RESUMO
BACKGROUND: Fish oil is an important source of healthy ω-3 fatty acids to be used in functional foods. However, its autoxidation susceptibility, aroma and solubility make it difficult to use. Its encapsulation could reduce these disadvantages. This manuscript focuses on the drying stage of the encapsulation process. Its objective was to study the encapsulation of fish oil with soy proteins by emulsification and lyophilization and compare microparticles characteristics with those processed identically but spray dried. RESULTS: Microparticles with different protein/oil ratios were prepared by emulsification and lyophilization. Soy proteins encapsulated fish oil in matrix-type microcapsules masking its typical odor and oily appearance. Microparticles dried by lyophilization showed a better solid recovery but lower encapsulation efficiency than those spray dried. Increasing protein/oil mass ratio of initial formulations seemed to favor initial lipid oxidation, but these differences were not appreciated when analyzing the oxidative stability over time (measured by Rancimat test). Porous structure and large surface area of lyophilized samples would favor oxygen easy penetration and exposition to free radicals, increasing lipid oxidation over time, while spray dried microparticles showed a good oxidative stability over time, like that of free oil. CONCLUSION: Drying processes were determinants in the morphology of microcapsules, the efficiency of encapsulation and protection exerted on the oil. Although emulsifying and drying processes caused certain initial oil oxidation, soy proteins managed to mask fish oil flavors and spray dried systems showed a good perspective of oxidative stability of fish oil over time, better than that of lyophilized microparticles. © 2021 Society of Chemical Industry.
Assuntos
Composição de Medicamentos/métodos , Óleos de Peixe/química , Proteínas de Soja/química , Cápsulas/química , Dessecação , Composição de Medicamentos/instrumentação , Estabilidade de Medicamentos , Liofilização , OxirreduçãoRESUMO
BACKGROUND: Microorganism for biological control of fruit diseases is an eco-friendly alternative to the use of chemical fungicides. RESULTS: This is the first study evaluating the electrospraying process to encapsulate the biocontrol yeast Meyerozyma caribbica. The effect of encapsulating material [Wey protein concentrate (WPC), Fibersol® and Trehalose], its concentration and storage temperature on the cell viability of M. caribbica, and in vitro and in vivo control of Colletotrichum gloeosporioides was evaluated. The processing with commercial resistant maltodextrin (Fibersol®) 30% (w/v) as encapsulating material showed the highest initial cell viability (95.97 ± 1.01%). The storage at 4 ± 1 °C showed lower losses of viability compared to 25 ± 1 °C. Finally, the encapsulated yeast with Fibersol 30% w/v showed inhibitory activity against anthracnose in the in vitro and in vivo tests, similar to yeast fresh cells. CONCLUSION: Electrospraying was a highly efficient process due to the high cell viability, and consequently, a low quantity of capsules is required for the postharvest treatment of fruits. Additionally, the yeast retained its antagonistic power during storage. © 2021 Society of Chemical Industry.
Assuntos
Agentes de Controle Biológico/química , Agentes de Controle Biológico/farmacologia , Carica/microbiologia , Colletotrichum/efeitos dos fármacos , Composição de Medicamentos/métodos , Mangifera/microbiologia , Saccharomycetales/química , Antibiose , Colletotrichum/crescimento & desenvolvimento , Composição de Medicamentos/instrumentação , Frutas/microbiologia , Viabilidade Microbiana , Saccharomycetales/fisiologiaRESUMO
Numerous hydrophobic compounds are important ingredients for drug discovery and development. Hydrophobicity has been a major hurdle limiting the therapeutic efficacy of drugs. Drugs with low solubility are biopharmaceutically classified as class II and class IV drugs. Other challenges facing the pharmaceutical industry include low bioavailability, poor dissolution and erratic absorption of various compounds. In recent years, several technologies and methods have been developed to improve the solubility of drugs, meanwhile various mechanisms of improving solubility of compounds have been proposed. This review explores recent advances and techniques used to enhance solubility of lipophilic or low-solublility drugs. We summarize several strategies, such as rotor stator colloid mill, jet mill, ball mill, spray drying, hot melt extrusion, supercritical fluid and structural modification, including salt formation, and co-crystallization.
Assuntos
Química Farmacêutica/métodos , Composição de Medicamentos/métodos , Interações Hidrofóbicas e Hidrofílicas , Preparações Farmacêuticas/química , Portadores de Fármacos/química , Composição de Medicamentos/instrumentação , Sistemas de Liberação de Medicamentos , SolubilidadeRESUMO
Poor aqueous drug solubility represents a major challenge in oral drug delivery. A novel approach to overcome this challenge is drug amorphization inside a tablet, that is, on-demand drug amorphization. The amorphous form is a thermodynamically instable, disordered solid-state with increased dissolution rate and solubility compared to its crystalline counterpart. During on-demand drug amorphization, the drug molecularly disperses into a polymer to form an amorphous solid at elevated temperatures inside a tablet. This study investigates, for the first time, the utilization of photothermal plasmonic nanoparticles for on-demand drug amorphization as a new pharmaceutical application. For this, near-IR photothermal plasmonic nanoparticles were tableted together with a crystalline drug (celecoxib) and a polymer (polyvinylpyrrolidone). The tablets were subjected to a near-IR laser at different intensities and durations to study the rate of drug amorphization under each condition. During laser irradiation, the plasmonic nanoparticles homogeneously heated the tablet. The temperature was directly related to the rate and degree of amorphization. Exposure times as low as 180 s at 1.12 W cm-2 laser intensity with only 0.25 wt % plasmonic nanoparticles and up to 50 wt % drug load resulted in complete drug amorphization. Therefore, near-IR photothermal plasmonic nanoparticles are promising excipients for on-demand drug amorphization with laser irradiation.
Assuntos
Celecoxib/química , Composição de Medicamentos/métodos , Excipientes/efeitos da radiação , Lasers , Nanopartículas/efeitos da radiação , Composição de Medicamentos/instrumentação , Excipientes/química , Nanopartículas/química , Povidona/química , Solubilidade/efeitos da radiação , ComprimidosRESUMO
PURPOSE: Proper taste-masking formulation design is a critical issue for instant-dissolving tablets (IDTs). The purpose of this study is to use the electronic tongue to design the additives of the 3D printed IDTs to improve palatability. METHODS: A binder jet 3D printer was used to prepare IDTs of levetiracetam. A texture analyzer and dissolution apparatus were used to predict the oral dispersion time and in vitro drug release of IDTs, respectively. The palatability of different formulations was investigated using the ASTREE electronic tongue in combination with the design of experiment and a model for masking bitter taste. Human gustatory sensation tests were conducted to further evaluate the credibility of the results. RESULTS: The 3D printed tablets exhibited rapid dispersion (<30 s) and drug release (2.5 min > 90%). The electronic tongue had an excellent ability of taste discrimination, and levetiracetam had a good linear sensing performance based on a partial least square regression analysis. The principal component analysis was used to analyze the signal intensities of different formulations and showed that 2% sucralose and 0.5% spearmint flavoring masked the bitterness well and resembled the taste of corresponding placebo. The results of human gustatory sensation test were consistent with the trend of the electronic tongue evaluation. CONCLUSIONS: Owing to its objectivity and reproducibility, this technique is suitable for the design and evaluation of palatability in 3D printed IDT development.
Assuntos
Composição de Medicamentos/instrumentação , Nariz Eletrônico , Excipientes/química , Levetiracetam/química , Paladar , Administração Oral , Composição de Medicamentos/métodos , Humanos , Levetiracetam/administração & dosagem , Impressão Tridimensional , Reprodutibilidade dos Testes , ComprimidosRESUMO
PURPOSE: We aimed to evaluate the feasibility of cross-linked polystyrene (CPS)-yttrium-stabilized zirconia (YSZ) bead mixtures as a novel optimization approach for fast, effective production of drug nanosuspensions during wet stirred media milling (WSMM). METHODS: Aqueous suspensions of 10% fenofibrate (FNB, drug), 7.5% HPC-L, and 0.05% SDS were wet-milled at 3000-4000 rpm and 35%-50% volumetric loading of CPS:YSZ bead mixtures (CPS:YSZ 0:1-1:0 v:v). Laser diffraction, SEM, viscometry, DSC, and XRPD were used for characterization. An nth-order model described the breakage kinetics, while a microhydrodynamic model allowed us to gain insights into the impact of bead materials. RESULTS: CPS beads achieved the lowest specific power consumption, whereas YSZ beads led to the fastest breakage. Breakage followed second-order kinetics. Optimum conditions were identified as 3000 rpm and 50% loading of 0.5:0.5 v/v CPS:YSZ mixture from energy-cycle time-heat dissipation perspectives. The microhydrodynamic model suggests that YSZ beads experienced more energetic/forceful collisions with smaller contact area as compared with CPS beads owing to the higher density-elastic modulus of the former. CONCLUSIONS: We demonstrated the feasibility of CPS-YSZ bead mixtures and rationalized its optimal use in WSMM through their modulation of breakage kinetics, energy utilization, and heat dissipation.
Assuntos
Composição de Medicamentos/instrumentação , Fenofibrato/química , Nanopartículas/química , Reagentes de Ligações Cruzadas/química , Estudos de Viabilidade , Tamanho da Partícula , Poliestirenos/química , Suspensões , Fatores de Tempo , Ítrio/química , Zircônio/químicaRESUMO
PURPOSE: Present (i) an infrared (IR)-based Process Analytical Technology (PAT) installed in a lab-scale freeze-dryer and (ii) a micro freeze-dryer (MicroFD®) as effective tools for freeze-drying design space calculation of the primary drying stage. METHODS: The case studies investigated are the freeze-drying of a crystalline (5% mannitol) and of an amorphous (5% sucrose) solution processed in 6R vials. The heat (Kv) and the mass (Rp) transfer coefficients were estimated: tests at 8, 13 and 26 Pa were carried out to assess the chamber pressure effect on Kv. The design space of the primary drying stage was calculated using these parameters and a well-established model-based approach. The results obtained using the proposed tools were compared to the ones in case Kv and Rp were estimated in a lab-scale unit through gravimetric tests and a thermocouple-based method, respectively. RESULTS: The IR-based method allows a non-gravimetric estimation of the Kv values while with the micro freeze-dryer gravimetric tests require a very small number of vials. In both cases, the obtained values of Kv and Rp, as well as the resulting design spaces, were all in very good agreement with those obtained in a lab-scale unit through the gravimetric tests (Kv) and the thermocouple-based method (Rp). CONCLUSIONS: The proposed tools can be effectively used for design space calculation in substitution of other well-spread methods. Their advantages are mainly the less laborious Kv estimation process and, as far as the MicroFD® is concerned, the possibility of saving time and formulation material when evaluating Rp.
Assuntos
Desenho Assistido por Computador/instrumentação , Composição de Medicamentos/métodos , Liofilização/métodos , Modelos Químicos , Química Farmacêutica , Composição de Medicamentos/instrumentação , Liofilização/instrumentação , Manitol/química , Espectrofotometria Infravermelho/instrumentação , Espectrofotometria Infravermelho/métodos , Sacarose/químicaRESUMO
PURPOSE: Sterile filtration can be a particular challenge when processing very large glycoconjugate vaccines. The objective of this study was to examine the sterile filtration performance of a series of glycoconjugate vaccines produced by coupling different polysaccharide serotypes to an immunogenic protein. METHODS: Sterile filtration was performed at constant filtrate flux using 0.22 µm pore size Durapore® polyvinylidene fluoride membranes. Glycoconjugates were characterized by dynamic light scattering, rheological measurements, and nanoparticle tracking analysis (NTA). Confocal microscopy was used to examine glycoconjugate capture profiles within the membrane. Transmembrane pressure data were analyzed using a recently developed fouling model. RESULTS: All glycoconjugates deposited in a narrow band near the entrance of the Durapore® membranes. The rate of fouling varied significantly for the different serotypes, with the fouling parameter correlated with the fraction of glycoconjugates larger than 200 nm in size. CONCLUSIONS: The fouling behavior and sterile filter capacity of the different glycoconjugate serotypes are determined primarily by the presence of large species (>200 nm in size) as determined by nanoparticle tracking analysis. The modified intermediate pore blockage model provides a framework for predicting the sterile filtration performance for these glycoconjugate vaccines.
Assuntos
Composição de Medicamentos/normas , Contaminação de Medicamentos/prevenção & controle , Glicoconjugados/normas , Vacinas Conjugadas/normas , Composição de Medicamentos/instrumentação , Composição de Medicamentos/métodos , Filtração/instrumentação , Filtração/normas , Glicoconjugados/química , Membranas Artificiais , Filtros Microporos , Tamanho da Partícula , Vacinas Conjugadas/químicaRESUMO
BACKGROUND: Although N13-ammonia has favorable properties among FDA approved radiotracers, complexity of implementation has limited its use. We describe the initial patient experience of N13-ammonia PET imaging using a compact N13-ammonia production system. METHODS: N13 was produced using the ION-12SC, a 12MeV, 10uA superconducting minimally shielded cyclotron, and reduced to N13-ammonia in an automated multi-use purification unit. Patients were power injected with 9.3 ± 1.1 mCi (344.1 ± 40.7 MBq) of N13-ammonia for rest imaging, and 18.8 ± 0.9 mCi (695.6 ± 33.3 MBq) of N13-ammonia was injected at peak hyperemia for stress testing. Images were interpreted for relative perfusion, left ventricular volumes/function, blood flow quantification, and scored for image quality. RESULTS: In total 97 patients underwent 98 N13-ammonia PET scans (32 rest only/65 rest-stress/1 stress only). Image quality was 91.8% good or excellent. None were poor/non-diagnostic. Study durations were acceptable. Tracer related radiation dosimetry to patients was 0.7 ± 0.1 mSv (rest only), and 2.1 ± 0.1 mSv (rest-stress). CONCLUSION: Clinical N13-ammonia production by the Ionetix ION-12SC delivers high quality myocardial PET perfusion images in a rapid protocol.
Assuntos
Amônia , Doença da Artéria Coronariana/diagnóstico por imagem , Imagem de Perfusão do Miocárdio , Radioisótopos de Nitrogênio , Tomografia por Emissão de Pósitrons combinada à Tomografia Computadorizada , Idoso , Ciclotrons , Composição de Medicamentos/instrumentação , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , SupercondutividadeRESUMO
BACKGROUND: Throughout the past decade, Pickering emulsion has been increasingly utilized for the encapsulation of bioactive compounds due to its high stability and biocompatibility. In the present work, palm tocotrienols were initially encapsulated in a calcium carbonate Pickering emulsion, which was then subjected to alginate gelation and subsequent chitosan coating. The effects of wall material (alginate and chitosan) concentrations, gelation pH and time, and chitosan coating time on the encapsulation efficiency of palm tocotrienols were explored. RESULTS: Our findings revealed that uncoated alginate microcapsules ruptured upon drying and exhibited low encapsulation efficiency (13.81 ± 2.76%). However, the addition of chitosan successfully provided a more complex and rigid external wall structure to enhance the stability of the microcapsules. By prolonging the crosslinking time from 5 to 30 min and increasing the chitosan concentration from 0.1% to 0.5%, the oil encapsulation efficiency was increased by 28%. Under the right gelation pH (pH 4), the extension of gelation time from 1 to 12 h resulted in an increase in alginate-Ca2+ crosslinkings, thus strengthening the microcapsules. CONCLUSION: With the optimum formulation and process parameters, a high encapsulation efficiency (81.49 ± 1.75%) with an elevated oil loading efficiency (63.58 ± 2.96%) were achieved. The final product is biocompatible and can potentially be used for the delivery of palm tocotrienols. © 2021 Society of Chemical Industry.
Assuntos
Alginatos/química , Quitosana/química , Composição de Medicamentos/métodos , Tocotrienóis/química , Cápsulas/química , Composição de Medicamentos/instrumentação , Emulsões/química , Géis/química , Concentração de Íons de HidrogênioRESUMO
BACKGROUND: Anthocyanins were extracted from grape skins by a combination of ethanolic-ultrasonic assisted methods and were then encapsulated by freeze-drying in soy phosphatidylcholine vesicles with the addition of different polymers, such as pectin, acacia gum, and whey protein isolate. The goal of this research was to microencapsulate anthocyanin compounds extracted from grape skins, to characterize the stability and behavior of the vesicles and then to use them to obtain a new light formulated mayonnaise. RESULTS: The particle size ranged from 900 nm in the control condition to 250 nm in vesicles loaded with whey proteins. The powders showed higher encapsulation efficiency for all variants, ranging from 81 to 96%. Vibrational spectroscopy revealed better inclusion of anthocyanins in polysaccharide-based coacervates, whereas in protein-based coacervates a possible interaction of anthocyanins with amine groups was observed. The vesicles were tested for in vitro release, and the results confirmed the gradual release of the anthocyanins in both stages of digestion, with a residual content of about 50% in the vesicles. The powders displayed high stability during storage in the dark at 4 °C. The panelists appreciated the new light formulated mayonnaises enriched with 10% dried vesicles compared with the control sample, in particular samples with acacia gum. CONCLUSION: The study revealed that polymer-loaded vesicles presented stability in simulated gastrointestinal fluids and have proved successful in obtaining new light enriched mayonnaises. © 2020 Society of Chemical Industry.
Assuntos
Antocianinas/química , Composição de Medicamentos/métodos , Extratos Vegetais/química , Polímeros/química , Vitis/química , Composição de Medicamentos/instrumentação , Frutas/química , Tamanho da Partícula , Polímeros/síntese química , Pós/químicaRESUMO
BACKGROUND: Although the structure and physicochemical properties of large ring cyclodextrins (LR-CDs) exhibit unique characteristics, and also possess very strong water solubility and high safety, little is known about the embedding performance of macrocyclodextrin. Encapsulation refers to a complex of tea tree oil (TTO) with the wall material, protecting the core material or changing its properties from adverse external factors, controlling its release rate against the evaporation and degradation of essential oils. In the present study, LR-CDs complexed with TTO were prepared by co-precipitation methods. RESULTS: The mass ratio of LR-CDs-TTO was six and the maximum complexation efficiency was 86.23%. Fourier-transform infrared spectroscopy analysis presented the loss of characteristic peaks related to TTO in the complex and no other additional peaks were observed. X-ray diffraction examination demonstrated several sharp peaks and intensity peaks at the diffraction angle of the TTO-LR-CDs complex. 1 H-NMR indicated a chemical shift as a result of the interaction between the molecules in the inclusion complex. Moreover, the thermal stability and aqueous solubility of TTO were enhanced after synergy with LR-CDs; particularly, the solubility of the complex was increased by 329-fold. The volatile characteristics of the encapsulated and original TTO were identical. CONCLUSION: The results of the present study show that TTO was efficaciously complexed with LR-CDs and exhibited enhanced solubility and thermal stability. © 2020 Society of Chemical Industry.
Assuntos
Ciclodextrinas/química , Composição de Medicamentos/métodos , Óleos Voláteis/química , Óleo de Melaleuca/química , Composição de Medicamentos/instrumentação , Estabilidade de Medicamentos , Temperatura Alta , Solubilidade , Espectroscopia de Infravermelho com Transformada de Fourier , Volatilização , Difração de Raios XRESUMO
BACKGROUND: Hydroxyl-sanshools are mainly responsible for the numb taste and biological activities of Zanthoxylum bungeanum, but they show low water solubility, high volatility and easy degradation, which limit their application in the catering and food industries. Thus microcapsules of Z. bungeanum essential oil (ZBEO) were prepared to prevent numb-taste substance attenuation. RESULTS: The complex effects of hydroxypropyl-ß-cyclodextrin (HPCD) with other materials, such as konjac glucomannan octenyl succinate (KGOS), octenyl succinic anhydride-modified starch (OSAS), soy protein isolate (SPI) and gum arabic (GA), on the protection of the main numb-taste substance of ZBEO were investigated. Scanning electron microscopy and Fourier transform infrared spectroscopy analysis indicated that ZBEO was successfully encapsulated in the complex wall materials. X-ray diffraction indicated that the loaded essential oil did not affect the crystalline form of the wall material. The stability of the numb-taste substance α-sanshool in the microcapsules prepared with the complex microcapsule wall materials was higher than that in single-wall microcapsules. Storage stability evaluation indicated that microcapsules prepared with a combination of HPCD and SPI showed the greatest effect in maintaining the stability of the main numb-taste substance α-sanshool in ZBEO at room temperature, low pH and in high-salt conditions. CONCLUSION: Complex wall materials of polysaccharide and protein could effectively protect the numb-taste substance degradation of Z. bungeanum during processing and storage. © 2021 Society of Chemical Industry.
Assuntos
Composição de Medicamentos/métodos , Aromatizantes/química , Mananas/química , Óleos Voláteis/química , Extratos Vegetais/química , Proteínas de Soja/química , Zanthoxylum/química , Amorphophallus/química , Composição de Medicamentos/instrumentação , Cinética , Espectroscopia de Infravermelho com Transformada de Fourier , VolatilizaçãoRESUMO
BACKGROUND: Rapid dissolution in digestive tract and moisture sorption during ambient storage are the two challenges of dry probiotic preparations. To solve these problems, microcapsules with shellac (LAC) addition containing Limosilactobacillus reuteri TMW 1.656 were designed in this work to provide a good moisture barrier and to provide controlled release in digestive tract, based on the hydrophobicity and acid-resistance of LAC. Four microcapsules were prepared using the method of emulsification/external gelation based on the crosslinking reaction between alginate or LAC with calcium ion, including alginate/sucrose (ALG), alginate/shellac/sucrose (ALG/LAC), alginate/whey protein isolate/sucrose (ALG/WPI) and alginate/whey protein isolate/shellac/sucrose (ALG/WPI/LAC). RESULTS: Measurements of physical properties showed that microcapsules with LAC addition (ALG/WPI/LAC and ALG/LAC) had larger particle size, much denser structure, lower hygroscopicity and slower solubilization in water, which agreed with the primary microcapsule design. Probiotic survivals in digestive juices followed the order of ALG/WPI/LAC ≥ ALG/WPI ≥ ALG/LAC > ALG. Probiotic stability after heating and ambient storage both exhibited the order of ALG/WPI/LAC > ALG/LAC ≈ ALG/WPI > ALG, which can be explained by the decreased hygroscopicity with adding LAC. CONCLUSION: LAC addition contributed to better probiotic survivals after freeze drying, simulated digestion, heating and ambient storage, and whey protein isolate (WPI) addition had a synergistic effect. Microcapsule hygroscopicity was closely related with probiotic survivals after heating and ambient storage, while microcapsule solubilization was closely related with probiotic survivals in simulated juices. Within our knowledge, this is the first report to improve probiotic stability during ambient storage based on LAC hydrophobicity. © 2020 Society of Chemical Industry.
Assuntos
Preparações de Ação Retardada/química , Composição de Medicamentos/métodos , Lactobacillaceae/química , Probióticos/química , Alginatos/química , Cápsulas/química , Composição de Medicamentos/instrumentação , Armazenamento de Medicamentos , Trato Gastrointestinal/microbiologia , Humanos , Concentração de Íons de Hidrogênio , Lactobacillaceae/crescimento & desenvolvimento , Viabilidade Microbiana , Tamanho da Partícula , Resinas Vegetais/químicaRESUMO
BACKGROUND: The supplementation of folic acid in food is essential in the human diet. The present study aimed to encapsulate folic acid at different concentrations (5, 10 and 15% (w/w) on a dry basis) in potato starch nanofibers produced through electrospinning. The starch/folic acid nanofibers were evaluated through morphology, Fourier transform infrared (FTIR) spectra, thermal properties, encapsulation efficiency (EE) and in vitro simulation of the human digestion. The nanofibers were also evaluated based on the folic acid content after thermal treatment (100 and 180 °C) and UVA irradiation (1 and 24 h). RESULTS: Folic acid incorporation influenced the morphology of the nanofibers to display a homogeneous and beadless morphology for nanofibers containing 15% folic acid compared with the other nanofibers (0, 5 and 10% folic acid). The mean diameter varied from 75 to 81 nm. Folic acid characteristic bands and peaks were not found in the nanofiber FTIR spectra and thermograms, respectively. The EE was 73, 87 and 95% for nanofibers with 5, 10 and 15% folic acid, respectively. CONCLUSIONS: The starch nanofibers protected folic acid from high temperature and UVA irradiation and during in vitro digestion, showing a release of the vitamin at the end of the simulation (intestinal conditions). The supplementation of folic acid in foods can be effectively achieved by its encapsulation into starch nanofibers, to ensure its protection and controlled release. © 2020 Society of Chemical Industry.
Assuntos
Composição de Medicamentos/métodos , Excipientes/química , Ácido Fólico/química , Nanofibras/química , Extratos Vegetais/química , Solanum tuberosum/química , Amido/química , Suplementos Nutricionais/análise , Digestão , Composição de Medicamentos/instrumentação , Estabilidade de Medicamentos , Ácido Fólico/metabolismo , Temperatura Alta , Humanos , Raios UltravioletaRESUMO
Loss-in-Weights (LiW) feeders are commonly oriented in a horizontal way. In this work, an experimental proof of concept, including mechanical and electrical design, construction, and operation, of a vertical LiW feeder prototype is performed. In a systematic design process, based on functional design specifications, the semi-automated vertical LiW feeder for dosing a wide range of powders, especially cohesive ones, is developed. The new dosing machine is assessed with regard to a number of key features such as high dosing accuracy, first-in-first-out powder discharge, easily interchange of the powder container, and flexibility in controlling the speed of the auger and stirrer motors independently. An experimental sensitivity analysis to study the functionality of the dosing machine and to investigate the weight variability of the weighing platform, i.e. mass flow rate, and quantity of dosed mass, is carried out. The results of the sensitivity analysis and the powder dosing tests of five diverse powders using different auger and stirrer geometries verified the proof of concept prototype.HighlightsA systematic design approach for validating a proof of concept of a vertical loss in weight feeder is appliedA full mechanical CAD design and implementation along with electric installation and software programming are executedSensitivity analysis approach is performed to validate the functionality of the semi-automated machine and successfully dispense dissimilar powders tested with different process parametersThe machine is characterized with a number of key features: first-in-first-out powder discharge, high dosing accuracy, flexible and modular concept design, flexibility in controlling the speed of the auger and the stirrer independently, lightweight and user-friendly design.
Assuntos
Composição de Medicamentos/métodos , Excipientes/química , Tecnologia Farmacêutica/métodos , Composição de Medicamentos/instrumentação , Desenho de Equipamento , Pós , Estudo de Prova de Conceito , Tecnologia Farmacêutica/instrumentaçãoRESUMO
Granule size distribution (GSD) is one of the critical quality attributes in the roller compaction (RC) process. Determination of GSD for newly developed pharmaceutical compounds with unknown ribbon breakage behaviors at the RC milling step requires a quantitative insight into process parameters and ribbon attributes. Despite its pivotal role in mapping the process operating conditions to achieve desired granule size, limited work has been presented in literature with a focus on RC-milling modeling. In this study, a multi-variate mathematical model is presented to simulate the full size-distribution of granulated ribbons as a function of ribbon mechanical properties. Experimental data with a lab-scale oscillating milling apparatus were generated using ribbons made of various powder compositions. Model parameters were determined by fitting it to experimental data sets. Parameters obtained from the first step were correlated to ribbon Young's modulus. The model was validated by predicting GSD of data that were excluded in model development step. Predictive capabilities of the developed model were further explored by simulating GSD profiles of a granulated pharmaceutical excipient obtained at three different conditions of a real-scale Gerteis RC system. While maintaining the milling operating conditions similar to the lab-scale apparatus (i.e., screen size and spacing, and low rotor speed), the proposed modeling approach successfully predicted the GSD of roller compacted MCC powder as the model compound. This model can be alternatively utilized in conjunction with an RC model in order to facilitate the process understanding to obtain granule attributes as part of Quality-by-Design paradigm.
Assuntos
Módulo de Elasticidade , Excipientes/síntese química , Modelos Teóricos , Tamanho da Partícula , Tecnologia Farmacêutica/métodos , Composição de Medicamentos/instrumentação , Excipientes/farmacocinética , Análise Multivariada , Pós , Comprimidos , Resistência à TraçãoRESUMO
The control of root-feeding wireworms has become more challenging as synthetic soil insecticides have been progressively phased out due to environmental risk concerns. Innovative microbial control alternatives such as the so-called attract-and-kill strategy depend on the rapid and successful development of dried encapsulated microorganisms, which is initiated by rehydration. Casein is a functional additive that is already used in food or pharmaceutical industry due to its water binding capacity. Cross-linked forms such as formalin-casein (FC), exhibit altered network structures. To determine whether FC influences the rehydration of alginate beads in order to increase the efficacy of an attract-and-kill formulation for wireworm pest control, we incorporated either casein or FC in different alginate/starch formulations. We investigated the porous properties of alginate/starch beads and subsequently evaluated the activities of the encapsulated entomopathogenic fungus Metarhizium brunneum and the CO2 producing yeast Saccharomyces cerevisiae. Adding caseins altered the porous structure of beads. FC decreased the bead density from (1.0197 ± 0.0008) g/mL to (1.0144 ± 0.0008) g/mL and the pore diameter by 31%. In contrast to casein, FC enhanced the water absorbency of alginate/starch beads by 40%. Furthermore, incorporating FC quadrupled the spore density on beads containing M. brunneum and S. cerevisiae, and simultaneous venting increased the spore density even by a factor of 18. Moreover, FC increased the total CO2 produced by M. brunneum and S. cerevisiae by 29%. Thus, our findings suggest that rehydration is enhanced by larger capillaries, resulting in an increased water absorption capacity. Our data further suggest that gas exchange is improved by FC. Therefore, our results indicate that FC enhances the fungal activity of both fungi M. brunneum and S. cerevisiae, presumably leading to an enhanced attract-and-kill efficacy for pest control.
Assuntos
Caseínas/química , Composição de Medicamentos/métodos , Formaldeído/química , Metarhizium/química , Saccharomyces cerevisiae/química , Água/química , Adsorção , Alginatos/química , Animais , Besouros/crescimento & desenvolvimento , Besouros/microbiologia , Composição de Medicamentos/instrumentação , Larva/crescimento & desenvolvimento , Larva/microbiologia , Metarhizium/fisiologia , Controle Biológico de Vetores , Porosidade , Saccharomyces cerevisiae/fisiologiaRESUMO
Drug delivery systems (DDSs) have great potential for improving the treatment of several diseases, especially microbial infections and cancers. However, the formulation procedures of DDSs remain challenging, especially at the nanoscale. Reducing batch-to-batch variation and enhancing production rate are some of the essential requirements for accelerating the translation of DDSs from a small scale to an industrial level. Microfluidic technologies have emerged as an alternative to the conventional bench methods to address these issues. By providing precise control over the fluid flows and rapid mixing, microfluidic systems can be used to fabricate and engineer different types of DDSs with specific properties for efficient delivery of a wide range of drugs and genetic materials. This review discusses the principles of controlled rapid mixing that have been employed in different microfluidic strategies for producing DDSs. Moreover, the impact of the microfluidic device design and parameters on the type and properties of DDS formulations was assessed, and recent applications in drug and gene delivery were also considered.
Assuntos
Composição de Medicamentos/métodos , Sistemas de Liberação de Medicamentos/métodos , Técnicas de Transferência de Genes/instrumentação , Microfluídica/métodos , Nanomedicina/métodos , Composição de Medicamentos/instrumentação , Dispositivos Lab-On-A-Chip , Microfluídica/instrumentação , Nanomedicina/instrumentação , NanopartículasRESUMO
Controlling the surface area, pore size and pore volume of microcapsules is crucial for modulating their activity in applications including catalytic reactions, delivery strategies or even cell culture assays, yet remains challenging to achieve using conventional bulk techniques. Here we describe a microfluidics-based approach for the formation of monodisperse silica-coated micron-scale porous capsules of controllable sizes. Our method involves the generation of gas-in water-in oil emulsions, and the subsequent rapid precipitation of silica which forms around the encapsulated gas bubbles resulting in hollow silica capsules with tunable pore sizes. We demonstrate that by varying the gas phase pressure, we can control both the diameter of the bubbles formed and the number of internal bubbles enclosed within the silica microcapsule. Moreover, we further demonstrate, using optical and electron microscopy, that these silica capsules remain stable under particle drying. Such a systematic manner of producing silica-coated microbubbles and porous microparticles thus represents an attractive class of biocompatible material for biomedical and pharmaceutical related applications.