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The functional food sector has shown tremendous growth in recent years with the application of probiotic bacteria as "food additives". The utilization of probiotic bacteria in food presents many challenges related to their growth, survival, viability, stability and functionality in food processing, storage and consumption as well as changes of sensory characteristics of probiotic foods. Although dairy foods are currently the most common food carrier to deliver probiotics, an increasing number of non-dairy food matrices exhibit potential for delivery of probiotics. This review provides more recent insight into the emergence of non-dairy probiotics products, the interactions between probiotics and different food matrices and the challenges in developing such products. Some of the technical issues are also reviewed and discussed. These issues include the efficacy of probiotic bacteria in non-chilled, low pH or high water activity foods; the potential loss of bacterial viability, additionally unwanted fermentation and changes of the sensory characteristics of food products which may result in poor microbiological quality and low acceptability to consumers.
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Microbiología de Alimentos , Alimentos Funcionales , Probióticos , Manipulación de Alimentos , Humanos , Lactobacillus/fisiologíaRESUMEN
This study investigated a chemically crosslinked poly(vinyl alcohol) (PVA) hydrogel controlled drug delivery system to deliver the anti-inflammatory drug dexamethasone (DEX). The PVA hydrogels, with different crosslinking densities, were characterized by swelling studies, electron scanning microscopy, viscosity, Fourier transform infrared spectroscopy (FTIR) and in vitro release assessment. Increasing crosslinking density slowed and decreased swelling and water absorption. FTIR analysis suggested DEX has possible interactions with the crosslinker and the PVA polymer. In vitro release of DEX from PVA hydrogels was sustained for 33 days and appeared to fit the Higuchi and Korsmeyer-Peppas models. This work indicates the likelihood of PVA hydrogel as a controlled drug release system for DEX for anti-inflammatory uses.
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Antiinflamatorios/administración & dosificación , Preparaciones de Acción Retardada/química , Dexametasona/administración & dosificación , Hidrogeles/química , Alcohol Polivinílico/química , Antiinflamatorios/química , Reactivos de Enlaces Cruzados/química , Dexametasona/química , Liberación de Fármacos , Espectroscopía Infrarroja por Transformada de Fourier , ViscosidadRESUMEN
Beta-carotene is a potent antioxidant for maintaining human health. However, its oral absorption is low due to poor aqueous solubility of less than 1 µg/ml. A microemulsion delivery system was designed to solubilize beta-carotene toward enhancing its oral bioavailability. From seven pseudoternary diagrams constructed, three systems were selected with large microemulsion areas suitable for oral administration and dilution in the predominately aqueous gastrointestinal fluids. Conductivity and rheology characterization were conducted along four dilution lines within the selected systems. Three pseudoternary-phase diagrams were selected with large microemulsion regions, >60% of the total phase diagram area, which provide microemulsions with higher drug-loading capacity. A phenomenon was observed by which both propylene glycol and Capmul MCM EP stabilize the microstructure of the microemulsions has been proposed based on the characterization studies. An optimal bicontinuous microemulsion formulation was selected comprising 12% orange oil, 24% Capmul MCM, 18% Tween 20, 6% Labrasol, 20% propylene glycol and 20% water, with a high beta-carotene loading capacity of 140.8 µg/ml and droplet size of 117.4 nm. In conclusion, the developed novel microemulsion formulation allows solubilizing beta-carotene and is a promising basis for further development as a functional beverage.
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Antioxidantes/administración & dosificación , Emulsiones/química , Vehículos Farmacéuticos/química , beta Caroteno/administración & dosificación , Administración Oral , Antioxidantes/química , Humanos , Tamaño de la Partícula , Transición de Fase , Propilenglicol/química , Solubilidad , Viscosidad , beta Caroteno/químicaRESUMEN
The selection criteria of ideal probiotic bacteria are complex and involve many factors. One key criterion is based on the ability of the probiotic bacteria to adhere to the epithelial lining of the gastrointestinal tract. The objective of this study was to evaluate and compare the adherence and influence on membrane integrity of 2 selected lactobacilli isolates-Lactobacillus rhamnosus MI13 (dairy food origin) and L. plantarum RC2 (bovine rumen origin)-to Caco-2 cells in the presence and absence of Escherichia coli. The adhesion and influence on membrane integrity properties of the 2 Lactobacillus isolates were compared with Escherichia coli, a human commensal bacterium. From the adhesion studies, we concluded that the bovine rumen isolate exhibited better adherence to Caco-2 cells than the dairy food isolate. In contrast, the dairy food isolate better protected the Caco-2 monolayer from damage induced by ethanol.
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Adhesión Bacteriana/fisiología , Membrana Celular/microbiología , Lacticaseibacillus rhamnosus/fisiología , Lactobacillus plantarum/fisiología , Probióticos/aislamiento & purificación , Animales , Células CACO-2 , Bovinos , Estructuras de la Membrana Celular , Escherichia coli/fisiología , Humanos , Rumen/microbiologíaRESUMEN
BACKGROUND: (+)-catechin, as the most common catechin isomer, is recognized to be an antioxidant which benefits the skin in many ways. The purpose of the present study was to prepare and evaluate a suitable liposomal delivery systems for (+)-catechin topical application. METHODS: In this study, catechin-loaded conventional liposomal delivery system, deformable conventional liposomal delivery system and deformable liposomes prepared by reverse-phase evaporation (REV) method were compared. The three systems were characterized for liposome particle size, zeta-potential, entrapment efficiency, drug release, permeability across porcine skin and catechin deposition in the skin. RESULTS: It was revealed that the size of deformable conventional liposomes before freeze-drying and deformable REV liposomes after freeze-drying range from 335.6 ± 71.7 nm to 551.1 ± 53.4 nm, respectively, which were considered to be suitable for skin delivery. The deformable REV liposomes had a higher aqueous volume and thus were able to entrap greater amounts of hydrophilic (+)-catechin (50.0 ± 5.9%) compared to conventional (30.0 ± 3.8%) and deformable conventional liposomes (36.1 ± 4.6%). All liposomal formulations exhibited a prolonged catechin release. Compared to deformable liposomes, the REV deformable liposomes showed a significantly better deposition of (+)-catechin while catechin solution did not permeate into the porcine ear skin. CONCLUSION: Among all formulations studied, deformable REV liposomes were considered to be favorable for catechin topical delivery.
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Catequina/administración & dosificación , Catequina/química , Sistemas de Liberación de Medicamentos/métodos , Absorción Cutánea/efectos de los fármacos , Animales , Catequina/análisis , Cromatografía de Fase Inversa/métodos , Liposomas , Técnicas de Cultivo de Órganos , Absorción Cutánea/fisiología , PorcinosRESUMEN
The objective of this study was to qualitatively and quantitatively evaluate bovine lactoferrin (bLf) and its stability using a rapid RP-HPLC method. bLf could be rapidly detected within 20 min and quantitated at levels down to 5 µg/mL, and the equation of linearity was y = 86.10x + 178.31 with the correlation coefficient (r(2)) 0.9997. Quantitative data obtained in the present study proved the improved RP-HPLC method to be a sensitive and accurate analytical tool for bLf determination. The proteolytic cleavage of bLf in simulated human gastrointestinal fluids was further analyzed by RP-HPLC, and found to follow pseudo-first-order kinetics. The typical equation obtained by pepsin was log(10) [A(t)]/[A(0)] = -0.03x (r(2) = 0.85), and log(10) [A(t)]/[A(0)] = -0.01x (r(2) = 0.81) for trypsin and chymotrypsin combination. Pepsinolysis of bLf in simulated gastric fluid was relatively fast with the half-life t(1/2) 23.1 min. The digestion of bLf in simulated intestinal fluid was slower with about a 3-fold increase in half-life (69.3 min). After the complete proteolysis of bLf, small cleaved peptide fragments were fully separated and identified by RP-HPLC. The proteolytic study indicated that this validated RP-HPLC was able to evaluate bLf stability though monitoring the derivatization products.
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Cromatografía Líquida de Alta Presión/métodos , Lactoferrina/análisis , Lactoferrina/metabolismo , Modelos Biológicos , Animales , Bovinos , Cromatografía de Fase Inversa/métodos , Jugo Gástrico/química , Jugo Gástrico/metabolismo , Humanos , Cinética , Lactoferrina/química , Límite de Detección , Modelos Lineales , Pepsina A/metabolismo , Reproducibilidad de los ResultadosRESUMEN
AIM: The aim of this project is to use pectin- and chitosan-modified solid lipid nanoparticles for bovine lactoferrin to enhance its cellular uptake and transport. METHODS: Solid lipid particles containing bovine lactoferrin (bLf) were formulated through the solvent evaporation technique, incorporating stearic acid along with either chitosan or pectin modification. bLf cellular uptake and transport were evaluated in vitro using the human adenocarcinoma cell line Caco-2 cell model. RESULTS AND DISCUSSION: The bLf-loaded SLPs showed no significant effect on cytotoxicity and did not induce apoptosis within the eight-hour investigation. The use of confocal laser scanning microscopy confirmed that bLf follows the receptor-mediated endocytosis, whereas the primary mechanism for the cellular uptake of SLPs was endocytosis. The bLf-loaded SLPs had significantly more cellular uptake compared to bLf alone, and it was observed that this impact varied based on the time, temperature, and concentration. Verapamil and EDTA were determined to raise the apparent permeability coefficients (App) of bLf and bLf-loaded SLPs. CONCLUSION: This occurred because they hindered efflux by interacting with P-glycoproteins and had a penetration-enhancing influence. These findings propose the possibility of an additional absorption mechanism for SLPs, potentially involving active transportation facilitated by the P-glycoprotein transporter in Caco-2 cells. These results suggest that SLPs have the potential to be applied as effective carriers to improve the oral bioavailability of proteins and peptides.
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CONTEXT: Injectable implants are biodegradable, syringeable formulations that are injected as liquids, but form a gel inside the body due to a change in pH, ions or temperature. OBJECTIVE: To investigate the effect of polymer concentration, pH, ions and temperature on the gel formation of ß-glucan, a natural cell-wall polysaccharide derived from barley, with particular emphasis on two-phase system formation after addition of dextran or PEG. MATERIALS AND METHODS: Oscillation viscometry was used to evaluate the gel character by measuring flow index (N), storage (G') and loss (G") moduli. Two-phase systems were further characterized for hardness and syringeability using a texture analyzer. Finally, in vitro release characteristics were determined using Franz diffusion cells. RESULTS: Oscillation viscometry revealed that only addition of dextran or PEG resulted in distinct gel formation. This was seen by a decrease in N after polymer addition. Moreover, hardness (in g) of the gels increased significantly (p < 0.001) from 3.65 ± 0.43 to 34.30 ± 8.90 (dextran) and 805.80 ± 5.30 (PEG) 24 h after polymer addition. In vitro release profiles showed significantly (p < 0.05) reduced AUC(0-8 h), k and percentage of drug released from two-phase systems compared to ß-glucan dispersions, with the PEG system resulting in the lowest amount released over 8 h (15.1 ± 1.6%). DISCUSSION: The unfavorable mixing enthalpy and higher water affinity of PEG resulted in the formation of a dense ß-glucan gel. CONCLUSION: 1.5% (w/w) ß-glucan combined with PEG at a ratio of 1:3 seemed to be the most promising injectable formulation with respect to fastest gel formation, increased hardness and sustained release.
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Materiales Biocompatibles/química , Portadores de Fármacos/química , Péptidos/administración & dosificación , Proteínas/administración & dosificación , beta-Glucanos/química , Dextranos/química , Implantes de Medicamentos , Excipientes/química , Fluoresceína/análisis , Geles , Dureza , Concentración de Iones de Hidrógeno , Modelos Químicos , Transición de Fase , Polietilenglicoles/química , Reología , Solubilidad , Espectrometría de Fluorescencia , ViscosidadRESUMEN
Fertiliser has been a vital part of agriculture due to it boosting crop productivity and preventing starvation throughout the world. Despite this huge contribution, the application of nitrogen (N) fertilisers results in N leaching and the formation of greenhouse gases, which threaten the environment and human health. To minimise the impacts, slow/controlled release fertilisers (S/CRFs) have been being developed since the beginning of the 20th century. Despite the efforts made over a century, the basic terminological and classification information of these fertilisers remains vague. The scientific knowledge published in S/CRF patents has also been overlooked since the beginning. This review focused on the information gaps, clarified the definitions, differentiation and classification methods that have been randomly used in previous literature. The objectives, formulations and technologies of 109 controlled release urea patents involving sulphur coated urea, polymer coated urea and urea matrix fertilisers published in the years since these products emerged were also reviewed to 1) highlight the overlooked scientific knowledge in the patents; 2) understand the evolutionary processes and current research states of the products; 3) clarify research preferences and challenges to date; 4) identify remaining gaps for the future direction. It is expected that the organised basic information and the patent knowledge highlighted in this paper can be new resources and foster the development of S/CRFs in the future.
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Fertilizantes , Urea , Agricultura/métodos , Preparaciones de Acción Retardada , Humanos , Nitrógeno , TecnologíaRESUMEN
Liquid polymeric systems that can undergo phase change (sol to gel) upon administration into the teat canal of cow's mammary gland can serve as a physical barrier to invading pathogens and can also serve as a reservoir for controlled release of therapeutic agents. The aim of the study was to investigate the phase behavior, rheological and mechanical properties of selected in situ gelling systems. Six in situ gelling polymer formulations were identified using phase behavior studies. Rheological studies revealed pseudoplastic flow with thixotropy. All six formulations showed significantly different viscosity, pseudoplasticity and thixotropy values except for CMC1 and HPMC2 which where statistically similar. The gel strength was dependent on the solvent system used and amount of water in the system. These in situ gelling systems have the potential to serve as a platform for development of intramammary formulations intended for administration into the teat canal of the cow's mammary gland. They can serve as a physical barrier or a matrix for controlled drug release.
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Geles/química , Polímeros/química , Reología , Solventes/química , Agua/química , Alginatos/química , Animales , Carboximetilcelulosa de Sodio/química , Bovinos , Fenómenos Químicos , Química Farmacéutica , Sistemas de Liberación de Medicamentos , Ácido Glucurónico/química , Ácidos Hexurónicos/química , Interacciones Hidrofóbicas e Hidrofílicas , Derivados de la Hipromelosa , Metilcelulosa/análogos & derivados , Metilcelulosa/química , Polisacáridos Bacterianos/química , ViscosidadRESUMEN
Electrospun nanofibers have been extensively studied for encapsulated drugs releasing from the inside of the fiber matrix, but have been barely looked at for their potential to control release as a semi-permeable membrane. This study investigated molecular transport behaviors across nanofiber membranes with different micro-structure sizes and compositions. Four types of membranes were made by 5% and 10% poly (ε-caprolactone) (PCL) solutions electro-spun with or without 50 nm calcium carbonate (CaCO3) nanoparticles. The membranes were tested for thickness, fiber diameter, pore size, porosity, tensile strength and elongation, contact angle of water and their impacts on molecular transport behaviors. The presence of the CaCO3 nanoparticles made the 5% membranes stronger and stiffer but the 10% membranes weaker and less stiff due to the different (covering or embedded) locations of the nanoparticles with the corresponding fibers. Solute transport studies using caffeine as the model drug found the 5% membranes further retarded release from the 10% membranes, regardless of only half the amount of material being used for synthesis. The addition of CaCO3 nanoparticles aided the water permeation process and accelerated initial transports. The difference in release profiles between 5% and 10% membranes suggests different release mechanisms, with membrane-permeability dominated release for 5% PCL membranes and solute-concentration-gradient dominated release for 10% PCL membranes.
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Treatment and prevention of cattle mastitis remains a formidable challenge due to the anatomical and physiological constraints of the cow udder. In this study, we investigated polymeric excipients and solvents that can form, (when combined) novel, non-toxic and biocompatible in situ gelling formulations in the mammary gland of bovine cattle. We also report on a new approach to screen intramammary formulations using fresh excised cow teats. Fourteen hydrophilic polymers and six solvents were evaluated for in vitro cytotoxicity and biocompatibility towards cultured bovine mammary epithelial cells (MAC-T), microscopic and macroscopic examination upon contact with excised cow teats. No significant cytotoxicity (p > 0.05) was observed with polyethylene oxides, hydroxypropyl methylcellulose, carboxymethyl cellulose, sodium alginate and xanthan gum. Polycarbophil and carbopol polymers showed significantly higher cytotoxicity (p < 0.05). Concentration-dependent cytotoxicity was observed for glycerin, propylene glycol, polyethylene glycol 400, ethanol, N-methyl-2-pyrrolidone and 2-pyrrolidone, with the 2-pyrrolidone solvents showing higher cytotoxic effects (p < 0.05). In situ gelling formulations comprising hydroxypropyl methylcellulose or carboxymethyl cellulose and solvents in specific ratios were biocompatible at higher concentrations with MAC-T cells compared to alginates. All investigated formulations could undergo in situ sol-to-gel phase transformation, forming non-toxic gels with good biocompatibility in excised cow teats hence, showing potential for use as intramammary carriers for sustained drug delivery.
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Novel superhydrophobic sodium carboxymethyl cellulose (CMC) modified polyurethane (MPU) was developed as the membrane material for controlled-release fertilizer (CRF) by cross-linking polymerization of 4,4'-diphenylmethane diisocyanate (MDI) and CMC-based modified polyol (CMP) which was made by grafting CMC onto polyether polyol (TMN-450). The modified polyurethane coated fertilizer (MPUCF) was prepared by using MPU as the membrane material through a fluidized bed device. Analysis results of 13C NMR showed that the coatings of PUCF and MPUCF were prepared by connecting hydroxyl to isocyanate groups to form a carbamate. MPU had lower water absorption rates than PU, and MPUCF coating showed excellent hydrophobicity. Scanning electron microscope (SEM) revealed that MPUCF coating surface was much more smooth and flat than that of PUCF. Furthermore, the nitrogen (N) release longevity of MPUCF can increased to 140 days when the coating rate was 5%. It is concluded that MPU was an excellent superhydrophobic coating material for CRF.
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Fertilizantes , Polímeros , Carboximetilcelulosa de Sodio , Interacciones Hidrofóbicas e Hidrofílicas , Isocianatos , Poliuretanos , Agua/químicaRESUMEN
Energy supplementation may reduce oxidative stress by correcting a negative energy balance, but in some contexts, it has been shown to increase oxidative stress, especially at peak lactation. The current experiment examined if a pelleted energy supplement with or without the addition of Lactobacillus-fermented seaweed or seaweed plus terrestrial plants extracts affected oxidative stress of ewes from late gestation through to weaning and ewe and lamb production from lambing to weaning. Treatments were either no supplement (CON-), a pelleted supplement only (CON+, 100 g/ewe per d), CON+ with seaweed extract only (SWO, 10 mL/ewe per day), or CON+ with seaweed plus an arrangement of terrestrial plant extract (SWP, 10 mL/ewe per d). Ewes (n = 160; mean initial BW = 72.3 ± 9.5 kg [mean ± SD]) were randomized to pastures (n = 4 pastures per treatment with 10 ewes each). After lambing, ewes with twins were reallocated to pastures (n = 3 pastures per treatment with 10 ewes each) according to lambing date. At 4 wk in milk, supplementation tended to reduce total antioxidant status (TAS; P = 0.10) and increased glutathione peroxidase (GPx) activity compared with nonsupplemented ewes (P = 0.04). The addition of seaweed and terrestrial plants extracts to the concentrate, that is, SWO and SWP, increased TAS and reduced GPx activity compared with CON+ (P < 0.01). Supplementation increased milk yield at weeks 4, 6, and 8 of lactation, and protein, lactose, and total milk solids yield at peak lactation (week 4; P < 0.05). The CON- ewes had greater somatic cell count than the supplemented ewes at weeks 4, 8, and 10 of lactation (P = 0.03). Our results suggest that energy supplementation, alone, increases oxidative stress of lactating ewes, which may relate to increased oxidative phosphorylation. Most importantly, these results indicate that in situations where energy supplementation is needed to increase animal performance, negative effects of energy supplementation around peak lactation can be offset by the addition of Lactobacillus-fermented plant extracts (SWO and SWP) to improve antioxidant status.
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Alimentación Animal , Lactancia , Alimentación Animal/análisis , Animales , Dieta/veterinaria , Suplementos Dietéticos , Femenino , Lactobacillus , Leche , Extractos Vegetales/farmacología , Embarazo , OvinosRESUMEN
This study demonstrates an effective technique for separating and purifying viable bacteria from samples that interfere with viability staining. The viability of Bifidobacterium longum ATCC 15707 was assessed using Percoll Buoyant Density Gradient Centrifugation (PBDC) to separate bacteria from complex non-dairy food matrices and Quantitative Fluorescence Microscopy (QFM) to determine individual cells using LIVE/DEAD BacLight bacterial viability staining. Water agar (3%) was used to retain cells of B. longum and offered a lower fluorescence background with BacLight viability staining, compared with fixation on polycarbonate (PC) black membrane. The effect of drying temperatures and non-dairy foods on viability of B. longum was assessed. B. longum coated on oat, peanut or raisin was separated by filtration, low- and high-speed centrifugation, flotation and sedimentation buoyant density centrifugation. Purified cells were subsequently deposited on water agar for rehydration followed by LIVE/DEAD BacLight viability staining and enumeration. Conventional plate counting was also conducted to compare viability results. Finally, this method was applied to assess cell membrane damages of B. longum incorporated onto non-dairy foods during 24â¯h drying. Furthermore, viability assessment of B. longum coated onto oat, peanut, or raisin was much lower by plate counting compared to viability staining. Drying appeared to have a greater impact when viability was assessed by plate counting compared to viability staining. IMPORTANCE: Enumeration of viable beneficial bacteria from function foods presents a significant bottleneck for product development and quality control. Interference with microscopic and/or fluorescent techniques by ingredients, time required to incubate plated microbes, and the transient nature of the colony forming unit make rapid assessment of viable bacteria difficult. Viability assessment of Bifidobacterium longum ATCC 15707 by Percoll Buoyant Density Gradient Centrifugation with LIVE/DEAD BacLight viability staining on water agar (3%) was in agreement with serial dilution enumeration. Without the need for incubation viability assessment by staining provided a more rapid means to assess the impact of drying on the viability of B. longum coated onto oat, peanut or raisin.
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Bifidobacterium longum/crecimiento & desarrollo , Microbiología de Alimentos/métodos , Viabilidad Microbiana , Microscopía Fluorescente/métodos , Centrifugación por Gradiente de Densidad/métodos , Recuento de Colonia Microbiana/métodos , Povidona , Dióxido de Silicio , Coloración y Etiquetado/métodosRESUMEN
A chitosan-pectin (CS-PEC) biopolymeric hydrogel wound dressing was investigated for lidocaine delivery. Here we demonstrate for the first time the feasibility of three-dimensional (3D) printed CS-PEC hydrogel incorporating the local anaesthetic drug lidocaine hydrochloride (LDC) as a potential wound dressing candidate. The hydrogels were prepared by physical crosslinking of CS and PEC polysaccharides. The scaffolds were printed using an extrusion-based 3D printer using a mechanical positive displacement dispensing system followed by lyophilisation. The 3D printed hydrogels showed good printability, dimensional integrity and self-adhesion to skin. The high swelling ratio and water absorption of 3D printed hydrogels indicated suitability for absorbing exudates and maintaining a moist wound healing environment. Fourier transform infrared (FTIR) spectroscopy results indicated that the CS-PEC hydrogel was formed by hydrogen bonds. Incorporation of LDC in the hydrogel did not interfere with its functional stability. In vitro drug release studies of LDC over 6â¯h fitted the Korsmeyer-Peppas model. This work demonstrates the possibility of a 3D printed hydrogel as a suitable candidate for wound dressings.
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Vendajes , Quitosano/química , Sistemas de Liberación de Medicamentos , Hidrogeles/química , Lidocaína/farmacología , Pectinas/química , Impresión Tridimensional , Adhesividad , Rastreo Diferencial de Calorimetría , Liberación de Fármacos , Estudios de Factibilidad , Cinética , Espectroscopía Infrarroja por Transformada de Fourier , Andamios del Tejido/química , AguaRESUMEN
This study reports on the fabrication of a controlled release system for the delivery of levonorgestrel (LNG) for long-term contraception. LNG was encapsulated in chemically cross-linked chitosan (CS) microspheres, and microspheres presented a spherical geometry with a good particle size distribution (polydispersity index (PDI) < 0.1). The LNG-CS microspheres were classified based on their particle size range, <63, 63-125, and 125-300 µm, where the 125-300 µm particles were selected to be incorporated into a physically cross-linked and annealed PVA hydrogel matrix to prolong the drug release. PVA concentrations and the annealing treatment influenced the swelling behavior of PVA hydrogels. Fourier transform infrared (FTIR) spectroscopy indicated that CS was successfully cross-linked through the formation of a Schiff base; the PVA hydrogel was formed through hydrogen bonding without reacting with LNG, which was only physically entrapped, thus maintaining its stability. Differential scanning calorimetry (DSC) showed that freeze-thaw and annealing processes increased the degree of crystallinity in the PVA hydrogel. In vitro drug release assessments for all formulations showed zero order without any burst release. Over a period of 100 days, 34, 27, and 21% of LNG was released from the CS-LNG microspheres in the size ranges < 63, 63-125, and 125-300 µm, respectively, while only 14, 11, and 9% of LNG was released when the CS-LNG microspheres were incorporated into 10, 15, and 20% PVA hydrogels, respectively. The drug release kinetics exhibited both diffusion- and swelling-controlled mechanisms following the Korsmeyer-Peppas model. This work presents a promising delivery system for long-term contraception with controlled zero-order release behaviors.
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Customisation of sustained and controlled release of contraceptives plays a key role in veterinary applications. A biodegradable projectile containing different doses of contraceptive progesterone was prepared using fused deposition modelling 3D printing. Three concentrations of progesterone (2, 5 and 10% w/w) with polylactic acid was prepared as a 1.75â¯mm filament by hot melt extrusion. Solvent dissolution tests confirmed the successful incorporation of progesterone in the polymer while microscopic (SEM) studies indicated the drug was melted and thoroughly mixed with the polymer matrix and pore-formation after dissolution. A significant suppression of melting temperature of polymer from 166 to 145⯰C was noted by thermal analysis (DSC) studies of the drug loaded systems. Interaction between the contraceptive drug and the polymer via hydrogen bonding was revealed from the spectroscopic (FTIR) studies. In vitro release behaviour was assessed over a five-month period, for 2% and 5% progesterone loaded projectiles release profiles fitted zero order whereas 10% loaded projectiles fitted the Higuchi model. Penetration assessment confirmed the drug loaded PLA projectiles provided sufficient specific kinetic energy required to penetrate thin and medium-thickness skins. This work demonstrates the feasibility of fused deposition modelling 3D printing as suitable process for manufacturing ballistic customised drug delivery devices.
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Anticonceptivos/administración & dosificación , Sistemas de Liberación de Medicamentos , Impresión Tridimensional , Progesterona/administración & dosificación , Administración Cutánea , Animales , Anticonceptivos/química , Preparaciones de Acción Retardada/administración & dosificación , Preparaciones de Acción Retardada/química , Liberación de Fármacos , Caballos , Poliésteres/administración & dosificación , Poliésteres/química , Progesterona/química , OvinosRESUMEN
Cataracts are one of the most prevalent diseases of the lens, affecting its transparency and are the leading cause of reversible blindness in the world. The clarity of the lens is essential for its normal physiological function of refracting light onto the retina. Currently there is no pharmaceutical treatment for prevention or cure of cataracts and surgery to replace the affected lens remains the gold standard in the management of cataracts. Pharmacological treatment for prevention of cataracts is hindered by many physiological barriers that must be overcome by a therapeutic agent to reach the avascular lens. Various therapeutic agents and formulation strategies are currently being investigated to prevent cataract formation as access to surgery is limited. This review provides a summary of recent research in the field of drug delivery to the lens for the management of cataracts including models used to study cataract treatments and discusses the future perspectives in the field.