RESUMO
Although titanium and its alloys are widely used as dental implants, they cannot induce the formation of new bone around the implant, which is a basis for the functional integrity and long-term stability of implants. This study focused on the functionalization of the titanium/titanium oxide surface as the gold standard for dental implants, with electrospun composite fibers consisting of polyvinylpyrrolidone and Ca2+ ions. Polymer fibers as carriers of Ca2+ ions should gradually dissolve, releasing Ca2+ ions into the environment of the implant when it is immersed in a model electrolyte of artificial saliva. Scanning electron microscopy, energy dispersive X-ray spectroscopy and attenuated total reflectance Fourier transform infrared spectroscopy confirmed the successful formation of a porous network of composite fibers on the titanium/titanium oxide surface. The mechanism of the formation of the composite fibers was investigated in detail by quantum chemical calculations at the density functional theory level based on the simulation of possible molecular interactions between Ca2+ ions, polymer fibers and titanium substrate. During the 7-day immersion of the functionalized titanium in artificial saliva, the processes on the titanium/titanium oxide/composite fibers/artificial saliva interface were monitored by electrochemical impedance spectroscopy. It can be concluded from all the results that the composite fibers formed on titanium have application potential for the development of osteoinductive and thus more biocompatible dental implants.
Assuntos
Cálcio , Implantes Dentários , Titânio , Titânio/química , Cálcio/química , Cálcio/metabolismo , Povidona/química , Humanos , Íons/química , Espectroscopia de Infravermelho com Transformada de Fourier , Saliva Artificial/química , Materiais Biocompatíveis/química , Espectrometria por Raios X , Osteogênese/efeitos dos fármacosRESUMO
Additive manufacturing can develop regenerative scaffolds for wound healing. 3D printing offers meticulous porosity, mechanical integrity, cell adhesion and cost-effectiveness. Herein, we prepared ink composed of carboxymethyl cellulose (CMC), polyvinylpyrrolidone (PVP), collagen, and oregano extract for the fabrication of tissue constructs. The blend was optimized to form a homogeneous ink and rheological characterization demonstrated shear thinning behavior. The scaffolds were printed using Direct Ink Write (DIW) at a flow speed of 4 mm3/s and a layer height of 0.18 mm. The fabricated scaffolds demonstrated an ultimate tensile strength (UTS) and toughness of 730 KPa and 2.72 MJ/m3, respectively. Scanning Electron Microscopy (SEM) revealed an average pore size of 300 ± 30 µm. Fourier transform infrared spectroscopy (FTIR) analysis confirmed that all materials were present. The contact angle of the composite scaffold was 68° ± 1°. Moreover, the scaffolds presented 82 % mass loss (degradation) in phosphate buffer saline (PBS) over 14 days. The composite scaffold exhibited inhibition zones of 9 mm and 12 mm against Staphylococcus aureus and Escherichia coli, respectively. The PVP/CMC/collagen/oregano 3D printed scaffolds exhibited excellent biocompatibility with the mesenchymal stem cells and humman dermal fibroblast cells, confirmed by water-soluble tetrazolium - 8 (WST-8) assay (test conducted for 7 days). The enhanced angiogenic potential of said scaffold was assesed by release of vascular endothelial growth factor followed by further validation through in-vivo CAM assay. Thus, confirming suitability for the potential wound healing application.
Assuntos
Carboximetilcelulose Sódica , Colágeno , Origanum , Povidona , Alicerces Teciduais , Cicatrização , Povidona/química , Cicatrização/efeitos dos fármacos , Carboximetilcelulose Sódica/química , Carboximetilcelulose Sódica/farmacologia , Alicerces Teciduais/química , Colágeno/química , Colágeno/farmacologia , Humanos , Origanum/química , Staphylococcus aureus/efeitos dos fármacos , Impressão Tridimensional , Materiais Biocompatíveis/química , Materiais Biocompatíveis/farmacologia , Escherichia coli/efeitos dos fármacos , Tinta , Fibroblastos/efeitos dos fármacos , Fibroblastos/citologia , Células-Tronco Mesenquimais/efeitos dos fármacos , Células-Tronco Mesenquimais/citologia , Antibacterianos/farmacologia , Antibacterianos/química , Porosidade , Resistência à Tração , AnimaisRESUMO
This study aimed to enhance the properties of polyvinylpyrrolidone (PVP) for use as biocompatible facial masks. To achieve this, nanofibers were developed by blending PVP with cellulose nanofibers (CNFs) and Aloe vera (AV) powder using electrospinning. The results showed that incorporating CNFs and AV into the PVP matrix led to the formation of smooth and uniform nanofibers. In particular, adding 3-6 wt% AV powder in PVP/CNF composites improved fiber diameter distribution and uniformity compared to pure PVP. The PVP/CNF/AV nanofibers exhibited desirable properties for facial mask applications. They displayed 86-93 % porosity, which allowed for efficient moisture absorption capacity of up to 1829 %, and excellent water vapor permeability rate of 3.92 g/m2h. The mechanical properties of the electrospun nanofiber composites were evaluated through tensile testing. The results showed that Young's modulus values decreased progressively with the addition of CNFs and AV powder to the PVP polymer matrix, indicating a plasticizing effect that enhances flexibility. The fracture strain remained similar across all composites, suggesting that CNFs and AV did not significantly weaken the PVP matrix. The tensile strength initially increased with CNF addition but decreased with incremental AV loading. Biocompatibility studies revealed that all nanofibers exhibited excellent fibroblast viability, surpassing 98 %. This indicates that incorporating CNFs and AV did not compromise cell viability, further highlighting the suitability of the PVP/CNF/AV composites for facial mask applications.
Assuntos
Aloe , Materiais Biocompatíveis , Celulose , Nanofibras , Povidona , Nanofibras/química , Povidona/química , Celulose/química , Materiais Biocompatíveis/química , Aloe/química , Resistência à Tração , Permeabilidade , Porosidade , Teste de Materiais , Animais , Vapor , Sobrevivência Celular/efeitos dos fármacos , Camundongos , Fibroblastos/efeitos dos fármacos , Fibroblastos/citologiaRESUMO
The metastability of amorphous formulations poses barriers to their safe and widespread commercialization. The propensity of amorphous solid dispersions (ASDs) to crystallize is directly linked to their molecular structure. Amorphous structures are inherently complex and thus difficult to fully characterize by experiments, which makes structural simulations an attractive route for investigating which structural characteristics correlate with ASD stability. In this study, we use empirical potential structure refinement (EPSR) to create molecular models of ketoprofen-poly(vinylpyrrolidone) (KTP/PVP) ASDs with 0-75 wt % drug loading. The EPSR technique uses X-ray total scattering measurements as constraints, yielding models that are consistent with the X-ray data. We perform several simulations to assess the sensitivity of the EPSR approach to input parameters such as intramolecular bond rotations, PVP molecule length, and PVP tacticity. Even at low drug loading (25 wt %), â¼40% of KTP molecules participate in KTP-KTP hydrogen bonding. The extent of KTP-PVP hydrogen bonding does not decrease significantly at higher drug loadings. However, the models' relative uncertainties are too large to conclude whether ASDs' lower stabilities at high drug loadings are due to changes in drug-excipient hydrogen bonding or a decrease in steric hindrance of KTP molecules. This study illustrates how EPSR, combined with total scattering measurements, can be a powerful tool for investigating structural characteristics in amorphous formulations and developing ASDs with improved stability.
Assuntos
Cetoprofeno , Povidona , Difração de Raios X , Cetoprofeno/química , Povidona/química , Difração de Raios X/métodos , Cristalização , Química Farmacêutica/métodos , Composição de Medicamentos/métodos , Modelos Moleculares , Estabilidade de MedicamentosRESUMO
Uveitis comprises a cluster of intraocular inflammatory disorders characterized by uncontrolled autoimmune responses and excessive oxidative stress leading to vision loss worldwide. In the present study, curcumin (CUR) was conjugated with polyvinylpyrrolidone (PVP) to form PVP-CUR nanoparticles with significantly elevated solubility and outstanding multiple radical scavenging abilities. In vitro studies revealed that PVP-CUR nanoparticles markedly mitigated oxidative stress and reduced apoptosis in a H2O2-induced human retinal pigment epithelial cell line (ARPE-19) and promoted phenotypic polarization from M1 to M2 in an LPS-induced human microglial cell line (HMC3). Further in vivo studies demonstrated the prominent therapeutic effects of PVP-CUR nanoparticles on experimental autoimmune uveitis (EAU), which relieved clinical and pathological progression, improved perfusion and tomographic manifestations of retinal vessels, and reduced blood-retinal barrier (BRB) leakage; these effects may be mediated by mitigating oxidative stress and attenuating macrophage/microglia-elicited inflammation. Notably, treatment with PVP-CUR nanoparticles was shown to regulate metabolite alterations in EAU rats, providing novel insights into the underlying mechanisms involved. Additionally, the PVP-CUR nanoparticles showed great biocompatibility in vivo. In summary, our study revealed that PVP-CUR nanoparticles may serve as effective and safe nanodrugs for treating uveitis and other oxidative stress- and inflammation-related diseases.
Assuntos
Doenças Autoimunes , Curcumina , Nanopartículas , Estresse Oxidativo , Povidona , Uveíte , Animais , Curcumina/administração & dosagem , Curcumina/farmacologia , Curcumina/química , Curcumina/uso terapêutico , Uveíte/tratamento farmacológico , Uveíte/imunologia , Uveíte/metabolismo , Povidona/química , Povidona/administração & dosagem , Nanopartículas/administração & dosagem , Nanopartículas/química , Humanos , Doenças Autoimunes/tratamento farmacológico , Linhagem Celular , Estresse Oxidativo/efeitos dos fármacos , Epitélio Pigmentado da Retina/efeitos dos fármacos , Epitélio Pigmentado da Retina/metabolismo , Ratos , Feminino , Ratos Endogâmicos Lew , Barreira Hematorretiniana/efeitos dos fármacos , Barreira Hematorretiniana/metabolismo , MasculinoRESUMO
Increased antineoplastic drug concentrations in wastewater stem from ineffective treatment plants and increased usage. Although microrobots are promising for pollutant removal, they face hurdles in developing a superstructure with superior adsorption capabilities, biocompatibility, porosity, and pH stability. This study focused on adjusting the PVP concentration from 0.05 to 0.375 mM during synthesis to create a favorable CMOC structure for drug absorption. Lower PVP concentrations (0.05 mM) yielded a three-dimensional nanoflower structure of CaMoO4 and CuS nanostructures, whereas five-fold concentrations (0.25 mM) produced a porous structure with a dense CuS core encased in a transparent CaMoO4 shell. The magnetically movable and pH-stable COF@CMOC microrobot, achieved by attaching CMOC to cobalt ferrite (CoF) NPs, captured doxorubicin efficiently, with up to 57 % efficiency at 200 ng/mL concentration for 30 min, facilitated by electrostatic interaction, hydrogen bonding, and pore filling of DOX. The results demonstrated that DOX removal through magnetic motion showed superior performance, with an estimated improvement of 57% compared to stirring conditions (17 %). A prototype PDMS microchannel system was developed to study drug absorption and microrobot recovery. The CaMoO4 shell of the microrobots exhibited remarkable robustness, ensuring long-lasting functionality in harsh wastewater environments and improving biocompatibility while safeguarding the CuS core from degradation. Therefore, microrobots are a promising eco-friendly solution for drug extraction. These microrobots show promise for the selective removal of doxorubicin from contaminated wastewater.
Assuntos
Cobalto , Nanoestruturas , Povidona , Águas Residuárias , Poluentes Químicos da Água , Águas Residuárias/química , Povidona/química , Porosidade , Poluentes Químicos da Água/química , Poluentes Químicos da Água/análise , Nanoestruturas/química , Cobalto/química , Concentração de Íons de Hidrogênio , Adsorção , Doxorrubicina/química , Compostos Férricos/químicaRESUMO
To develop a submucosal injection material with sustained submucosal lifting for endoscopic submucosal dissection (ESD), this study designed and prepared a novel composite thermosensitive hydrogel system with high pH chitosan-polyvinylpyrrolidone-ß-glycerophosphate (HpHCS-PVP-GP). HpHCS improved the injectability of the hydrogels and retained the rapid gelation ability at low concentrations. The modification of PVP significantly improved the stability of low-temperature hydrogel precursor solutions and the integrity of hydrogels formed at 37 °C through hydrogen bonds between PVP and HpHCS. A mathematical model was established using response surface methodology (RSM) to evaluate the synergistic effect of HpHCS, GP, and PVP concentrations on gelation time. This RSM model and submucosal lifting evaluation using in vitro pig esophageal models were used to determine the optimal formula of HpHCS-PVP-GP hydrogels. Although the higher PVP concentration (5 % (w/v)) prolonged gelation time, it improved hydrogel mechanical strength, resulting in better submucosal lifting performance. The experiments of Bama mini pigs showed that the heights of the cushions elevated by the HpHCS-5%PVP-GP hydrogel remained about 80 % 1 h after injection. Repeated injections were avoided, and the hydrogel had no cytotoxicity after electric cutting. Therefore, the HpHCS-PVP-GP thermosensitive hydrogel might be a promising submucosal injection material for ESD.
Assuntos
Quitosana , Ressecção Endoscópica de Mucosa , Hidrogéis , Povidona , Temperatura , Hidrogéis/química , Animais , Suínos , Povidona/química , Quitosana/química , Ressecção Endoscópica de Mucosa/métodos , Injeções , Glicerofosfatos/químicaRESUMO
Inclusion complexes require higher concentration of Beta cyclodextrins (ßCD) resulting in increased formulation bulk, toxicity, and production costs. This systematic review offers a comprehensive analysis using Quality by design (QbD) as a tool to predict potential applications of Polyvinylpyrrolidone (PVP) as a ternary substance to address issues of inclusion complexes. We reviewed 623 documents from 2013 to 2023 and Eighteen (18) research papers were selected for statistical and meta-analysis using the QbD concept to identify the most critical factors for selecting drugs and effect of PVP on inclusion complexes. The QbD analysis revealed that Molecular weight (MW), Partition coefficient (Log P), and the auxiliary substance ratio directly affected complexation efficiency (CE), thermodynamic stability in terms of Gibbs free energy (ΔG), and percent drug release. However, Stability constant (Ks) remained unaffected by any of these parameters. The results showed that low MW (250), median Log P (6), and a ßCD: PVP ratio of 2:3 would result in higher CE, lower G, and improved drug release. PVP improves drug solubility, enhances delivery and therapeutic outcomes, and counteracts increased drug ionization due to decreased pH. In certain cases, its bulky nature and hydrogen bonding with CD molecules can form non-inclusion complexes. The findings of the study shows that there is potential molecular interaction between PVP and ß-cyclodextrins, which possibly enhances the stability of inclusion complexes for drug with low MW and log P values less than 9. The systematic review shows a comprehensive methodology based on QbD offers a replicable template for future investigations into drug formulation research.
Assuntos
Ciclodextrinas , Povidona , Solubilidade , beta-Ciclodextrinas , beta-Ciclodextrinas/química , Química Farmacêutica/métodos , Ciclodextrinas/química , Liberação Controlada de Fármacos , Excipientes/química , Peso Molecular , Projetos Piloto , Povidona/química , TermodinâmicaRESUMO
This study presents a novel approach by utilizing poly(vinylpyrrolidone)s (PVPs) with various topologies as potential matrices for the liquid crystalline (LC) active pharmaceutical ingredient itraconazole (ITZ). We examined amorphous solid dispersions (ASDs) composed of ITZ and (i) self-synthesized linear PVP, (ii) self-synthesized star-shaped PVP, and (iii) commercial linear PVP K30. Differential scanning calorimetry, X-ray diffraction, and broad-band dielectric spectroscopy were employed to get a comprehensive insight into the thermal and structural properties, as well as global and local molecular dynamics of ITZ-PVP systems. The primary objective was to assess the influence of PVPs' topology and the composition of ASD on the LC ordering, changes in the temperature of transitions between mesophases, the rate of their restoration, and finally the solubility of ITZ in the prepared ASDs. Our research clearly showed that regardless of the PVP type, both LC transitions, from smectic (Sm) to nematic (N) and from N to isotropic (I) phases, are effectively suppressed. Moreover, a significant difference in the miscibility of different PVPs with the investigated API was found. This phenomenon also affected the solubility of API, which was the greatest, up to 100 µg/mL in the case of starPVP 85:15 w/w mixture in comparison to neat crystalline API (5 µg/mL). Obtained data emphasize the crucial role of the polymer's topology in designing new pharmaceutical formulations.
Assuntos
Varredura Diferencial de Calorimetria , Itraconazol , Cristais Líquidos , Povidona , Solubilidade , Difração de Raios X , Itraconazol/química , Cristais Líquidos/química , Povidona/química , Varredura Diferencial de Calorimetria/métodos , Difração de Raios X/métodos , Polímeros/química , Antifúngicos/química , Composição de Medicamentos/métodos , Cristalização , Química Farmacêutica/métodosRESUMO
During the past several decades, nanostructures have played their increasing influences on the developments of novel nano drug delivery systems, among which, double-chamber Janus nanostructure is a popular one. In this study, a new tri-channel spinneret was developed, in which two parallel metal capillaries were nested into another metal capillary in a core-shell manner. A tri-fluid electrospinning was conducted with a solvent mixture as the shell working fluid for ensuring the formation of an integrated Janus nanostructure. The scanning electronic microscopic results demonstrated that the resultant nanofibers had a linear morphology and two distinct compartments within them, as indicated by the image of a cross-section. Fourier Transformation Infra-Red spectra and X-Ray Diffraction patterns verified that the loaded poorly water-soluble drug, i.e. icariin, presented in the Janus medicated nanofibers in an amorphous state, which should be attributed to the favorable secondary interactions between icariin and the two soluble polymeric matrices, i.e. hydroxypropyl methyl cellulose (HPMC) and polyvinylpyrrolidone (PVP). The in vitro dissolution tests revealed that icariin, when encapsulated within the Janus nanofibers, exhibited complete release within a duration of 5 min, which was over 11 times faster compared to the raw drug particles. Furthermore, the ex vivo permeation tests demonstrated that the permeation rate of icariin was 16.2 times higher than that of the drug powders. This improvement was attributed to both the rapid dissolution of the drug and the pre-release of the trans-membrane enhancer sodium lauryl sulfate from the PVP side of the nanofibers. Mechanisms for microformation, drug release, and permeation were proposed. Based on the methodologies outlined in this study, numerous novel Janus nanostructure-based nano drug delivery systems can be developed for poorly water-soluble drugs in the future.
Assuntos
Sistemas de Liberação de Medicamentos , Liberação Controlada de Fármacos , Flavonoides , Derivados da Hipromelose , Nanofibras , Povidona , Solventes , Nanofibras/química , Animais , Solventes/química , Povidona/química , Flavonoides/química , Flavonoides/administração & dosagem , Flavonoides/farmacocinética , Sistemas de Liberação de Medicamentos/métodos , Derivados da Hipromelose/química , Solubilidade , Absorção Cutânea , Masculino , RatosRESUMO
Biopolymers have the utmost significance in biomedical applications and blending synthetic polymers has shown favorable characteristics versus individual counterparts. The utilization of the blends can be restricted through the use of toxic chemical agents such as initiators or crosslinkers. In this regard, a chemical agent-free ionizing irradiation is a beneficial alternative for preparing the hydrogels for biomedical applications. In this study, carboxymethyl chitosan (CM-CS), guar gum (GG), and poly(vinylpyrrolidone) (PVP) based ternary blends (TB) were crosslinked using various doses of ionizing irradiation to fabricate hydrogels. The prepared hydrogels were characterized for physicochemical properties, swelling analysis, biological assays, and drug delivery applications. Swelling analysis in distilled water revealed that the hydrogels exhibit excellent swelling characteristics. An in vitro cytocompatibility assay showed that the hydrogels have greater than 90% cell viability for the human epithelial cell line and a decreasing cell viability trend for the human alveolar adenocarcinoma cell line. In addition, the prepared hydrogels possessed excellent antibacterial characteristics against gram-positive Staphylococcus aureus (S. aureus) and gram-negative Escherichia coli (E. coli). Finally, the release studies of anti-inflammatory Quercus acutissima (QA) loaded hydrogels exhibited more than 80% release in phosphate-buffered saline (pH = 7.4). These findings suggest that TB hydrogels can be used as suitable carrier media for different release systems and biomedical applications.
Assuntos
Antibacterianos , Antineoplásicos , Sobrevivência Celular , Quitosana , Escherichia coli , Galactanos , Hidrogéis , Mananas , Gomas Vegetais , Povidona , Staphylococcus aureus , Quitosana/química , Quitosana/análogos & derivados , Quitosana/síntese química , Quitosana/farmacologia , Gomas Vegetais/química , Galactanos/química , Hidrogéis/química , Hidrogéis/síntese química , Hidrogéis/farmacologia , Mananas/química , Antibacterianos/farmacologia , Antibacterianos/química , Antibacterianos/síntese química , Humanos , Staphylococcus aureus/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Povidona/química , Antineoplásicos/farmacologia , Antineoplásicos/química , Antineoplásicos/síntese química , Sobrevivência Celular/efeitos dos fármacos , Portadores de Fármacos/química , Liberação Controlada de Fármacos , Células A549RESUMO
Peripheral nerve injuries (PNI) impact millions of individuals in the United States, prompting thousands of nerve repair procedures annually. Nerve conduits (NC) are commonly utilized to treat nerve injuries under 3 cm but larger gaps still pose a challenge for successful peripheral nerve regeneration (PNR) and functional recovery. This is partly attributed to the absence of bioactive agents such as stem cells or growth factors in FDA-approved conduits due to safety, harvesting, and reproducibility concerns. Therefore, curcumin, a bioactive phytochemical, has emerged as a promising alternative bioactive agent due to its ability to enhance PNR and overcome said challenges. However, its hydrophobicity and rapid degradation in aqueous solutions are considerable limitations. In this work, a nanoscale delivery platform with tannic acid (TA) and polyvinylpyrrolidone (PVP) was developed to encapsulate curcumin for increased colloidal and chemical stability. The curcumin nanoparticles (CurNPs) demonstrate significantly improved stability in water, reduced degradation rates, and controlled release kinetics when compared to free curcumin. Further, cell studies show that the CurNP is biocompatible when introduced to neuronal cells (SH-SY5Y), rat Schwann cells (RSC-S16), and murine macrophages (J774 A.1) at 5 µM, 5 µM, and 10 µM of curcumin, respectively. As a result of these improved physicochemical properties, confocal fluorescence microscopy revealed superior delivery of curcumin into these cells when in the form of CurNPs compared to its free form. A hydrogen peroxide-based oxidative stress study also demonstrated the CurNP's potential to protect J774 A.1 cells against excessive oxidative stress. Overall, this study provides evidence for the suitability of CurNPs to be used as a bioactive agent in NC applications.
Assuntos
Curcumina , Nanopartículas , Curcumina/farmacologia , Curcumina/química , Animais , Ratos , Nanopartículas/química , Camundongos , Humanos , Sistemas de Liberação de Medicamentos , Regeneração Nervosa/efeitos dos fármacos , Polímeros/química , Células de Schwann/efeitos dos fármacos , Liberação Controlada de Fármacos , Taninos/química , Taninos/farmacologia , Linhagem Celular , Estresse Oxidativo/efeitos dos fármacos , Povidona/químicaRESUMO
The use of targeted drug delivery systems, including those based on selective absorption by certain receptors on the surface of the target cell, can lead to a decrease in the minimum effective dose and the accompanying toxicity of the drug, as well as an increase in therapeutic efficacy. A fullerene C60 conjugate (FA-PVP-C60) with polyvinylpyrrolidone (PVP) as a biocompatible spacer and folic acid (FA) as a targeting ligand for tumor cells with increased expression of folate receptors (FR) was obtained. Using 13C NMR spectroscopy, FT-IR, UV-Vis spectrometry, fluorometry and thermal analysis, the formation of the conjugate was confirmed and the nature of the binding of its components was established. The average particle sizes of the conjugate in aqueous solutions and cell culture medium were determined using dynamic light scattering (DLS) and nanoparticle tracking analysis (NTA). The FA-PVP-C60 showed antiradical activity against â¢DPPH, â¢OH and O2â¢-, but at the same time, it was shown to generate 1O2. It was found that the conjugate in the studied concentration range (up to 200 µg/mL) is non-toxic in vitro and does not affect the cell cycle. To confirm the ability of the conjugate to selectively accumulate through folate-mediated endocytosis, its uptake into cells was analyzed by flow cytometry and confocal microscopy. It was shown that the conjugate is less absorbed by A549 cells with low FR expression than by HeLa, which has a high level of expression of this receptor.
Assuntos
Sistemas de Liberação de Medicamentos , Ácido Fólico , Fulerenos , Povidona , Ácido Fólico/química , Ácido Fólico/farmacologia , Humanos , Povidona/química , Fulerenos/química , Fulerenos/farmacologia , Sistemas de Liberação de Medicamentos/métodos , Linhagem Celular Tumoral , Células A549 , Células HeLa , Tamanho da PartículaRESUMO
The aim of this study was to investigate whether it is possible to prevent oolemma lysis after Piezo-assisted intracytoplasmic sperm injection (Piezo-ICSI) caused by abnormal membrane rupture. A total of 489 mature oocytes were obtained from 85 patients who underwent Piezo-ICSI in an infertility clinic. Inseminated oocytes were classified into the following two groups: normal rupture and abnormal rupture, and a portion of abnormally ruptured oocytes was randomly exposed to 7% PVP solution. Normal fertilization rate, degeneration rate, proportion of high-quality embryos on day 3, blastocyst formation, and morphologically high-quality blastocysts were compared. Abnormal rupture was defined as cytoplasmic membrane rupture before piezo pulse driving. Among the abnormal rupture groups, the normal fertilization and degeneration rates were compared between the high-stretched (ruptured at ≥ 50% during oocyte membrane stretching) and low-stretched (< 50% position) oocytes.The degeneration rate was significantly higher in abnormally ruptured oocytes than in normally ruptures oocytes (14.3% vs 1.3%, p < 0.001), and there was no significant difference in embryonic development after fertilization. PVP treatment immediately after oolemma rupture significantly decreased the degeneration rate (6.0% vs 19.7%, p = 0.031) and increased the normal fertilization rate. Similarly, there were no significant differences in the developmental potential. Furthermore, pregnancy outcome data showed no significant differences in pregnancy and live birth rates. The degeneration rate was reduced by treating low-stretched oocytes with PVP.Exposure to polyvinylpyrrolidone (PVP) immediately after abnormal membrane rupture represents an effective strategy to prevent oocyte degeneration. This is the first study to propose a strategy for the prevention of oocyte degeneration in Piezo-ICSI. These findings are expected to reduce the oocyte degeneration rate and increase normal fertilization rate as well as assist patients who can only acquire oocytes with weak plasma membranes.
Assuntos
Membrana Celular , Oócitos , Povidona , Injeções de Esperma Intracitoplásmicas , Humanos , Injeções de Esperma Intracitoplásmicas/métodos , Feminino , Adulto , Desenvolvimento Embrionário/efeitos dos fármacos , Gravidez , Fertilização/efeitos dos fármacos , MasculinoRESUMO
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 , SolubilidadeRESUMO
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 FourierRESUMO
The results of the synthesis of microcrystalline calcium phosphates such as hydroxoapatite, pyrophosphate, and tricalcium phosphate are presented herein. The influence of the addition of polyvinylpyrrolidone (PVP) on the phase characteristics of the resulting high-temperature ceramic sample is considered. The X-ray results show that hydroxyapatite (HAp) consists of a Ca5(PO4)3(OH) phase, while the sample with the addition of polyvinylpyrrolidone contains ß-Ca3(PO4)2 (65.5%) and ß-Ca2P2O7 (34.5%) phases calcium phosphates (CPs). IR spectroscopy was used to characterize the compositions of the samples. An important characteristic of the obtained samples is the elemental Ca/P ratio, which was determined via energy-dispersive analysis. The data obtained are consistent with the composition of dental enamel apatites, namely, in the CPs (1.27) and HAp (1.40). SEM was used to study the morphology of the surfaces of hydroxyapatite particles. Polyvinylpyrrolidone polymer fibers were obtained using the electroforming method with the inclusion of CPs in the composition. The fibers were oriented randomly, and nanoscale hydroxyapatite particles were incorporated into the fiber structure. Solubility data of the HAp, CPs, and Fibers in a physiological solution at room temperature and human body temperature were obtained. The solubility of the resulting HAp turned out to be higher than the solubility of the CPs. In turn, the concentration of Ca2+ in a physiological solution of PVP composite fibers with the inclusion of CPs was lower than that in powdered CPs.
Assuntos
Fosfatos , Povidona , Humanos , Temperatura , Fosfatos de Cálcio/química , Durapatita/química , Apatitas , Difração de Raios XRESUMO
Objective: Adverse effects of polyvinylpyrrolidone (PVP) on sperm membrane and chromatin have been proven in many studies. Among the natural products proposed as an alternative for PVP, thymoquinone (TQ)-a major constituent of Nigella sativa plant- has been suggested as a potential natural spermostasis. Therefore, this study aimed to compare the effects of TQ with PVP for sperms motility, survival, DNA denaturation, and DNA fragmentation in normozoospermic men (men with a normal or healthy sperm profile). Methods: An experimental trial was carried out on 30 normozoospermic men of the Andrology Unit of (Shahid Beheshti Hospital, Isfahan, Iran). Each washed semen samples were divided into four fractions and was randomly treated with TQ (50 µg/ml), %5 PVP, and %10 PVP (M/V) which was compared to untreated fraction (control). Results: There was a significant difference between the four groups in terms of motility, viability, DNA denaturation, and fragmentation (P <0.05). TQ caused sperm immobility, while 5% PVP and 10% PVP decreased (98 and 99%, respectively) sperm motility compared to control. TQ did not affect sperm viability compared to the control group, but PVP decreased it. Besides, TQ did not affect DNA denaturation and fragmentation, but PVP increased it. Conclusion: TQ could be used as an alternative natural spermostasis with less adverse effects rather than PVP which causes more efficient immobilization and isolation of individual sperm cells.
RESUMO
Amorphous solid dispersions (ASD) are known to enhance the absorption of poorly water-soluble drugs. In this work we synthesise well-defined Polyvinylpyrrolidone (PVP) to establish the impact of dispersity and chain-end functionality on the physical properties of Curcumin (CUR)/PVP ASD. Thermodynamic characterisation of synthesised PVP emphasises a strong effect of the dispersity on the glass transition temperature (Tg), 50 °C higher for synthesised PVP than for commercial PVP K12 of same molar mass. This increase of Tg affects the thermodynamic properties of CUR/PVP ASD successfully formulated up to 70 wt% of CUR by milling or solvent evaporation. The evolution of both the Tg and CUR solubility values versus CUR content points out the development of fairly strong CUR-PVP interactions that strengthen the antiplasticising effect of PVP on the Tg of ASD. However, for ASD formulated with commercial PVP this effect is counterbalanced at low CUR content by a plasticising effect due to the shortest PVP chains. Moreover, the overlay of the phase and state diagrams highlights the strong impact of the polymer dispersity on the stability of CUR/PVP ASD. ASD formulated with low dispersity PVP are stable on larger temperature and concentration ranges than those formulated with PVP K12.
Assuntos
Curcumina , Polímeros , Povidona , Solubilidade , Temperatura de TransiçãoRESUMO
Chitosan/polyvinylpyrrolidone composite films containing hydroalcoholic Ziziphora clinopodioides extract were developed and evaluated for their potential use as wound dressings. The physical and chemical properties of the films were extensively explored, including swelling capacity, mechanical properties, antimicrobial activity, and microstructural characteristics. The results showed that the addition of Ziziphora extract significantly increased the swelling capacity of the films by 561.24% to 1175% (p < 0.05). While tensile strength and Young's modulus were enhanced, elongation at the breaking point decreased with increasing volume percentages of Ziziphora extract. Variance analysis indicated no statistically significant effect on the tensile properties of the films with varying Ziziphora extract content (p < 0.05). Furthermore, films incorporated with Ziziphora extract demonstrated antimicrobial properties. Scanning electron microscopy (SEM) analysis revealed that samples lacking Ziziphora extract had a smooth surface, while those containing the extract displayed a rough texture that may potentially accelerate the wound healing process.