:00 GMT

DOPC + OTAB + DNA Complexes – Effect of Ionic Strength and Surface Charge Density on DNA Condensation

Sun, 18 May 2025 00:00:00 GMT

The effect of ionic strength and surface charge density of the lipoplexes formed from the cationic surfactant octadecyltrimethylammonium bromide (OTAB) and the neutral phospholipid 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC) on DNA condensation was studied using fluorescence spectroscopy. The structure of lipoplexes was examined by small- and wide-angle X-ray scattering (SAXS/WAXS). The efficiency of DNA condensation was monitored by relative changes in the intensity of the emission of the fluorescence probe ethidium bromide (EtBr). A high OTAB/DNA charge ratio of 10:1 is required for efficient condensation at all ionic strengths. The increasing mole ratio of OTAB/DOPC supports DNA condensation, while the process is significantly hindered by a high ionic strength. Only ~55% of DNA was found to be condensed by OTAB/DOPC = 1 mol mol−1 complexes in 150 mmol l−1 of NaCl. A condensed fluid lamellar phase (Lαc) was detected in the DOPC + OTAB + DNA complexes. The SAXS patterns show regular DNA–DNA packing only in complexes prepared in a medium of low ionic strength (<50 mmol l−1). Interestingly, free DNA in the supernatant of DOPC + OTAB + DNA complexes was not detected by UV/Vis spectrometry, indicating its trapping in the lipoplexes.

Comparative analysis of PLGA ocuserts of brimonidine tartrate prepared with different methods

Sat, 17 May 2025 00:00:00 GMT

The eye is a highly sensitive organ with multiple physiological barriers that limit drug bioavailability and reduce patient compliance. Research studies are still going on to discover a novel drug delivery system for ocular delivery. The current research aims to develop and compare the PLGA ocuserts of brimonidine tartrate (BT) by different methods. These BT-loaded PLGA ocuserts offer a promising alternative to commercially available BT eye drops. Ocuserts could significantly minimize the challenges encountered with eye drops like lacrimation, blinking-induced washout, dosing frequency, penetration, stability, and controlled release issues. The BT-loaded PLGA ocuserts were prepared using two methods: solvent casting method (SCM) and glass substrate method (GSM). Both SCM and GSM formulations exhibited smooth texture, pH levels within the range of 6.88±0.24 to 6.90±0.28, uniform thickness (SCM: 0.47±0.10 mm; GSM: 0.29±0.03 mm), minimal weight variation (SCM: 7.83±0.38 mg; GSM: 6.55±0.76 mg), sterility, and appropriate swelling indices (SCM: 6.69±0.33%; GSM: 5.40±0.27%). The evaluation results of SCM and GSM ocuserts revealed positive attributes for ophthalmic use. Noteworthy distinctions emerged in folding endurance, with SCM ocuserts demonstrating significantly higher endurance (87.17±4.34 folds) than GSM ocuserts (71.33±4.82 folds). Moreover, SCM ocuserts exhibited superior drug entrapment efficiency (88.26±3.33 %) to GSM ocuserts (74.91±4.39 %). Stability studies confirmed good stability over a 6-month period, while in vitro (italics) drug release study indicated better controlled release properties for SCM than GSM. Findings demonstrate that SCM emerged as an effective method for preparation of polymeric films in various pharmaceutical industries, including transdermal patches, scaffolds in tissue engineering, flexible wound healing films, biodegradable drug delivery systems, and pharmaceutical packaging as well.

Antibacterial Activity of Green Tea and Peppermint Extracts Against Enterococcus faecalis and the Potential of EGCG in Oral Health

Sat, 19 Apr 2025 00:00:00 GMT

Aim Enterococcus faecalis is a significant pathogen in endodontic infections, often leading to treatment failure in root canal therapy and contributing to chronic infections. The growing concern over antimicrobial resistance highlights the need for alternative treatment approaches. This study aims to evaluate the antibacterial properties of aqueous green tea (Camellia sinensis) and peppermint (Mentha × piperita) extracts, focusing on their phytochemical profiles and antibacterial activity against E. faecalis, a major pathogen in endodontic infections. Material and Methods Phytochemical analysis of green tea and peppermint extracts was conducted to determine the content of key compounds, including tannins, flavonoids, hydroxycinnamic acid derivatives, and total polyphenols. The antibacterial activity of green tea and peppermint extracts, as well as their key compounds, (–)-epigallocatechin gallate (EGCG), (–)-epicatechin, caffeic acid, and rosmarinic acid, was assessed using the broth dilution method to determine the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) against E. faecalis clinical strains. Results Green tea extract showed superior antibacterial activity (MIC/MBC 1.25–2.5/5–10 mg mL−1), with EGCG exhibiting the highest efficacy (MIC/MBC 0.25–0.5/1 mg mL−1). Peppermint extract demonstrated moderate antibacterial activity, with its active compounds, caffeic acid and rosmarinic acid, showing higher MIC/MBC values. A 1:1 mixture of both extracts demonstrated antagonistic effects, yielding higher MIC and MBC values compared to the individual extracts. Conclusions The results suggest that green tea, particularly EGCG, holds significant potential for oral health applications due to its strong antibacterial activity against E. faecalis. The findings indicate that green tea could contribute to the effective treatment of E. faecalis-related infections, although the combination of green tea and peppermint extracts may not provide additive benefits.

Characterization and Bioactivity of Silver Nanoparticles Synthesized from Melissa officinalis Extract: A Green Nanotechnology Approach

Tue, 15 Apr 2025 00:00:00 GMT

Silver nanoparticles (AgNPs) were synthesized via a green chemistry approach using Melissa officinalis aqueous extract as both a reducing and stabilizing agent. The formation of AgNPs was confirmed visually by a color change from light yellow to dark brown and spectroscopically by a distinct surface plasmon resonance band between 350 and 500 nm. The formulation containing 2 mM AgNO3 and 4% (v/v) extract at pH 8 and 37 °C exhibited optimal nanoparticle formation. Fourier transform infrared (FTIR) analysis revealed the presence of hydroxyl, carbonyl, and amine functional groups, indicating that phenolic and flavonoid compounds acted as reducing and capping agents. Dynamic light scattering (DLS) showed a broad hydrodynamic distribution, while scanning electron microscopy (SEM) confirmed that the primary nanoparticles were spherical with an average diameter of approximately 60 nm. X-ray diffraction (XRD) patterns indicated a face-centered cubic crystalline structure. Phytochemical analysis revealed a significant decrease in total phenolic and flavonoid contents following nanoparticle synthesis, confirming their involvement in the reduction and stabilization processes. Antioxidant assays (FRAP and DPPH) demonstrated that AgNPs retained or slightly enhanced activity compared to the crude extract, with FRAP values of 2.23 vs. 1.93 Eq/mg and DPPH inhibition of 86.72% vs. 78.31% at a concentration of 1 mg/mL. Antibacterial testing revealed selective activity against Staphylococcus aureus, with minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values of 8 µg/mL and 16 µg/mL, respectively. In contrast, only weak or no activity was observed against Escherichia coli and Proteus mirabilis. Cytotoxicity assays (MTT) on MCF-7 breast cancer cells showed that the M. officinalis extract exhibited greater anticancer activity (IC50 = 32 µg/mL) than the synthesized AgNPs, suggesting reduced bioavailability due to nanoparticle aggregation and lower cellular uptake. Overall, these findings demonstrate that M. officinalis-mediated AgNPs are spherical nanoscale particles (∼60 nm) with confirmed crystallinity, moderate stability, enhanced antioxidant activity, and selective antibacterial effects. Optimization of synthesis parameters could further improve their biomedical potential.

Effect of cisplatin on lipid peroxidation in the whole blood and plasma of female rats

Thu, 23 Jan 2025 00:00:00 GMT

AimCisplatin is known to induce oxidative stress and accumulation of reactive oxygen species (ROS), which are the primary causes of its undesirable side effects. Lipids are a major target of ROS undergoing oxidation upon interaction. Lipid peroxidation products are unstable and degrade into reactive compounds that can damage various biomolecules. Induction of oxidative stress and ROS formation is considered another mechanism of action of cisplatin. This article aims to investigate the effect of cisplatin on lipid peroxidation and the activity of the antioxidant enzyme catalase in whole blood and plasma. Materials and MethodsThe amount of lipid peroxidation products in blood and plasma of rats was determined by absorption of monochromatic ultraviolet light following extraction with a heptane–isopropyl alcohol mixture. The oxidative stress marker malondialdehyde (MDA) in blood and plasma was quantified using the thiobarbituric acid assay. Catalase activity in blood plasma of female rats was assessed using the ammonium molybdate method. ResultsThe data show that cisplatin induces significant changes in the levels of lipid peroxidation products, including conjugated dienes and trienes, in both whole blood and plasma of female rats. The oxidation index values calculated for lipid peroxidation products increased to varying degrees following cisplatin exposure. A dramatic increase in MDA concentration was observed in both whole blood and plasma of rats after exposure to cisplatin. In addition, cisplatin exposure resulted in a 55% reduction in catalase activity. ConclusionsThe results demonstrate that cisplatin promotes oxidative stress, increases lipid peroxidation level, and reduces catalase activity in blood. These findings provide insights into the mechanisms by which cisplatin may exert its anticancer effects while also contributing to its side effects.

Synergistic Antiproliferative Effects of Chondroitin Sulfate and Fucoidan in Tumor-derived Spheroids: Insights From a 3D Cell Culture Approach

Mon, 20 Jan 2025 00:00:00 GMT

The aim of the study was to investigate the effects of chondroitin sulfate (CS) and fucoidan (F), as well as their combination (CS + F) on the growth and viability of spheroids derived from the non-tumor cell line NIH3T3 and the tumor cell line Hepa1c1c7 using a three-dimensional (3D) cell culture model. Spheroids were formed using the liquid overlay method and treated with different concentrations of substances. Flow cytometry was used to quantitatively assess the representation of live, apoptotic, necrotic, and dead cells in the spheroids after treatment. Spheroids from the non-tumor cell line NIH3T3 after treatment with CS and fucoidan were nontoxic to the cells. By light microscopy, we observed a significant proliferative effect in the case of CS and combination of fucoidan and CS (F + CS). On the contrary, in spheroids from the Hepa1c1c7 tumor cell line, after treatment with our compounds, the compounds, especially fucoidan and a combination of CS and fucoidan, showed antiproliferative effects, which confirms their synergistic antiproliferative effect. According to flow cytometry in non-tumor NIH3T3 spheroids, CS had the most significant effect on the proportion of viable cells, which confirmed its proliferative effect (66.43 ± 4.43%). In spheroids derived from the Hepa1c1c7 tumor cell line, flow cytometry revealed the highest number of dead cells in spheroids after treatment with a combination of CS and fucoidan (19.84 ± 5.80%). Based on our results, we can conclude that a combination of CS and fucoidan showed a synergistic antiproliferative effect on Hepa1c1c7 cell cultures. The 3D cell cultures provide a more physiologically relevant platform for drug testing, highlighting the importance of understanding cell–extracellular matrix interactions in cancer research.

Abstract Collection from the 10th Annual Meeting of the European Section of the International Academy of Cardiovascular Sciences

Sat, 21 Dec 2024 00:00:00 GMT

Bovine Lung Peptides after Trypsinolysis Reveal Anti-Exudative Activity

Wed, 04 Dec 2024 00:00:00 GMT

Enzymatic hydrolysates of proteins isolated from cow lungs are used as anti-inflammatory agents for the growth and regeneration of new tissues. Hydrolysates were observed to inhibit the production of free radicals in cells and have a high anti-exudative activity even in low doses. In this study, we established the anti-exudative activity of peptides of protein hydrolysates isolated from bovine lungs. The anti-exudative activity of the peptides sum was compared with acetylsalicylic acid (ASA) and prednisolone, and the dynamics of inflammation were studied by tumour formation using carrageenan and formalin. Between 1 h and 24 h after administration of the drug, the effect of the peptides sum showed a significantly better indicator than the rest of the means. In general, the anti-exudative activity of the peptides sum was 2–3 times higher than the rest of the preparations. Biochemical indicators of prednisolone and peptides sum in two doses of 10−6 μg/kg and 10−4 μg/kg were studied. As a result of the study, it was found that the peptides sum at 10−6 μg/kg dose enhanced alanine aminotransferase (ALT) activity by 17.1% compared to those resulting from prednisolone treatment. In C-reactive protein (CRP) and antistreptolysin O (ASO) indicators, 10−4 μg/kg dose showed high activity. The sum of isolated peptides reduced ALT and ASO levels. This study provides additional support for preparing anti-inflammatory means from the peptides sum isolated from bovine lungs.

Capillary Electrophoresis with Diode Array Detection for the Quantification of Triptorelin and Lanreotide in Pharmaceutical Quality Control: Development, Validation, Greenness and Practicality Evaluation

Sun, 01 Dec 2024 00:00:00 GMT

Aim Capillary electrophoresis (CE)-based methods hold significant potential for routine use in pharmaceutical quality control (QC) laboratories. Therefore, this study aimed to develop a novel, green, and simple hydrodynamically open-system capillary zone electrophoresis method with diode-array detection (CZE-DAD) for the simultaneous analysis of lanreotide and triptorelin in a single electrophoretic run and to objectively evaluate the analytical technique’s greenness and practicality for application in the pharmaceutical QC settings. Materials and Methods The two therapeutic peptides were analysed using a commercially available CZE-DAD analytical system. The separation process was optimised by changing the composition and concentration of the background electrolyte (BGE). The developed method was validated in accordance with the International Conference on Harmonisation (ICH) Q2(R1) guidelines, and Diphereline® (powdered form for injection, 0.1 mg of triptorelin acetate) was used as a real dosage form of triptorelin. Greenness and practicality were evaluated using Green Analytical Procedure Index (GAPI), Analytical GREEnness (AGREE), and Blue Applicability Grade Index (BAGI) metrics. Results The optimised method utilised 250 mmol/L formic acid as the BGE, achieving high separation efficiency and short migration times, where both the peptides were analysed in <5 min. The method showed excellent linearity (r2 > 0.99), precision (relative standard deviation [RSD] <7.1%), and accuracy (92.7%–113.6%). The limit of detection (LOD) and limit of quantification (LOQ) were determined to be 0.5 μg/mL and 2 μg/mL, respectively. The method was also found to be environmentally friendly, with high scores achieved in both the GAPI and AGREE assessments, while also being practical, with a BAGI score of >60. Conclusions The newly developed CZE-DAD method proved to be a reliable, efficient, and environmentally sustainable alternative to liquid chromatography (LC)-based methods for the analysis of lanreotide and triptorelin. The method’s acceptable validation parameters and favourable greenness and practicality scores support its high application potential in pharmaceutical QC laboratories.

In vitro mechanism of luteolin suppresses enhanced endothelial permeability

Thu, 26 Sep 2024 00:00:00 GMT

Luteolin, a flavonoid, has been reported to inhibit the enhanced endothelial permeability in vitro. The purpose of this study was to determine the mechanism of luteolin affected the in vitro suppression of elevated endothelial permeability involves protein kinase C activity and intracellular calcium concentration. The inducer bradykinin was tested using the in vitro vascular permeability assay in endothelial cells obtained from human umbilical vein endothelial cells (HUVECs). Protein kinase C assay test and the intracellular calcium concentration were also determined. Results revealed luteolin (5, 10, and 25 μM) significantly suppressed increased endothelial permeability (P < 0.001). The increased activity of protein kinase C was significantly suppressed by luteolin at the dose of 5 μM (P < 0.05), 10 μM (P < 0.01), and 25 μM (P < 0.01). The increased concentration of intracellular calcium was significantly suppressed by luteolin at the dose of 10 μM (P < 0.01) and 25 μM (P < 0.001). Collectively, these results showed luteolin suppressed the activity of protein kinase C and suppressed the increased concentration of intracellular calcium when HUVECs were induced by bradykinin, leading to the suppression of increased endothelial permeability as the nitric oxide-cyclic guanosine monophosphate (NO-cGMP ) pathway was being inactivated. This may explain the pharmacologic properties of luteolin, which is anti-inflammatory, antioxidant, and neuroprotective. These results also revealed the potential use of luteolin in treating many other diseases involve endothelial permeability.

Characterisation of the lipolytic enzymatic activities of fungal rizoenzymes from Rhizopus oryzae in comparison to pancreatin from pigs

Sat, 10 Aug 2024 00:00:00 GMT

Aim In case of exocrine pancreatic insufficiency (EPI), the replacement of digestive enzymes with, for example porcine pancreatin or fungal rizoenzymes, is unavoidable under certain conditions. Current guidelines indicate that preparations from porcine pancreas have more advantageous physicochemical properties compared to those from fungi, especially at high bile salt concentrations, and that the latter can, therefore, only be used clinically to a limited extent. Since rizoenzymes are increasingly used in clinical practice, the present in vitro study investigated efficiency of enzymatic activity of rizoenzymes in comparison to pancreatin under various physiological and partly extreme environmental conditions. Materials and Methods The lipolytic properties of two typical preparations containing digestive enzymes from porcine pancreatin and rizoenzymes were compared (same dosage of activity units) at different pH values (pH 3–9), with the addition of different bile salt concentrations (0–15 mmol/L sodium taurocholate). Lipolytic activity was measured by quantifying the fatty acids released from olive oil substrate by liquid chromatography–tandem mass spectrometry after enzymatic digestion. Results For both enzyme preparations, the lipolytic activity maximum was reached at pH 7 with comparable fatty acid conversion rates (57% pancreatin, 58% rizoenzymes). However, in contrast to pancreatin, rizoenzymes were already active for certain fatty acids from pH 3 to 4. At a bile salt concentration up to 10 mmol/L taurocholate, there was an increase in activity of both enzyme preparations (rizoenzymes 69% vs. pancreatin 58% enzymatic conversion). Only at rather unphysiological concentration of 15 mmol/L during EPI, there was a slight decrease in activity (to 56%) for the rizoenzymes. Conclusions Rizoenzymes are an alternative therapeutic option for EPI. Relevant differences between rizoenzymes and pancreatin with regard to lipolytic activity under different physicochemical conditions could not be demonstrated in this study, whereas a potential advantage in favor of rizoenzymes activity at already low pH values was observed.