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OBJECTIVE: In the current research, 6-gingerol (GA)-loaded nanofiber drug delivery system were developed, and their potential usage in wound healing was evaluated. SIGNIFICANCE: This study investigates the effectiveness of nanofibrous membranes composed of sodium alginate (SA), poly(vinyl alcohol) (PVA), and 6-gingerol (GA) as delivery systems for anti-inflammatory agents in the context of wound dressings. METHODS: GA-loaded SA/PVA nanofiber was prepared using electrospinning. In vitro characterization of this nanofiber included the examination of comprehensive in vitro characterization, anti-inflammatory and antioxidant activities, cytotoxicity, a scratch tes and in vivo skin test. RESULTS: GA was extracted from Zingiber officinale, and its successful isolation was confirmed through analyses such as H-NMR, C-NMR. Then GA was electrospuned into the SA/PVA nanofibers, and scanning electron microscopy (SEM) imaging revealed that the fiber diameters of the formulations ranged between 148 nm and 176 nm. Anti-inflammatory and antioxidant studies demonstrated that the effectiveness of GA increased with higher doses; however, this increase was accompanied by decreased cell viability. In vitro release studies revealed that GA exhibited a burst release within the first 8 h, followed by a controlled release, reaching completion within 24 h. Within the scope of in vitro release kinetics, release data are mathematically compatible with the Weibull model with high correlation. The scratch test results indicated that TB2 (%1 GA) promoted epithelialization. Furthermore, it was determined that TB2 (%1 GA) did not cause any irritation. CONCLUSIONS: As a result, TB2 shows promise as a formulation for wound dressings, offering potential benefits in the field of wound care.
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This study aimed to develop new generation cakes that were fortified with calcined ZnO nanoparticles (CZnO), uncalcined ZnO nanoparticles (UCZnO), beads (B(CZnO)) synthesized by encapsulating the CZnO with sodium alginate (SA), and the beads (B(UCZnO)) synthesized by encapsulating the UCZnO with sodium alginate (SA) and investigated the zinc (Zn) release in fortified cakes in simulated body fluids (SBF). The present study represents a novel method for increasing intestinal absorption and bioavailability of dietary zinc with zinc nanoparticles for use in the preparation of Zn fortified cakes as a dietary supplement to compensate for zinc deficiency in humans. The results revealed that a rapid increase in the release time and rate in the SGF solution was noted in the UCZnO added cakes. It was attributed to increased intestinal absorption and bioavailability as a result of the ultra-small size of ZnO. Also, ZnO release kinetics in SBF was also studied and data were adjusted into different kinetic models involving zero-order, first-order, Higuchi, and Korsmeyer-Peppas models. The present investigation recommends adding UCZnO to the cakes to control and increase the release from the cakes. Supplementary Information: The online version contains supplementary material available at 10.1007/s13197-023-05840-x.
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Globally, more than 6 million metric tons of agricultural plastic films are used to increase crop yields and reduce the use of water and herbicides, resulting in the contamination of soil and water by plastic debris and additives. However, knowledge of the occurrence and release of additives from agricultural films is limited. In this study, suspect screening with high-resolution mass spectrometry, one-dimensional Fickian diffusion models, and linear free energy relationships (LFERs) were used to determine the occurrence and mass transfer of various additives from agricultural plastic films. A total of 89 additives were tentatively identified in 40 films, and 62 of them were further validated and quantified. The aqueous concentrations of 26 released additives reached mg L-1 after a 28 day incubation at 25 °C. Diffusion models and LFERs demonstrated that the film-water partition coefficient and the diffusivity in the polymer, the two critical parameters controlling the mass transfer, could be predicted using Abraham descriptors. The findings of this study highlighted the need for future research on the environmental fate and risk assessment of previously neglected additives in agricultural plastic films and other similar products.
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Plásticos , Agua , Plásticos/análisis , Agricultura , Polímeros , SueloRESUMEN
OBJECTIVE: In the current research, lornoxicam-loaded in situ gels were developed, and their potential usage in ocular inflammation was evaluated. SIGNIFICANCE: Lornoxicam cyclodextrin complex prepared with hydroxypropyl methylcellulose and poloxamer P407 because of the low viscosity of in situ gels to provide easy application. However, washing and removing it from the ocular surface becomes difficult due to the gelation formation with heat. METHODS: A three-level factorial experimental design was used to evaluate the effects of poloxamer 407 concentration, polymer type, and polymer concentration on viscosity, pH, gelation capacity, gelation time, and gelation temperature, which were considered the optimal indicators of lornoxicam-containing formulations. RESULTS: As a result of the three-level factorial experimental design, the optimized formulation contained 15 (%w/v) poloxamer 407 and 1 (%w/v) hydroxypropyl methylcellulose. The optimize formulation viscosity 25 °C = 504 ± 49cP, viscosity 35 °C = 11247 ± 214cP, pH = 6.80 ± 0.01, gelation temprature = 35 ± 0.2 °C, and gelation time= 34 ± 0.2 s was obtained. In the in vitro release studies, 68% of lornoxicam was released with a burst effect in the first three hours; then, the release continued for eight hours with controlled release. Release kinetics of the formulations were modeled mathematically, and it was found to be compatible with the Korsemeyer-Peppas and Weibull models. In cell culture studies, cell viability at 100 µg/mL was 83% and 96% for NL6 and NL6-CD, respectively. In Draize's in vivo test, no negative conditions occurred in rats. CONCLUSIONS: Therefore, the NL6-CD formulation has the potential to be a favorable option for treating ocular inflammation.
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Calor , Poloxámero , Ratas , Animales , Derivados de la Hipromelosa , Proyectos de Investigación , Geles , Temperatura , Inflamación , ViscosidadRESUMEN
Vascular graft infections are a severe complication in vascular surgery, with a high morbidity and mortality. Prevention and treatment involve the use of antibiotic- or antiseptic-impregnated artificial vascular grafts, but currently, there are no commercially available infection-proof small-diameter vascular grafts (SDVGs). In this work we investigated the antimicrobic activity of two SDVGs prototypes loaded with tobramycin and produced via the electrospinning of drug-doped PLGA (polylactide-co-glycolide) solutions. Differences in rheological and conductivity properties of the polymer solutions resulted in non-identical fibre morphology that deeply influenced the hydration profile and consequently the in vitro cumulative drug release, which was investigated by using a spectrofluorimetric technique. Using DDSolver Excel add-in, modelling of the drug release kinetic was performed to evaluate the release mechanism involved: Prototype 1 showed a sustained and diffusive driven drug release, which allowed for the complete elution of tobramycin within 2 weeks, whereas Prototype 2 resulted in a more extended drug release controlled by both diffusion and matrix relaxation. Time-kill assays performed on S. aureus and E. coli highlighted the influence of burst drug release on the decay rate of bacterial populations, with Prototype 1 being more efficient on both microorganisms. Nevertheless, both prototypes showed good antimicrobic activity over the 5 days of in vitro testing.
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The target of the current investigation was the delivery of oseltamivir phosphate (OSE) into the lung adenocarcinoma tissues by means of designing nanosized, non-toxic and biocompatible pegylated Eudragit based NPs and investigating their anticancer and antiangiogenic activity. The rationale for this strategy is to provide a novel perspective to cancer treatment with OSE loaded pegylated ERS NPs under favor of smaller particle size, biocompatible feature, cationic characteristic, examining their selective effectiveness on lung cell lines (A549 lung cancer cell line and CCD-19Lu normal cell line) and examining antiangiogenic activity by in vivo CAM analysis. For this purpose, OSE encapsulated pegylated ERS based NPs were developed and investigated for zeta potential, particle size, encapsulation efficiency, morphology, DSC, FT-IR, 1H NMR analyses. In vitro release, cytotoxicity, determination apoptotic pathways and in vivo CAM assay were carried out. Considering characterizations, NPs showed smaller particle size, cationic zeta potential, relatively higher EE%, nearly spherical shape, amorphous matrix formation and prolonged release pattern (Peppas-Sahlin and Weibull model with Fickian and non-Fickian release mechanisms). Flow cytometry was used to assess the apoptotic pathways using the Annexin V-FITC/PI staining assay, FITC Active Caspase-3 staining assay, and mitochondrial membrane potential detection tests. Activations on caspase-3 pathways made us think that OSE loaded pegylated ERS NPs triggered to apoptosis using intrinsic pathway. As regards to the in vivo studies, OSE loaded pegylated ERS based NPs demonstrated strong and moderate antiangiogenic activity for ERS-OSE 2 and ERS-OSE 3, respectively. With its cationic character, smaller particle size, relative superior EE%, homogenous amorphous polymeric matrix constitution indicated using solid state tests, prolonged release manner, highly selective to the human lung adenocarcinoma cell lines, could trigger apoptosis intrinsically and effectively, possess good in vivo antiangiogenic activity, ERS-OSE 2 formulation is chosen as a promising candidate and a potent drug delivery system to treat lung cancer.
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Resinas Acrílicas/química , Inhibidores de la Angiogénesis/farmacología , Apoptosis/efectos de los fármacos , Membrana Corioalantoides/irrigación sanguínea , Portadores de Fármacos , Neoplasias Pulmonares/tratamiento farmacológico , Nanopartículas , Neovascularización Patológica , Neovascularización Fisiológica/efectos de los fármacos , Oseltamivir/farmacología , Polietilenglicoles/química , Células A549 , Animales , Embrión de Pollo , Preparaciones de Acción Retardada , Composición de Medicamentos , Liberación de Fármacos , Humanos , Neoplasias Pulmonares/metabolismo , Neoplasias Pulmonares/patología , Nanotecnología , Oseltamivir/químicaRESUMEN
Controlled release matrices have predictable drug release kinetics, provide drugs for an extended period of time, and reduce dosing frequency with improved patient compliance as compared with conventional tablet dosage forms. In the current research work, losartan potassium controlled release matrix tablets were fabricated and prepared with rate altering agents; that is, Ethocel grade 100 combined with Carbopol 934PNF. Various drug to polymer ratios were used. HPMC, CMC, and starch were incorporated in some of the matrices by replacing some amount of filler (5%). The direct compression method was adopted for the preparation of matrices. In phosphate buffer (pH 6.8), the dissolution study was conducted by adopting the USP method-I as the specified method. Drug release kinetics was determined and dissolution profiles were also compared with the reference standard. Prolonged release was observed for all matrices, but those with Ethocel 100FP Premium showed more extended release. The co-excipient (HPMC, CMC, and starch) exhibited enhancement in the drug release rates, while all controlled release matrices released the drug by anamolous non-Fickian diffusion mechanism. This combination of polymers (Ethocel grade 100 with Carbopol 934PNF) efficiently extended the drug release rates up to 24 h. It is suggested that these matrix tablets can be given in once a day dosage, which might improve patient compliance, and the polymeric blend of Ethocel grade 100 with Carbopol 934PNF might be used in the development of prolonged release matrices of other water-soluble drugs.
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Losartán , Preparaciones de Acción Retardada/química , Preparaciones de Acción Retardada/farmacocinética , Preparaciones de Acción Retardada/farmacología , Losartán/química , Losartán/farmacocinética , Losartán/farmacología , ComprimidosRESUMEN
BACKGROUND: Bioactive compound delivery systems must provide stability against severe food processing and environmental conditions. Cress seed gum (CSG) with high thermal stability can be a promising polysaccharide for preparing physically cross-linked hydrogel as a curcumin delivery system. In the present study, CSG (0.05, 0.10 and 0.15 g kg-1 ) and calcium chloride (CaCl2 ) (0.00, 0.02, 0.04, 0.06 and 0.10 g kg-1 ) solutions were used for hydrogel fabrication. RESULTS: Physicochemical properties of hydrogels were evaluated by entrapment efficiency, loading capacity and swelling degree, differential scanning calorimetry, scanning electron microscopy, in vitro release and free radical scavenging capacity assessments. Accordingly, 0.15 g kg-1 CSG-0.02 g kg-1 CaCl2 hydrogel was revealed to have high entrapment efficiency (93.6 ± 1.59%), loading capacity (0.92 ± 0.00%) and swelling degree (105.96 ± 12.99%), as well as heat stability above 103 °C. CSG hydrogel significantly (P < 0.05) protected the antioxidant activity of curcumin against thermal process. The curcumin release in the acidic stomach medium was negligible, although it increased significantly in the simulated intestinal environment (42.5 ± 0.75%), which followed the Peppas model. CONCLUSION: As a result, CSG hydrogel can protect curcumin during food thermal processing and digestion time. Therefore, CSG hydrogel can play a valued role in modern-day food formulations with an increasing consumer preference for plant-derived materials. © 2021 Society of Chemical Industry.
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Brassicaceae/química , Curcumina/química , Portadores de Fármacos/química , Sistemas de Liberación de Medicamentos/métodos , Hidrogeles/química , Gomas de Plantas/química , Sistemas de Liberación de Medicamentos/instrumentación , Estabilidad de Medicamentos , CalorRESUMEN
House dust mite (HDM) sublingual immunotherapy (SLIT) in the form of SLIT-tablets is now an established treatment option for HDM allergy and HDM-induced allergic asthma. In SLIT-tablet immunotherapy allergen extracts are formulated as dry tablets and administered under the tongue where it must be solubilized in saliva in order to be able to interact with the immune system of the sublingual mucosa. Solubilization of the extract must occur within a short time span of about one minute after administration, determined by the sublingual holding time recommended by the manufacturer. Currently, two types of HDM SLIT-tablets are available. Both tablet types contain natural HDM extracts from two common HDM species as the active ingredient, but differ with regard to formulation as one tablet type is based on a freeze-dried tablet formulation while the other is based on a compressed formulation. HDM extracts contain a number of major and minor allergens, which in combination provide the allergenic activity that drives the immunological response and in turn the clinical efficacy of the tablets. Here, a biologically relevant human immunoglobulin E (IgE)-based assay is used to compare the ability of the two HDM SLIT-tablet types to deliver HDM allergenic reactivity from the dry tablet into soluble form. The experiments demonstrate that the freeze-dried formulation delivers HDM allergenic activity into solution faster and more efficiently than the compressed formulation.
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Alérgenos/inmunología , Antígenos Dermatofagoides/inmunología , Inmunoglobulina E/sangre , Pyroglyphidae/inmunología , Inmunoterapia Sublingual , Comprimidos , Animales , Composición de Medicamentos , HumanosRESUMEN
This article provides an analysis of dissolution kinetics associated with formulations subjected to different dissolution methods with the purpose of revealing credible direction on selection of apparatus type and hydrodynamics on in vitro drug release profiles using three different formulations. The dissolution kinetics of immediate release (IR) and controlled release (CR) ibuprofen tablets under different hydrodynamic conditions were determined, and potential existence of any correlation between USP apparatus I and II were analyzed using adequate kinetic models. Two types of CR tablets based on PEO (polyethylene oxide-N80) and HPMC (hydroxypropyl methylcellulose- K100M) polymers were prepared. Marketed ibuprofen 200-mg IR tablets were also used. Dissolution studies were carried out using USP 34 apparatuses I and II methods at stirring speed of 100 and 50 rpm in 900 mL phosphate buffer, pH 7.2 at 37°C. The drug release profiles for each formulation was determined and statistically analyzed using model-dependent, model-independent (f 2 ), and ANOVA methods. No significant dissolution differences existed between IR tablets, whereas CR tablets were significantly impacted by apparatus types and hydrodynamics. PEO matrices displayed higher sensitivity to hydrodynamics relative to HPMC matrices, and differences in dissolution profiles were confirmed by ANOVA and boxplot analysis. It is concluded that in the case of CR systems, selection of apparatus type and adherence to the monograph specifications and hydrodynamic conditions is critical, while for IR tablets, both apparatus types and agitation rates had no significant impact on drug release rate, suggesting the possibility of apparatus interchangeability if desired.
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Preparaciones de Acción Retardada/química , Comprimidos/química , Química Farmacéutica/métodos , Liberación de Fármacos , Hidrodinámica , Derivados de la Hipromelosa/química , Ibuprofeno/química , Cinética , Metilcelulosa/análogos & derivados , Metilcelulosa/química , Polietilenglicoles/química , Polímeros/química , SolubilidadRESUMEN
Starch polymer matrices were developed with the incorporation of 1% clove essential oil (EO) (Syzygium aromaticum) aiming for use as active packaging for sausages. At the concentration of 1% EO in the polymer matrix, it showed exponential behavior with respect to oil release over 30 days, with faster release in the beginning and a tendency towards a reduction in release velocity over time. The presence of OE in the biofilm led to significant differences versus the control in terms of aroma and flavor parameters. It was found that EO had an antioxidant effect in sausages with a significant difference between treatments with respect to TBA (thiobarbituric acid) values at the end of a 15 day period of refrigerated storage. There were no significant variations in pH and Aw among treatments during the evaluated period. A significant negative correlation (-0.78) between brightness (L*) and the lipid oxidation of the products was observed.
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The present study was performed to optimise the formulation of a muco-adhesive buccal patch for insulin nanoparticles (NPs) delivery. Insulin NPs were synthesised by an ionic gelation technique using N-di methyl ethyl chitosan cysteine (DMEC-Cys) as permeation enhancer biopolymer, tripolyphosphate (TPP) and insulin. Buccal patches were developed by solvent-casting technique using chitosan and gelatine as muco-adhesive polymers. Optimised patches were embedded with 3 mg of insulin-loaded NPs with a homogeneous distribution of NPs in the muco-adhesive matrix, which displayed adequate physico-mechanical properties. The drug release characteristics, release mechanism and kinetics were investigated. Data fitting to Peppas equation with a correlation coefficient indicated that the mechanism of drug release followed an anomalous transport that means drug release was afforded through drug diffusion along with polymer erosion. In vitro drug release, release kinetics, physical and mechanical studies for all patch formulations reflected the ideal characteristics of this buccal patch for the delivery of insulin NPs.
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Quitosano , Gelatina , Insulina , Nanopartículas/química , Administración Bucal , Quitosano/química , Quitosano/farmacocinética , Gelatina/química , Gelatina/farmacocinética , Humanos , Insulina/química , Insulina/farmacocinéticaRESUMEN
This work was envisaged to develop compression-coated tablets using a blend of Ca(+2) ion cross-linked carboxymethyl xanthan gum (CMXG) and sodium alginate (SAL) for delayed release of immediate pulse release tablets of prednisolone (PDL) in the colon without the need of colonic bacterial intervention for degradation of the polysaccharide coat. The core tablets containing PDL and other compatible excipients were prepared by direct compression method and subsequently compression coated with different ratios of CMXG and SAL. Long T lag, the time required to restrict the drug release below 10%, and short T rap, the time required for immediate release following the T lag, were considered as suitable release parameters for evaluation of colon targeting of PDL tablets. Among the various compression coats, a blend of CMXG and SAL in a ratio of 1.5:3.5 provided T lag of 5.12 ± 0.09 h and T rap of 6.50 ± 0.05 h. The increase in microcrystalline cellulose (MCC) and crospovidone (CP) in the core tablets did not change T lag significantly although decreased the T rap marginally. Inclusion of an osmogen in the core tablets decreased the T lag to 4.05 ± 0.08 h and T rap to 3.56 ± 0.06 h. The increase in coat weight to 225 mg provided a reasonably long T lag (6.06 ± 0.09 h) and short T rap (4.36 ± 0.20 h). Drug release from most of the formulations followed the Hixson-Crowell equation and sigmoidal pattern as confirmed by the Weibull equation. In conclusion, tablets, compression coated with CMXG and SAL in a ratio of 1.5:3.5 and having 225-mg coat weight, were apparently found suitable for colon targeting.
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Colon/metabolismo , Prednisolona/química , Comprimidos Recubiertos/química , Alginatos/química , Celulosa/química , Química Farmacéutica/métodos , Sistemas de Liberación de Medicamentos/métodos , Liberación de Fármacos , Excipientes/química , Ácido Glucurónico/química , Ácidos Hexurónicos/química , Polisacáridos/química , Polisacáridos Bacterianos/química , Prednisolona/administración & dosificación , Presión , Comprimidos Recubiertos/administración & dosificaciónRESUMEN
During the COVID-19 pandemic, a substantial quantity of disposable face masks was discarded, consisting of three layers of nonwoven fabric. However, their improper disposal led to the release of microplastics (MPs) and nanoplastics (NPs) when they ended up in aquatic environments. To analyze the release kinetics and size characteristics of these masks, release experiments were performed on commercially available disposable masks over a period of 7 days and micro- and nanoplastic releases were detected using fiber counting and nanoparticle tracking analysis. The study's findings revealed that there was no significant difference (p > 0.05) in the quantity of MPs released among the layers of the masks. However, the quantity of NPs released from the middle layer of the mask was 25.9 ± 1.3 × 108 to 81.3 ± 5.3 × 108 particles/piece, significantly higher than the inner and outer layers (p < 0.05). The release process of micro/nanoplastics (M/NPs) from each layer of the mask followed the Elovich equation and the power function equation, indicating that the release was divided into two stages. MPs in the range of 1-500 µm and NPs in the range of 100-300 nm dominated the release from each layer of the mask, accounting for an average of 93.81% and 67.52%, respectively. Based on these findings, recommendations are proposed to reduce the release of M/NPs from masks during subsequent use.
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COVID-19 , Máscaras , Microplásticos , Plásticos , Microplásticos/análisis , COVID-19/prevención & control , Humanos , Contaminantes Químicos del Agua/análisis , SARS-CoV-2 , Nanopartículas/químicaRESUMEN
The kinetic release of phenolic compounds from biodegradable films with Clitoria ternatea flower extract (ECT) in different food-simulant fluids and compostability were evaluated for the first time. This work aimed to incorporate ECT in starch-PVA-based film formulations, and the antioxidant capacity, total phenolic compounds, opacity, color, mechanical properties, compostability, and polyphenol release in different fluid simulants were determined. The results obtained showed that antioxidant activity and the total phenolic compounds were ECT dose dependent. Due to its antioxidant properties, ECT interfered with the film's composting process, reaching an average weight loss of 70 %. Additionally, the addition of ECT interfered with the mechanical properties, reducing the tensile strength, probably due to the plasticizer effect. The type of simulating fluid influenced the release of polyphenols from the films, and the presence of water favored the release because it hydrated and swelled the starch-PVA matrix, facilitating diffusion. The classic zero- and first-order models were the most effective in describing the release kinetics of polyphenols from the films. The results of this study demonstrate that the antioxidant potential and the release of polyphenols from starch-PVA-based films in different simulated fluids allow their application in active packaging, making them a sustainable alternative for food preservation.
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Antioxidantes , Clitoria , Antioxidantes/farmacología , Almidón , Fenoles , Polifenoles , Flores , Embalaje de AlimentosRESUMEN
Researchers continuously focused on the fabrication of innovative drug delivery systems to prevent microbial infections while minimizing systemic side effects. Among these, pH-sensitive antibiotic release systems based on bio-based materials have gained great attention due to their ability to precisely modulate drug kinetics and enhance therapeutic efficacy. Herein, pH-sensitive alginate/hyaluronic acid/gelatin ternary blended films were fabricated for the controlled release of ampicillin. Swelling capacity, hydrolytic degradation profile, pH reversibility and in vitro ampicillin release behavior of produced films were investigated in both simulated gastric (pH 1.2) and intestinal (pH 7.4) environments. The cumulative release amount of ampicillin at pH 1.2 (61.0 ± 1.07 mg drug/g polymer) was greater than that of at pH 7.4 (43.0 ± 1.05 mg drug/g polymer) proved that release behavior of ampicillin for produced films is pH-dependent. Based on the fitted release data, best fit was found as the first-order kinetic model with the highest R2 values of 0.966 and 0.962 for both pH conditions. According to Korsmeyer-Peppas model, drug release mechanism is also controlled by case II-transport. Furthermore, produced films demonstrated excellent cytocompatibility. All results revealed that obtained films could be a promising drug carrier to traditional targeting systems for site-specific, pH-sensitive ampicillin delivery in both gastric and intestine.
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Alginatos , Ampicilina , Portadores de Fármacos , Liberación de Fármacos , Gelatina , Ácido Hialurónico , Ampicilina/química , Ampicilina/farmacología , Ácido Hialurónico/química , Concentración de Iones de Hidrógeno , Gelatina/química , Portadores de Fármacos/química , Cinética , Alginatos/química , Antibacterianos/química , Antibacterianos/farmacología , AnimalesRESUMEN
Inhaled colistin is used to treat pneumonia and respiratory infections through nebulization or dry powder inhalers. Nevertheless, the development of a metered-dose inhaler (MDI) for colistin, which could enhance patient convenience and treatment efficacy, has not yet been developed. Colistin is known for its ability to induce cellular toxicity. Gold nanoparticles (AuNPs) can potentially mitigate colistin toxicity. Therefore, this study aimed to evaluate the antimicrobial effectiveness of colistin conjugated with chitosan-capped gold nanoparticles (Col-CS-AuNPs) and their potential formulation for use with MDIs to deliver the aerosol directly to the deep lung. Fourier-transform infrared spectroscopy, nuclear magnetic resonance, and elemental analysis were used to characterize the synthesized Col-CS-AuNPs. Drug release profiles fitted with the most suitable release kinetic model were evaluated. An MDI formulation containing 100 µg of colistin per puff was prepared. The aerosol properties used to determine the MDI performance included the fine particle fraction, mass median aerodynamic diameter, and geometric standard deviation, which were evaluated using the Andersen Cascade Impactor. The delivered dose uniformity was also determined. The antimicrobial efficacy of the Col-CS-AuNP formulation in the MDI was assessed. The chitosan-capped gold nanoparticles (CS-AuNPs) and Col-CS-AuNPs had particle sizes of 44.34 ± 1.02 and 174.50 ± 4.46 nm, respectively. CS-AuNPs effectively entrapped 76.4% of colistin. Col-CS-AuNPs exhibited an initial burst release of up to 60% colistin within the first 6 h. The release mechanism was accurately described by the Korsmeyer-Peppas model, with an R2 > 0.95. The aerosol properties of the Col-CS-AuNP formulation in the MDI revealed a high fine particle fraction of 61.08%, mass median aerodynamic diameter of 2.34 µm, and geometric standard deviation of 0.21, with a delivered dose uniformity within 75-125% of the labeled claim. The Col-CS-AuNP MDI formulation completely killed Escherichia coli at 5× and 10× minimum inhibitory concentrations after 6 and 12 h of incubation, respectively. The toxicity of CS-AuNP and Col-CS-AuNP MDI formulations in upper and lower respiratory tract cell lines was lower than that of free colistin. The stability of the Col-CS-AuNP MDI formulation was maintained for at least 3 months. The Col-CS-AuNP MDI formulation effectively eradicated bacteria over a 12-h period, showing promise for advancing lung infection treatments.
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Surgical site infections (SSIs) after spinal surgery present significant challenges, including poor antibiotic penetration and biofilm formation on implants, leading to frequent treatment failures. Polymethylmethacrylate (PMMA) is widely used for localized drug delivery in bone infections, yet quantifying individual drug release kinetics is often impractical. This retrospective study analyzed 23 cases of deep SSIs (DSSIs) following spinal surgery treated with antibiotic-loaded PMMA. A mathematical model estimated personalized drug release kinetics from PMMA, considering disease types, pathogens, and various antibiotics. The study found that vancomycin (VAN), ceftriaxone (CRO), and ceftazidime (CAZ) reached peak concentrations of 15.43%, 15.42%, and 15.41%, respectively, within the first two days, which was followed by a lag phase (4.91-4.92%) on days 2-3. On days 5-7, concentrations stabilized, with CRO at 3.22% and CAZ/VAN between 3.63% and 3.65%, averaging 75.4 µg/cm2. Key factors influencing release kinetics include solubility, diffusivity, porosity, tortuosity, and bead diameter. Notably, a patient with a low glomerular filtration rate (ASA IV) was successfully treated with a shortened 9-day intravenous VAN regimen, avoiding systemic complications. This study affirms the effectiveness of local drug delivery systems (DDS) in treating DSSIs and underscores the value of mathematical modeling in determining drug release kinetics. Further research is essential to optimize release rates and durations and to mitigate risks of burst release and tissue toxicity.
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Emulsion is a colloidal dispersion for delivering natural antimicrobial, antioxidant, and bioactive compounds to improve the product's quality. The present study aimed to develop the active emulsion film based on whey protein isolate (WPI) by adding oleic acid (OA) (0, 10, and 20% w/w) and green tea extract (GTE) (0 and 0.5% w/v) for cheese packaging. Results showed that the opacity, flexibility, and water barrier properties of WPI hydrogel-based film were significantly increased by adding 10% OA. Active release from emulsion-based films was governed by pH and the nature of food model systems. The minimum release occurred in the acidic food model system. After 5â h exposure in the acid food model system, the obtained release from the active film containing OA 0, 10, and 20% was 52.39, 48.97, and 57.24% of incorporated GTE, respectively. The log reduction value (LRV) of active emulsion film against bacteria was significantly affected by the food model system. Moreover, packed lactic coagulated cheese delivered more phenolic compound of GTE than processed spread cheese. Korsmeyer-Peppas model and Weibull with lag were suggested as appropriate models to forecast the release kinetic of GTE.
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Queso , Ácido Oléico , Proteína de Suero de Leche/química , Embalaje de Alimentos/métodos , Emulsiones , Antioxidantes/químicaRESUMEN
Masks-related microplastic pollution poses a new threat to the environment and human health that has gained increasing concern. However, the long-term release kinetics of microplastic from masks in aquatic environments have yet to studied, which hampers its risk assessment. Four types of masks, namely cotton mask, fashion mask, N95 mask, and disposable surgical mask were exposed to systematically simulated natural water environments to determine the time-dependent microplastic release characteristics at 3, 6, 9, and 12 months, respectively. In addition, the structure changes of employed masks were examined by scanning electron microscopy. Moreover, Fourier transform infrared spectroscopy was applied to analyze the chemical composition and groups of released microplastic fibers. Our results showed that the simulated natural water environment could degrade four types of masks and continuously produce microplastic fibers/fragments in a time-dependent manner. The dominant size of released particles/fibers was below 20 µm across four types of face masks. The physical structure of all four masks was damaged to varying degrees concomitant with photo-oxidation reaction. Collectively, we characterized the long-term release kinetics of microplastic from four types of commonly used masks under a well-mimic real word water environment. Our findings suggest that urgent action must be taken to properly manage disposable masks and ultimately limit the health threats associated with discarded masks.