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1.
Drug Dev Ind Pharm ; 49(2): 179-188, 2023 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-36961755

RESUMEN

To provide a theoretical foundation and a good understanding for the real manufacturing granulation process, this paper investigates the effect of particle properties on the mixing process in the high-shear wet granulator, a common equipment in one of the key technologies in the growth of the pharmaceutical industry that has rarely been used to examine particle mixing-related problems in previous numerical simulations. The discrete element method (DEM) and the relative standard deviation (RSD) to explore binary particle systems with a range of sizes, densities, and volume fractions, and measure the mixing homogeneity of the particles. Results show that, for binary particle systems, particle size, density, and volume fraction all significantly affect mixing homogeneity, with good mixing occurring for a single size and a 1:1 volume fraction for the same density. Similar Brazil nut effect and Reverse-Brazil nut effect occurrences were discovered for many particle systems at various stages. There is a size threshold for a given binary particle system. Then, in a binary system, particles of a single size and density had nearly similar vertical driving forces, and these forces may vary by up to 10 times with changes in size or density. In the end, granular temperature rises with radial position and reaches its highest point at the pelletizer's wall and the top of the impeller. Density has less of an impact on granule velocity fluctuation than size.


Asunto(s)
Industria Farmacéutica , Tecnología Farmacéutica , Tecnología Farmacéutica/métodos , Tamaño de la Partícula , Polvos
2.
AAPS PharmSciTech ; 23(8): 286, 2022 Oct 19.
Artículo en Inglés | MEDLINE | ID: mdl-36261755

RESUMEN

Computational modeling, machine learning, and statistical data analysis are increasingly utilized to mitigate chemistry, manufacturing, and control failures related to particle properties in solid dosage form manufacture. Advances in particle characterization techniques and computational approaches provide unprecedented opportunities to explore relationships between particle morphology and drug product manufacturability. Achieving this, however, has numerous challenges such as producing and appropriately curating robust particle size and shape data. Addressing these challenges requires a harmonized strategy from material sampling practices, characterization technique selection, and data curation to provide data sets which are informative on material properties. Herein, common sources of error in particle characterization and data compression are reviewed, and a proposal for providing robust particle morphology (size and shape) data to support modeling efforts, approaches for data curation, and the outlook for modeling particle properties are discussed.


Asunto(s)
Curaduría de Datos , Industria Farmacéutica , Polvos , Tamaño de la Partícula , Simulación por Computador
3.
Environ Res ; 191: 110192, 2020 12.
Artículo en Inglés | MEDLINE | ID: mdl-32956654

RESUMEN

Microplastic is exposed to numerous weathering processes in the environment, which change particle properties and thus influence transport behaviors, including settling and rising velocities in aquatic environments. However, the extent to which particles in the environment differ from virgin particles in their transport behaviors has not yet been investigated. The settling and rising velocities of weathered fluvial microplastic and macroplastic particles collected from environmental samples are determined in this study and the transferability of theoretical approaches to predicting their transport behaviors is examined. The settling velocities of the environmental particles were between 0.16 and 3.52 cm/s and the rising velocities between 0.18 and 19.85 cm/s. Formulas were applied that were developed using experiments with virgin microplastic, but do not account for the effects of environmental impacts such as degradation, fragmentation and biofouling on the velocities. Accordingly, the transferability of the formulas to environmental particles must be verified. The formulas proved to be suitable for describing the settling and rising velocities of environmental microplastic particles in the shapes of pellets, fragments and foams, and were less suitable for describing the velocities of films and macroplastic particles. Further experiments will be necessary in the future to integrate effects from biofilm and particle deformation on the transport behaviors to adequately model the behavior of the highly diverse micro- and macroplastic particles in the aquatic environment.


Asunto(s)
Incrustaciones Biológicas , Plásticos , Monitoreo del Ambiente , Tiempo (Meteorología)
4.
Part Fibre Toxicol ; 16(1): 29, 2019 07 09.
Artículo en Inglés | MEDLINE | ID: mdl-31288843

RESUMEN

BACKGROUND: Industrially produced quantities of TiO2 nanoparticles are steadily rising, leading to an increasing risk of inhalation exposure for both professionals and consumers. Particle inhalation can result in inflammatory and allergic responses, and there are concerns about other negative health effects from either acute or chronic low-dose exposure. RESULTS: To study the fate of inhaled TiO2-NP, adult rats were exposed to 2-h intra-tracheal inhalations of 48V-radiolabeled, 20 nm TiO2-NP aerosols (deposited NP-mass 1.4 ± 0.5 µg). At five time points (1 h, 4 h, 24 h, 7d, 28d) post-exposure, a complete balance of the [48V]TiO2-NP fate was quantified in organs, tissues, carcass, lavage and body fluids, including excretions. After fast mucociliary airway clearance (fractional range 0.16-0.31), long-term macrophage-mediated clearance (LT-MC) from the alveolar region is 2.6-fold higher after 28d (integral fraction 0.40 ± 0.04) than translocation across the air-blood-barrier (integral fraction 0.15 ± 0.01). A high NP fraction remains in the alveoli (0.44 ± 0.05 after 28d), half of these on the alveolar epithelium and half in interstitial spaces. There is clearance from both retention sites at fractional rates (0.02-0.03 d- 1) by LT-MC. Prior to LT-MC, [48V]TiO2-NP are re-entrained to the epithelium as reported earlier for 20 nm inhaled gold-NP (AuNP) and iridium-NP (IrNP). CONCLUSION: Comparing the 28-day biokinetics patterns of three different inhaled NP materials TiO2-NP, AuNP and IrNP, the long-term kinetics of interstitial relocation and subsequent re-entrainment onto the lung-epithelium is similar for AuNP and Ir-NP but slower than for TiO2-NP. We discuss mechanisms and pathways of NP relocation and re-entrainment versus translocation. Additionally, after 28 days the integral translocated fractions of TiO2-NP and IrNP across the air-blood-barrier (ABB) are similar and become 0.15 while the translocated AuNP fraction is only 0.04. While NP dissolution proved negligible, translocated TiO2-NP and IrNP are predominantly excreted in urine (~ 0.1) while the urinary AuNP excretion amounts to a fraction of only 0.01. Urinary AuNP excretion is below 0.0001 during the first week but rises tenfold thereafter suggesting delayed disagglomeration. Of note, all three NP dissolve minimally, since no ionic radio-label release was detectable. These biokinetics data of inhaled, same-sized NP suggest significant time-dependent differences of the ABB translocation and subsequent fate in the organism.


Asunto(s)
Exposición por Inhalación/análisis , Pulmón/metabolismo , Nanopartículas/química , Titanio/farmacocinética , Aerosoles , Animales , Líquido del Lavado Bronquioalveolar , Femenino , Tasa de Depuración Metabólica , Especificidad de Órganos , Tamaño de la Partícula , Ratas , Ratas Endogámicas WKY , Mucosa Respiratoria/metabolismo , Factores de Tiempo , Distribución Tisular , Titanio/química
5.
Drug Dev Ind Pharm ; 44(10): 1659-1667, 2018 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-29954227

RESUMEN

OBJECTIVE: The objective of this study was to characterize the properties of aqueous Sennae fructus extracts prepared by spray-drying at varying process conditions. SIGNIFICANCE: From an industrial point of view it is essential to develop a formulation which has a constant quality over the whole period of its specified shelf-life. METHOD: Sennae fructus extracts were spray-dried with different atomizing gas pressures, pump feed rates, and inlet temperatures. The extracts were analyzed for their physical properties and stored at accelerated conditions. Sennoside degradation was monitored by HPLC analysis. RESULTS: An increase of the atomizing gas pressure had the most pronounced influence on the decrease of moisture content and particle size. An increase of the inlet temperature led to a decrease of moisture content and particle density, as well as an increase of smooth particle amount. An increase in the pump feed rate, increased the moisture content and resulted in stable hollow spheres. The different conditions also led to smooth or wrinkled particle surfaces, and to golfball, donut, and shard particle shapes. The chemical stability of the sennosides differed from each other after storage. Stability-reducing factors were the moisture content of the samples and their hygroscopicities, as well as different particle morphologies. These factors were influenced by the inlet temperature of the spray-drying process. High inlet temperatures led to a positive influence on dryness and particle morphology and therefore on the stability of the sennosides. CONCLUSIONS: Variation of the process conditions affected the resulting particle properties and their storage stability of Sennae fructus extract.


Asunto(s)
Desecación/métodos , Extracto de Senna/análisis , Extracto de Senna/química , Senna , Tecnología Farmacéutica/métodos , Catárticos/análisis , Catárticos/química , Estabilidad de Medicamentos , Extractos Vegetales/análisis , Extractos Vegetales/química
6.
J Appl Microbiol ; 119(2): 315-30, 2015 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-26033178

RESUMEN

Effective modelling of the fate and transport of water-borne pathogens is needed to support federally required pollution-reduction plans, for water quality improvement planning, and to protect public health. Lack of understanding of microbial-particle interactions in water bodies has sometimes led to the assumption that bacteria move in surface waters not associated with suspended mineral and organic particles, despite a growing body of evidence suggesting otherwise. Limited information exists regarding the factors driving interactions between micro-organisms and particles in surface waters. This review discusses cellular, particle and environmental factors potentially influencing interactions and in-stream transport. Bacterial attachment in the aquatic environment can be influenced by properties of the cell such as genetic predisposition and physiological state, surface structures such as flagella and fimbriae, the hydrophobicity and electrostatic charge of the cell surface, and the presence of outer-membrane proteins and extracellular polymeric substances. The mechanisms and degree of attachment are also affected by characteristics of mineral and organic particles including the size, surface area, charge and hydrophobicity. Environmental conditions such as the solution chemistry and temperature are also known to play an important role. Just as the size and surface of chemical particles can be highly variable, bacterial attachment mechanisms are also diverse.


Asunto(s)
Bacterias/química , Adhesión Bacteriana , Agua Dulce/microbiología , Ecosistema , Ambiente , Agua Dulce/química
7.
Pharmaceutics ; 16(7)2024 Jun 30.
Artículo en Inglés | MEDLINE | ID: mdl-39065580

RESUMEN

Crystalline active pharmaceutical ingredients with comparable size and surface area can demonstrate surface anisotropy induced during crystallization or downstream unit operations such as milling. To the extent that varying surface properties impacts bulk powder properties, the final drug product performance such as stability, dissolution rates, flowability, and dispersibility can be predicted by understanding surface properties such as surface chemistry, energetics, and wettability. Here, we investigate the surface properties of different batches of Odanacatib prepared through either jet milling or fast precipitation from various solvent systems, all of which meet the particle size specification established to ensure equivalent biopharmaceutical performance. This work highlights the use of orthogonal surface techniques such as Inverse Gas Chromatography (IGC), Brunauer-Emmett-Teller (BET) surface area, contact angle, and X-ray Photoelectron Spectroscopy (XPS) to demonstrate the effect of processing history on particle surface properties to explain differences in bulk powder properties.

8.
Chemosphere ; 287(Pt 3): 132257, 2022 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-34547563

RESUMEN

Previous studies on cadmium adsorption of calcium carbonate have found that polymorph, and, crystallinity are influential factors for adsorbing cadmium ions. The predominant factor for cadmium adsorption has yet to be elucidated because these factors are linked. To overcome this, here each factor is investigated separately. First, atmospheric grinding prepared surf clam (aragonite phase) and scallop (calcite phase) shells with similar crystallite sizes and specific surface areas. Using adsorption isotherm models, kinetics, X-ray diffraction analysis, and TEM observations, both calcite and aragonite react with cadmium to form cadmium carbonate. The chemisorption follows the adsorption mechanism reported in the literature. Based on the Langmuir isotherm model fitting, the maximum adsorbed amount for the ground surf clam shells is 633.3 mg/g, while that for scallop shells is 195.8 mg/g. Then fine surf clam shell particles with a similar specific surface area, and with a relatively wide range of the aragonite ratio, and crystallite size are prepared via a combination of grinding and a subsequent calcination process. Our experiments where one explanatory variable is changed at a time demonstrate that the polymorph ratio and crystallite size of the ground shells play key roles in the chemisorption.


Asunto(s)
Cadmio , Contaminantes Químicos del Agua , Adsorción , Carbonato de Calcio , Concentración de Iones de Hidrógeno , Cinética
9.
Food Res Int ; 157: 111209, 2022 07.
Artículo en Inglés | MEDLINE | ID: mdl-35761531

RESUMEN

In this study we investigated the individual contribution of different ingredients to the lubrication properties of dairy-based model beverages containing whey protein (native or aggregated), micellar casein and emulsified oil in different combinations. In single-component systems, whey protein isolate (WPI) solutions showed the lowest friction coefficients of all protein samples. Whey protein aggregates (WPA, ∼247 nm, irregular morphology) led to higher friction coefficients than micellar casein isolate (MCI) with comparable size (∼207 nm, near spherical shape). When protein particles were combined, i.e. WPA and MCI, lubrication was not much affected. However, when WPI was added to either WPA or MCI, higher friction coefficients were observed compared to single-component systems. Emulsions (droplet size âˆ¼ 440 nm) provided better lubrication than the protein samples. Oil droplets stabilized by soy lecithin (SL) were more efficient at reducing friction than those stabilized by WPI. The friction coefficient of SE strongly increased in the presence of WPI. In comparison, lubrication of WE was less affected by the addition of WPI. These results show that different proteins affect the lubrication properties of emulsions stabilized with different emulsifiers in a different way. Our research also indicates that multicomponent systems are complex, and that control over the lubrication properties requires a better understanding of the contribution of individual components.


Asunto(s)
Bebidas , Caseínas , Emulsiones , Lubrificación , Proteína de Suero de Leche
10.
Carbohydr Polym ; 291: 119523, 2022 Sep 01.
Artículo en Inglés | MEDLINE | ID: mdl-35698326

RESUMEN

This research aimed to investigate the effect of starch gelatinization and swelling degree on the lubrication properties of starch aqueous suspensions. Three types of maize starch with different amylose content of 70% (HAS), 25% (NS), and <1% (WS) were used to vary the swelling capacities. The granule suspension of NS showed the highest swelling factor (SF) of 26.5, and gave the best lubrication capacity by decreasing friction by 78%. WS was only able to decrease friction by 50% due to a lower swelling capacity. The leached-out amylose increased friction of highly swollen granules (SF = 26.5) but decreased friction of stiff granules (SF = 2.5). Adding unstimulated human saliva to starch suspensions with native and limited swollen granules reduced friction and masked differences in friction coefficients among starch types. Both the salivary layer on the contact surfaces and the salivary proteins in the bulk phase played a role in determining lubrication properties.


Asunto(s)
Amilosa , Almidón , Fricción , Humanos , Lubrificación , Suspensiones
11.
J Agric Food Chem ; 70(23): 7139-7147, 2022 Jun 15.
Artículo en Inglés | MEDLINE | ID: mdl-35648591

RESUMEN

Enzymes are important catalysts for biological processes due to their high catalytic activity and selectivity. However, their low thermal stability limited their industrial applications. The present work demonstrates a simple and effective method for enzyme immobilization via spray drying. Alginate was used as a support material. Phytase, an important enzyme in the animal feed industry, was selected to study the effect of enzyme immobilization using alginate particles on its thermal stability. The physicochemical properties of alginate particles such as size, surface morphology, and heat resistance were studied. Successful immobilization of phytase was confirmed by confocal microscopy, and the immobilized phytase retained 58% of its original activity upon heating at 95 °C, compared to 4% when the alginate support material was absent. Phytase was released promptly in a simulated gastrointestinal tract with >95% of its original activity recovered. The spray drying method for phytase immobilization is scalable and applicable to other enzymes for various applications.


Asunto(s)
6-Fitasa , Alginatos , 6-Fitasa/química , Alginatos/química , Animales , Estabilidad de Enzimas , Enzimas Inmovilizadas/química , Concentración de Iones de Hidrógeno , Secado por Pulverización
12.
Nanomaterials (Basel) ; 12(18)2022 Sep 12.
Artículo en Inglés | MEDLINE | ID: mdl-36144949

RESUMEN

A dynamic process model for the simulation of nanoparticle fractionation in tubular centrifuges is presented. Established state-of-the-art methods are further developed to incorporate multi-dimensional particle properties (traits). The separation outcome is quantified based on a discrete distribution of particle volume, elongation and flatness. The simulation algorithm solves a mass balance between interconnected compartments which represent the separation zone. Grade efficiencies are calculated by a short-cut model involving material functions and higher dimensional particle trait distributions. For the one dimensional classification of fumed silica nanoparticles, the numerical solution is validated experimentally. A creation and characterization of a virtual particle system provides an additional three dimensional input dataset. Following a three dimensional fractionation case study, the tubular centrifuge model underlines the fact that a precise fractionation according to particle form is extremely difficult. In light of this, the paper discusses particle elongation and flatness as impacting traits during fractionation in tubular centrifuges. Furthermore, communications on separation performance and outcome are possible and facilitated by the three dimensional visualization of grade efficiency data. Future research in nanoparticle characterization will further enhance the models use in real-time separation process simulation.

13.
Sci Total Environ ; 838(Pt 2): 155831, 2022 Sep 10.
Artículo en Inglés | MEDLINE | ID: mdl-35568170

RESUMEN

A diverse array of natural and anthropogenic particles found in the aquatic environment, can act as carriers of co-transported matter (CTM), such as nutrients, genetic material and contaminants. Thus, understanding carrier particle transport will increase our understanding of local and global fluxes of exogenous CTM (affiliated with the particle) and endogenous CTM (an inherent part of the particle). In the present contribution, researchers from multiple disciplines collaborated to provide perspectives on the interactions between carrier particles and CTM, and the fundamentals of transport of particles found in the aquatic environment and the generic spherical smooth particles, often used to make predictions about particle behavior in suspension. Evidently, the particles in the aquatic environment show a great variety of characteristics and vary greatly from each other as well as from the generic particle. However, in spite of these differences, many fundamental concepts apply to particles in general. We emphasize the importance of understanding the basic concepts of transport of particle-associated CTM, and the main assumptions in the generic-founded models, which are challenged by the diverging characteristics of particles found in the aquatic environment, as paramount moving forward. Additionally, we identified the need for a conceptual and semantic link between different scientific fields of particle research and initiated the formation of a consistent terminology. Disciplinary and organizational (academic and funding) barriers need to be overcome to enable individual researchers to move beyond their knowledge sphere, to stimulate future interdisciplinary collaborations and to avoid research silos. Hereby, we can foster faster and better progress of evolving research fields on new and emerging anthropogenic carrier particles, and stimulate the development of solutions to the technological and environmental challenges.


Asunto(s)
Investigación Interdisciplinaria
14.
Foods ; 10(6)2021 Jun 04.
Artículo en Inglés | MEDLINE | ID: mdl-34199941

RESUMEN

Whey protein isolate (WPI) can be used effectively to produce food-grade particles for stabilizing Pickering emulsions. In the present study, crosslinking of WPI microgels using organic acids (tannic and citric acids) is proposed to improve their functionality in emulsions containing roasted coffee oil. It was demonstrated that crosslinking of WPI by organic acids reduces the microgels' size from ≈1850 nm to 185 nm and increases their contact angle compared to conventional WPI microgels, achieving values as high as 60°. This led to the higher physical stability of Pickering emulsions: the higher contact angle and smaller particle size of acid-crosslinked microgels contribute to the formation of a thinner layer of particles on the oil/water (O/W) interface that is located mostly in the water phase, thus forming an effective barrier against droplet coalescence. Particularly, emulsions stabilized by tannic acid-crosslinked WPI microgels presented neither creaming nor sedimentation up to 7 days of storage. The present work demonstrates that the functionality of these crosslinked WPI microgels can be tweaked considerably, which is an asset compared to other food-grade particles that mostly need to be used as such to comply with the clean-label policy. In addition, the applications of these particles for an emulsion are much more diverse as of the starting material.

15.
Int J Nanomedicine ; 15: 2071-2083, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-32273703

RESUMEN

BACKGROUND AND PURPOSE: Adjuvant can reduce vaccine dosage and acquire better immune protection to the body, which helps to deal with the frequent outbreaks of influenza. Nanoemulsion adjuvants have been proved efficient, but the relationship between their key properties and the controlled release which greatly affects immune response is still unclear. The present work explores the role of factors such as particle size, the polydispersity index (PDI), stability and the safety of nanoemulsions by optimizing the water concentration, oil phase and modes of carrying, to explain the impact of those key factors above on adjuvant effect. METHODS: Isopropyl myristate (IPM), white oil, soybean oil, and grape-kernel oil were chosen as the oil phase to explore their roles in emulsion characteristics and the adjuvant effect. ICR mice were immunized with an emulsion-inactivated H3N2 split influenza vaccine mixture, to compare the nanoemulsion's adjuvant with traditional aluminium hydroxide or complete Freund's adjuvant. RESULTS: Particle size of all the nanoemulsion formed in our experiment ranged from 20 nm to 200 nm and did not change much when diluted with water, while the PDI decreased obviously, indicating that the particles tended to become more dispersive. Formulas with 80% or 85.6% water concentration showed significant higher HAI titer than aluminium hydroxide or complete Freund's adjuvant, and adsorption rather than capsule mode showed higher antigen delivery efficiency. As mentioned about oil phase, G (IPM), F (white oil), H (soybean oil), and I (grape-kernel oil) showed a decreasing trend in their adjuvant efficiency, and nanoemulsion G was the best adjuvant with smaller and uniform particle size. CONCLUSION: Emulsions with a smaller, uniform particle size had a better adjuvant effect, and the adsorption mode was generally more efficient than the capsule mode. The potential adjuvant order of the different oils was as follows: IPM > white oil > soybean oil > grape-kernel oil.


Asunto(s)
Adyuvantes Inmunológicos/química , Sistemas de Liberación de Medicamentos/métodos , Emulsiones/química , Vacunas contra la Influenza/administración & dosificación , Nanoestructuras/química , Adyuvantes Inmunológicos/administración & dosificación , Adyuvantes Inmunológicos/farmacología , Animales , Emulsiones/administración & dosificación , Emulsiones/farmacología , Femenino , Subtipo H3N2 del Virus de la Influenza A , Vacunas contra la Influenza/inmunología , Ratones Endogámicos ICR , Aceites/química , Infecciones por Orthomyxoviridae/prevención & control , Tamaño de la Partícula , Aceite de Soja/química , Vacunas de Productos Inactivados , Agua/química
16.
Int J Pharm ; 541(1-2): 188-197, 2018 Apr 25.
Artículo en Inglés | MEDLINE | ID: mdl-29481945

RESUMEN

Solid dispersions (SDs) hold a proven potential in formulating poorly water-soluble drugs. The present paper investigates the interfacial phenomena associated with the bulk powder flow, water sorption, wetting and dissolution of the SDs prepared by a modified melt and quench-cooling (QC) method. Poorly water-soluble indomethacin (IND) was QC molten with solubilizing graft copolymer (Soluplus®) or polyol sugar alcohol (xylitol, XYL). The interfacial interactions of SDs with air/water were found to be reliant on the type (amorphous/crystalline) and amount of the carrier material used. The final SDs were composed of fused agglomerates (SOL) or large jagged particles (XYL) with good wetting and powder flow properties. The initial dissolution of IND was accelerated by both carrier materials studied. The QC molten SDs with amorphous Soluplus® significantly improved the dissolution rate of IND at pH 6.8 (79.9 ±â€¯0.2% at 30 min) compared to that of pure crystalline drug. The substantial improvement in the dissolution rate of IND was in connection with the amorphous state of the drug being stabilized by Soluplus® in the QC molten SDs. However, it is evident that a strong H-bond formation between the components in some regions of the QC molten SDs can limit the dissolution of IND. The QC molten two-phase SDs with a polyol carrier (XYL) showed rapid and continuous drug release without reaching a plateau.


Asunto(s)
Portadores de Fármacos/química , Composición de Medicamentos/métodos , Liberación de Fármacos , Indometacina/farmacocinética , Química Farmacéutica , Estabilidad de Medicamentos , Excipientes/química , Indometacina/química , Transición de Fase , Polietilenglicoles/química , Polivinilos/química , Polvos , Solubilidad , Xilitol/química
17.
Int J Biol Macromol ; 113: 640-647, 2018 Jul 01.
Artículo en Inglés | MEDLINE | ID: mdl-29428384

RESUMEN

The aim of present study was to investigate the effect of different ultrasound power on physicochemical property and functional performance of chicken actomyosin (CAM). The treated CAM had the lowest particle size and the highest absolute zeta potential at 150 W. The conformation changes of treated CAM exhibited the reduction in α-helix as well as the improvement of fluorescence intensity. Ultrasound power at 150 W could significantly increase protein hydrophobicity and reactive SH groups compared to the others (P < 0.05). The disappearance of specific peaks and lower endothermic peaks implied that the treated CAM became thermally instable. The microstructure of CAM revealed small and homogeneous sub-bunches treated by 100-150 W. Furthermore, the solubility and emulsion property of CAM was significantly increased at 150 W (P < 0.05). These results demonstrated that ultrasound treatment at the power of 100-150 W may be an appropriate range to modify CAM for enhancing its functional properties.


Asunto(s)
Actomiosina/química , Fenómenos Químicos , Ondas Ultrasónicas , Animales , Pollos , Industria de Alimentos , Interacciones Hidrofóbicas e Hidrofílicas , Tamaño de la Partícula , Solubilidad , Compuestos de Sulfhidrilo/química
18.
ACS Appl Mater Interfaces ; 9(12): 10435-10445, 2017 Mar 29.
Artículo en Inglés | MEDLINE | ID: mdl-28266206

RESUMEN

Calcium phosphate (CaP) nanoparticles are promising gene delivery carriers due to their bioresorbability, ease of preparation, high gene loading efficacy, and endosomal escape properties. However, the rapid aggregation of the particles needs to be addressed in order to have potential in vivo. In addition, there is a need to better understand the relationship between CaP nanoparticle properties and their interactions with cells. Here, a new synthesis route involving click chemistry was developed to prepare the PEGylated chelator PEG-inositol 1,3,4,5,6-pentakisphosphate (PEG-IP5) that can coat and stabilize CaP nanoparticles. Two methods (1 and 2) differing on the time of addition of the PEGylated chelator were employed to produce stabilized particles. Method 1 yielded amorphous aggregated spheres with a particle size of about 200 nm, whereas method 2 yielded 40 nm amorphous loose aggregates of clusters, which were quickly turned into needle bundle-like crystals of about 80 nm in a few hours. Nanoparticles prepared by method 1 were internalized with significantly higher efficiency in HepG2 cells than those prepared by method 2, and the uptake was dramatically influenced by the reaction time of Ca2+ and PO43- and sedimentation of the particles. Interestingly, morphological transformations were observed for both types of particles after different storage times, but this barely influenced their in vitro cellular uptake. The transfection efficiency of the particles prepared by method 1 was significantly higher, and none of the formulations tested showed signs of cytotoxicity. This study provides a better understanding of the properties (e.g., size, morphology, and crystallinity) of PEGylated CaP nanoparticles and how these influence the particles' in vitro uptake and transfection efficiency.


Asunto(s)
Nanopartículas , Fosfatos de Calcio , Quelantes , Técnicas de Transferencia de Gen , Tamaño de la Partícula , Polietilenglicoles , Transfección
19.
Int J Pharm ; 518(1-2): 138-154, 2017 Feb 25.
Artículo en Inglés | MEDLINE | ID: mdl-28025075

RESUMEN

Understanding interparticle interactions in powder systems is crucial to pharmaceutical powder processing. Nevertheless, there remains a great challenge in identifying the key factors affecting interparticle interactions. Factors affecting interparticle interactions can be classified in three different broad categories: powder properties, environmental conditions, and powder processing methods and parameters. Although, each of these three categories listed is known to affect interparticle interactions, the challenge remains in developing a mechanistic understanding on how combination of these three categories affect interparticle interactions. This review focuses on the recent advances on understanding the effect of powder properties, particularly particle properties, its effect on interparticle interactions and ultimately on powder bulk behaviour. Furthermore, this review also highlights how particle properties are affected by the particle processing route and parameters. Recent advances in developing a particle processing route to prepare particles with desired properties allowing desired interparticle interaction to deliver favoured powder bulk behaviour are also discussed. Perspectives for the development of potential particle processing approaches to control interparticle interaction are presented.


Asunto(s)
Polvos/química , Química Farmacéutica , Modelos Químicos
20.
Mater Sci Eng C Mater Biol Appl ; 72: 444-455, 2017 Mar 01.
Artículo en Inglés | MEDLINE | ID: mdl-28024608

RESUMEN

Cationic copolymers have been attractive to investigate due to their potential to complexation with anionic drugs and expected to use in the pharmaceutical application. In this study, the modified poly(ε-caprolactone)2-co-poly(ethylene glycol) copolymers (P(CL)2-PEG) were successfully synthesized by click reaction. The amount of small molecular cationic ligand, propargyltrimethyl ammonium iodide, was varied and grafted onto various mole ratios of P(CL) to PEG. The effects of P(CL) chain length and amount of the grafting cationic ligand on physicochemical properties of polymers and particles were studied. The number-average molecular weights of the copolymers grafted with cationic ligand were found ranging between 10,000 and 23,000g/mol as investigated by NMR. From DSC study, the results showed that the grafting ligand affected thermal behaviors of the copolymers by increasing the glass transition temperature and decreasing the melting temperature of the copolymers. Furthermore, these cationic copolymers could self-aggregate with their critical aggregation concentration depending on mole ratios of hydrophilic to hydrophobic portions. The particles containing higher amounts of the cationic ligand tended to aggregate in both acidic and basic pH environment and at high salt concentration. Additionally, particle size, size distribution (PdI), and morphology of self-assembling particles varied depending on P(CL) chain length and the amount of the grafting cationic ligand. The synthesized cationic copolymer showed a capability to encapsulate a high negatively charged drug, enoxaparin, with an encapsulation efficiency of 87%. After drug incorporation, the particles substantially changed in size, shape, PdI, and zeta potential to become more suitable for drug delivery. These cationic copolymers with flexible properties will be the candidate for further development as carriers for the delivery of negatively charged drugs.


Asunto(s)
Ligandos , Poliésteres/química , Polietilenglicoles/química , Rastreo Diferencial de Calorimetría , Cationes/química , Portadores de Fármacos/química , Concentración de Iones de Hidrógeno , Espectroscopía de Resonancia Magnética , Peso Molecular , Concentración Osmolar , Tamaño de la Partícula , Preparaciones Farmacéuticas/química , Preparaciones Farmacéuticas/metabolismo , Espectroscopía Infrarroja por Transformada de Fourier , Temperatura de Transición
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