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1.
Int J Mol Sci ; 25(13)2024 Jun 29.
Article in English | MEDLINE | ID: mdl-39000327

ABSTRACT

Microbial biofilms pose severe problems in the medical field and food industry, as they are the cause of many serious infections and food-borne diseases. The extreme biofilms' resistance to conventional anti-microbial treatments presents a major challenge to their elimination. In this study, the difference in resistance between Staphylococcus aureus DSMZ 12463 biofilms, biofilm-detached cells, and planktonic cells against microcapsules containing carvacrol was assessed. The antimicrobial/antibiofilm activity of low pH disinfection medium containing the microencapsulated carvacrol was also studied. In addition, the effect of low pH on the in vitro carvacrol release from microcapsules was investigated. The minimum inhibitory concentration of microencapsulated carvacrol was 0.625 mg mL-1. The results showed that biofilms exhibited greater resistance to microencapsulated carvacrol than the biofilm-detached cells and planktonic cells. Low pH treatment alone, by hydrochloric acid addition, showed no bactericidal effect on any of the three states of S. aureus strain. However, microencapsulated carvacrol was able to significantly reduce the planktonic cells and biofilm-detached cells below the detection limit (no bacterial counts), and the biofilm by approximatively 3 log CFU mL-1. In addition, results showed that microencapsulated carvacrol combined with low pH treatment reduced biofilm by more than 5 log CFU mL-1. Thus, the use of microencapsulated carvacrol in acidic environment could be a promising approach to combat biofilms from abiotic surfaces.


Subject(s)
Anti-Bacterial Agents , Biofilms , Cymenes , Microbial Sensitivity Tests , Staphylococcus aureus , Biofilms/drug effects , Staphylococcus aureus/drug effects , Staphylococcus aureus/physiology , Cymenes/pharmacology , Hydrogen-Ion Concentration , Anti-Bacterial Agents/pharmacology , Plankton/drug effects , Capsules , Drug Compounding/methods , Drug Resistance, Bacterial/drug effects
2.
Luminescence ; 39(7): e4824, 2024 Jul.
Article in English | MEDLINE | ID: mdl-39004773

ABSTRACT

Dabigatran (DBG), marketed as Pradaxa, is an anticoagulant medication prescribed for the treatment and mitigation of blood clots and to lower the risk of stroke in individuals with the heart condition known as atrial fibrillation. This medication is specifically indicated for preventing blood clots post hip or knee replacement surgeries and in patients with a prior history of clots. Compared to warfarin, dabigatran serves as a viable alternative that does not necessitate routine blood monitoring tests. The complimentary benefits associated with SALL (salting-out assisted liquid-liquid extraction) and the fluorogenic capabilities of benzofurazan. These methods were combined to provide an affordable and sensitive DBG assaying method. The spectral strength of the yellow luminous product was examined at 533.8 nm and by adjustment of a wavelength of 474.7 nm for excitation. To assess its linearity, the calibration chart was tested across a DBG concentration range of 30-500 ng/ml. Via accurate computation based on ICH, the detection limit (LD) was determined to be 9.5 ng/ml, and the strategy can quantify the DBG to a limit of 28 ng/ml. To ensure success, various crucial parameters for method implementation have been extensively studied and adapted. The validation of the strategy adhered to the policies outlined by ICH, affirming its precision in quantifying DBG in capsules. Furthermore, the inclusion of SALLE steps facilitated accurate monitoring of DBG in plasma samples, introducing a unique and advanced methodology for analyzing this compound in biological samples.


Subject(s)
Anticoagulants , Capsules , Dabigatran , Dabigatran/blood , Dabigatran/chemistry , Dabigatran/pharmacology , Humans , Anticoagulants/chemistry , Anticoagulants/blood , Anticoagulants/pharmacology , Fluorescent Dyes/chemistry , Liquid-Liquid Extraction , Spectrometry, Fluorescence , Limit of Detection , 4-Chloro-7-nitrobenzofurazan
3.
Drug Des Devel Ther ; 18: 2593-2608, 2024.
Article in English | MEDLINE | ID: mdl-38947224

ABSTRACT

Objective: To quantitatively assess all dosage forms of three active vitamin D and its analogs, namely, calcitriol, alfacalcidol, and eldecalcitol, to provide a basis for the selection of active vitamin D and its analogs in hospitals. Methods: In this study, three active vitamin D and its analogs were evaluated by quantitative scoring in five dimensions, including pharmaceutical properties (28 points), efficacy (27 points), safety (25 points), economy (10 points), and other attributes (10 points). Results: The final scores of quantitative assessment for the selection of alfacalcidol soft capsules, calcitriol soft capsules I, calcitriol soft capsules II, alfacalcidol tablets, alfacalcidol capsules, alfacalcidol oral drops, calcitriol injection, and eldecalcitol soft capsules were 73.17, 72.06, 71.52, 71.29, 69.62, 68.86, 65.60, 64.05 points. Conclusion: Based on the scoring results, alfacalcidol soft capsules, calcitriol soft capsules I, calcitriol soft capsules II, alfacalcidol tablets can be entered into the medication list of medical institutions as strongly recommended drugs. This study offers guidance on selecting and using active vitamin D and its analogs in hospitals, with consideration for the patient's needs.


Subject(s)
Hydroxycholecalciferols , Osteoporosis , Vitamin D , Humans , Osteoporosis/drug therapy , Vitamin D/administration & dosage , Vitamin D/analogs & derivatives , Hydroxycholecalciferols/administration & dosage , Hydroxycholecalciferols/therapeutic use , Technology Assessment, Biomedical , Bone Density Conservation Agents/administration & dosage , China , Calcitriol/analogs & derivatives , Calcitriol/administration & dosage , Capsules
4.
AAPS J ; 26(4): 82, 2024 Jul 12.
Article in English | MEDLINE | ID: mdl-38997548

ABSTRACT

Currently, Biopharmaceutics Classification System (BCS) classes I and III are the only biological exemptions of immediate-release solid oral dosage forms eligible for regulatory approval. However, through virtual bioequivalence (VBE) studies, BCS class II drugs may qualify for biological exemptions if reliable and validated modeling is used. Here, we sought to establish physiologically based pharmacokinetic (PBPK) models, in vitro-in vivo relationship (IVIVR), and VBE models for enteric-coated omeprazole capsules, to establish a clinically-relevant dissolution specification (CRDS) for screening BE and non-BE batches, and to ultimately develop evaluation criteria for generic omeprazole enteric-coated capsules. To establish omeprazole's IVIVR based on the PBPK model, we explored its in vitro dissolution conditions and then combined in vitro dissolution profile studies with in vivo clinical trials. The predicted omeprazole pharmacokinetics (PK) profiles and parameters closely matched the observed PK data. Based on the VBE results, the bioequivalence study of omeprazole enteric-coated capsules required at least 48 healthy Chinese subjects. Based on the CRDS, the capsules' in vitro dissolution should not be < 28%-54%, < 52%, or < 80% after two, three, and six hours, respectively. Failure to meet these dissolution criteria may result in non-bioequivalence. Here, PBPK modeling and IVIVR methods were used to bridge the in vitro dissolution of the drug with in vivo PK to establish the BE safety space of omeprazole enteric-coated capsules. The strategy used in this study can be applied in BE studies of other BCS II generics to obtain biological exemptions and accelerate drug development.


Subject(s)
Capsules , Drug Liberation , Models, Biological , Omeprazole , Therapeutic Equivalency , Omeprazole/pharmacokinetics , Omeprazole/administration & dosage , Omeprazole/chemistry , Humans , Male , Adult , Solubility , Young Adult , Administration, Oral , Proton Pump Inhibitors/pharmacokinetics , Proton Pump Inhibitors/administration & dosage , Proton Pump Inhibitors/chemistry , Female , Drugs, Generic/pharmacokinetics , Drugs, Generic/administration & dosage , Drugs, Generic/standards , Drugs, Generic/chemistry , Cross-Over Studies
5.
Int J Mol Sci ; 25(13)2024 Jun 28.
Article in English | MEDLINE | ID: mdl-39000223

ABSTRACT

Microparticles as a multicompartment drug delivery system are beneficial for poorly soluble drugs. Mucoadhesive polymers applied in microparticle technology prolong the contact of the drug with the mucosa surface enhancing drug bioavailability and extending drug activity. Sodium alginate (ALG) and hydroxypropyl methylcellulose (hypromellose, HPMC) are polymers of a natural or semi-synthetic origin, respectively. They are characterized by mucoadhesive properties and are applied in microparticle technology. Spray drying is a technology employed in microparticle preparation, consisting of the atomization of liquid in a stream of gas. In this study, the pharmaceutical properties of spray-dried ALG/HPMC microparticles with posaconazole were compared with the properties of physical mixtures of powders with equal qualitative and quantitative compositions. Posaconazole (POS) as a relatively novel antifungal was utilized as a model poorly water-soluble drug, and hard gelatin capsules were applied as a reservoir for designed formulations. A release study in 0.1 M HCl showed significantly prolonged POS release from microparticles compared to a mixture of powders. Such a relationship was not followed in simulated vaginal fluid (SVF). Microparticles were also characterized by stronger mucoadhesive properties, an increased swelling ratio, and prolonged residence time compared to physical mixtures of powders. The obtained results indicated that the pharmaceutical properties of hard gelatin capsules filled with microparticles were significantly different from hard gelatin capsules with mixtures of powders.


Subject(s)
Alginates , Capsules , Drug Delivery Systems , Gelatin , Hypromellose Derivatives , Triazoles , Alginates/chemistry , Gelatin/chemistry , Hypromellose Derivatives/chemistry , Drug Delivery Systems/methods , Triazoles/chemistry , Triazoles/administration & dosage , Triazoles/pharmacokinetics , Drug Liberation , Delayed-Action Preparations/chemistry , Antifungal Agents/administration & dosage , Antifungal Agents/chemistry , Antifungal Agents/pharmacokinetics , Microspheres
6.
Eur J Med Res ; 29(1): 367, 2024 Jul 16.
Article in English | MEDLINE | ID: mdl-39014507

ABSTRACT

BACKGROUND: Menopause, characterized by various physical and mental changes, is primarily caused by hormonal fluctuations, resulting in numerous complications. Recently, herbal treatments have gained significant attention for their minimal side effects compared to chemical drugs. This study aimed to investigate the effects of oral capsules containing Ocimum basilicum leaf extract (OBLE) on menopausal symptoms. METHODS: This placebo-controlled clinical trial study was conducted in 2020. The research focused on 60 menopausal women referred to Mashhad health centers. Eligible participants were administered either an OBLE 500 mg capsule or a placebo daily for 1 month. Menopause symptoms were evaluated using the Menopause Rating Scale (MRS) before, two weeks, and one month after the intervention. Data were analyzed using SPSS21, independent t, Mann-Whitney, and Friedman tests. A significance level of p < 0.05 was considered significant. RESULTS: The independent t-test indicated that the mean (SD) scores of menopausal symptoms in both the OBLE and placebo groups were initially similar before the intervention (P = 0.141). Two weeks after the intervention, the menopausal symptom scores were 9.5 ± 3.5 and 11.2 ± 5.6 in the OBLE and placebo groups, respectively (P = 0.163, df = 58, t = 1.4). After one month, the menopausal symptom scores were 6.9 ± 0.3 in the OBLE group and 11.26 ± 0.6 in the placebo group (P = 0.001, df = 58, t = 3.4). This indicates a significant difference between the two groups one month after the intervention, compared to before and two weeks after the intervention. Additionally, there was a significant difference in the scores of the physical and somato-vegetative dimension between the intervention and placebo groups two weeks and one month after the intervention (P < 0.05). CONCLUSION: The study results suggested that taking OBLE capsules led to a decrease in the scores of menopausal symptoms. This indicates that OBLE can be considered as a safe and cost-effective medicinal plant for alleviating menopausal symptoms among women.


Subject(s)
Capsules , Menopause , Ocimum basilicum , Plant Extracts , Plant Leaves , Humans , Female , Menopause/drug effects , Plant Extracts/pharmacology , Plant Extracts/administration & dosage , Middle Aged , Plant Leaves/chemistry , Ocimum basilicum/chemistry , Administration, Oral , Adult , Hot Flashes/drug therapy
7.
Phytomedicine ; 131: 155766, 2024 Aug.
Article in English | MEDLINE | ID: mdl-38865935

ABSTRACT

BACKGROUND: Migraine is widely recognized as the third most prevalent medical condition globally. Tianshu capsule (TSC), derived from "Da Chuan Xiong Fang" of the Jin dynasty, is integral in the clinical treatment of migraine. However, the chemical properties and therapeutic mechanisms of TSC different portions remain unclear. PURPOSE: This study was designed to investigate the effects of TSC different portions (including small molecular TSCP-SM and polysaccharides TSC-P) on migraine and explore the underlying mechanisms. STUDY DESIGN AND METHODS: First of all, migraine rats were established by nitroglycerin injection and treated with TSC, TSC-P, and TSC-SM. ELISA, qPCR, and immunofluorescence were used to evaluate the pharmacological effects on migraine rats. Secondly, UPLC-Q/TOF-MS and GC--MS were employed to detect the components of TSC-SM. PMP-HPLC, NMR, FT-IR, UV-Vis, AFM, and SEM were used for the chemical profiling of polysaccharides. Thirdly, the metabolic behavior profile of TSC-P was characterized by oral administrated fluorescence-labeled TSC-P and detected by NIRF imaging. Finally, the anti-migraine mechanisms were explored by determining the composition of gut microbiota, analyzing colonic short-chain fatty acids (SCFAs), and examining serum tryptophan-related metabolites. RESULTS: Both small molecules (45 volatiles and 114 small molecules) and polysaccharides (including Glc, Ara, Gal, and Gal A) have exhibited effectiveness in alleviating migraine, and this efficacy is associated with reduced CGRP and iNOS levels, along with increased ß-EP expressions. Further mechanistic exploration revealed that small-molecules exhibited effectiveness in migraine treatment by exerting antioxidative actions, while polysaccharides demonstrated superior therapeutic effects in regulating 5-HT levels. By monitoring the metabolic behavior of polysaccharides with fluorescent labeling, it was observed that TSC-P exhibited poor absorption. Instead, TSC-P demonstrated its therapeutic effects by modulating the aberrations in gut microbiota (including Alloprevotella, Muribaculaceae_ge, and Ruminococcaceae_UCG-005), cecum short-chain fatty acids (such as isobutyric, isovaleric, and valeric acids), and serum tryptophan-related metabolites (including indole-3-acetamide, tryptophol, and indole-3-propionic acid). CONCLUSION: This research provides innovative insights into chemical composition, metabolic behavior, and proposed anti-migraine mechanisms of TSC from a polarity-based perspective, and pioneering an exploration focused on the polysaccharide components within TSC for the first time.


Subject(s)
Drugs, Chinese Herbal , Migraine Disorders , Polysaccharides , Rats, Sprague-Dawley , Migraine Disorders/drug therapy , Animals , Male , Drugs, Chinese Herbal/pharmacology , Drugs, Chinese Herbal/chemistry , Rats , Polysaccharides/pharmacology , Polysaccharides/chemistry , Disease Models, Animal , Capsules
8.
J Agric Food Chem ; 72(23): 13240-13249, 2024 Jun 12.
Article in English | MEDLINE | ID: mdl-38825967

ABSTRACT

Acrolein (ACR), methylglyoxal (MGO), and glyoxal (GO) are a class of reactive carbonyl species (RCS), which play a crucial role in the pathogenesis of chronic and age-related diseases. Here, we explored a new RCS inhibitor (theanine, THE) and investigated its capture capacity on RCS in vivo by human experiments. After proving that theanine could efficiently capture ACR instead of MGO/GO by forming adducts under simulated physiological conditions, we further detected the ACR/MGO/GO adducts of theanine in the human urine samples after consumption of theanine capsules (200 and 400 mg) or green tea (4 cups, containing 200 mg of theanine) by using ultraperformance liquid chromatography-time-of-flight-high-resolution mass spectrometry. Quantitative assays revealed that THE-ACR, THE-2ACR-1, THE-MGO, and THE-GO were formed in a dose-dependent manner in the theanine capsule groups; the maximum value of the adducts of theanine was also tested. Furthermore, besides the RCS adducts of theanine, the RCS adducts of catechins could also be detected in the drinking tea group. Whereas, metabolite profile analysis showed that theanine could better capture RCS produced in the renal metabolic pathway than catechins. Our findings indicated that theanine could reduce RCS in the body in two ways: as a pure component or contained in tea leaves.


Subject(s)
Glutamates , Glyoxal , Pyruvaldehyde , Tea , Humans , Tea/chemistry , Glutamates/metabolism , Glutamates/analysis , Male , Pyruvaldehyde/metabolism , Pyruvaldehyde/chemistry , Glyoxal/metabolism , Glyoxal/chemistry , Adult , Acrolein/metabolism , Acrolein/chemistry , Capsules/chemistry , Camellia sinensis/chemistry , Camellia sinensis/metabolism , Female , Young Adult , Plant Extracts/chemistry , Plant Extracts/metabolism , Plant Extracts/administration & dosage , Chromatography, High Pressure Liquid
9.
Molecules ; 29(11)2024 May 31.
Article in English | MEDLINE | ID: mdl-38893474

ABSTRACT

Herbal medicine has been widely valued because of its remarkable efficacy and minimal side effects. The quantitative analysis of herbal medicines is essential to ensure their safety and efficacy. The simultaneous detection of multiple quality markers (Q-markers) has emerged as an important approach and trend in herbal medicine quality control. In recent years, non-targeted screening has become an effective strategy for the discovery and identification of unknown compounds. This study developed a non-targeted screening and quantitative analysis strategy to discover, identify and quantify the multiple components that truly represent the efficacy of Wuling capsule. Within this strategy, 18 types of flavonoids were tentatively discovered and identified from Wuling capsule by analyzing mass cleavage pathways, the precise molecular weights of compounds, and comparing the data with a database. Ten types of flavonoids were determined after the comparison of the standards. Additionally, following the evaluation of the regression equation, linear range, limit of detection (LOD), limit of quantitation (LOQ), precision, repeatability, and recovery of the proposed quantitative method, six flavonoids were quantified. This method successfully screened, identified, and quantified the potential active components in Wuling capsule, providing insights for improving the quality control standards in other herbal medicines.


Subject(s)
Drugs, Chinese Herbal , Flavonoids , Quality Control , Drugs, Chinese Herbal/chemistry , Drugs, Chinese Herbal/analysis , Drugs, Chinese Herbal/standards , Chromatography, High Pressure Liquid/methods , Flavonoids/analysis , Flavonoids/chemistry , Capsules , Tandem Mass Spectrometry/methods , Tandem Mass Spectrometry/standards , Limit of Detection , Reproducibility of Results
10.
Expert Rev Endocrinol Metab ; 19(4): 367-375, 2024 Jul.
Article in English | MEDLINE | ID: mdl-38842362

ABSTRACT

INTRODUCTION: Acromegaly is a rare endocrine disorder usually caused by a benign growth hormone‒secreting pituitary adenoma. Surgical adenoma resection is typically the first line of treatment, and medical therapy is used for patients with persistent disease following surgery, for adenoma recurrence, or for patients ineligible for, or declining, surgery. Approved somatostatin receptor ligands (SRLs) have been limited to injectable options, until recently. Oral octreotide capsules (OOC) are the first approved oral SRL for patients with acromegaly. AREAS COVERED: We review published reports and provide case study examples demonstrating practical considerations on the use of OOC. Using two hypothetical case scenarios, we discuss current treatment patterns, breakthrough symptoms and quality of life (QoL), efficacy of SRLs, OOC dose titration, evaluation of OOC treatment response, and incidence and management of adverse events. EXPERT OPINION: OOC are an option for patients with acromegaly including those who experience breakthrough symptoms, who have preference for oral therapies, or other reasons for declining injectable SRLs. OOC have been associated with improved patient-reported QoL measures compared with those reported for lanreotide and octreotide. Continued real-world experience will determine whether OOC, alone or in combination with other therapies, provides further advantages over current injectable acromegaly treatments.


Subject(s)
Acromegaly , Antineoplastic Agents, Hormonal , Octreotide , Quality of Life , Humans , Acromegaly/drug therapy , Octreotide/administration & dosage , Octreotide/therapeutic use , Octreotide/adverse effects , Administration, Oral , Antineoplastic Agents, Hormonal/administration & dosage , Antineoplastic Agents, Hormonal/therapeutic use , Antineoplastic Agents, Hormonal/adverse effects , Capsules , Adenoma/drug therapy , Growth Hormone-Secreting Pituitary Adenoma/drug therapy , Clinical Trials as Topic , Treatment Outcome
11.
Int J Biol Macromol ; 272(Pt 1): 132697, 2024 Jun.
Article in English | MEDLINE | ID: mdl-38843607

ABSTRACT

As a translucent functional gel with biodegradability, non-toxicity and acid resistance, gellan gum has been widely used in probiotic packaging, drug delivery, wound dressing, metal ion adsorption and other fields in recent years. Because of its remarkable gelation characteristics, gellan gum is suitable as the shell material of microcapsules to encapsulate functional substances, by which the functional components can improve stability and achieve delayed release. In recent years, many academically or commercially reliable products have rapidly emerged, but there is still a lack of relevant reports on in-depth research and systematic summaries regarding the process of microcapsule formation and its corresponding mechanisms. To address this challenge, this review focuses on the formation process and applications of gellan gum-based microcapsules, and details the commonly used preparation methods in microcapsule production. Additionally, it explores the impact of factors such as ion types, ion strength, temperature, pH, and others present in the solution on the performance of the microcapsules. On this basis, it summarizes and analyzes the prospects of gellan gum-based microcapsule products. The comprehensive insights from this review are expected to provide inspiration and design ideas for researchers.


Subject(s)
Capsules , Emulsions , Polysaccharides, Bacterial , Polysaccharides, Bacterial/chemistry , Capsules/chemistry , Emulsions/chemistry , Hydrogen-Ion Concentration , Temperature
12.
Molecules ; 29(12)2024 Jun 09.
Article in English | MEDLINE | ID: mdl-38930817

ABSTRACT

With the aim to obtain controlled-release systems and to preserve the antioxidant, immunomodulatory, and prebiotic activity of the bioactive compounds, microencapsulation of both honeydew honey and royal jelly into biopolymeric microparticles based on rye bran heteropolysaccharides (HPS) was successfully performed. Honeydew honey and royal jelly microcapsules were prepared by spray-drying method and were characterized in terms of morphology and biological properties. Due to the resistance of the obtained encapsulates to the acidic pH in the stomach and digestive enzymes, the microcapsules showed prebiotic properties positively influencing both the growth, retardation of the dying phase, and the pro-adhesive properties of probiotic bacteria, i.e., Bifidobacterium spp. and lactic acid bacteria. Moreover, as a result of fermentation of the microcapsules of bee products in the lumen of the large intestine, an increased synthesis of short-chain fatty acids, i.e., butyric acid, was found on average by 39.2% in relation to the SCFA concentrations obtained as a result of fermentation of native bee products, thus opening new perspectives for the exploitation of honeydew honey and royal jelly loaded microcapsules for nutraceutical applications.


Subject(s)
Capsules , Gastrointestinal Microbiome , Honey , Prebiotics , Animals , Gastrointestinal Microbiome/drug effects , Bees , Fatty Acids, Volatile/metabolism , Bifidobacterium/growth & development , Bifidobacterium/metabolism , Fermentation , Probiotics , Fatty Acids
13.
Arch Oral Biol ; 165: 106016, 2024 Sep.
Article in English | MEDLINE | ID: mdl-38838515

ABSTRACT

OBJECTIVES: To evaluate in vivo 1) the bioavailability of trans-resveratrol when administered through sublingual capsules; 2) the effect of resveratrol on the protein composition of the acquired enamel pellicle (AEP). DESIGN: Ten volunteers received a sublingual capsule containing 50 mg of trans-resveratrol. Unstimulated saliva was then collected after 0, 30, 60, and 120 min and AEP was collected after 120 min following administration of the capsule. In the next week, the volunteers received a placebo sublingual capsule, and saliva and AEP were collected again. Saliva samples were analyzed for free trans-resveratrol using high-performance liquid chromatopgraphy (HPLC), and AEP samples were subjected to proteomic analysis (nLC-ESI-MS/MS). RESULTS: Trans-resveratrol was detected in saliva at all the time points evaluated, with the peak at 30 min. A total of 242 proteins were identified in both groups. Ninety-six proteins were increased and 23 proteins were decreased in the Resveratrol group. Among the up-regulated proteins, isoforms of cystatins, PRPs, Mucin-7, Histatin-1, Lactotrasnferrin and Lysozyme-C were increased and the isoforms of Protein S100, Neutrophil defensins, Albumin, PRPs, and, Statherin were decreased in Resveratrol group. CONCLUSION: The sublingual capsule is effective at increasing the bioavailability of trans-resveratrol in saliva. Several proteins involved in important processes to maintain systemic and oral health homeostasis were identified. These proteins differently expressed due to the presence of trans-resveratrol deserve attention for future studies, since they have important functions, mainly related to antimicrobial action.


Subject(s)
Capsules , Dental Pellicle , Resveratrol , Saliva , Humans , Resveratrol/pharmacology , Resveratrol/pharmacokinetics , Resveratrol/administration & dosage , Saliva/metabolism , Saliva/chemistry , Male , Adult , Dental Pellicle/metabolism , Dental Pellicle/chemistry , Chromatography, High Pressure Liquid , Female , Biological Availability , Stilbenes/pharmacokinetics , Stilbenes/pharmacology , Stilbenes/administration & dosage , Proteomics , Tandem Mass Spectrometry , Salivary Proteins and Peptides/metabolism
14.
Sci Rep ; 14(1): 14802, 2024 06 26.
Article in English | MEDLINE | ID: mdl-38926468

ABSTRACT

Long-chain polyunsaturated fatty acids (LCPUFA) are of interest due to their potential health properties and have a significant role in reducing the risk of various chronic diseases in humans. It is commonly used as a supplement. However, lipid oxidation is an important negative factor caused by environmental, processing, and limited water solubility of LCPUFA, making them difficult to incorporate into food products. The objective of this research work was to prevent oxidation, extend shelf life, enhance the stability of fatty acids, and to achieve controlled release by preparing spray-dried powder (SDM). For spray-drying, aqueous emulsion blends were formulated using a 1:1 ratio of chia seed oil (CSO) and fish oil (FO) and using a laboratory-scale spray-dryer with varying conditions: inlet air temperature (IAT, 125-185 °C), wall material (WM, 5-25%), pump speed (PS, 3-7 mL/min), and needle speed (NS, 3-11 s). The maximum alpha-linolenic acid (ALA) content was 33 ± 1%. The highest values of eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) in the microcapsules were 8.4 ± 0.4 and 13 ± 1%, respectively. Fourier transform infrared and X-Ray diffraction analysis results indicated that SDM was successfully formulated with Gum Arabic and maltodextrin (MD). The blending without encapsulation of CSO and FO was digested more efficiently and resulted in more oil being released with simulated gastric fluid (SGF), simulated intestinal fluid (SIF), and SGF + SIF conditions without heating. No significant changes were observed for saturated, monounsaturated, and LCPUFA, whether exposed or not to gastrointestinal conditions. However, compared to the release of SDM, it can be useful for designing delivery systems for the controlled release of essential fatty acids.


Subject(s)
Capsules , Fish Oils , Spray Drying , Fish Oils/chemistry , Plant Oils/chemistry , Salvia/chemistry , Fatty Acids/chemistry , Humans
15.
J Ethnopharmacol ; 333: 118510, 2024 Oct 28.
Article in English | MEDLINE | ID: mdl-38945468

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Pain and inflammation are the most frequent reasons for which people seek medical care. Currently available analgesics against these conditions produce fatal adverse effects. NPK 500 capsules is an alternative herbal analgesic employed to treat dysmenorrhea, peptic ulcer and pain. NPK 500 is produced from Cassia sieberiana. A plant used in traditional medicine to treat pain and inflammation. AIM OF THE STUDY: This study reports the analysis, phytochemical characterization and mechanism of analgesic and anti-inflammatory activities of two NPK 500 capsules, called old and new NPK500 capsules (ONPK500 and NNPK500) respectively. MATERIALS AND METHODS: Physicochemical, organoleptic, GC-MS and LC-MS methods were employed to analyze the NPK 500 capsules. Analgesic activity was evaluated using tail immersion, Randall-Selitto and acetic acid induced writing tests. Anti-inflammatory activity was evaluated using carrageenan-induced rat paw inflammation. Additionally, pro-inflammatory mediators such as prostaglandin E2 (PGE2), inducible nitric oxide synthase (iNOS), cyclooxygenase 1 and 2 (COX-2 and COX-1) were quantified in the sera of the rats using Enzyme Linked Immunosorbent Assay (ELISA) kits. RESULTS: Thirteen major compounds were characterized in the NNPK 500 capsules via the GC-MS and LC-MS spectroscopies. Kaempferol was the major compound characterized in addition to physcion, ß-sitosterol 3-O-ß-D-glucopyranoside, betulinic acid and nine others. Physicochemical and organoleptic indices of the capsules were also derived for its authentication and quality control. Furthermore, NNPK 500 0.5-1.5 mg/kg p.o. produce significant (P < 0.5) analgesic activity (160-197%) higher than that of ONPK500 (109.8%) and Morphine (101%) in the tail immersion test. The analgesic activity of NNPK 500 0.5-1.5 mg/kg p.o. (171.0-258.3%) and ONPK 500 (179.5%) were also significant (P < 0.01) and higher than that of Aspirin (103.00%) in the Randall-Selitto test. Both capsules also demonstrated significant (P < 0.5) analgesic and anti-inflammatory activities in the acetic acid-induced writhing and carrageenan-indued paw edema tests respectively. The two NPK500 capsules also, significantly (P < 0.5) inhibited PGE2 and iNOS but not COX-2 and COX-1 in the carrageenan-indued paw edema test. CONCLUSION: These results show that NNPK 500 and ONPK 500 capsules possessed potent analgesic and anti-inflammatory activities via inhibition of PGE2 and iNOS as a result of their chemical constituents. NPK500 capsules thus, relief acute pain and inflammation without causing gastrointestinal, renal or hepatic injuries, since they did not inhibit COX-1.


Subject(s)
Analgesics , Anti-Inflammatory Agents , Cassia , Dinoprostone , Dysmenorrhea , Nitric Oxide Synthase Type II , Animals , Dinoprostone/metabolism , Anti-Inflammatory Agents/pharmacology , Anti-Inflammatory Agents/therapeutic use , Nitric Oxide Synthase Type II/metabolism , Analgesics/pharmacology , Analgesics/therapeutic use , Analgesics/chemistry , Female , Cassia/chemistry , Dysmenorrhea/drug therapy , Dysmenorrhea/chemically induced , Rats , Plant Extracts/pharmacology , Plant Extracts/chemistry , Plant Extracts/therapeutic use , Carrageenan , Capsules , Mice , Edema/drug therapy , Edema/chemically induced , Male , Rats, Sprague-Dawley , Cyclooxygenase 2/metabolism
16.
Nanotechnology ; 35(36)2024 Jun 20.
Article in English | MEDLINE | ID: mdl-38861959

ABSTRACT

Here we report the liquid-solid interaction in droplet-based triboelectric nanogenerators (TENG) for estimation of human Na+/K+levels. The exploitation of PVDF-HFP encapsulated WS2as active layer in the droplet-based TENG (DTENG) leads to the generation of electrical signal during the impact of water droplet. Comparison over the control devices indicates that surface quality and dielectric nature of the PVDF-HFP/WS2composite largely dictates the performance of the DTENG. The demonstration of excellent sensitivity of the DTENG towards water quality indicates its promising application towards water testing. In addition, the alteration in output signal with slightest variation in ionic concentration (Na+or K+) in water has been witnessed and is interpreted with charge transfer and ion transfer processes during liquid-solid interaction. The study reveals that the ion mobility largely affects the ion adsorption process on the active layer of PVDF-HFP/WS2and thus generates distinct output profiles for diverse ions like Na+and K+. Following that, the DTENG characteristics have been exploited to artificial urine where the varying output signals have been recorded for variation in urinary Na+ion concentration. Therefore, the deployment of PVDF-HFP/WS2in DTENG holds promising application towards the analyse of ionic characteristics of body fluids.


Subject(s)
Nanostructures , Fluorocarbon Polymers/chemistry , Polyvinyls/chemistry , Nanostructures/chemistry , Capsules , Tungsten Compounds/chemistry , Sulfides/chemistry , Electricity , Potassium/chemistry , Ions/chemistry , Chlorine/chemistry
17.
Eur Phys J E Soft Matter ; 47(6): 37, 2024 Jun 03.
Article in English | MEDLINE | ID: mdl-38829453

ABSTRACT

In this study, we demonstrate the fabrication of polymersomes, protein-blended polymersomes, and polymeric microcapsules using droplet microfluidics. Polymersomes with uniform, single bilayers and controlled diameters are assembled from water-in-oil-in-water double-emulsion droplets. This technique relies on adjusting the interfacial energies of the droplet to completely separate the polymer-stabilized inner core from the oil shell. Protein-blended polymersomes are prepared by dissolving protein in the inner and outer phases of polymer-stabilized droplets. Cell-sized polymeric microcapsules are assembled by size reduction in the inner core through osmosis followed by evaporation of the middle phase. All methods are developed and validated using the same glass-capillary microfluidic apparatus. This integrative approach not only demonstrates the versatility of our setup, but also holds significant promise for standardizing and customizing the production of polymer-based artificial cells.


Subject(s)
Artificial Cells , Polymers , Artificial Cells/chemistry , Polymers/chemistry , Polymers/chemical synthesis , Emulsions/chemistry , Capsules/chemistry , Microfluidics/methods , Water/chemistry , Microfluidic Analytical Techniques , Proteins/chemistry
18.
Article in English | MEDLINE | ID: mdl-38889492

ABSTRACT

Chuanwang xiaoyan capsules (CWXYC) have anti-inflammatory and detoxification effect, are used in the treatment of acute and chronic tonsillitis, pharyngitis and other inflammation-related diseases clinically. However, the anti-inflammatory mechanisms have not been elucidated. This study aimed to investigate the anti-inflammatory mechanisms of CWXYC using cell metabolomics and network pharmacology strategy. Specifically, CWXYC could efficiently reduce the content of nitric oxide (NO), the cytokines Interleukin-6 (IL-6) and tumor necrosis factor alpha (TNF-α) in LPS-induced RAW264.7 cells. Furthermore, metabolomics was performed to achieve 23 differential metabolites and 9 metabolic pathways containing glutamate metabolism, glutathione metabolism, arginine and proline metabolism, urea cycle, malate-aspartate shuttle, phosphatidylcholine biosynthesis, transfer of acetyl groups into mitochondria, cysteine metabolism and ammonia recycling. The results of network pharmacology showed that CWXYC could treat inflammation through 10 active components, 10 key targets and 55 pathways. Then the results of molecular docking also approved that there existed strong binding energy between the active components and the key targets. Finally, metabolomics and network pharmacology were integrated to get core targets AKT1, SRC and EGFR. Western blot experiments verified that CWXYC could exert anti-inflammatory effect by down-regulating the activated Akt1 and Src proteins. This study demonstrated that CWXYC exerted effects against inflammation, and the potential mechanisms were elucidated. These novel findings will provide an important basis for further mechanism investigations.


Subject(s)
Anti-Inflammatory Agents , Drugs, Chinese Herbal , Metabolomics , Network Pharmacology , Mice , Animals , Drugs, Chinese Herbal/pharmacology , Drugs, Chinese Herbal/chemistry , Metabolomics/methods , Anti-Inflammatory Agents/pharmacology , Anti-Inflammatory Agents/chemistry , RAW 264.7 Cells , Molecular Docking Simulation , Metabolome/drug effects , Nitric Oxide/metabolism , Capsules , Interleukin-6/metabolism
19.
Int J Biol Macromol ; 273(Pt 2): 132944, 2024 Jul.
Article in English | MEDLINE | ID: mdl-38851616

ABSTRACT

Lignin-based microcapsules are extremely attractive for their biodegradability and photolysis resistance. However, the water-soluble all-lignin shells were unsatisfactory in terms of rainfall and foliar retention, and lacked the test of agricultural production practices. Herein, a novel microcapsule based on a flexible skeleton formed by interfacial polymerization and absorbed with lignin particles (LPMCs) was prepared in this study. Further analysis demonstrated that the shell was formed by cross-linking the two materials in layers and showed excellent flexibility and photolysis resistance. The pesticide loaded LPMCs showed about 98.68 % and 73.00 % improvement in scour resistance and photolysis resistance, respectively, as compared to the bare active ingredient. The foliar retention performance of LPMCs was tested in peanut plantations during the rainy season. LPMCs loaded with pyraclostrobin (Pyr) and tebuconazole (Teb) exhibited the best foliar disease control and optimum plant architecture, resulting in an increase in yield of about 5.36 %. LPMCs have a promising application prospect in the efficient pesticide utilization, by controlling its deformation, adhesion and release, an effective strategy for controlling diseases and managing plant growth was developed.


Subject(s)
Capsules , Lignin , Plant Leaves , Lignin/chemistry , Plant Leaves/chemistry , Strobilurins/chemistry , Ultraviolet Rays , Triazoles/chemistry , Photolysis , Arachis/chemistry , Pesticides/chemistry
20.
Int J Biol Macromol ; 273(Pt 1): 133031, 2024 Jul.
Article in English | MEDLINE | ID: mdl-38866283

ABSTRACT

This research focuses on the challenges of efficiently constructing drug carriers and evaluating their dynamic release in vitro simulation. By using pickering emulsion and layer-by-layer self-assembly methods. The microcapsules had tea tree oil as the core material, SiO2 nanoparticles as stabilizers, and chitosan and hyaluronic acid as shell materials. The microencapsulation mechanism, as well as the effects of core-shell mass ratio and stirring, were discussed. Specifically, a dynamic circulation simulation microchannel system was designed and manufactured based on 3D printing technology. In this simulation system, the release rate of microcapsules is accelerated and the trend changes, with its behavior aligning with the Boltzmann model. The study demonstrates the advantages of self-assembled inorganic-organic drug-loaded microcapsules in terms of controllable fabrication and ease of functional modification, and shows the potential of 3D printed cyclic microchannel systems in terms of operability and simulation fidelity in drug and physiological analysis.


Subject(s)
Capsules , Chitosan , Drug Liberation , Hyaluronic Acid , Printing, Three-Dimensional , Chitosan/chemistry , Hyaluronic Acid/chemistry , Drug Carriers/chemistry
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