RESUMO
In the present study fast dispersible nimodipine tablets were developed by direct compression method using quality by design (QbD) approach as per the central composite design by selecting avicel PH 102 (X1) and crospovidone (X2) as independent variables while % friability (R1), disintegration (R2) and hardness (R3) as output variables. Powder blends were assessed for flow characterization. At post compressional stage, several quality assessments were carried out. Particles morphology was observed using scanning electron microscopy (SEM). The stability study on the drug and optimized formulation were determined using thermal gravimetric analysis (TGA) and differential thermal analysis (DTA). RSM plots expressed the interaction of avicel PH 102 and crospovidone to determine the adequate quantities of excipients for the optimized formulation. Polynomial equations were used to validate the experimental design. The optimized formulations were evaluated for friability, disintegration and hardness. Results indicated that formulation (F4) containing avicel PH 102 (35%) and crospovidone (5%) was selected as best optimized formulation having friability 0.59%, disintegration 9 sec, % dissolution 95.703% and hardness 4.14 kg. Results of kinetics models indicated that all the developed formulations followed weibull model.
Assuntos
Química Farmacêutica , Nimodipina , Química Farmacêutica/métodos , Cinética , Povidona , Solubilidade , Comprimidos , CeluloseRESUMO
The solid dispersion technique is the most effective and widely used approach for increasing the solubility and release of drugs that have low water solubility. Mirtazapine (MRT) is an atypical antidepressant used to treat severe depression. MRT has a low oral bioavailability (about 50%) due to its low water solubility (BCS class II). The study's goal was to determine optimum conditions for incorporating MRT into various polymer types utilizing the solid dispersion (SD) technique, with the goal of selecting the most suitable formula with the optimal aqueous solubility, loading efficiency, and dissolution rate. The D-optimal design was used to pick the optimal response. The optimum formula was subjected to physicochemical evaluation by Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD), and scanning electron microscopy (SEM). In vivo bioavailability study was conducted on white rabbits' plasma samples. MRT-SDs were prepared by the solvent evaporation method using Eudragit (RL-100, RS-100, E-100, L-100-55), PVP K-30, and PEG 4000 with different drug/polymer percentages (33.33%, 49.99%, and 66.66%). Results showed that the optimum formula obtained using PVP K-30 at a drug percentage of 33.33% gave a loading efficiency of 100.93%, an aqueous solubility of 0.145 mg/ml, and a dissolution rate of 98.12% after 30 min. These findings demonstrated promising enhancement of MRT properties and increasing its oral bioavailability by 1.34-fold more than plain drug.
Assuntos
Química Farmacêutica , Polímeros , Animais , Coelhos , Espectroscopia de Infravermelho com Transformada de Fourier/métodos , Mirtazapina , Química Farmacêutica/métodos , Disponibilidade Biológica , Polímeros/química , Povidona/química , Difração de Raios X , Solubilidade , Água , Varredura Diferencial de Calorimetria , Portadores de Fármacos/químicaRESUMO
In forensic crime scene investigations, biological fluids such as blood are commonly found in soil. However, the analysis of blood-stained soil can be challenging due to the presence of inhibitors which limit the effective extraction and amplification of the deoxyribonucleic acid (DNA) required to produce a reportable DNA profile. There are some extraction methods that have been applied to blood-stained soil in forensic science, but these have produced sporadic results. This research has taken a number of different extraction methods from the fields of ancient DNA and environmental DNA and broken them down into the individual steps of pre-treatment, incubation, separation and purification. These steps were assessed independently then combined into various extraction methods to determine the best technique that can effectively and reliably profile human DNA from blood-stained soil. Testing involved assessment of three extraction buffers, (cetyltrimethylammonium bromide, guanidine thiocyanate, and proteinase K), four pre-treatment methods, (polyvinylpyrrolidone, ethylenediaminetetraacetic acid, hydrochloric acid, and sodium hydroxide), three separation steps, (centrifugation, phenol chloroform, and chloroform) and four purification steps, (size exclusion chromatography, bind elute columns, isopropanol precipitation and silica magnetic beads). The most effective procedure was found to be a polyvinylpyrrolidone pre-treatment with a proteinase K extraction buffer followed by magnetic silica bead purification with or without centrifugation. However, centrifugation separation was found to be equally effective after the pre-treatment step as after the incubation step. Our results shows that most of the current forensic procedures would benefit from the addition of a pre-treatment step prior to processing through the automated DNA profiling pipeline.
Assuntos
Manchas de Sangue , Solo , Humanos , Reação em Cadeia da Polimerase/métodos , DNA/análise , Clorofórmio/análise , Povidona , Endopeptidase K , Dióxido de SilícioRESUMO
Dyes are recalcitrait organic pollutants threatening the aquatic environment and human health. In the present study, a novel low-cost hybrid membrane was fabricated by coating polyurethane foam (PUF) with polyacrylonitrile/polyvinylpyrrolidone (PAN/PVP) via phase inversion technique from casting solutions consisting of PAN and PVP with Dimethyl formamide (DMF) and applied for removal of cationic (Methylene Blue (MB)) and anionic (Methyl Orange (MO)) dyes from aqueous solutions. The as-prepared membrane was first characterized by Scan Electron Microscope (SEM), Fourier Transform Infrared (FTIR), Energy Dispersive Spectrometry (EDS), etc. Then, batch experiments were conducted to optimize the adsorption conditions, including contact time, adsorbent dose, dyes concentration, and pH. The dye removal results fitted with pseudo first and second-order kinetics; Langmuir, Freundlich, and Temkin isotherms' models. The maximum dye decolorization was approximately 97% and 95% within 60 and 120 min using 0.5 and 1 g of the fabricated composite for MB and MO, respectively. The kinetic studies showed rapid sorption dynamics following a second-order kinetic model. In addition, dye adsorption equilibrium data fitted well to the Freundlich isotherm with monolayer maximum adsorption capacity of 6.356 and 3.321 mg/g for MO and MB dye, respectively. Thus, the novel hybrid membrane is promising as a cheap and efficient adsorbent for the removal of both cationic and anionic dyes from wastewater. The current study demonstrated a new avenue to achieve efficient management of dyes in aquatic environments.
Assuntos
Corantes , Poluentes Químicos da Água , Resinas Acrílicas , Adsorção , Ânions , Cátions , Corantes/química , Humanos , Concentração de Íons de Hidrogênio , Cinética , Azul de Metileno/química , Poliuretanos , Povidona , Poluentes Químicos da Água/químicaRESUMO
Paracetamol-loaded tablets were printed by fused deposition modelling technique, using polyvinyl alcohol as a backbone polymer and Affinisol™ HPMC as a plasticizer in all formulations. Four different strategies were applied in order to accelerate the drug release from the tablets. First, different release enhancers were added: sodium starch glycolate, croscarmellose sodium, Kollidon CL and mannitol. Kollidon CL and mannitol showed the greatest influence on the drug dissolution rate. The second strategy included lowering the infill density, which did not make any significant changes in dissolution profiles, according to the calculated similarity factor. Then the best two release enhancers from the first strategy were combined (Kollidon CL and mannitol) and this proved to be the most effective in the drug release acceleration. The fourth strategy, increasing the percentage of the release enhancers in formulation, revealed the importance of their concentration limits. In summary, the drug release accelerated from 58% released after 5 h to reaching the plateau within 2 h. In silico physiologically-based biopharmaceutics modelling showed that formulations with mannitol and Kollidon CL, especially the formulation containing a combination of these release enhancers, can provide relatively fast drug release and extent of drug absorption that complies with an immediate release tablet.
Assuntos
Excipientes , Impressão Tridimensional , Liberação Controlada de Fármacos , Povidona , Comprimidos , Tecnologia FarmacêuticaRESUMO
We report a robust technique to fabricate a cost-efficient Raman substrate which is composed of polyvinylpyrrolidone (PVP) coated gold nanoparticles layer on commercial aluminum foil. The layer of metal nanoparticles on the aluminum foil, i.e., the nanoparticle-on-mirror (NPoM) structure was fabricated by spraying nanoparticle colloidal solution directly on the foil. The detection limit (LOD) of NPoM substrate is investigated by performing the SERS for Rhodamine 6G (R6G) with the concentration ranging from mM to nM without any post treatment of the substrate. The findings show that the LOD of 1 nM and maximum intensity enhancement factor of ~ 24 is accomplished. Field enhancement owing to reflection from the metallic mirror is the reason behind the signal enhancement and it would be beneficial for routine clinical applications, trace chemical detection, and disease diagnostics.
Assuntos
Nanopartículas Metálicas , Análise Espectral Raman , Análise Custo-Benefício , Ouro , PovidonaRESUMO
Due to the antibacterial characteristics, numerous-growing applications of silver nanoparticles (AgNPs) and its coated forms impact water treatment by ozone. The influence of ozone on the aggregation of bare AgNPs and polyvinylpyrrolidone-capped form (PVP-AgNPs) was investigated, as toxicity of NPs depends on particle aggregation/surface charge. Full factorial experimental design was employed to investigate the impact of pH, concentration of NPs' suspension, and ozonation time on bare and PVP-capped AgNPs. Z-Average, zeta potential, and polydispersity index (PdI) of NPs were measured as aggregation criteria. The most effective variables on aggregation of NPs were the coating layer (40-75.5% contribution), pH (14.1-29.6% contribution), and ozonation time (6.5-10.1% contribution), respectively. The aggregation rate increased with increasing ozonation time and decreased with pH. The aggregation of ozonated AgNPs (Z-average up to ~ 4000 nm) was much greater than that of ozonated PVP-AgNPs (Z-average up to ~ 450 nm) due to interaction of ozone-PVP stabilizing layer. During ozonation, the PVP-AgNPs' surface charge shifted from - 6.62 (steric repulsion) to - 29.17 mV (electrosteric repulsion) at pH 7.5, thereby requiring more treatment time to aggregate compared with AgNPs. Graphical abstract.
Assuntos
Nanopartículas Metálicas , Ozônio , Antibacterianos , Povidona , PrataRESUMO
This research planned to ameliorate an aqueous solubility and dissolution of Curcumin (CUR) by the formulation of inclusion complex with ß-cyclodextrin (ß-CD) and polyvinylpyrrolidone (PVP). The phase solubility study was performed to assess the solubility of CUR. The prepared CUR complex assessed for dissolution study, physicochemical evaluation, in-vitro antioxidant activity, molecular modeling, and anti-inflammatory assessment. The pivotal findings of phase-solubility studies demonstrate apparent stability constant (Kc) and complexation efficiency (CE) values for CUR-ß-CD and CUR-ß-CD-PVP complex was 175.4 M -1, 1.15% and 833.3.2 M -1 and 5.21%, respectively. The characterization results revealed amorphization of crystalline state (CUR) into amorphous state. The maximum drug release found with the ternary CUR complex (F7), i.e. 45.41 ± 3.78% in 6 h study. The chemical shift in the NMR supports that the aromatic ring of CUR is completely complexed inside the ß-CD cavity. The antioxidant activity of pure CUR was found to be 58.02 ± 2.21% and CUR ternary complex (F7) showed significantly higher activity to 96.02 ± 2.46%. The in-vivo effect of CUR complex (F7) was also found significantly higher than that of pure CUR. The molecular modeling study depicted that PVP increased the stability of the ternary complex by forming the link between CUR and ß-CD. Thus, the ternary inclusion complex of CUR-ß-CD-PVP could contribute as an innovative outcome in the enhancement of solubility and in-vivo activity.
Assuntos
Anti-Inflamatórios/farmacologia , Curcumina , Povidona/química , beta-Ciclodextrinas , Anti-Inflamatórios/química , Simulação de Acoplamento Molecular , SolubilidadeRESUMO
Aim: This work aimed to develop a mucoadhesive film composed of a triblock copolymer (poloxamer 407), polyvinyl alcohol and polyvinylpyrrolidone for buccal modified delivery of metronidazole. Materials & methods: Three film formulations containing different polymer amounts were prepared by solvent casting. They were characterized as physicochemical, mechanical and mucoadhesive properties, and in vitro metronidazole release profiles. Results: Films displayed physicochemical, mechanical and mucoadhesive characteristics dependent of polymeric composition and drug presence. They could rapidly swell and promote the fast drug release (80% in 20 min) that was governed by Fickian diffusion. The films showed total disintegration in less than 90 s and total drug release in 30 min. Conclusion: Therefore, the formulations represent a promising alternative for modifying of buccal metronidazole delivery for pharmaceutical applications.
Assuntos
Álcool de Polivinil , Povidona , Adesividade , Administração Bucal , Sistemas de Liberação de Medicamentos , Metronidazol , Mucosa Bucal , PoloxâmeroRESUMO
In the present work, biodegradable and flexible chitosan/polyvinylpyrrolidone (CHP) polymeric substrate was fabricated by solvent casting method. This is a novel demonstration of the combination of natural polymer (chitosan) and synthetic polymer (PVP) for next-generation semiconductor device applications. The ZnO thin films were successfully synthesized on these polymeric substrates by facile drop-casting method for gas sensing applications. The hydrogen gas sensing properties of ZnO deposited on the polymeric substrate and SiO2 substrate show similar performance. The structural, morphological, optical, thermal, and tensile strength of the CHP substrate were studied using X-ray diffraction (XRD), Scanning electron microscopy (SEM), UV-visible spectroscopy, Derivative thermogravimetric analysis (DTG), and Universal testing machine (UTM), respectively. Our study suggests that the biodegradable CH/PVP flexible polymeric substrate provides a new way for the implementation of an eco-friendly green substrate in numerous electronic device applications.
Assuntos
Quitosana/química , Análise Custo-Benefício , Hidrogênio/análise , Povidona/química , Óxido de Zinco/química , Quitosana/economia , Hidrogênio/economia , Tamanho da Partícula , Povidona/economia , Semicondutores/economia , Propriedades de Superfície , Óxido de Zinco/síntese química , Óxido de Zinco/economiaRESUMO
BACKGROUND: Due to the appearance of resistant bacterial strains against the antimicrobial drugs and the reduced efficiency of these valuable resources, the health of a community and the economies of countries have been threatened. OBJECTIVE: In this study, the antibacterial assessment of zinc sulfide nanoparticles (ZnS NPs) against Streptococcus pyogenes and Acinetobacter baumannii has been performed. METHODS: ZnS NPs were synthesized through a co-precipitation method using polyvinylpyrrolidone (PVP), polyvinyl alcohol (PVA) and polyethylene glycol (PEG-4000). The size and morphology of the synthesized ZnS NPs were determined by a scanning electron microscope (SEM) and it was found that the average size of the applied NPs was about 70 nm. In order to evaluate the antibacterial effect of the synthesized ZnS NPs, various concentrations (50µg/mL, 100 µg/mL and 150 µg/mL) of ZnS NPs were prepared. Antibacterial assessments were performed through the disc diffusion method in Mueller Hinton Agar (MHA) culture medium and also the optical density (OD) method was performed by a UV-Vis spectrophotometer in Trypticase™ Soy Broth (TSB) medium. Then, in order to compare the antibacterial effects of the applied NPs, several commercial antibiotics including penicillin, amikacin, ceftazidime and primaxin were used. RESULTS: The achieved results indicated that the antibacterial effects of ZnS NPs had a direct relation along with the concentrations and the concentration of 150 µg/mL showed the highest antibacterial effect in comparison with others. In addition, the ZnS NPs were more effective on Acinetobacter baumannii. CONCLUSION: The findings of this research suggest a novel approach against antibiotic resistance.
Assuntos
Acinetobacter baumannii/efeitos dos fármacos , Antibacterianos/química , Nanopartículas Metálicas/química , Streptococcus pyogenes/efeitos dos fármacos , Sulfetos/química , Compostos de Zinco/química , Amicacina/farmacologia , Animais , Antibacterianos/farmacologia , Ceftazidima/farmacologia , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Combinação Imipenem e Cilastatina/farmacologia , Desenvolvimento de Medicamentos , Resistência Microbiana a Medicamentos , Humanos , Testes de Sensibilidade Microbiana , Penicilinas/farmacologia , Polietilenoglicóis/química , Álcool de Polivinil/química , Povidona/química , Ratos , Sulfetos/farmacologia , Compostos de Zinco/farmacologiaRESUMO
Empagliflozin (EGF) received USFDA approval in 2014 for oral use to control the glucose levels in adults with type 2 diabetes mellitus. Albeit, a systematic drug-excipient compatibility study of EGF has not been reported in the open literature. As physical and chemical interactions affect the performance of the formulation, this study intended to unveil the drug and excipients interactions which would later help in development of a robust solid dosage form. Differential scanning calorimetry (DSC) was applied as a screening tool for the assessment of compatibility between EGF and the list of excipients mentioned in the EMEA summary of product characteristics (SmPC)-section 6.1, along with mannitol and polyvinylpyrrolidone. Thermogravimetric analysis (TGA), Fourier Transform Infrared Spectroscopy (FTIR), X-ray Powder Diffraction (PXRD) and Hot Stage Microscopy (HSM) methods were utilized to appraise the interpretation of DSC results adequately. Isothermal stress testing (IST) studies of EGF were performed using the selected excipients to check the presence of interaction products (IPs) and the drug content by HPLC. Additional peaks were observed in the EGF-macrogol mixture than the drug peak in the HPLC analysis after two and half months, and those were separated and identified by the Ultra-High Performance Liquid Chromatography-Quadrupole Time of Flight Mass Spectrometry (UHPLC-QTOF-MS). Overall, EGF had shown compatibility with 13 selected excipients; however, initial observation of DSC and IST studies indicated plausible interaction of the EGF with macrogol.
Assuntos
Compostos Benzidrílicos/química , Excipientes/química , Glucosídeos/química , Varredura Diferencial de Calorimetria/métodos , Química Farmacêutica/métodos , Cromatografia Líquida de Alta Pressão/instrumentação , Formas de Dosagem , Manitol/química , Povidona/química , Espectroscopia de Infravermelho com Transformada de Fourier/métodos , Difração de Raios X/métodosAssuntos
Resinas Acrílicas/química , Materiais Biocompatíveis/química , Hidrogéis/química , Povidona/química , Alicerces Teciduais/química , Resinas Acrílicas/metabolismo , Materiais Biocompatíveis/metabolismo , Adesão Celular , Linhagem Celular , Proliferação de Células , Eritrócitos , Humanos , Hidrogéis/metabolismo , Interações Hidrofóbicas e Hidrofílicas , Mucosa Bucal/citologia , Porosidade , Povidona/metabolismo , Engenharia Tecidual , ÁguaRESUMO
OBJECTIVE: Silver nanoparticles (AgNPs) can be difficult or expensive to obtain or synthesize for laboratories in resource-limited facilities. The purpose of this work was to optimize a synthesis method for a fast, facile, and cost-effective synthesis of AgNPs with antimicrobial activity, which can be readily implemented in non-specialized facilities and laboratories. RESULTS: The optimized method uses a rather simple and rapid chemical reduction process that involves the addition of a polyvinylpyrrolidone solution to a warmed silver nitrate solution under constant vigorous stirring, immediately followed by the addition of sodium borohydride. The total synthesis time is less than 15 min. The obtained AgNPs exhibit an aspect ratio close to 1, with an average size of 6.18 ± 5 nm. AgNPs displayed potent antimicrobial activity, with Minimal Inhibitory Concentration values of ≤ 4 µg mL-1 for Staphylococcus aureus and ≤ 2 µg mL-1 for Candida albicans. The resulting method is robust and highly reproducible, as demonstrated by the characterization of AgNPs from different rounds of syntheses and their antimicrobial activity.
Assuntos
Antibacterianos/síntese química , Antifúngicos/síntese química , Nanopartículas Metálicas/química , Prata/química , Antibacterianos/farmacologia , Antifúngicos/farmacologia , Boroidretos/química , Candida albicans/efeitos dos fármacos , Técnicas de Química Sintética , Nanopartículas Metálicas/ultraestrutura , Testes de Sensibilidade Microbiana , Tamanho da Partícula , Povidona/química , Nitrato de Prata/química , Staphylococcus aureus/efeitos dos fármacosRESUMO
This study demonstrates an effective technique for separating and purifying viable bacteria from samples that interfere with viability staining. The viability of Bifidobacterium longum ATCC 15707 was assessed using Percoll Buoyant Density Gradient Centrifugation (PBDC) to separate bacteria from complex non-dairy food matrices and Quantitative Fluorescence Microscopy (QFM) to determine individual cells using LIVE/DEAD BacLight bacterial viability staining. Water agar (3%) was used to retain cells of B. longum and offered a lower fluorescence background with BacLight viability staining, compared with fixation on polycarbonate (PC) black membrane. The effect of drying temperatures and non-dairy foods on viability of B. longum was assessed. B. longum coated on oat, peanut or raisin was separated by filtration, low- and high-speed centrifugation, flotation and sedimentation buoyant density centrifugation. Purified cells were subsequently deposited on water agar for rehydration followed by LIVE/DEAD BacLight viability staining and enumeration. Conventional plate counting was also conducted to compare viability results. Finally, this method was applied to assess cell membrane damages of B. longum incorporated onto non-dairy foods during 24â¯h drying. Furthermore, viability assessment of B. longum coated onto oat, peanut, or raisin was much lower by plate counting compared to viability staining. Drying appeared to have a greater impact when viability was assessed by plate counting compared to viability staining. IMPORTANCE: Enumeration of viable beneficial bacteria from function foods presents a significant bottleneck for product development and quality control. Interference with microscopic and/or fluorescent techniques by ingredients, time required to incubate plated microbes, and the transient nature of the colony forming unit make rapid assessment of viable bacteria difficult. Viability assessment of Bifidobacterium longum ATCC 15707 by Percoll Buoyant Density Gradient Centrifugation with LIVE/DEAD BacLight viability staining on water agar (3%) was in agreement with serial dilution enumeration. Without the need for incubation viability assessment by staining provided a more rapid means to assess the impact of drying on the viability of B. longum coated onto oat, peanut or raisin.
Assuntos
Bifidobacterium longum/crescimento & desenvolvimento , Microbiologia de Alimentos/métodos , Viabilidade Microbiana , Microscopia de Fluorescência/métodos , Centrifugação com Gradiente de Concentração/métodos , Contagem de Colônia Microbiana/métodos , Povidona , Dióxido de Silício , Coloração e Rotulagem/métodosRESUMO
A new breed of nanocomposite-based spray-on sensor is developed for in-situ active structural health monitoring (SHM). The novel nanocomposite sensor is rigorously designed with graphene as the nanofiller and polyvinylpyrrolidone (PVP) as the matrix, fabricated using a simple spray deposition process. Electrical analysis, as well as morphological characterization of the spray-on sensor, was conducted to investigate percolation characteristic, in which the optimal threshold (~0.91%) of the graphene/PVP sensor was determined. Owing to the uniform and stable conductive network formed by well-dispersed graphene nanosheets in the PVP matrix, the tailor-made spray-on sensor exhibited excellent piezoresistive performance. By virtue of the tunneling effect of the conductive network, the sensor was proven to be capable of perceiving signals of guided ultrasonic waves (GUWs) with ultrahigh frequency up to 500 kHz. Lightweight and flexible, the spray-on nanocomposite sensor demonstrated superior sensitivity, high fidelity, and high signal-to-noise ratio under dynamic strain with ultralow magnitude (of the order of micro-strain) that is comparable with commercial lead zirconate titanate (PZT) wafers. The sensors were further networked to perform damage characterization, and the results indicate significant application potential of the spray-on nanocomposite-based sensor for in-situ active GUW-based SHM.
Assuntos
Técnicas Biossensoriais , Grafite/química , Monitorização Fisiológica/instrumentação , Nanocompostos/química , Humanos , Chumbo/química , Povidona/química , Titânio/química , Ondas Ultrassônicas , Zircônio/químicaRESUMO
Nano-MoS2 has been extensively investigated in materials science and biomedicine. However, the effects of different methods of exposure on their translocation, biosafety, and biotransformation-related degradability remain unclear. In this study, we combined the advantages of synchrotron radiation (SR) X-ray absorption near-edge structure (XANES) and high-resolution single-cell SR transmission X-ray microscopy (SR-TXM) with traditional analytical techniques to investigate translocation, precise degraded species/ratio, and correlation between the degradation and toxicity levels of polyvinylpyrrolidone-modified 2H-phase MoS2 nanosheets (MoS2-PVP NSs). These NSs demonstrated different biodegradability levels in biomicroenvironments with H2O2, catalase, and human myeloperoxidase (hMPO) (H2O2 < catalase < hMPO). The effects of NSs and their biodegraded byproducts on cell viability and 3D translocation at the single-cell level were also assessed. Toxicity and translocation in mice via intravenous (i.v.), intraperitoneal (i.p.), and intragastric (i.g.) administration routes guided by fluorescence (FL) imaging were investigated within the tested dosage. After i.g. administration, NSs accumulated in the gastrointestinal organs and were excreted from feces within 48 h. After i.v. injection, NSs showed noticeable clearance due to their decreased accumulation in the liver and spleen within 30 days when compared with that in the i.p. group, which exhibited slight accumulation in the spleen. This work paves the way for understanding the biological behaviors of nano-MoS2 using SR techniques that provide more opportunities for future applications.
Assuntos
Dissulfetos/farmacocinética , Dissulfetos/toxicidade , Molibdênio/farmacocinética , Molibdênio/toxicidade , Nanoestruturas/toxicidade , Povidona/farmacocinética , Povidona/toxicidade , Animais , Biotransformação , Sobrevivência Celular/efeitos dos fármacos , Dissulfetos/administração & dosagem , Dissulfetos/química , Vias de Administração de Medicamentos , Masculino , Camundongos Endogâmicos BALB C , Molibdênio/administração & dosagem , Molibdênio/química , Nanomedicina , Nanoestruturas/administração & dosagem , Nanoestruturas/química , Povidona/administração & dosagem , Povidona/química , Distribuição TecidualRESUMO
This study is a comprehensive evaluation of praziquantel (PZQ) behavior upon grinding considering the influence of milling temperature (cryogenic vs room temperature), frequency and time and presence of polymers (milled raw PZQ vs comilled PZQ/povidone and PZQ/crospovidone at 50:50â¯w/w) on two experimental responses (residual crystallinity and PZQ recovery). To this aim a full factorial design was set up and the responses of the experimental design were statistically assessed. The powder temperature, measured in different milling conditions, was found to increase with increasing milling frequency and time, up to a maximum recorded value of 46.9⯰C (after 90â¯min at R.T.), for all the three powder systems. When PZQ was ground in RT environment, the recovery was 100%, independently from frequency and time of milling. Its residual crystallinity remained pronounced (>70%) upon milling, even if treated at the most severe conditions. Conversely, when the drug was milled in presence of the polymers, it showed a higher tendency to degradation and amorphysation, independently from the choice of the polymer. The use of cryogenic conditions, operating at temperatures lower than PZQ glass transition, permitted to dramatically reduce PZQ residual crystallinity when the drug was ground by itself. In the case of binary mixtures, the switch to a cryogenic environment did not affect significantly the experimental responses, but permitted to obtain a more predictable trend of both drug recovery and residual crystallinity when varying time and frequency of milling.
Assuntos
Praziquantel/química , Cristalização/métodos , Composição de Medicamentos/métodos , Polímeros/química , Povidona/química , Pós/química , TemperaturaRESUMO
The objective of this study was to develop sustained release matrix tablets of atenolol (AT) using different concentrations of polyvinyl acetate-polyvinylpyrrolidone mixture (KSR) (20, 30, or 40%) with various types of fillers such as spray dried lactose (SP.D.L), avicel pH 101 (AV), and emcompress (EMS). The physical characteristics of the prepared tablets were evaluated. Characterization of the optimized formulation was performed using Fourier transform (FT)-IR spectroscopy and differential scanning calorimetry (DSC). Moreover, the in vitro release profiles of AT formulations were investigated in different pH dissolution media. Drug release kinetics and mechanisms were also determined. The results revealed that there was no potential incompatibility of the drug with the polymer. The release profiles of AT were affected by the concentration of KSR, fillers used, and pH of the dissolution media. The drug release kinetic from most of the formulations obeyed Higuchi diffusion model. The selected formulae were investigated for their stability by storage at 30 and 40°C with atmospheric humidity and 75% relative humidity (RH), respectively. The results demonstrated that no change in the physicochemical properties of the tablets stored at 30°C/atmospheric RH in comparison with some changes at 40°C/75% RH. Finally, the in vivo study provided an evidence that the optimized AT tablet containing 40% KSR and SP.D.L exhibited prominent higher oral bioavailability and more efficient sustained-release effect than the drug alone or the commercial tablet product. It is noteworthy that KSR could be considered as a promising useful release retardant for the production of AT sustained release matrix tablets.
Assuntos
Polivinil/química , Povidona/química , Atenolol , Varredura Diferencial de Calorimetria , Preparações de Ação Retardada , Técnicas In Vitro , Espectroscopia de Infravermelho com Transformada de Fourier , ComprimidosRESUMO
After ultrasonic-assisted extraction, four lycoris radiata alkaloids: galanthamine, homolycorine, lycorenine, and tazettine were determined by capillary electrophoresis electrochemiluminescence. Polyvinylpyrrolidone was added to the running buffer (RB) to obtain better resolution. Experimental conditions influencing the determination were examined, including the additives, detection potential, separation voltage, injection voltage and time, and RB pH and concentration. Under optimal experimental conditions, the baseline separation of the four alkaloids occurred within 16min. The proposed method displayed the following linear ranges (in ng/mL): galanthamine [60-5000], homolycorine [40-5000], lycorenine [5.0-1500], and tazettine [8.0-2500]. The detection limits in ng/mL, (S/N=3), were galanthamine [14], homolycorine [11], lycorenine [1.8], and tazettine [3.1]. Intra-day and inter-day RSDs for the four alkaloids of the six replicates were less than 2.7% and 3.1%, respectively. The recoveries in% were: tazettine [102.5], lycorenine [98.20], galanthamine [97.30], and homolycorine [98.33].