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1.
Small ; 20(25): e2306054, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38299478

RESUMEN

Nanosized drug crystals have been reported with enhanced apparent solubility, bioavailability, and therapeutic efficacy compared to microcrystal materials, which are not suitable for parenteral administration. However, nanocrystal design and development by bottom-up approaches are challenging, especially considering the non-standardized process parameters in the injection step. This work aims to present a systematic step-by-step approach through Quality-by-Design (QbD) and Design of Experiments (DoE) for synthesizing drug nanocrystals by a semi-automated nanoprecipitation method. Curcumin is used as a drug model due to its well-known poor water solubility (0.6 µg mL-1, 25 °C). Formal and informal risk assessment tools allow identifying the critical factors. A fractional factorial 24-1 screening design evaluates their impact on the average size and polydispersity of nanocrystals. The optimization of significant factors is done by a Central Composite Design. This response surface methodology supports the rational design of the nanocrystals, identifying and exploring the design space. The proposed joint approach leads to a reproducible, robust, and stable nanocrystalline preparation of 316 nm with a PdI of 0.217 in compliance with the quality profile. An orthogonal approach for particle size and polydispersity characterization allows discarding the formation of aggregates. Overall, the synergy between advanced data analysis and semi-automated standardized nanocrystallization of drugs is highlighted.


Asunto(s)
Nanopartículas , Nanopartículas/química , Preparaciones Farmacéuticas/química , Tamaño de la Partícula , Automatización , Cristalización , Curcumina/química
2.
Nanotechnology ; 35(43)2024 Aug 09.
Artículo en Inglés | MEDLINE | ID: mdl-39074485

RESUMEN

Solution-processed perovskite solar cells (PSCs) have demonstrated a tremendous growth in power conversion efficiency (PCE). A high-quality, defect-free perovskite-based active layer is a key point to enhance PSC performance. Introduction of additives and interlayers have proved to be an effective tool to passivate surface defects, control crystal growth, and improve PSC stability. Antisolvent engineering has emerged recently as a new approach, which aims to adjust perovskite layer properties and enhance the PCE and stability of PSC devices. Here, we demonstrate that carbon dots (CDs) may serve as a prospective additive for antisolvent engineering. Nitrogen-rich amphiphilic CDs were synthesized from amines by a solvothermal method and used as an additive to chlorobenzene for a perovskite layer fabrication. The interaction between perovskite and functional groups in CDs promotes improved crystallization of an active perovskite layer and defects passivation, bringing higher PSCs efficiency, stability, and suppressed hysteresis. Under optimized CD concentration, the maximum PCE increased by 34% due to the improved short-circuit current and fill factor, and the device maintains 87% of its initial efficiency after 6 d of storage under ambient conditions.

3.
Macromol Rapid Commun ; 45(6): e2300629, 2024 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-38134957

RESUMEN

Three sulfonate-containing polyelectrolytes are elaborately designed and used to passivate perovskite film with the anti-solvent method. Under the influence of the secondary monomer, three copolymers present various chemical configurations and deliver different modification effects. Fluorene-thiophene copolymer STF has linear and highly-conjugated chain. STF-perovskite film presents large crystal grains. Fluorene-carbazole copolymer SCF has flexible chain and easily enters into grain boundary areas. SCF-perovskite film is homogenous and continuous. Fluorene-fluorene copolymer SPF agglomerates on the surface and is not applicable to the anti-solvent method. The full investigation demonstrates that STF and SCF not only conduct surface defect passivation, but also improve the film quality by being involved in the perovskite's crystallization process. Compared with the control device, the devices with STF and SCF deliver high efficiency and excellent stability. The unencapsulated devices with STF and SCT maintain ≈80% of the initial power conversion efficiency (PCE) after 40 days of storage under 30-40% relative humidity. SCF performs better and the device maintains 60% of the initial PCE after 20 days of storage under 60-80% relative humidity.


Asunto(s)
Compuestos de Calcio , Óxidos , Polímeros , Titanio , Polielectrolitos , Alcanosulfonatos , Fluorenos , Solventes
4.
Chem Pharm Bull (Tokyo) ; 72(1): 21-27, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38171901

RESUMEN

Pirarubicin (THP) shows more rapid intracellular uptake, more effective antitumor activity, and less cardiac toxicity, compared to doxorubicin. However, THP is distributed to both tumor and normal tissues indiscriminately. This study aimed to develop a nanosuspension to deliver THP to tumor tissues more efficiently. Fatty-acid-modified THPs (FA-THPs; octanoic acid, dodecanoic acid, palmitic acid-THPs) were synthesized to increase the hydrophobicity of THP. Nanosuspensions of these FA-THPs were then prepared using an antisolvent precipitation technique. Among the FA-THPs, the most efficiently drug-loaded nanosuspension was obtained from palmitic acid-THP (pal-THP) using an aqueous antisolvent containing bovine serum albumin as a stabilizer. The pal-THP nanoparticles in the nanosuspension were confirmed to be of optimal size (100-125 nm) for delivery to tumor tissues using dynamic light scattering and transmission electron microscopy. The pal-THP nanosuspension showed cytotoxicity in colon 26 cells. The nanosuspension was shown to disintegrate in the presence of surfactants such as lecithin, liberating pal-THP, which was converted to free THP in acidic media. It is therefore proposed that pal-THP nanoparticles that reach tumor cells after intravenous administration would exert antitumor effect by liberating pal-THP (i.e., disintegration of nanoparticles by the interaction with cell membrane), followed by the release of free THP in the acidic milieu of tumor cells. These findings indicate that FA-THP nanosuspensions, particularly pal-THP nanosuspension, hold promise as a candidate for cancer treatment. However, further in vivo studies are necessary.


Asunto(s)
Ácidos Grasos , Nanopartículas , Ácido Palmítico , Doxorrubicina/farmacología , Albúmina Sérica Bovina , Suspensiones , Tamaño de la Partícula , Solubilidad
5.
Nano Lett ; 23(10): 4479-4486, 2023 May 24.
Artículo en Inglés | MEDLINE | ID: mdl-37140170

RESUMEN

Inorganic CsPbIBr2 perovskite solar cells (PSCs) have accomplished many milestones, yet their progress has been constrained by ion migration and phase separation. This study explores the modulation of perovskite crystallization kinetics and halide ion migration through chlorobenzene (CB) antisolvent with bis(pentafluorophenyl)zinc (Zn(C6F5)2) additive. The photoluminescence and absorption spectra reveal the significantly reduced phase segregaton in CsPbIBr2 film treated by CB with Zn(C6F5)2. Moreover, this research analyzes the CsPbIBr2 film's free carrier lifetime, diffusion length, and mobility using time-resolved microwave conductivity and transient absorption spectroscopy after Zn(C6F5)2 modification. Consequently, the modified CsPbIBr2 PSCs offer a 12.57% power conversion efficiency (PCE), the highest value among CsPbIBr2 PSCs with negligible hysteresis and prolonged stability. Furthermore, under 1-m-deep water, CsPbIBr2 PSCs display a PCE of 14.18%. These findings provide an understanding of the development of phase-segregation-free CsPbIBr2 films and showcase the prospective applications of CsPbIBr2 PSCs in underwater power systems.

6.
Molecules ; 29(3)2024 Feb 04.
Artículo en Inglés | MEDLINE | ID: mdl-38338458

RESUMEN

Porous materials are widely used as an effective strategy for the solubilization of insoluble drugs. In order to improve the solubility and bioavailability of low water-solubility drugs, it is necessary to prepare porous materials. Mannitol is one of the most popular excipients in food and drug formulations. In this study, porous mannitol was investigated as a drug carrier for low water solubility drugs. Its fabrication, drug loading, and drug release mechanisms were investigated. Porous mannitol was fabricated using the co-spray-antisolvent process and utilizing polyvinylpyrrolidone K30 (PVP K30) as the template agent. Porous mannitol particles were prepared by changing the proportion of the template agent, spraying the particles with mannitol, and eluting with ethanol in order to regulate their pore structure. In subsequent studies, porous mannitol morphology and characteristics were determined systematically. Furthermore, curcumin and ibuprofen, two poorly water-soluble drugs, were loaded into porous mannitol, and their release profiles were analyzed. The results of the study indicated that porous mannitol can be prepared using PVP K30 as a template and that the amount of template agent can be adjusted in order to control the structure of the porous mannitol. When the template agent was added in amounts of 1%, 3%, and 5%, the mannitol pore size increased by 167.80%, 95.16%, and 163.98%, respectively, compared to raw mannitol. Molecular docking revealed that mannitol and drugs are adsorbents and adhere to each other by force interaction. The cumulative dissolution of curcumin and ibuprofen-loaded porous mannitol reached 69% and 70%, respectively. The release mechanism of curcumin and ibuprofen from drug-loaded mannitol was suitable for the Korsmeyer-Peppas kinetic model. In summary, the co-spray-antisolvent method proved effective in fabricating porous materials rapidly, and porous mannitol had a remarkable effect on drug solubilization. The results obtained are conducive to the development of porous materials.


Asunto(s)
Curcumina , Ibuprofeno , Porosidad , Curcumina/química , Manitol/química , Simulación del Acoplamiento Molecular , Solubilidad , Povidona/química , Agua/química , Portadores de Fármacos
7.
Angew Chem Int Ed Engl ; 63(1): e202316116, 2024 Jan 02.
Artículo en Inglés | MEDLINE | ID: mdl-37983741

RESUMEN

The water-soluble salt-template technique holds great promise for fabricating 3D porous materials. However, an equipment-free and pore-size controllable synthetic approach employing salt-template precursors at room temperature has remained unexplored. Herein, we introduce a green room-temperature antisolvent precipitation strategy for creating salt-template self-assembly precursors to universally produce 3D porous materials with controllable pore size. Through a combination of theoretical simulations and advanced characterization techniques, we unveil the antisolvent precipitation mechanism and provide guidelines for selecting raw materials and controlling the size of precipitated salt. Following the calcination and washing steps, we achieve large-scale and universal production of 3D porous materials and the recycling of the salt templates and antisolvents. The optimized nitrogen-doped 3D porous carbon (N-3DPC) materials demonstrate distinctive structural benefits, facilitating a high capacity for potassium-ion storage along with exceptional reversibility. This is further supported by in situ electrochemical impedance spectra, in situ Raman spectroscopy, and theoretical calculations. The anode shows a high rate capacity of 181 mAh g-1 at 4 A g-1 in the full cell. This study addresses the knowledge gap concerning the room-temperature synthesis of salt-template self-assembly precursors for the large-scale production of porous materials, thereby expanding their potential applications for electrochemical energy conversion and storage.

8.
Small ; 19(3): e2205088, 2023 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-36424142

RESUMEN

Surface defects-mediated nonradiative recombination plays a critical role in the performance and stability of perovskite solar cells (PSCs) and surface post-treatment is widely used for efficient PSCs. However, the commonly used surface passivation strategies are one-off and the passivation defect ability is limited, which can only solve part of the defects in the topmost surface area. Here, a secondary anti-solvent strategy is proposed to further reduce surface defects based on conventional surface passivation for the first time. Based on this, the crystallization quality of 2D Dion-Jacobson perovskite is enhanced and the surface defects density is further reduced by nearly two orders. In addition, a gradient structure of perovskite with n = 2 phases located at the top of the film and 3D-like phases located at the bottom of the film can also be obtained. The modulated perovskite film boosts the efficiency of 2D perovskites (n = 5) up to 19.55%. This strategy is also very useful in other anti-solvent processed perovskite dipping systems, which paves a promising avenue for minimizing surface defects toward highly efficient perovskite devices.

9.
Small ; 19(28): e2301323, 2023 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-36988022

RESUMEN

The pinhole-free and defect-less perovskite film is crucial for achieving high efficiency and stable perovskite solar cells (PSCs), which can be prepared by widely used anti-solvent crystallization strategies. However, the involvement of anti-solvent requires precise control and inevitably brings toxicity in fabrication procedures, which limits its large-scale industrial application. In this work, a facile and effective co-solvent engineering strategy is introduced to obtain high- quality perovskite film while avoiding the usage of anti-solvent. The uniform and compact perovskite polycrystalline films have been fabricated through the addition of co-solvent that owns strong coordination capacity with perovskite components , meanwhile possessing the weaker interaction with main solvent . With those strategies, a champion power conversion efficiency (PCE) of 22% has been achieved with the optimal co-solvent, N-methylpyrrolidone (NMP) and without usage of anti-solvent. Subsequently, PSCs based on NMP show high repeatability and good shelf stability (80% PCE remains after storing in ambient condition for 30 days). Finally, the perovskite solar module (5 × 5 cm) with 7 subcells connects in series yielding champion PCE of 16.54%. This strategy provides a general guidance of co-solvent selection for PSCs based on anti-solvent free technology and promotes commercial application of PSCs.

10.
Small ; 19(52): e2305246, 2023 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-37635119

RESUMEN

Pure δ-formamidinium lead triiodide (δ-FAPbI3 ) single crystal for highly efficient perovskite solar cell (PCS) with long-term stability is prepared by a new method consisting of liquid phase reaction of FAI and PbI2 in N,N-dimethyl formamide and antisolvent crystallization using acetonitrile. In this method, the incorporation of any impurity into the crystal is excluded by the molecular recognition of the crystal growth site. This pure crystal is used to fabricate α-FAPbI3 inverted PSCs which showed excellent power conversion efficiency (PCE) due to much-reduced trap-states. The champion device exhibited a high PCE of 23.48% under the 1-Sun condition. Surface-treated devices with 3-(aminomethyl)pyridine showed a significantly improved PCE of 25.07%. In addition, the unencapsulated device maintained 97.22% of its initial efficiency under continuous 1-Sun illumination for 1,000 h at 85 °C in an N2 atmosphere ensuring long-term thermal and photo stabilities of PSCs, whereas the control device kept only 89.93%.

11.
Molecules ; 28(12)2023 Jun 13.
Artículo en Inglés | MEDLINE | ID: mdl-37375289

RESUMEN

In this study, the crystal appearance of industrial grade 2,6-diamino-3,5-dinitropyridine (PYX) was mostly needle-shaped or rod-shaped with an average aspect ratio of 3.47 and roundness of 0.47. According to national military standards, the explosion percentage of impact sensitivity s about 40% and friction sensitivity is about 60%. To improve loading density and pressing safety, the solvent-antisolvent method was used to optimize the crystal morphology, i.e., to reduce the aspect ratio and increase the roundness value. Firstly, the solubility of PYX in DMSO, DMF, and NMP was measured by the static differential weight method, and the solubility model was established. The results showed that the Apelblat equation and Van't Hoff equation could be used to clarify the temperature dependence of PYX solubility in a single solvent. Scanning electron microscopy (SEM) was used to characterize the morphology of the recrystallized samples. After recrystallization, the aspect ratio of the samples decreased from 3.47 to 1.19, and roundness increased from 0.47 to 0.86. The morphology was greatly improved, and the particle size decreased. The structures before and after recrystallization were characterized by infrared spectroscopy (IR). The results showed that no chemical structure changes occurred during recrystallization, and the chemical purity was improved by 0.7%. According to the GJB-772A-97 explosion probability method, the mechanical sensitivity of explosives was characterized. After recrystallization, the impact sensitivity of explosives was significantly reduced from 40% to 12%. A differential scanning calorimeter (DSC) was used to study the thermal decomposition. The thermal decomposition temperature peak of the sample after recrystallization was 5 °C higher than that of the raw PYX. The thermal decomposition kinetic parameters of the samples were calculated by AKTS software, and the thermal decomposition process under isothermal conditions was predicted. The results showed that the activation energy (E) of the samples after recrystallization was higher by 37.9~527.6 kJ/mol than raw PYX, so the thermal stability and safety of the recrystallized samples were improved.

12.
Angew Chem Int Ed Engl ; 62(28): e202300971, 2023 Jul 10.
Artículo en Inglés | MEDLINE | ID: mdl-37165542

RESUMEN

The unprecedented development of perovskite solar cells (PSCs) makes them one of the most promising candidates for terawatt-scale green energy production with low cost. However, the high boiling point solvents during the solution-processed film deposition cause anisotropic crystal growth and toxic solvent vapor during high-throughput manufacturing. Here, a dual-component green solvent consisting of isopropyl acetate and acetonitrile is proposed to form a volatile perovskite precursor, which can realize the high-quality perovskite thin film deposition by intermediate phase regulation. A room-temperature stable perovskite intermediate phase is constructed with the engagement of isopropyl acetate as co-solvent, which suppresses the exploding nucleation rate in volatile perovskite precursor, providing a fine grain growth rate and wide processing window in scalable film deposition. The corresponding PSCs fabricated by blade coating without anti-solvents or gas quenching achieve power conversion efficiency (PCE) of 16.37 % and 15.29 % for the areas of 14.08 cm2 and 37.83 cm2 , respectively.

13.
Stomatologiia (Mosk) ; 102(5): 14-18, 2023.
Artículo en Ruso | MEDLINE | ID: mdl-37937918

RESUMEN

OBJECTIVE: The aim of the study to study of physical, mechanical and biocompatible properties of the matrices manufactured by antisolvent 3D printing from the solutions of polylactide-co-glycolide in tetraglycol. MATERIAL AND METHODS: Three-dimensional scaffolds were made from a solution of polylactide-co-glycolide mixed with tetraglycol using antisolvent 3D printing. The elastic properties and the structure of the obtained matrices were studied. MTT-test and staining with PKH-26, Calcein-AM, DAPI with subsequent fluorescence microscopy were used to study biological properties. RESULTS: The three-dimensional scaffolds had good mechanical properties. Young's modulus value was 18±2 MPa, tensile strength was 0.43±0.05 MPa. The relative survival rate of cells after the first day was 99.58±2.28%, on the 14th day - 98.14±2.22%. The structure of the scaffold promoted cell adhesion and spreading on its surface. CONCLUSION: The polylactide-co-glycolide matrices produced by antisolvent printing have high porosity, biocompatibility and good mechanical properties. It is allowed to use them in the future as a basis for personalized constructions for the replacement of extensive bone defects of the maxillofacial region.


Asunto(s)
Cirugía Bucal , Andamios del Tejido , Humanos , Andamios del Tejido/química , Ingeniería de Tejidos/métodos , Impresión Tridimensional , Odontología , Porosidad
14.
Mar Drugs ; 20(4)2022 Mar 29.
Artículo en Inglés | MEDLINE | ID: mdl-35447909

RESUMEN

Fucoxanthin (FX) is a marine carotenoid that has proven to be a promising marine drug due to the multiple bioactivities it possesses. However, the instability and poor bioavailability of FX greatly limit its application in pharmaceuticals or functional foods. In this study, the creative construction of a solid lipid nanoparticle-microcapsule delivery system using mixed lipids of palm stearin and cholesterol wrapped with gelatin/Arabic gum to load lipophilic FX was fabricated, aiming to improve the stability and bioavailability of FX. The results showed that the encapsulated efficiency (EE) and drug loading capacity (LC) of optimized FX microcapsules (FX-MCs) obtained were as high as 96.24 ± 4.60% and 0.85 ± 0.04%, respectively, after single-factor experiments. The average particle size was 1154 ± 54 nm with negative Zeta potential (-20.71 ± 0.93 mV) as depicted with size-zeta potential spectrometer. The differential scanning calorimeter (DSC) and thermogravimetric analyzer (TG) results indicated that FX-MC has a higher Tg and slower weight loss than FX monomers (FX crystal) and blank MCs. Besides, The Fourier transform infrared spectrometer (FTIR) confirmed the good double encapsulation of FX into the solid lipid and composite coacervate. Moreover, the encapsulated FX showed higher storage stability, sustained release (55.02 ± 2.80% release in 8 h), and significantly improved bioavailability (712.33%) when compared to free FX. The research results can provide a principle theoretical basis for the development and application of FX in pharmaceuticals or functional foods.


Asunto(s)
Nanopartículas , Disponibilidad Biológica , Cápsulas , Colesterol , Portadores de Fármacos/química , Liposomas , Nanopartículas/química , Tamaño de la Partícula , Xantófilas
15.
Drug Dev Ind Pharm ; 48(12): 683-693, 2022 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-36533708

RESUMEN

OBJECTIVE: The purpose of this work was to improve EP solubility by using a sono-crystalization approach to reduce particle size and hence, increase the dissolution rate. Significance Eplerenone (EP) is an antagonist of the aldosterone receptor and is used for the treatment of hypertension and chronic heart failure. EP was classed as biopharmaceutical classification (BCS) class II because of its poor solubility and high permeability, which retards dissolution rate and drug absorption, and decreases bioavailability. METHODS: Three-factors and two-level (23) multifactorial design have been employed to study the effect of independent variables which are drug concentration; (X1), stabilizer type (X2), and stabilizer concentration (X3) on responses; saturated solubility of EP in distilled water (Y1), saturated solubility in acidic media pH 1.2 (Y2), particle size (Y3), and polydispersity index, PDI (Y4). Also, they were characterized by Fourier transformed infrared spectroscopy (FTIR), Powder X-ray diffraction (PXRD), Differential scanning calorimetry (DSC), and yield percentage. The optimum formula was further subjected to an in-vitro release study. RESULTS: The optimized formulation showed a saturated solubility of EP as 1.29, and 1.86 (mg/ml) in distilled water and acidic media (pH 1.2) respectively. Also, the particle size of 133 nm, and PDI of 0.824 with a small percentage of the difference between the observed and predicted values. Ninety-one percent of EP was released within 10 min., and it was completely released within 45 min. with a significantly higher release rate compared to raw drug. CONCLUSION: This work resulted in a satisfactory enhancement of solubility and dissolution rate which, is suitable for further in-vivo analysis.


Asunto(s)
Nanopartículas , Agua , Solubilidad , Solventes/química , Eplerenona , Cristalización , Agua/química , Tamaño de la Partícula , Rastreo Diferencial de Calorimetría , Disponibilidad Biológica , Difracción de Rayos X , Nanopartículas/química
16.
Molecules ; 27(20)2022 Oct 18.
Artículo en Inglés | MEDLINE | ID: mdl-36296630

RESUMEN

Auricularia auricula-judae polysaccharide (AAP)-based nanoparticles (NPs) prepared via an anti-solvent precipitation approach were studied. Response surface methodology (RSM) design was carried out on the basis of single factor experiments, using average size and polydispersity index (PDI) as indicators. The optimal preparation conditions were determined to include an AAP concentration of 1 mg/mL, a pH of 8, and an anti-solvent/solvent volume ratio of 6. The average particle sizes of the AAP-NPs, PDI and electrical characteristic (ζ-potential) were found to be 150.27 ± 3.21 nm, 0.135 ± 0.012 and -31.10 ± 0.52 mV, respectively. Furthermore, Fourier transform infrared spectroscopy (FTIR) was used to determine the chemical structure of the AAP-NPs. It was observed that the intensity of AAP-NPs in the wide spectral band of 3000-3750 cm-1 was significantly stronger than that of the AAP, as was the characteristic peak of carboxyl anion, and the characteristic band moved to shorter wavelengths. Subsequent thermogravimetric analysis showed that the antisolvent precipitation method improved the thermal stability of the AAP, while scanning electron microscopy (SEM) and X-ray diffraction (XRD) showed that the morphology of AAP-NPs was uniform and well-distributed, and that their single crystal structures had remained unaffected during the process. Moreover, the DPPH and ABTS scavenging activities of AAP-NPs were increased, and the IC50 values were 0.544 ± 0.241 mg/mL and 0.755 ± 0.226 mg/mL, respectively.


Asunto(s)
Antioxidantes , Nanopartículas , Antioxidantes/farmacología , Antioxidantes/química , Polisacáridos/química , Nanopartículas/química , Solventes/química
17.
Inflammopharmacology ; 30(1): 327-341, 2022 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-35006455

RESUMEN

Curcumin presents a promising anti-inflammatory potential, but its low water-solubility and bioavailability hinder its application. In this sense, cocrystallization represents a tool for improving physicochemical properties, solubility, permeability, and bioavailability of new drug candidates. Thus, the aim of this work was to produce curcumin cocrystals (with n-acetylcysteine as coformer, which possesses anti-inflammatory and antioxidant activities), by the anti-solvent gas technique using supercritical carbon dioxide, and to test its antinociceptive and anti-inflammatory potential. The cocrystal was characterized by differential scanning calorimetry, powder X-ray diffraction and scanning electron microscopy. The cocrystal solubility and antichemotaxic activity were also assessed in vitro. Antinociceptive and anti-inflammatory activities were carried out in vivo using the acetic acid-induced abdominal writhing and carrageenan-induced paw oedema assays in mice. The results demonstrated the formation of a new crystalline structure, thereby confirming the successful formation of the cocrystal. The higher solubility of the cocrystal compared to pure curcumin was verified in acidic and neutral pH, and the cocrystal inhibited the chemotaxis of neutrophils in vitro. In vivo assays showed that cocrystal presents increased antinociceptive and anti-inflammatory potency when compared to pure curcumin, which could be related to an improvement in its bioavailability.


Asunto(s)
Curcumina , Acetilcisteína/farmacología , Analgésicos/farmacología , Animales , Antiinflamatorios/farmacología , Cristalización/métodos , Curcumina/farmacología , Ratones , Solubilidad , Solventes/química
18.
Pharm Dev Technol ; 27(10): 999-1008, 2022 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-36322612

RESUMEN

Antisolvent crystallization approach using either water (in conventional crystallization process (WAS)), or supercritical CO2 (in supercritical anti-solvent crystallization (SCAS)), was employed in presence of hydroxypropyl methylcellulose (HPMC) to enhance the dissolution of curcumin. The impact of pressure, temperature and depressurization time on the SCAS process was studied using the Box-Behnken design to achieve the highest saturation solubility. A physical mixture of curcumin-HPMC was prepared for comparison purposes. Saturation solubility, scanning electron microscopy, differential scanning calorimetry, X-ray diffraction analysis and Fourier transform infrared spectroscopy were conducted to characterize the solid-state characteristics of the crystallized samples. Dissolution studies helped in ascertaining the effects of the crystallization techniques on the performance of the formulation. Curcumin crystalized by different antisolvent displayed varied shapes, sizes, saturation solubility's and dissolution properties. In SCAS process, the maximum saturation solubility (2.83 µg/mL) was obtained when the pressure, temperature and depressurization time were 275 bars, 55 °C, and 22 min respectively. The SCAS samples showed the highest dissolution (70%) in 30 min compared to WAS (27%), physical mixture (18%) and unprocessed curcumin (16%). The improved dissolution rate of SCAS sample originates from the development of sponge-like particles with augmented porosity, decreased crystallinity as well as increased solubility of curcumin.


Asunto(s)
Curcumina , Curcumina/química , Solubilidad , Dióxido de Carbono , Agua , Cristalización/métodos , Solventes/química , Rastreo Diferencial de Calorimetría , Difracción de Rayos X , Microscopía Electrónica de Rastreo
19.
J Food Sci Technol ; 59(3): 1131-1139, 2022 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-35185212

RESUMEN

Gum tragacanth nanoparticles were prepared using a combination of intense ultrasound energy and anti-solvent precipitation methods in this research. Results showed that smaller particles were produced by increasing sonication time. As well, increasing the sonication power led to smaller particles, however, increased aggregation. Accordingly, tragacanth solutions with 0.5 and 1% (w/v) concentrations were prepared and mixed with ethanol (ratio 1:10 v/v) after ultrasound treatment with two different drop-wise and direct methods to investigate the effect of anti-solvent addition method on the precipitation of tragacanth particles. The nanoparticle images showed that the concentration of the 0.5% tragacanth solution and the direct mixing method was suitable for particle production with desirable size (72 ± 10 nm) and uniformity. FTIR, XRD, and STA studies showed that the tragacanth chemical composition did not change, and only its particle size decreased. Investigation of wettability showed a contact angle of 88.9 ± 1.7 degrees for nanoparticles providing partial wetting of the particles at the interface. Investigation of the solution viscosities of 0.5% tragacanth gum and tragacanth nanoparticles showed that the viscosity of the nanoparticles solution was significantly lower than that of the tragacanth (p < 0.05) indicating the intense effect of ultrasonication on this property. It can be concluded that the high viscosity of tragacanth gum is not due to its chemical composition but is due to its complex structure.

20.
Nanotechnology ; 33(9)2021 Dec 07.
Artículo en Inglés | MEDLINE | ID: mdl-34808612

RESUMEN

A systematic study of the synthetic procedure to improve quantum efficiency of luminescent hybrid perovskite QDs through ligand-assisted precipitation method is presented. Particularly, the influence of the dielectric constant and dipole moment of the antisolvent on the reaction time and the photophysical properties of the QDs is highlighted. After evaluating the influence of antisolvents and optimizing experimental parameters such as reaction time and Pb excess of the precursor, colloidal crystalline MAPbBr3QDs with exceptionally high absolute quantum yield up to 97.7% in solution and 69.1% in solid film were obtained. Finally, MAPbBr3QDs precipitated from anisole were processed like UV-curable nanocomposite as efficient down conversion layer resulting in very narrow green emission light-emitting diode.

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