Supercritical CO₂-Assisted Spray Drying of Strawberry-Like Gold-Coated Magnetite Nanocomposites in Chitosan Powders for Inhalation.
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ABSTRACT:
SUBMITTER: Silva MC
PROVIDER: S-EPMC5344610 | biostudies-other | 2017 Jan
REPOSITORIES: biostudies-other
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Project description:Local delivery of small interfering RNA (siRNA) to the lungs constitutes a promising new area in drug delivery. The present study evaluated parameters of importance for spray drying of siRNA-loaded poly(D,L-lactide-co-glycolide) (PLGA) nanoparticles (NPs) into nanocomposite microparticles intended for inhalation. The spray drying process was optimised using a statistical design of experiment and by evaluating powder characteristics upon systematic variation of the formulation parameters. Concentration, carbohydrate excipient (trehalose, lactose and mannitol) and the ratio of NP to excipient were varied to monitor the effects on moisture content, particle morphology, particle size and powder yield. The identified optimum conditions were applied for spray drying of siRNA-loaded nanocomposite microparticles, resulting in a product with a low water content (0.78% w/w) and an aerodynamic particle diameter considered suitable for inhalation. The use of mannitol in the formulation allowed a significantly lower moisture content than trehalose and lactose. The inclusion of 50% (w/w) or higher amounts of NPs resulted in a marked change in the surface morphology of the spray-dried particles. Importantly, the integrity and biological activity of the siRNA were preserved during the spray drying process. In conclusion, the present results show that spray drying is a suitable technique for producing nanocomposite microparticles comprising siRNA-containing PLGA NPs for potential use in inhalation therapy.
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Project description:In this study, the chitosan-based release microspheres were prepared by spray drying method. Chitosan was used as the carrier material, and Panax notoginseng extract, Codonopsis extract, and Atractylodes extract (the mass ratio was 2:7:5) were active substance. The spray drying preparation process of microsphere was optimized by single factor experiment and L9 (34) orthogonal design. Drug loading (DL), particle size, and sustained release performance of microspheres were investigated. The mass fraction of chitosan was 1.5%, the mass ratio of drug to chitosan was 1:3, the inlet air temperature was 130°C, and the injection rate was 400 ml/hr. The chitosan-based microspheres prepared under the above conditions had a smooth surface, and the DL was 23.87 ± 0.93%; the average particle diameter was 10.27 ± 1.05 ?m, and the encapsulation efficiency (EE) of the microspheres was 91.28 ± 1.04%. The preparation process of chitosan-based drug microsphere prepared by spray drying method was simple and stable. The prepared microspheres in this paper showed a sustained release effect in vitro.
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Project description:BACKGROUND:OZ439 is a new chemical entity which is active against drug-resistant malaria and shows potential as a single-dose cure. However, development of an oral formulation with desired exposure has proved problematic, as OZ439 is poorly soluble (BCS Class II drug). In order to be feasible for low and middle income countries (LMICs), any process to create or formulate such a therapeutic must be inexpensive at scale, and the resulting formulation must survive without refrigeration even in hot, humid climates. We here demonstrate the scalability and stability of a nanoparticle (NP) formulation of OZ439. Previously, we applied a combination of hydrophobic ion pairing and Flash NanoPrecipitation (FNP) to formulate OZ439 NPs 150 nm in diameter using the inexpensive stabilizer hydroxypropyl methylcellulose acetate succinate (HPMCAS). Lyophilization was used to process the NPs into a dry form, and the powder's in vitro solubilization was over tenfold higher than unprocessed OZ439. METHODS:In this study, we optimize our previous formulation using a large-scale multi-inlet vortex mixer (MIVM). Spray drying is a more scalable and less expensive operation than lyophilization and is, therefore, optimized to produce dry powders. The spray dried powders are then subjected to a series of accelerated aging stability trials at high temperature and humidity conditions. RESULTS:The spray dried OZ439 powder's dissolution kinetics are superior to those of lyophilized NPs. The powder's OZ439 solubilization profile remains constant after 1 month in uncapped vials in an oven at 50 °C and 75% RH, and for 6 months in capped vials at 40 °C and 75% RH. In fasted-state intestinal fluid, spray dried NPs achieved 80-85% OZ439 dissolution, to a concentration of 430 µg/mL, within 3 h. In fed-state intestinal fluid, 95-100% OZ439 dissolution is achieved within 1 h, to a concentration of 535 µg/mL. X-ray powder diffraction and differential scanning calorimetry profiles similarly remain constant over these periods. CONCLUSIONS:The combined nanofabrication and drying process described herein, which utilizes two continuous unit operations that can be operated at scale, is an important step toward an industrially-relevant method of formulating the antimalarial OZ439 into a single-dose oral form with good stability against humidity and temperature.
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Project description:The development of new materials is needed to address the environmental challenges of wastewater treatment. The phosphorylation of guar gum combined with its association to chitosan allows preparing an efficient sorbent for the removal of U(VI) from slightly acidic solutions. The incorporation of magnetite nanoparticles enhances solid/liquid. Functional groups are characterized by FTIR spectroscopy while textural properties are qualified by N2 adsorption. The optimum pH is close to 4 (deprotonation of amine and phosphonate groups). Uptake kinetics are fast (60 min of contact), fitted by a pseudo-first order rate equation. Maximum sorption capacities are close to 1.28 and 1.16 mmol U g-1 (non-magnetic and magnetic, respectively), while the sorption isotherms are fitted by Langmuir equation. Uranyl desorption (using 0.2 M HCl solutions) is achieved within 20-30 min; the sorbents can be recycled for at least five cycles (5-6% loss in sorption performance, complete desorption). In multi-component solutions, the sorbents show marked preference for U(VI) and Nd(III) over alkali-earth metals and Si(IV). The zone of exclusion method shows that magnetic sorbent has antibacterial effects against both Gram+ and Gram- bacteria, contrary to non-magnetic material (only Gram+ bacteria). The magnetic composite is highly promising as antimicrobial support and for recovery of valuable metals.
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Project description:This study aimed to offer an alternative way for delivering the benefits of the mandarin fruit juice to consumers via spray drying microencapsulation. Two mandarin cultivars, Afourer (A) and Richard Special (RS), were studied. Three types of juice sample were prepared, i.e., the whole fruit juice (A3 & RS3), the flavedo-removed fruit juice (A2 & RS2), and the peel-removed fruit juice (A1 & RS1) samples. Gum Acacia and maltodextrin (ratio of 1:1, w/w) were chosen as wall matrices for aiding the drying of the juice samples while using a microfluidic-jet spray dryer. The properties of the fruit powder (colour, water activity, bulk/trapped density, solubility, hygroscopicity, morphology) and the retention of major phytochemicals (i.e., phenolic and volatile compounds) were examined. The results showed that the powders produced from the whole fruit juices (A3 and RS3) gave higher yellow colour with a regular winkled surface than other powders (A1 & RS1, and A2 & RS2). The water activity of mandarin powders was in a range of 0.14 to 0.25, and the solubility was around 74% with no significant difference among all of the powders. The whole fruit powders had a significantly higher concentration of phenolic compounds (A3, 1023 µg/100 mg vs. A2, 809 µg/100 mg vs. A1, 653 µg/100 mg) and aroma compounds (A3, 775,558 µg/L vs. A2, 125,617 µg/L vs. A1, 12,590 µg/L). This study contributed to the delivery of phenolic and flavour compounds of the mandarin fruits, at the same time minimising waste generation during processing. It also gave insight into the production of spray-dried powders from the whole mandarin fruits.
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Project description:In this study, supercritical fluid-assisted spray-drying (SA-SD) was applied to achieve the micronization of fenofibrate particles possessing surface-active additives, such as d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS), sucrose mono palmitate (Sucroester 15), and polyoxyethylene 52 stearate (Myrj 52), to improve the pharmacokinetic and pharmacodynamic properties of fenofibrate. For comparison, the same formulation was prepared using a spray-drying (SD) process, and then both methods were compared. The SA-SD process resulted in a significantly smaller mean particle size (approximately 2 μm) compared to that of unprocessed fenofibrate (approximately 20 μm) and SD-processed particles (approximately 40 μm). There was no significant difference in the effect on the particle size reduction among the selected surface-active additives. The microcomposite particles prepared with surface-active additives using SA-SD exhibited remarkable enhancement in their dissolution rate due to the synergistic effect of comparably moderate wettability improvement and significant particle size reduction. In contrast, the SD samples with the surface-active additives exhibited a decrease in dissolution rate compared to that of the unprocessed fenofibrate due to the absence of particle size reduction, although wettability was greatly improved. The results of zeta potential and XPS analyses indicated that the surface-active additive coverage on the surface layer of the SD-processed particles with a better wettability was higher than that of the SA-SD-processed composite particles. Additionally, after rapid depletion of hydrophilic additives that were excessively distributed on the surfaces of SD-processed particles, the creation of a surface layer rich in poorly water-soluble fenofibrate resulted in a decrease in the dissolution rate. In contrast, the surface-active molecules were dispersed homogeneously throughout the particle matrix in the SA-SD-processed microparticles. Furthermore, improved pharmacokinetic and pharmacodynamic characteristics were observed for the SA-SD-processed fenofibrate microparticles compared to those for the SD-processed fenofibrate particles. Therefore, the SA-SD process incorporating surface-active additives can efficiently micronize poorly water-soluble drugs and optimize their physicochemical and biopharmaceutical characteristics.
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Project description:This review covers recent developments in the area of particle engineering via spray drying. The last decade has seen a shift from empirical formulation efforts to an engineering approach based on a better understanding of particle formation in the spray drying process. Microparticles with nanoscale substructures can now be designed and their functionality has contributed significantly to stability and efficacy of the particulate dosage form. The review provides concepts and a theoretical framework for particle design calculations. It reviews experimental research into parameters that influence particle formation. A classification based on dimensionless numbers is presented that can be used to estimate how excipient properties in combination with process parameters influence the morphology of the engineered particles. A wide range of pharmaceutical application examples -- low density particles, composite particles, microencapsulation, and glass stabilization -- is discussed, with specific emphasis on the underlying particle formation mechanisms and design concepts.
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Project description:To develop stable and inhalable dry powder formulations with long shelf life, we spray dried polyplexes consisting of siRNA and a polyethylenimine based block copolymer in presence of mannitol or trehalose. We investigated the effect of inlet (T-In) and outlet (T-Out) temperature on the recovery of siRNA as well as adsorption effects within the tubing material. Choosing a low abrasion silicon tubing prevented siRNA loss due to adsorption. Mannitol and trehalose formulations preserved siRNA integrity regardless of excipient concentration and temperature at T-Out below the siRNA melting temperature. Trehalose formulations allowed full siRNA recovery whereas mannitol formulations resulted in spray drying induced losses of ~20 % siRNA and of 50-60 % polymer. Mannitol formulations showed optimal aerodynamic characteristics as confirmed by next generation impaction analysis based upon siRNA content. All spray dried formulations resulted in GFP silencing comparable or better than freshly prepared polyplexes. To test if the observed results could be transferred, formulations of siRNA and transferrin-PEI conjugates were spray dried, characterized and used to transfect primary human T cells ex vivo. Results confirmed successful silencing of the Th2 transcription factor GATA3 in primary CD4+ T cells with spray dried formulations as a potential treatment for severe asthma.
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Project description:Spin-crossover (SCO) triazole-based coordination polymers can be synthesized by micelle techniques, which almost always lead to rod-shaped nanoparticles. In order to notably reach new morphologies, we explore here the potentiality of the spray-drying (SD) method to get SCO materials. Three SCO coordination polymers and a mononuclear complex are investigated. In all cases, the SD method obtains particles definitely showing SCO. The features of the latter are yet always different from those of the referenced materials, in the sense that SCO is more gradual and incomplete, in adequacy with the poor crystallinity of the powders obtained by SD. In the case of coordination polymers, the particles are preferentially spherical. Indications of possible polymorphism and/or new materials induced by the use of the SD method are evidenced. In the case of the mononuclear complex, the SD method has allowed reproducing, in a quick and easy way, the well-known bulk compound. This exploratory work demonstrates the relevance of the concept and opens the way to a systematic scrutiny of all the experimental parameters to tune the size, morphology, and properties of the SD-synthesized SCO particles.
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Project description:An optimum carrier rugosity is essential to achieve a satisfying drug deposition efficiency for the carrier based dry powder inhalation (DPI). Therefore, a non-organic spray drying technique was firstly used to prepare nanoporous mannitol with small asperities to enhance the DPI aerosolization performance. Ammonium carbonate was used as a pore-forming agent since it decomposed with volatile during preparation. It was found that only the porous structure, and hence the specific surface area and carrier density were changed at different ammonium carbonate concentration. Furthermore, the carrier density was used as an indication of porosity to correlate with drug aerosolization. A good correlation between the carrier density and fine particle fraction (FPF) (r2 = 0.9579) was established, suggesting that the deposition efficiency increased with the decreased carrier density. Nanoporous mannitol with a mean pore size of about 6 nm exhibited 0.24-fold carrier density while 2.16-fold FPF value of the non-porous mannitol. The enhanced deposition efficiency was further confirmed from the pharmacokinetic studies since the nanoporous mannitol exhibited a significantly higher AUC0-8h value than the non-porous mannitol and commercial product Pulmicort. Therefore, surface modification by preparing nanoporous carrier through non-organic spray drying showed to be a facile approach to enhance the DPI aerosolization performance.
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