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1.
Carbohydr Polym ; 335: 122107, 2024 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-38616081

RESUMO

In this study, the polyvinylpyrrolidone-alizarin nanoparticles (PVP-AZ NPs) with favorable water dispersion and the carbon quantum dots (RQDs) with aggregate induced emission effect were synthesized to construct an eco-friendly film for food freshness monitoring. The introduction of PVP-AZ NPs and RQDs enhanced the network structure and thermal stability of the cassava starch/polyvinyl alcohol film, and reduced its crystallinity and light transmittance via non-covalent binding with the film-forming matrix. The developed film exhibited visually recognizable colorimetric and fluorescent responses to ammonia at 0.025-25 mg/mL, and it can be reused at least 6 times. Practical application experiment proved that the film, as an indicator label, can achieve accurate, real-time, and visual dynamic monitoring of the freshness of shrimp stored at 25 °C, 4 °C, and - 20 °C under daylight (orange yellow to purple) and UV light (red to blue). The integration of multivariate detection technology can eliminate the interference of external factors by self-correction to improve sensitivity and reliability, which provides a reference for the development of other food quality and safety monitoring platforms.


Assuntos
Antraquinonas , Manihot , Animais , Álcool de Polivinil , Reprodutibilidade dos Testes , Alimentos Marinhos , Crustáceos , Povidona , Amido
2.
Skin Res Technol ; 30(4): e13671, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38558153

RESUMO

BACKGROUND: Nowadays, diabetic wound healing remains a crucial challenge due to their protracted and uncertain healing process. Traditional Chinese medicine (TCM) has demonstrated the therapeutic value of Sanguis draconis (SD)-Salvia miltiorrhiza (SMR) Herb Pair in diabetic wound healing. However, new administration modes are urgently needed for their convenient and wide-ranging applications. OBJECTIVE: We propose a soluble polyvinylpyrrolidone-based microneedle patch containing the herbal extracts of SD and SMR (MN-SD@SMR) for diabetic wound healing. METHODS: The herbal extracts of SD and SMR are purification and concentration via traditional lyophilization. SD endowed MN-SD@SMR with functions to improve high glycemic blood environment and migration of keratinocyte and fibroblast cells. RESULTS: SMR in MN-SD@SMR could improve blood flow velocity and microcirculation in the wound area. The effectiveness of transdermal release and mechanical strengths of MN-SD@SMR were verified. CONCLUSION: Integrating the advantages of these purified herbal compositions, we demonstrated that MN-SD@SMR had a positive healing effect on the wounds in vitro and vivo. These results indicate that soluble polyvinylpyrrolidone-based microneedle patch containing the herbal extracts of SD and SMR has a promising application value due to their superior capability to promote diabetic wound healing.


Assuntos
Diabetes Mellitus , Medicamentos de Ervas Chinesas , Salvia miltiorrhiza , Humanos , Povidona , Diabetes Mellitus/tratamento farmacológico , Cicatrização
3.
AAPS PharmSciTech ; 25(4): 81, 2024 Apr 10.
Artigo em Inglês | MEDLINE | ID: mdl-38600252

RESUMO

MALCORE®, a novel manufacturing technology for drug-containing particles (DCPs), relies on the melt granulation method to produce spherical particles with high drug content. The crucial aspect of particle preparation through MALCORE® involves utilizing polymers that dissolve in the melt component, thereby enhancing viscosity upon heating. However, only aminoalkyl methacrylate copolymer E (AMCE) has been previously utilized. Therefore, this study aims to discover other polymers and comprehend the essential properties these polymers need to possess. The results showed that polyvinylpyrrolidone (PVP) was soluble in the stearic acid (SA) melt component. FTIR examination revealed no interaction between SA and polymer. The phase diagram was used to analyze the state of the SA and polymer mixture during heating. It revealed the mixing ratio and temperature range where the mixture remained in a liquid state. The viscosity of the mixture depended on the quantity and molecular weight of the polymer dissolved in SA. Furthermore, the DCPs prepared using PVP via MALCORE® exhibited similar pharmaceutical properties to those prepared with AMCE. In conclusion, understanding the properties required for polymers in the melt granulation process of MALCORE® allows for the optimization of manufacturing conditions, such as temperature and mixing ratios, for efficient and consistent drug layering.


Assuntos
Polímeros , Povidona , Tecnologia Farmacêutica/métodos , Temperatura , Excipientes , Tecnologia , Metacrilatos , Composição de Medicamentos/métodos , Solubilidade
5.
J Photochem Photobiol B ; 254: 112904, 2024 May.
Artigo em Inglês | MEDLINE | ID: mdl-38579534

RESUMO

The fluorescence lifetime of a porphyrinic photosensitizer (PS) is an important parameter to assess the aggregation state of the PS even in complex biological environments. Aggregation-induced quenching of the PS can significantly reduce the yield of singlet oxygen generation and thus its efficiency as a medical drug in photodynamic therapy (PDT) of diseased tissues. Hydrophobicity and the tendency to form aggregates pose challenges on the development of efficient PSs and often require carrier systems. A systematic study was performed to probe the impact of PS structure and encapsulation into polymeric carriers on the fluorescence lifetime in solution and in the intracellular environment. Five different porphyrinic PSs including chlorin e6 (Ce6) derivatives and tetrakis(m-hydroxyphenyl)-porphyrin and -chlorin were studied in free form and combined with polyvinylpyrrolidone (PVP) or micelles composed of triblock-copolymers or Cremophor. Following incubation of HeLa cells with these systems, fluorescence lifetime imaging combined with phasor analysis and image segmentation was applied to study the lifetime distribution in the intracellular surrounding. The data suggest that for free PSs, the structure-dependent cell uptake pathways determine their state and emission lifetimes. PS localization in the plasma membrane yielded mostly monomers with long fluorescence lifetimes whereas the endocytic pathway with subsequent lysosomal deposition adds a short-lived component for hydrophilic anionic PSs. Prolonged incubation times led to increasing contributions from short-lived components that derive from aggregates mainly localized in the cytoplasm. Encapsulation of PSs into polymeric carriers led to monomerization and mostly fluorescence emission decays with long fluorescence lifetimes in solution. However, the efficiency depended on the binding strength that was most pronounced for PVP. In the cellular environment, PVP was able to maintain monomeric long-lived species over prolonged incubation times. This was most pronounced for Ce6 derivatives with a logP value around 4.5. Micellar encapsulation led to faster release of the PSs resulting in multiple components with long and short fluorescence lifetimes. The hydrophilic hardly aggregating PS exhibited a mostly stable invariant lifetime distribution over time with both carriers. The presented data are expected to contribute to optimized PDT treatment protocols and improved PS-carrier design for preventing intracellular fluorescence quenching. In conclusion, amphiphilic and concurrent hydrophobic PSs with high membrane affinity as well as strong binding to the carrier have best prospects to maintain their photophysical properties in vivo and serve thus as efficient photodynamic diagnosis and PDT drugs.


Assuntos
Fotoquimioterapia , Porfirinas , Humanos , Fármacos Fotossensibilizantes/química , Células HeLa , Polímeros/química , Porfirinas/química , Povidona/química , Micelas , Linhagem Celular Tumoral
6.
Am Psychol ; 79(3): 344-346, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38635196

RESUMO

In this invited commentary, I address what I see as the major contributions Rubenstein et al. (2024) have made to challenging the hegemony of exposure therapies for trauma-exposed persons. These include a thorough review of the history of the rise of exposure therapies, the identification of posttrauma responses as forms of anxiety disorders, and an extensive discussion of the neurobiology of the trauma response. Additionally, Rubenstein et al. expose the very high dropout rates in studies of exposure therapies and ways in which many traumatized people have not found them helpful. This article brings the so-called "gold standard" back to its rightful position as one possible, occasionally helpful way of assisting some, but not all, traumatized people. (PsycInfo Database Record (c) 2024 APA, all rights reserved).


Assuntos
Terapia Implosiva , Humanos , Povidona , Transtornos de Ansiedade
7.
Methods Mol Biol ; 2782: 113-122, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38622396

RESUMO

Mitochondria-associated membranes (MAMs) are regions where the endoplasmic reticulum (ER) interacts with mitochondria and regulate lipid trafficking, calcium signaling, ER stress, and inflammation activation. Isolation of MAMs from endothelial cells is vital for studying insight into the immune regulation of many inflammatory diseases. Endothelial cells (ECs) are critical innate immune cells due to their paracrine function of secreting interleukins, chemokines, cytokines, and growth factors, as well as expressing levels of pattern recognition receptors including toll-like receptors (TLRs). Furthermore, ECs regulate and recruit monocytes by expressing adhesion molecules including vascular cell adhesion molecule-1 (VCAM-1), intercellular adhesion molecule-1 (ICAM-1), P-selectin, and E-selectin, to facilitate monocyte diapedesis in areas of damage and inflammation. This protocol consists of step-by-step instructions on isolating pure MAMs and other subcellular fractions from endothelial cells, which is critical to understanding ER and mitochondria crosstalks in endothelial functions in health and disease.


Assuntos
Células Endoteliais , 60482 , Povidona , Dióxido de Silício , Humanos , Células Endoteliais/metabolismo , Mitocôndrias/metabolismo , Inflamação/metabolismo
8.
Molecules ; 29(6)2024 Mar 14.
Artigo em Inglês | MEDLINE | ID: mdl-38542923

RESUMO

Our research aimed to develop an amorphous solid dispersion (ASD) of myricetin (MYR) with Polyvinylpyrrolidone K30 (PVP30) to enhance its solubility, dissolution rate, antioxidant, and neuroprotective properties. Employing a combination of solvent evaporation and freeze drying, we successfully formed MYR ASDs. XRPD analysis confirmed complete amorphization in 1:8 and 1:9 MYR-PVP weight ratios. DSC thermograms exhibited a single glass transition (Tg), indicating full miscibility. FT-IR results and molecular modeling confirmed hydrogen bonds stabilizing MYR's amorphous state. HPLC analysis indicated the absence of degradation products, ensuring safe MYR delivery systems. Solubility, dissolution rate (pH 1.2 and 6.8), antioxidant (ABTS, DPPH, CUPRAC, and FRAP assays), and in vitro neuroprotective activities (inhibition of cholinesterases: AChE and BChE) were significantly improved compared to the pure compound. Molecular docking studies revealed that MYR had made several hydrogen, hydrophobic, and π-π stacking interactions, which could explain the compound's potency to inhibit AChE and BChE. MYR-PVP 1:9 w/w ASD has the best solubility, antioxidant, and neuroprotective activity. Stability studies confirmed the physical stability of MYR-PVP 1:9 w/w ASD immediately after dissolution and for two months under ambient conditions. Our study showed that the obtained ASDs are promising systems for the delivery of MYR with the potential for use in alleviating the symptoms of neurodegenerative diseases.


Assuntos
Antioxidantes , Flavonoides , Povidona , Espectroscopia de Infravermelho com Transformada de Fourier , Antioxidantes/farmacologia , Simulação de Acoplamento Molecular , Solubilidade , Povidona/química
9.
Bioconjug Chem ; 35(4): 499-516, 2024 Apr 17.
Artigo em Inglês | MEDLINE | ID: mdl-38546823

RESUMO

Nanodroplet formation is important to achieve supersaturation of active pharmaceutical ingredients (APIs) in an amorphous solid dispersion. The aim of the current study was to explore how polymer composition, architecture, molar mass, and surfactant concentration affect polymer-drug nanodroplet morphology with the breast cancer API, GDC-0810. The impact of nanodroplet size and morphology on dissolution efficacy and drug loading capacity was explored using polarized light microscopy, dynamic light scattering, and cryogenic transmission electron microscopy. Poly(N-isopropylacrylamide-stat-N,N-dimethylacrylamide) (PND) was synthesized as two linear derivatives and two bottlebrush derivatives with carboxylated or PEGylated end-groups. Hydroxypropyl methylcellulose acetate succinate grade MF (HPMCAS-MF) and poly(vinylpyrrolidone-co-vinyl acetate) (PVPVA) were included as commercial polymer controls. We report the first copolymerization synthesis of a PVPVA bottlebrush copolymer, which was the highest performing excipient in this study, maintaining 688 µg/mL GDC-0810 concentration at 60 wt % drug loading. This is likely due to strong polymer-drug noncovalent interactions and the compaction of GDC-0810 along the PVPVA bottlebrush backbone. Overall, it was observed that the most effective formulations had a hydrodynamic radius less than 25 nm with tightly compacted nanodroplet morphologies.


Assuntos
Cinamatos , Indazóis , Polímeros , Povidona/análogos & derivados , Solubilidade
10.
Int J Pharm ; 655: 123997, 2024 Apr 25.
Artigo em Inglês | MEDLINE | ID: mdl-38484861

RESUMO

The superior flexibility, efficient drug loading, high surface-to-volume ratio, ease of formulation, and cost-controlled production are considered exceptional advantages of nanofibers (NFs) as a smart delivery system. Deflazacort (DEF) is an anti-inflammatory and immunosuppressant agent. It is categorized as a poorly soluble class II drug. In this study, DEF-loaded polymeric nanofibrous using the electrospinning technique mats, Polyvinyl pyrrolidone (PVP) with or without Poloxamer 188 (PX) were used as mat-forming polymers. Microscopical imaging, drug content (%), and in vitro dissolution studies were conducted for all NFs formulae (F1-F7). All NFs improved the DEF dissolution compared to the unprocessed form, with the superiority of the PVP/PX hybrid. The optimized formula (F7) exhibited an average diameter of 655.46 ± 90.4 nm and % drug content of 84.33 ± 5.58. The dissolution parameters of DEF loaded in PVP/PX NFs (F7) reflected a release of 95.3 % ± 3.1 and 102.6 % ± 1.7 after 5 and 60 min, respectively. NFs (F7) was investigated for drug-polymer compatibility using Fourier-Transform Infrared Spectroscopy (FTIR), Powder X-ray diffraction analysis (PXRD), and Differential Scanning Calorimetry (DSC). In vivo anti-inflammatory study employing male Sprague-Dawley rats showed a significant reduction of rat paw edema for F7 (p < 0.05) compared with unprocessed DEF with a normal epidermal and dermal skin structure comparable to the healthy negative control. Immunohistochemical and morphometric data displayed similarities between the immune reaction of F7 and the negative healthy control. The finding of this work emphasized that DEF loaded in PVP/PX NFs could be considered a useful strategy for enhancing the therapeutic performance of DEF.


Assuntos
Nanofibras , Povidona , Pregnenodionas , Masculino , Ratos , Animais , Povidona/química , Polivinil , Poloxâmero , Nanofibras/química , Solubilidade , Ratos Sprague-Dawley , Polímeros/química , Espectroscopia de Infravermelho com Transformada de Fourier/métodos , Anti-Inflamatórios , Varredura Diferencial de Calorimetria
11.
ACS Appl Bio Mater ; 7(3): 1671-1681, 2024 Mar 18.
Artigo em Inglês | MEDLINE | ID: mdl-38447193

RESUMO

Copper sulfide nanoparticles (CuS) hold tremendous potential for applications in photothermal therapy (PTT) and photoacoustic imaging (PAI). However, the conventional chemical coprecipitation method often leads to particle agglomeration issues. To overcome this challenge, we utilized polyvinylpyrrolidone (PVP) as a stabilizing agent, resulting in the synthesis of small PVP-CuS nanoparticles named PC10, PCK30, and PC40. Our study aimed to investigate how different molecular weights of PVP influence the nanoparticles' crystalline characteristics and essential properties, especially their photoacoustic and photothermal responses. While prior research on PVP-assisted CuS nanoparticles has been conducted, our study delves deeper into this area, providing insights into optical properties. Remarkably, all synthesized nanoparticles exhibited a crystalline structure, were smaller than 10 nm, and featured an absorbance peak at 1020 nm, indicating their robust photoacoustic and photothermal capabilities. Among these nanoparticles, PC10 emerged as the standout performer, displaying superior photoacoustic properties. Our photothermal experiments demonstrated significant temperature increases in all cases, with PC10 achieving an impressive efficiency of 51%. Moreover, cytotoxicity assays revealed the nanoparticles' compatibility with cells, coupled with an enhanced incidence of apoptosis compared to necrosis. These findings underscore the promising potential of PVP-stabilized CuS nanoparticles for advanced cancer theranostics.


Assuntos
Nanopartículas , Neoplasias , Humanos , Povidona , Peso Molecular , Fototerapia , Neoplasias/diagnóstico por imagem , Neoplasias/terapia , Nanopartículas/uso terapêutico
12.
Int J Mol Sci ; 25(5)2024 Feb 28.
Artigo em Inglês | MEDLINE | ID: mdl-38474022

RESUMO

In this study, amorphous solid dispersions (ASDs) of pterostilbene (PTR) with polyvinylpyrrolidone polymers (PVP K30 and VA64) were prepared through milling, affirming the amorphous dispersion of PTR via X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC). Subsequent analysis of DSC thermograms, augmented using mathematical equations such as the Gordon-Taylor and Couchman-Karasz equations, facilitated the determination of predicted values for glass transition (Tg), PTR's miscibility with PVP, and the strength of PTR's interaction with the polymers. Fourier-transform infrared (FTIR) analysis validated interactions maintaining PTR's amorphous state and identified involved functional groups, namely, the 4'-OH and/or -CH groups of PTR and the C=O group of PVP. The study culminated in evaluating the impact of amorphization on water solubility, the release profile in pH 6.8, and in vitro permeability (PAMPA-GIT and BBB methods). In addition, it was determined how improving water solubility affects the increase in antioxidant (ABTS, DPPH, CUPRAC, and FRAP assays) and neuroprotective (inhibition of cholinesterases: AChE and BChE) properties. The apparent solubility of the pure PTR was ~4.0 µg·mL-1 and showed no activity in the considered assays. For obtained ASDs (PTR-PVP30/PTR-PVPVA64, respectively) improvements in apparent solubility (410.8 and 383.2 µg·mL-1), release profile, permeability, antioxidant properties (ABTS: IC50 = 52.37/52.99 µg·mL-1, DPPH: IC50 = 163.43/173.96 µg·mL-1, CUPRAC: IC0.5 = 122.27/129.59 µg·mL-1, FRAP: IC0.5 = 95.69/98.57 µg·mL-1), and neuroprotective effects (AChE: 39.1%/36.2%, BChE: 76.9%/73.2%) were confirmed.


Assuntos
Antioxidantes , Benzotiazóis , Povidona , Ácidos Sulfônicos , Resveratrol , Povidona/química , Polímeros/química , Solubilidade , Difração de Raios X , Água , Varredura Diferencial de Calorimetria , Espectroscopia de Infravermelho com Transformada de Fourier
13.
Chemosphere ; 353: 141542, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38428535

RESUMO

The escalating global concern regarding antibiotic pollution necessitates the development of advanced water treatment strategies. This study presents an innovative approach through the fabrication and evaluation of a Polyethersulfone (PES) membrane adorned with GO-TiO2 nanocomposites. The objective is to enhance the removal efficiency of various antibiotics, addressing the challenge of emerging organic compounds (EOCs) in water systems. The nanocomposite membranes, synthesized via the phase inversion method, incorporate hydrophilic agents, specifically GO-TiO2 nanocomposites and Polyvinylpyrrolidone (PVP). The resultant membranes underwent comprehensive characterization employing AFM, EDS, tensile strength testing, water contact angle measurements, and FESEM to elucidate their properties. Analysis revealed a substantial improvement in the hydrophilicity of the modified membranes attributed to the presence of hydroxyl groups within the GO-TiO2 structure. AFM images demonstrated an augmentation in surface roughness with increasing nanocomposite content. FESEM images unveiled structural modifications, leading to enhanced porosity and augmented water flux. The pure water flux elevated from 0.980 L/m2.h-1 for unmodified membranes to approximately 6.85 L/m2.h-1 for membranes modified with 2 wt% nanocomposites. Membrane performance analysis indicated a direct correlation between nanocomposite content and antibiotic removal efficiency, ranging from 66.52% to 89.81% with 4 wt% nanocomposite content. Furthermore, the nanocomposite-modified membrane exhibited heightened resistance to fouling. The efficacy of the membrane extended to displaying potent antibacterial properties against microbial strains, including S. aureus, E. coli, and Candida. This study underscores the immense potential of GO-TiO2 decorated PES membranes as a sustainable and efficient solution for mitigating antibiotic contamination in water systems. The utilization of nanocomposite membranes emerges as a promising technique to combat the presence of EOC pollutants, particularly antibiotics, in water bodies, thus addressing a critical environmental concern.


Assuntos
Nanocompostos , Polímeros , Povidona , Sulfonas , Antibacterianos/farmacologia , Azitromicina , Amoxicilina , Ciprofloxacina , Escherichia coli , Staphylococcus aureus , Nanocompostos/química , Membranas Artificiais
14.
Drug Dev Ind Pharm ; 50(4): 331-340, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38456721

RESUMO

OBJECTIVE: This study aimed to optimize the formulation of carbidopa/levodopa orally disintegrating tablets (ODTs) in order to improve their disintegration performance, and facilitate easier medication intake for Parkinson's patients. METHOD: The response surface methodology (RSM) was used to optimize the formulation, with the content of cross-linked polyvinylpyrrolidone (PVPP), microcrystalline cellulose (MCC), and mannitol (MNT) as independent variables, and disintegration time as the response parameter. Python was utilized to model Carr Indices and mixing time to determine the suitable mixing time. Direct compression (DC) was used for the preparation of ODTs. RESULT: The optimization process resulted in the following values for the independent variables: 7.04% PVPP, 22.02% MCC, and 16.21% MNT. By optimizing the mixing time using Python, it was reduced to 14.19 min. The ODTs prepared using the optimized formulation and a mixing time of 14.19 min exhibited disintegration times of 16.74 s in vitro and 17.63 s in vivo. The content uniformity of levodopa and carbidopa was found to be 100.83% and 99.48%, respectively. CONCLUSION: The ODTs optimized using RSM and Python demonstrated excellent disintegration performance, leading to a decrease in the time the drug exists in solid form in the oral cavity. This improvement in disintegration time reduced the difficulty of swallowing for patients and enhanced medication compliance, while still ensuring that ODTs prepared by DC had sufficient mechanical strength to meet storage and transportation requirements.


Assuntos
Carbidopa , Levodopa , Povidona/análogos & derivados , Humanos , Solubilidade , Administração Oral , Manitol , Comprimidos/química , Composição de Medicamentos/métodos
15.
Int J Pharm ; 654: 123965, 2024 Apr 10.
Artigo em Inglês | MEDLINE | ID: mdl-38442796

RESUMO

The oral bioavailability of paclitaxel is limited due to low solubility and high affinity for the P-glycoprotein (P-gp) efflux transporter. Here we hypothesized that maximizing the intestinal paclitaxel levels through apparent solubility enhancement and controlling thesimultaneous release of both paclitaxel and the P-gp inhibitor encequidar from amorphous solid dispersions (ASDs) would increase the oral bioavailability of paclitaxel. ASDs of paclitaxel and encequidar in polyvinylpyrrolidone K30 (PVP-K30), hydroxypropylmethylcellulose 5 (HPMC-5), and hydroxypropylmethylcellulose 4 K (HPMC-4K) were hence prepared by freeze-drying. In vitro dissolution studies showed that both compounds were released fastest from PVP-K30, then from HPMC-5, and slowest from HPMC-4K ASDs. The dissolution of paclitaxel from all polymers resulted in stable concentration levels above the apparent solubility. The pharmacokinetics of paclitaxel after oral administration to male Sprague-Dawley rats was investigated with or without 1 mg/kg encequidar, as amorphous solids or polymer-based ASDs. The bioavailability of paclitaxel increased 3- to 4-fold when administered as polymer-based ASDs relative to solid amorphous paclitaxel. However, when amorphous paclitaxel was co-administered with encequidar, either as an amorphous powder or as a polymer-based ASD, the bioavailability increased 2- to 4-fold, respectively. Interestingly, a noticeable increase in paclitaxel bioavailability of 24-fold was observed when paclitaxel and encequidar were co-administered as HPMC-5-based ASDs. We, therefore, suggest that controlling the dissolution rate of paclitaxel and encequidar in order to obtain simultaneous and timed release from polymer-based ASDs is a strategy to increase oral paclitaxel bioavailability.


Assuntos
Polímeros , Povidona , Ratos , Masculino , Animais , Disponibilidade Biológica , Ratos Sprague-Dawley , Derivados da Hipromelose , Solubilidade
16.
Int J Pharm ; 654: 123972, 2024 Apr 10.
Artigo em Inglês | MEDLINE | ID: mdl-38458404

RESUMO

A core-sheath structure is one of the methods developed to overcome the challenges often faced when using monolithic fibers for drug delivery. In this study, fibers based on polyvinylpyrrolidone (core) and ethyl cellulose (sheath) were successfully produced using a novel core-sheath pressure-spinning process. For comparison, these two polymers were also processed into as blend fibers. All samples were then investigated for their performances in releasing water-soluble ampicillin (AMP) and poorly water-soluble ibuprofen (IBU) model drugs. Scanning electron,digital and confocal microscopy confirmed that fibers with a core-sheath structure were successfully made. Fourier transform infrared spectroscopy showed the success of the pressure-spinning technique in encapsulating AMP/IBU in all fiber samples. Compared to blend fibers, the core-sheath fibers had better performance in encapsulating both water-soluble and poorly water-soluble drugs. Moreover, the core-sheath structure was able to reduce the initial burst release and provided a better sustained release profile than the blend fiber analog. In conclusion, the pressure-spinning method was capable of producing core-sheath and blend fibers that could be used for the loading of either hydrophilic or hydrophobic drugs for controlled drug delivery systems.


Assuntos
Celulose/análogos & derivados , Nanofibras , Povidona , Povidona/química , Liberação Controlada de Fármacos , Sistemas de Liberação de Medicamentos/métodos , Preparações Farmacêuticas , Água , Nanofibras/química
17.
Int J Biol Macromol ; 264(Pt 2): 130814, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38479664

RESUMO

Recently, various advancements have been made in the development of functional polymeric materials for innovative applications. Herein this work, functionalization of sterculia gum (SG) was carried out via grafting of poly(2-(methacryloyloxy) ethyltrimethylammonium chloride) (METAC)-polyvinyl pyrrolidone (PVP) to develop hydrogel dressings as a platform for use in drug delivery (DD). The innovation of the present work is the exploration of inherent antioxidant and antimicrobial properties of the SG along with antimicrobial characteristic of poly(METAC) and PVP, to design the doxycycline encapsulated hydrogel dressings for better wound healing. FESEM, EDS and AFM analyzed the surface morphology of hydrogels. FTIR, 13C NMR and XRD inferred inclusion of poly(METAC)-PVP into polymers. 13C NMR confirmed the incorporation of poly(METAC) and PVP onto gum by the presence of a peak at 54.74 ppm because of methyl carbon attached to quaternary nitrogen of poly(METAC) and at 45.48 ppm due to the ring carbon of PVP along with FTIR peak at 949 cm-1 because of CN bending of quaternary nitrogen of poy (METAC). Thermal characterization of copolymers has been performed using TGA analysis. One gram of copolymeric hydrogel dressing absorbed 6.51 ± 0.03 g simulated salivary fluid (SSF) and 7.65 ± 0.03 g simulated wound fluid (SWF). Release of doxycycline drug occurred in a sustained manner and followed the Non-Fickian diffusion mechanism from hydrogels. The release profile was most effectively described by Hixon-Crowell kinetic model. Hydrogel demonstrated biocompatibility and expressed thrombogenicity 79.7 ± 4.9 % during its polymer-blood interactions. Copolymer revealed mucoadhesive property, requiring a force of 77.00 ± 0.01 mN to detach from bio-membrane. Additionally, it exhibited antioxidant features, showing 43.81 ± 0.286 % free radical scavenging. Hydrogel dressings were mechanically stable and revealed 0.76 ± 0.09 N mm-2 tensile strength and 9.18 ± 0.01 N burst strength. Polymer films were permeable to oxygen and water vapor and were impermeable to microorganisms. Hydrogel dressings exhibited antimicrobial properties against Pseudomonas aeruginosa and Staphylococcus aureus bacteria. Overall, these properties displayed the suitability of hydrogels for wound dressing (WD) applications which may actively enhance wound healing.


Assuntos
Anti-Infecciosos , Sterculia , Hidrogéis/química , Sterculia/química , Doxiciclina , Antioxidantes/farmacologia , Antioxidantes/química , Goma de Karaya/química , Polímeros/química , Povidona , Carbono , Nitrogênio , Antibacterianos/farmacologia , Antibacterianos/química
18.
Tissue Cell ; 87: 102318, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38377632

RESUMO

Diabetes is a global problem that threatens human health. Cell therapy methods using stem cells, and tissue engineering of pancreatic islets as new therapeutic approaches have increased the chances of successful diabetes treatment. In this study, to differentiate Wharton's Jelly-derived mesenchymal stem cells (WJ-MSCs) into insulin-producing cells (IPCs) with improved maturity, and function, platelet-rich plasma (PRP)-Polyvinylpyrrolidone (PVP)-Polycaprolactone (PCL)/PCL scaffold was designed. The two-dimensional (2D) control group included cell culture without differentiation medium, and the experimental groups included 2D, and three-dimensional (3D) groups with pancreatic beta cell differentiation medium. WJ-MSCs-derived IPCs on PRP-PVP-PCL/PCL scaffold took round cluster morphology, the typical pancreatic islets morphology. Real-time PCR, immunocytochemistry, and flowcytometry data showed a significant increase in pancreatic marker genes in WJ-MSCs-derived IPCs on the PRP-PVP-PCL/PCL scaffold compared to the 2D-experimental group. Also, using the ELISA assay, a significant increase in the secretion of insulin, and C-peptide was measured in the WJ-MSCs-derived IPCs of the 3D-experimental group compared to the 2D experimental group, the highest amount of insulin (38 µlU/ml), and C-peptide (43 pmol/l) secretion was in the 3D experimental group, and in response to 25 mM glucose solution, which indicated a significant improvement in the functional level of the WJ-MSCs-derived IPCs in the 3D group. The results showed that the PRP-PVP-PCL/PCL scaffold can provide an appropriate microenvironment for the engineering of pancreatic islets, and the generation of IPCs.


Assuntos
Diabetes Mellitus , Células-Tronco Mesenquimais , Poliésteres , Povidona/análogos & derivados , Geleia de Wharton , Humanos , Peptídeo C , Diferenciação Celular , Células Cultivadas
19.
ACS Appl Bio Mater ; 7(3): 1842-1851, 2024 Mar 18.
Artigo em Inglês | MEDLINE | ID: mdl-38416807

RESUMO

The growing concerns regarding foodborne illnesses related to fresh produce accentuate the necessity for innovative material solutions, particularly on surfaces that come into close contact with foods. This study introduces a sustainable, efficient, and removable antimicrobial and antifouling coating ideally suited for hydrophobic food-contact surfaces such as low-density polyethylene (LDPE). Developed through a crosslinking reaction involving tannic acid, gelatin, and soy protein hydrolysate, these coatings exhibit proper stability in aqueous washing solutions and effectively combat bacterial contamination and prevent biofilm formation. The unique surface architecture promotes the formation of halamine structures, enhancing antimicrobial efficacy with a rapid contact killing effect and reducing microbial contamination by up to 5 log10 cfu·cm-2 against both Escherichia coli (Gram-negative) and Listeria innocua (Gram-positive). Notably, the coatings are designed for at least five recharging cycles under mild conditions (pH6, 20 ppm free active chlorine) and can be easily removed with hot water or steam to refresh the depositions. This removal process not only conveniently aligns with existing sanitation protocols in the fresh produce industry but also facilitates the complete eradication of potential developed biofilms, outperforming uncoated LDPE coupons. Overall, these coatings represent sustainable, cost-effective, and practical advancements in food safety and are promising candidates for widespread adoption in food processing environments.


Assuntos
Anti-Infecciosos , Incrustação Biológica , Polifenóis , Polietileno , Anti-Infecciosos/farmacologia , Povidona , Escherichia coli
20.
Pharm Dev Technol ; 29(3): 258-264, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38407128

RESUMO

The aim of this study was to evaluate the suitability of a non-disruptive Raman spectroscopic method to quantify drug concentrations below 5 w% within a polymer matrix produced by hot-melt extrusion (HME). For calibration, praziquantel (PZQ)-polyvinylpyrrolidone-vinylacetat-copolymer (PVP-VA) mixtures were extruded. By focusing the laser light of the Raman probe to a diameter of 1 mm and implementing a self-constructed filament holder, the signal-to-noise (S/N) ratio could be reduced considerably. The obtained Raman spectra show quite high fluorescence, which is likely to be caused by dissolved pharmaceutical active ingredient (API) in the polymer matrix. For content determination, HPLC analysis was conducted as a reference method using the same filament segments. A partial least squares (PLS) model, regressing the PZQ concentrations from HPLC method analysis versus the off-line collected Raman spectra, was developed. The linear correlation for a suitable extrusion run for the production of low-dosed filaments (extrusion 1, two kneading zones) is acceptable (R2 = 0.9915) while the correlation for a extrusion set-up with low miscibility (extrusion 2; without kneading zone) is unacceptable (R2 = 0.5349). The predictive performance of the calibration model from extrusion 1 is rated by the root mean square error of estimation (RMSEE), which was 0.08%. This calibration can now be used to validate the content of low-dosed filaments during HME.


Assuntos
Povidona , Análise Espectral Raman , Análise Espectral Raman/métodos , Povidona/química , Polímeros/química , Tecnologia de Extrusão por Fusão a Quente , Composição de Medicamentos/métodos , Temperatura Alta
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