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1.
Drug Des Devel Ther ; 18: 2593-2608, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38947224

RESUMO

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.


Assuntos
Hidroxicolecalciferóis , Osteoporose , Vitamina D , Humanos , Osteoporose/tratamento farmacológico , Vitamina D/administração & dosagem , Vitamina D/análogos & derivados , Hidroxicolecalciferóis/administração & dosagem , Hidroxicolecalciferóis/uso terapêutico , Avaliação da Tecnologia Biomédica , Conservadores da Densidade Óssea/administração & dosagem , China , Calcitriol/análogos & derivados , Calcitriol/administração & dosagem , Cápsulas
2.
Luminescence ; 39(7): e4824, 2024 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-39004773

RESUMO

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.


Assuntos
Anticoagulantes , Cápsulas , Dabigatrana , Dabigatrana/sangue , Dabigatrana/química , Dabigatrana/farmacologia , Humanos , Anticoagulantes/química , Anticoagulantes/sangue , Anticoagulantes/farmacologia , Corantes Fluorescentes/química , Extração Líquido-Líquido , Espectrometria de Fluorescência , Limite de Detecção , 4-Cloro-7-nitrobenzofurazano
3.
Int J Mol Sci ; 25(13)2024 Jun 28.
Artigo em Inglês | MEDLINE | ID: mdl-39000223

RESUMO

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.


Assuntos
Alginatos , Cápsulas , Sistemas de Liberação de Medicamentos , Gelatina , Derivados da Hipromelose , Triazóis , Alginatos/química , Gelatina/química , Derivados da Hipromelose/química , Sistemas de Liberação de Medicamentos/métodos , Triazóis/química , Triazóis/administração & dosagem , Triazóis/farmacocinética , Liberação Controlada de Fármacos , Preparações de Ação Retardada/química , Antifúngicos/administração & dosagem , Antifúngicos/química , Antifúngicos/farmacocinética , Microesferas
4.
Int J Mol Sci ; 25(13)2024 Jun 29.
Artigo em Inglês | MEDLINE | ID: mdl-39000327

RESUMO

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.


Assuntos
Antibacterianos , Biofilmes , Cimenos , Testes de Sensibilidade Microbiana , Staphylococcus aureus , Biofilmes/efeitos dos fármacos , Staphylococcus aureus/efeitos dos fármacos , Staphylococcus aureus/fisiologia , Cimenos/farmacologia , Concentração de Íons de Hidrogênio , Antibacterianos/farmacologia , Plâncton/efeitos dos fármacos , Cápsulas , Composição de Medicamentos/métodos , Farmacorresistência Bacteriana/efeitos dos fármacos
5.
AAPS J ; 26(4): 82, 2024 Jul 12.
Artigo em Inglês | MEDLINE | ID: mdl-38997548

RESUMO

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.


Assuntos
Cápsulas , Liberação Controlada de Fármacos , Modelos Biológicos , Omeprazol , Equivalência Terapêutica , Omeprazol/farmacocinética , Omeprazol/administração & dosagem , Omeprazol/química , Humanos , Masculino , Adulto , Solubilidade , Adulto Jovem , Administração Oral , Inibidores da Bomba de Prótons/farmacocinética , Inibidores da Bomba de Prótons/administração & dosagem , Inibidores da Bomba de Prótons/química , Feminino , Medicamentos Genéricos/farmacocinética , Medicamentos Genéricos/administração & dosagem , Medicamentos Genéricos/normas , Medicamentos Genéricos/química , Estudos Cross-Over
6.
Eur J Med Res ; 29(1): 367, 2024 Jul 16.
Artigo em Inglês | MEDLINE | ID: mdl-39014507

RESUMO

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.


Assuntos
Cápsulas , Menopausa , Ocimum basilicum , Extratos Vegetais , Folhas de Planta , Humanos , Feminino , Menopausa/efeitos dos fármacos , Extratos Vegetais/farmacologia , Extratos Vegetais/administração & dosagem , Pessoa de Meia-Idade , Folhas de Planta/química , Ocimum basilicum/química , Administração Oral , Adulto , Fogachos/tratamento farmacológico
7.
Artigo em Inglês | MEDLINE | ID: mdl-38889492

RESUMO

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.


Assuntos
Anti-Inflamatórios , Medicamentos de Ervas Chinesas , Metabolômica , Farmacologia em Rede , Camundongos , Animais , Medicamentos de Ervas Chinesas/farmacologia , Medicamentos de Ervas Chinesas/química , Metabolômica/métodos , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/química , Células RAW 264.7 , Simulação de Acoplamento Molecular , Metaboloma/efeitos dos fármacos , Óxido Nítrico/metabolismo , Cápsulas , Interleucina-6/metabolismo
8.
Int J Biol Macromol ; 273(Pt 2): 132944, 2024 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-38851616

RESUMO

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.


Assuntos
Cápsulas , Lignina , Folhas de Planta , Lignina/química , Folhas de Planta/química , Estrobilurinas/química , Raios Ultravioleta , Triazóis/química , Fotólise , Arachis/química , Praguicidas/química
9.
Int J Biol Macromol ; 273(Pt 1): 133031, 2024 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-38866283

RESUMO

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.


Assuntos
Cápsulas , Quitosana , Liberação Controlada de Fármacos , Ácido Hialurônico , Impressão Tridimensional , Quitosana/química , Ácido Hialurônico/química , Portadores de Fármacos/química
10.
Int J Biol Macromol ; 273(Pt 2): 133139, 2024 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-38878929

RESUMO

The microencapsulation of polysaturated fatty acids by spray drying remains a challenge due to their susceptibility to oxidation. In this work, antioxidant Pickering emulsions were attempted as feeds to produce oxidation stable tuna oil microcapsules. The results indicated that the association between chitosan (CS) and ovalbumin (OVA) was a feasible way to fabricate antioxidant and wettable complexes and a high CS percentage favored these properties. The particles could yield tuna oil Pickering emulsions with enhanced oxidation stability through high-pressure homogenization, which were successfully spray dried to produce microcapsules with surface oil content of 8.84 % and microencapsulation efficiency of 76.65 %. The microcapsules exhibited significantly improved oxidation stability and their optimum peroxide values after storage at 50 °C, 85 % relative humidity, or natural light for 15 d were 48.67 %, 60.07 %, and 39.69 % respectively lower than the powder derived from the OVA-stabilized emulsion. Hence, Pickering emulsions stabilized by the CS/OVA polyelectrolyte complexes are potential in the production of oxidation stable polyunsaturated fatty acid microcapsules by spray drying.


Assuntos
Cápsulas , Quitosana , Emulsões , Ovalbumina , Oxirredução , Secagem por Atomização , Atum , Quitosana/química , Emulsões/química , Ovalbumina/química , Animais , Óleos de Peixe/química , Polieletrólitos/química , Antioxidantes/química , Tamanho da Partícula
11.
Molecules ; 29(12)2024 Jun 09.
Artigo em Inglês | MEDLINE | ID: mdl-38930817

RESUMO

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.


Assuntos
Cápsulas , Microbioma Gastrointestinal , Mel , Prebióticos , Animais , Microbioma Gastrointestinal/efeitos dos fármacos , Abelhas , Ácidos Graxos Voláteis/metabolismo , Bifidobacterium/crescimento & desenvolvimento , Bifidobacterium/metabolismo , Fermentação , Probióticos , Ácidos Graxos
12.
Int J Biol Macromol ; 273(Pt 1): 132872, 2024 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-38942671

RESUMO

Diseases caused by viruses pose a significant risk to the health of aquatic animals, for which there are presently no efficacious remedies. Interferon (IFN) serving as an antiviral agent, is frequently employed in clinical settings. Due to the unique living conditions of aquatic animals, traditional injection of interferon is cumbersome, time-consuming and labor-intensive. This study aimed to prepare IFN microcapsules through emulsion technique by using resistant starch (RS) and carboxymethyl chitosan (CMCS). Optimization was achieved using the Box-Behnken design (BBD) response surface technique, followed by the creation of microcapsules through emulsification. With RS at a concentration of 1.27 %, a water­oxygen ratio of 3.3:7.4, CaCl2 at 13.67 %, CMCS at 1.04 %, the rate of encapsulation can escalate to 80.92 %. Rainbow trout infected with Infectious hematopoietic necrosis virus (IHNV) and common carp infected with Spring vireemia (SVCV) exhibited a relative survival rate (RPS) of 65 % and 60 % after treated with IFN microcapsules, respectively. Moreover, the microcapsules effectively reduced the serum AST levels and enhanced the expression of IFNα, IRF3, ISG15, MX1, PKR and Viperin in IHNV-infected rainbow trout and SVCV-infected carp. In conclusion, this integrated IFN microcapsule showed potential as an antiviral agent for treatment of viral diseases in aquaculture.


Assuntos
Interferon-alfa , Oncorhynchus mykiss , Proteínas Recombinantes , Animais , Oncorhynchus mykiss/virologia , Interferon-alfa/farmacologia , Proteínas Recombinantes/farmacologia , Cápsulas , Antivirais/farmacologia , Antivirais/química , Composição de Medicamentos , Quitosana/química , Quitosana/análogos & derivados , Vírus da Necrose Hematopoética Infecciosa/efeitos dos fármacos , Sistemas de Liberação de Medicamentos , Doenças dos Peixes/virologia , Doenças dos Peixes/tratamento farmacológico
13.
Biomacromolecules ; 25(7): 4118-4138, 2024 Jul 08.
Artigo em Inglês | MEDLINE | ID: mdl-38857534

RESUMO

Postmodification of alginate-based microspheres with polyelectrolytes (PEs) is commonly used in the cell encapsulation field to control microsphere stability and permeability. However, little is known about how different applied PEs shape the microsphere morphology and properties, particularly in vivo. Here, we addressed this question using model multicomponent alginate-based microcapsules postmodified with PEs of different charge and structure. We found that the postmodification can enhance or impair the mechanical resistance and biocompatibility of microcapsules implanted into a mouse model, with polycations surprisingly providing the best results. Confocal Raman microscopy and confocal laser scanning microscopy (CLSM) analyses revealed stable interpolyelectrolyte complex layers within the parent microcapsule, hindering the access of higher molar weight PEs into the microcapsule core. All microcapsules showed negative surface zeta potential, indicating that the postmodification PEs get hidden within the microcapsule membrane, which agrees with CLSM data. Human whole blood assay revealed complex behavior of microcapsules regarding their inflammatory and coagulation potential. Importantly, most of the postmodification PEs, including polycations, were found to be benign toward the encapsulated model cells.


Assuntos
Alginatos , Cápsulas , Poliaminas , Polieletrólitos , Alginatos/química , Polieletrólitos/química , Cápsulas/química , Poliaminas/química , Animais , Camundongos , Humanos , Microesferas
14.
Arch Oral Biol ; 165: 106016, 2024 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-38838515

RESUMO

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.


Assuntos
Cápsulas , Película Dentária , Resveratrol , Saliva , Humanos , Resveratrol/farmacologia , Resveratrol/farmacocinética , Resveratrol/administração & dosagem , Saliva/metabolismo , Saliva/química , Masculino , Adulto , Película Dentária/metabolismo , Película Dentária/química , Cromatografia Líquida de Alta Pressão , Feminino , Disponibilidade Biológica , Estilbenos/farmacocinética , Estilbenos/farmacologia , Estilbenos/administração & dosagem , Proteômica , Espectrometria de Massas em Tandem , Proteínas e Peptídeos Salivares/metabolismo
15.
Sci Rep ; 14(1): 14802, 2024 06 26.
Artigo em Inglês | MEDLINE | ID: mdl-38926468

RESUMO

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.


Assuntos
Cápsulas , Óleos de Peixe , Secagem por Atomização , Óleos de Peixe/química , Óleos de Plantas/química , Salvia/química , Ácidos Graxos/química , Humanos
16.
Artif Cells Nanomed Biotechnol ; 52(1): 345-354, 2024 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-38829715

RESUMO

Cell encapsulation into spherical microparticles is a promising bioengineering tool in many fields, including 3D cancer modelling and pre-clinical drug discovery. Cancer microencapsulation models can more accurately reflect the complex solid tumour microenvironment than 2D cell culture and therefore would improve drug discovery efforts. However, these microcapsules, typically in the range of 1 - 5000 µm in diameter, must be carefully designed and amenable to high-throughput production. This review therefore aims to outline important considerations in the design of cancer cell microencapsulation models for drug discovery applications and examine current techniques to produce these. Extrusion (dripping) droplet generation and emulsion-based techniques are highlighted and their suitability to high-throughput drug screening in terms of tumour physiology and ease of scale up is evaluated.


3D microencapsulation models of cancer offer a customisable platform to mimic key aspects of solid tumour physiology in vitro. However, many 3D models do not recapitulate the hypoxic conditions and altered tissue stiffness established in many tumour types and stages. Furthermore, microparticles for cancer cell encapsulation are commonly produced using methods that are not necessarily suitable for scale up to high-throughput manufacturing. This review aims to evaluate current technologies for cancer cell-laden microparticle production with a focus on physiological relevance and scalability. Emerging techniques will then be touched on, for production of uniform microparticles suitable for high-throughput drug discovery applications.


Assuntos
Descoberta de Drogas , Neoplasias , Humanos , Neoplasias/patologia , Neoplasias/tratamento farmacológico , Neoplasias/metabolismo , Descoberta de Drogas/métodos , Encapsulamento de Células/métodos , Modelos Biológicos , Cápsulas , Animais , Composição de Medicamentos/métodos , Microambiente Tumoral/efeitos dos fármacos
17.
Int J Biol Macromol ; 272(Pt 1): 132843, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38830489

RESUMO

The study aimed to inhibit the stimulating impact of garlic oil (GO) on the stomach and attain high release in the intestine during digestion. So, wheat porous starch (WPS) was modified with octenyl succinic acid (OSA) and malic acid (MA) to obtain esterified WPS, OWPS and MWPS, respectively. The differences in physicochemical, encapsulation, and digestive properties of two GO microcapsules, WPI/OWPS/GO and WPI/MWPS/GO microcapsules produced by using OWPS and MWPS as variant carrier materials and whey protein isolate (WPI) as the same coating agent, were compared. The results found that OWPS had greater amphiphilicity, while MWPS had better hydrophobicity and anti-digestive ability than WPS. Encapsulation efficiency of WPI/OWPS/GO (94.67 %) was significantly greater than WPI/MWPS/GO (91.44 %). The digestion inhibition and low GO release (approximately 23 %) of WPI/OWPS/GO and WPI/MWPS/GO microcapsules in the gastric phase resulted from the protective effect of WPI combined with the good adsorption and lipophilicity of OWPS and MWPS. Especially, WPI/OWPS/GO microcapsule was relatively stable in the gastric phase and had sufficient GO release (67.24 %) in the intestinal phase, which was significantly higher than WPI/MWPS/GO microcapsule (56.03 %), benefiting from the adsorption and digestive properties of OWPS, and resulting in a total cumulative GO release rate of 90.86 %.


Assuntos
Digestão , Amido , Triticum , Proteínas do Soro do Leite , Proteínas do Soro do Leite/química , Amido/química , Triticum/química , Porosidade , Cápsulas , Fenômenos Químicos , Óleos de Plantas/química , Interações Hidrofóbicas e Hidrofílicas , Composição de Medicamentos , Alho/química
18.
Eur Phys J E Soft Matter ; 47(6): 37, 2024 Jun 03.
Artigo em Inglês | MEDLINE | ID: mdl-38829453

RESUMO

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.


Assuntos
Células Artificiais , Polímeros , Células Artificiais/química , Polímeros/química , Polímeros/síntese química , Emulsões/química , Cápsulas/química , Microfluídica/métodos , Água/química , Técnicas Analíticas Microfluídicas , Proteínas/química
19.
Nanotechnology ; 35(36)2024 Jun 20.
Artigo em Inglês | MEDLINE | ID: mdl-38861959

RESUMO

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.


Assuntos
Nanoestruturas , Polímeros de Fluorcarboneto/química , Polivinil/química , Nanoestruturas/química , Cápsulas , Compostos de Tungstênio/química , Sulfetos/química , Eletricidade , Potássio/química , Íons/química , Cloro/química
20.
Phytomedicine ; 131: 155766, 2024 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-38865935

RESUMO

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.


Assuntos
Medicamentos de Ervas Chinesas , Transtornos de Enxaqueca , Polissacarídeos , Ratos Sprague-Dawley , Transtornos de Enxaqueca/tratamento farmacológico , Animais , Masculino , Medicamentos de Ervas Chinesas/farmacologia , Medicamentos de Ervas Chinesas/química , Ratos , Polissacarídeos/farmacologia , Polissacarídeos/química , Modelos Animais de Doenças , Cápsulas
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