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1.
Polymers (Basel) ; 15(11)2023 May 31.
Artículo en Inglés | MEDLINE | ID: mdl-37299348

RESUMEN

Changes in the properties of resin-based polymers exposed to the oral environment can emerge when chlorhexidine (CHX) is incorporated to develop bioactive systems for treating denture stomatitis. Three reline resins loaded with CHX were prepared: 2.5 wt% in Kooliner (K), 5 wt% in Ufi Gel Hard (UFI), and Probase Cold (PC). A total of 60 specimens were submitted to physical aging (1000 cycles of thermal fluctuations, 5-55 °C) or chemical aging (28 days of pH fluctuations in artificial saliva, 6 h at pH = 3, 18 h at pH = 7). Knoop microhardness (30 s, 98 mN), 3-point flexural strength (5 mm/min), and surface energy were tested. Color changes (ΔE) were determined using the CIELab system. Data were submitted to non-parametric tests (α = 0.05). After aging, bioactive K and UFI specimens were not different from the controls (resins without CHX) in mechanical and surface properties. Thermally aged CHX-loaded PC specimens showed decreased microhardness and flexural strength but not under adequate levels for function. The color change was observed in all CHX-loaded specimens that underwent chemical aging. The long-term use of CHX bioactive systems based on reline resins generally does not impair removable dentures' proper mechanical and aesthetic functions.

2.
Int J Pharm ; 631: 122470, 2023 Jan 25.
Artículo en Inglés | MEDLINE | ID: mdl-36516927

RESUMEN

The high recurrence rate of common denture stomatitis after antifungal treatment is still concerning. This condition is caused by low patient compliance and incomplete local elimination of the main etiological factor - Candida albicans, often associated with other microorganisms, such as Streptococcus species. Impregnating denture materials with antimicrobials for local delivery is a strategy that can overcome the side effects and improve the efficacy of conventional treatments (topical and/or systemic). In this work, we describe the development of three hard autopolymerizing reline acrylic resins (Kooliner, Ufi Gel Hard, and Probase Cold) loaded with different percentages of chlorhexidine (CHX). The novel formulations were characterized based on their antimicrobial activity, mechanical, morphological and surface properties, in-vitro drug release profiles, and cytotoxicity. The addition of CHX in all resins did not change their chemical and mechanical structure. Among all the tested formulations, Probase Cold loaded with 5 wt% CHX showed the most promising results in terms of antimicrobial activity and lack of serious detrimental mechanical, morphological, surface, and biological properties.


Asunto(s)
Antiinfecciosos , Clorhexidina , Humanos , Ensayo de Materiales , Resinas Acrílicas/química
3.
Foods ; 12(1)2022 Dec 29.
Artículo en Inglés | MEDLINE | ID: mdl-36613384

RESUMEN

Food packaging is the best way to protect food while it moves along the entire supply chain to the consumer. However, conventional food packaging poses some problems related to food wastage and excessive plastic production. Considering this, the aim of this work was to examine recent findings related to bio-based alternative food packaging films by means of conventional methodologies and additive manufacturing technologies, such as 3D printing (3D-P), with potential to replace conventional petroleum-based food packaging. Based on the findings, progress in the development of bio-based packaging films, biopolymer-based feedstocks for 3D-P, and innovative food packaging materials produced by this technology was identified. However, the lack of studies suggests that 3D-P has not been well-explored in this field. Nonetheless, it is probable that in the future this technology will be more widely employed in the food packaging field, which could lead to a reduction in plastic production as well as safer food consumption.

4.
Drug Deliv Transl Res ; 12(6): 1395-1407, 2022 06.
Artículo en Inglés | MEDLINE | ID: mdl-34545538

RESUMEN

In dentistry, the use of biomaterial-based drug delivery systems (DDS) aiming the release of the active compounds directly to the site of action is slowly getting more awareness among the scientific and medical community. Emerging technologies including nanotechnological platforms are offering novel approaches, but the majority are still in the proof-of-concept stage. This study critically reviews the potential use of DDS in anesthesiology, oral diseases, cariology, restorative dentistry, periodontics, endodontics, implantology, fixed and removable prosthodontics, and orthodontics with a special focus on infections. It also stresses the gaps and challenges faced. Despite numerous clinical and pharmacological advantages, some disadvantages of DDS pose an obstacle to their widespread use. The biomaterial's biofunctionality may be affected when the drug is incorporated and may cause an additional risk of toxicity. Also, the release of sub-therapeutic levels of drugs such as antibiotics may lead to microbial resistance. Multiple available techniques for the manufacture of DDS may affect drug release profiles and their bioavailability. If the benefits outweigh the costs, DDS may be potentially used to prevent or treat oral pathologies as an alternative to conventional strategies. A case-by-case approach must be followed.


Asunto(s)
Odontología , Ortodoncia , Materiales Biocompatibles , Sistemas de Liberación de Medicamentos , Periodoncia
5.
Colloids Surf B Biointerfaces ; 208: 112057, 2021 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-34464911

RESUMEN

Staphylococcus aureus medical devices related-infections, such as blood stream catheter are of major concern. Their prevention is compulsory and strategies, not prone to the development of resistance, to prevent S. aureus biofilms on catheter surfaces (e.g. silicone) are needed. In this work two different approaches using sophorolipids were studied to prevent S. aureus biofilm formation on medical grade silicone: i) an antiadhesive strategy through covalent bond of sophorolipids to the surface; ii) and a release strategy using isolated most active sophorolipids. Sophorolipids produced by Starmerella bombicola, were characterized by UHPLC-MS and RMN, purified by automatic flash chromatography and tested for their antimicrobial activity towards S. aureus. Highest antimicrobial activity was observed for C18:0 and C18:1 diacetylated lactonic sophorolipids showing a MIC of 50 µg mL-1. Surface modification with acidic or lactonic sophorolipids when evaluating the anti-adhesive or release strategy, respectively, was confirmed by contact angle, FTIR-ATR and AFM analysis. When using a mixture of acidic sophorolipids covalently bonded to silicone surface as antiadhesive strategy cytocompatible surfaces were obtained and a reduction of 90 % on biofilm formation was observed. Nevertheless, if a release strategy is adopted with purified lactonic sophorolipids a higher effect is achieved. Most promising compound was C18:1 diacateylated lactonic sophorolipid that showed no cellular viability reduction when a concentration of 1.5 mg mL-1 was selected and a reduction on biofilm around 5 log units. Results reinforce the applicability of these antimicrobial biosurfactants on preventing biofilms and disclose that their antimicrobial effect is imperative when comparing to their antiadhesive properties.


Asunto(s)
Infecciones Relacionadas con Catéteres , Staphylococcus aureus Resistente a Meticilina , Infecciones Relacionadas con Catéteres/prevención & control , Glucolípidos/farmacología , Humanos , Ácidos Oléicos , Saccharomycetales , Staphylococcus aureus
6.
Carbohydr Polym ; 254: 117433, 2021 Feb 15.
Artículo en Inglés | MEDLINE | ID: mdl-33357906

RESUMEN

Driven by the need to find alternatives to control Staphylococcus aureus infections, this work describes the development of chitosan-based particulate systems as carriers for antimicrobial glycolipids. By using a simple ionic gelation method stable nanoparticles were obtained showing an encapsulation efficiency of 41.1 ± 8.8 % and 74.2 ± 1.3 % and an average size of 210.0 ± 15.7 nm and 329.6 ± 8.0 nm for sophorolipids and rhamnolipids chitosan-nanoparticles, respectively. Glycolipids incorporation and particle size was correspondingly corroborated by FTIR-ATR and TEM analysis. Rhamnolipids chitosan nanoparticles (RLs-CSp) presented the highest antimicrobial effect towards S. aureus (ATCC 25923) exhibiting a minimal inhibitory concentration of 130 µg/mL and a biofilm inhibition ability of 99 %. Additionally, RLs-CSp did not interfere with human dermal fibroblasts (AG22719) viability and proliferation under the tested conditions. The results revealed that the RLs-CSp were able to inhibit bacterial growth showing adequate cytocompatibility and might become, after additional studies, a valuable approach to prevent S. aureus related infections.


Asunto(s)
Antibacterianos/química , Quitosano/química , Portadores de Fármacos , Glucolípidos/química , Ácidos Oléicos/química , Staphylococcus aureus/efectos de los fármacos , Tensoactivos/química , Antibacterianos/aislamiento & purificación , Antibacterianos/farmacología , Biopelículas/efectos de los fármacos , Biopelículas/crecimiento & desarrollo , Ciclo Celular/efectos de los fármacos , Línea Celular , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Fibroblastos/citología , Fibroblastos/efectos de los fármacos , Glucolípidos/aislamiento & purificación , Glucolípidos/farmacología , Humanos , Pruebas de Sensibilidad Microbiana , Nanopartículas/química , Nanopartículas/ultraestructura , Ácidos Oléicos/aislamiento & purificación , Ácidos Oléicos/farmacología , Tamaño de la Partícula , Staphylococcus aureus/crecimiento & desarrollo , Tensoactivos/aislamiento & purificación , Tensoactivos/farmacología
7.
Int J Pharm ; 593: 120097, 2021 Jan 25.
Artículo en Inglés | MEDLINE | ID: mdl-33217547

RESUMEN

Polymeric platforms obtained by three-dimensional (3D) printing are becoming increasingly important as multifunctional therapeutic systems for bone treatment applications. In particularly, researchers aim to control bacterial biofilm on these 3D-platforms and enhance re-growing bone tissue, at the same time. This study aimed to fabricate a 3D-printed polylactic acid platform loaded with hydroxyapatite (HA), iron oxide nanoparticles (IONPs) and an antibiotic (minocycline) with tuneable properties and multistimuli response. IONPs were produced by a facile chemical co-precipitation method showing an average diameter between 11 and 15 nm and a superparamagnetic behaviour which was preserved when loaded into the 3D-platforms. The presence of two types of nanoparticles (IONPs and HA) modify the nanomorphological/nanotopographical feature of the 3D-platforms justifying their adequate bioactivity profile and in vitro cellular effects on immortalized and primary osteoblasts, including cytocompatibility and increased osteogenesis-related gene expression (RUNX2, BGLAP and SPP1). Disk diffusion assays and SEM analysis confirmed the effect of the 3D-platforms loaded with minocycline against Staphylococcus aureus. Altogether results showed that fabricated 3D-platforms combined the exact therapeutic antibiofilm dose of the antibiotic against S. aureus, with the enhanced osteogenic stimulation of the HA and IONPs nanoparticles which is a disruptive approach for bone targeting applications.


Asunto(s)
Nanopartículas de Magnetita , Nanopartículas , Antibacterianos/farmacología , Regeneración Ósea , Huesos , Osteogénesis , Impresión Tridimensional , Staphylococcus aureus , Andamios del Tejido
8.
Int J Mol Sci ; 21(15)2020 Jul 31.
Artículo en Inglés | MEDLINE | ID: mdl-32751908

RESUMEN

This work reports the versatility of polydopamine (PD) when applied as a particle coating in a composite of polylactide (PLA). Polydopamine was observed to increase the particle-matrix interface strength and facilitate the adsorption of drugs to the material surface. Here, barium sulfate radiopaque particles were functionalized with polydopamine and integrated into a polylactide matrix, leading to the formulation of a biodegradable and X-ray opaque material with enhanced mechanical properties. Polydopamine functionalized barium sulfate particles also facilitated the adsorption and release of the antibiotic levofloxacin. Analysis of the antibacterial capacity of these composites and the metabolic activity and proliferation of human dermal fibroblasts in vitro demonstrated that these materials are non-cytotoxic and can be 3D printed to formulate complex biocompatible materials for bone fixation devices.


Asunto(s)
Sulfato de Bario/química , Materiales Biocompatibles , Indoles/química , Poliésteres/química , Polímeros/química , Ingeniería de Tejidos , Andamios del Tejido , Antibacterianos/farmacología , Supervivencia Celular/efectos de los fármacos , Células Cultivadas , Portadores de Fármacos/química , Fibroblastos , Humanos , Levofloxacino/farmacología , Fenómenos Mecánicos
9.
Int J Pharm ; 572: 118821, 2019 Dec 15.
Artículo en Inglés | MEDLINE | ID: mdl-31711981

RESUMEN

Periodontal diseases remain a challenge due to a complex interplay of factors involving a chronic inflammatory activation and bacteria internalization in periodontal cells. In this work, chitosan-nanoparticles loaded with minocycline (MH-NPs), a tetracycline with antimicrobial and anti-inflammatory effects, were developed for in situ delivery in the periodontal milieu aiming to improve drug effectiveness. A general cytocompatibility evaluation and a detailed approach to address the cellular uptake process, trafficking pathways and the modulation of relevant inflammatory gene expression was conducted using human gingival fibroblasts. Results show that MH-NPs with an adequate cytocompatible profile can be internalized by distinct endocytic processes (macropinocytosis and clathrin-mediated endocytosis). The ability to modulate autophagy with the delivery within the same endosomal/lysosomal pathway as periodontal pathogens was observed, which increases the intracellular drug effectiveness. Porphyromonas gingivalis LPS-stimulated cultures, grown in the presence of MH-NPs, were found to express significantly reduced levels of inflammation-related markers (IL-1b, TNFα, CXCL-8, NFKB1). These nanoparticles can be potentially used in periodontal disease treatment conjoining the ability of intracellular drug targeting with significant anti-inflammatory effects.


Asunto(s)
Antibacterianos/administración & dosificación , Antiinflamatorios/administración & dosificación , Quitosano/química , Minociclina/administración & dosificación , Antibacterianos/farmacología , Antiinflamatorios/farmacología , Células Cultivadas , Sistemas de Liberación de Medicamentos , Fibroblastos/efectos de los fármacos , Fibroblastos/patología , Encía/citología , Encía/efectos de los fármacos , Encía/microbiología , Humanos , Inflamación/tratamiento farmacológico , Inflamación/patología , Minociclina/farmacología , Nanopartículas , Enfermedades Periodontales/tratamiento farmacológico , Porphyromonas gingivalis/efectos de los fármacos
10.
Mater Sci Eng C Mater Biol Appl ; 101: 15-26, 2019 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-31029308

RESUMEN

3D-printing and additive manufacturing can be powerful techniques to design customized structures and produce synthetic bone grafts with multifunctional effects suitable for bone repair. In our work we aimed the development of novel multifunctionalized 3D printed poly(lactic acid) (PLA) scaffolds with bioinspired surface coatings able to reduce bacterial biofilm formation while favoring human bone marrow-derived mesenchymal stem cells (hMSCs) activity. For that purpose, 3D printing was used to prepare PLA scaffolds that were further multifunctionalized with collagen (Col), minocycline (MH) and bioinspired citrate- hydroxyapatite nanoparticles (cHA). PLA-Col-MH-cHA scaffolds provide a closer structural support approximation to native bone architecture with uniform macroporous, adequate wettability and an excellent compressive strength. The addition of MH resulted in an adequate antibiotic release profile that by being compatible with local drug delivery therapy was translated into antibacterial activities against Staphylococcus aureus, a main pathogen associated to bone-related infections. Subsequently, the hMSCs response to these scaffolds revealed that the incorporation of cHA significantly stimulated the adhesion, proliferation and osteogenesis-related gene expression (RUNX2, OCN and OPN) of hMSCs. Furthermore, the association of a bioinspired material (cHA) with the antibiotic MH resulted in a combined effect of an enhanced osteogenic activity. These findings, together with the antibiofilm activity depicted strengthen the appropriateness of this 3D-printed PLA-Col-MH-cHA scaffold for future use in bone repair. By targeting bone repair while mitigating the typical infections associated to bone implants, our 3D scaffolds deliver an integrated strategy with the combined effects further envisaging an increase in the success rate of bone-implanted devices.


Asunto(s)
Regeneración Ósea/efectos de los fármacos , Colágeno/farmacología , Durapatita/farmacología , Minociclina/farmacología , Nanopartículas/química , Poliésteres/farmacología , Impresión Tridimensional , Ingeniería de Tejidos/métodos , Adsorción , Antibacterianos/farmacología , Biopelículas/efectos de los fármacos , Liberación de Fármacos , Regulación de la Expresión Génica/efectos de los fármacos , Humanos , Células Madre Mesenquimatosas/citología , Células Madre Mesenquimatosas/efectos de los fármacos , Células Madre Mesenquimatosas/metabolismo , Células Madre Mesenquimatosas/ultraestructura , Pruebas de Sensibilidad Microbiana , Oseointegración/efectos de los fármacos , Osteogénesis/efectos de los fármacos , Osteogénesis/genética , Staphylococcus aureus/efectos de los fármacos , Andamios del Tejido/química
11.
Mater Sci Eng C Mater Biol Appl ; 93: 529-538, 2018 Dec 01.
Artículo en Inglés | MEDLINE | ID: mdl-30274086

RESUMEN

In depth knowledge of the thermal properties of drugs is particularly important when they are designed for incorporation into a thermoplastic polymer matrix. In this paper a representative set of Urinary Tract Infection (UTI) antibiotics were studied using thermogravimetric analysis (TGA) and differential scanning calorimetry (DSC), and then blended via solvent-casting method with poly(D,L-lactide-co-ε-caprolactone). Of these, amoxicillin, cefdinir, levofloxacin and norfloxacin showed a co-continuous morphology with the polyester, whereas blends with ciprofloxacin, nitrofurantoin and tobramycin resulted in two immiscible phases. E. coli susceptibility results showed that the activity of these antibiotics was not affected by the interactions with the polymer matrix. The presence of the drug did not change the hydrolytic degradation kinetics of this fully amorphous polyester (KMw of ~0.050 days-1). However, the release profiles from the long-term studies (105 days) with a 10 or 30% of antibiotic-loaded films were quite different. While water was able to penetrate the polymer matrix and elute the entire levofloxacin content in the first 8 h, the burst release of cefdinir reached a value under 75%. A more interesting profile was obtained with nitrofurantoin, suggesting that a lengthy treatment is achievable. <30% of the drug was burst released, ~55% eluted by diffusion up to day 42 and the rest driven by the weight loss of the bioabsorbable polyester.


Asunto(s)
Antibacterianos , Escherichia coli/crecimiento & desarrollo , Membranas Artificiales , Poliésteres/química , Sistema Urinario , Antibacterianos/química , Antibacterianos/farmacocinética , Preparaciones de Acción Retardada/química , Preparaciones de Acción Retardada/farmacocinética
12.
J Chromatogr Sci ; 55(7): 757-765, 2017 Aug 01.
Artículo en Inglés | MEDLINE | ID: mdl-28444354

RESUMEN

Simple, economic and environmental friendly high-performance liquid chromatography methods for levofloxacin and minocycline quantification in biomimetic media were developed and validate including their stability at body temperature, an often neglected evaluation parameter. Both methods are similar only differing in the wavelength setting, i.e., for levofloxacin and minocycline quantification the UV detection was set at 284 and at 273 nm, respectively. The separation of both antibiotics was achieved using a reversed-phase column and a mobile phase consisting of acetonitrile and water (15:85) with 0.6% triethylamine, adjusted to pH 3. As an internal standard for levofloxacin quantification, minocycline was used and vice versa. The calibration curves for both methods were linear (r = 0.99) over a concentration range of 0.3-16 µg/mL and 0.5-16 µg/mL for levofloxacin and minocycline, respectively, with precision, accuracy and recovery in agreement with international guidelines requirement. Levofloxacin revealed stability in all media and conditions, including at 37°C, with exception to freeze-thaw cycle conditions. Minocycline presented a more accentuated degradation profile over prolonged time courses, when compared to levofloxacin. Reported data is of utmost interest for pharma and biomaterials fields regarding the research and development of new local drug-delivery-systems containing either of these two antibiotics, namely when monitoring the in vitro release studies of those systems.


Asunto(s)
Cromatografía Líquida de Alta Presión/métodos , Levofloxacino/análisis , Minociclina/análisis , Calibración , Medios de Cultivo , Estabilidad de Medicamentos , Límite de Detección , Modelos Lineales , Reproducibilidad de los Resultados
13.
Mini Rev Med Chem ; 17(14): 1364-1376, 2017.
Artículo en Inglés | MEDLINE | ID: mdl-27629996

RESUMEN

BACKGROUND: Multiple strategies have been recommended for prevention and control of antibacterial resistance. Solutions will need to be found soon if we are not to run the serious risk of losing the ability to treat bacterial infections, especially the ones arising from multi-resistant strains. Deep knowledge of the resistance mechanisms followed by novel therapeutic drugs and vaccines are needed. A consolidated, multidisciplinary and regulated strategy is required by this challenge. OBJECTIVE: This review will be focused on new strategies to control infections. Among strategies to tackle antibiotic resistance that have been under investigation, are the use of antimicrobial peptides, phage therapy and phage enzymes, therapeutic antibodies, quorum sensing inhibitors and, finally, the antibacterial nanomedicines. Although all of the approaches seem to be effective, and at least one of them has been in use for relatively a long time (phage therapy), antibacterial nanomedicines show the most diverse range of different approaches regarding potential translation to clinics. RESULTS & CONCLUSION: Several advances have been made but a great effort is still mandatory in order to reach feasible, effective and marketable novel antimicrobial products.


Asunto(s)
Antibacterianos/farmacología , Bacterias/efectos de los fármacos , Infecciones Bacterianas/tratamiento farmacológico , Infecciones Bacterianas/microbiología , Antibacterianos/síntesis química , Antibacterianos/química , Farmacorresistencia Bacteriana/efectos de los fármacos , Pruebas de Sensibilidad Microbiana
14.
Int J Pharm ; 513(1-2): 697-708, 2016 Nov 20.
Artículo en Inglés | MEDLINE | ID: mdl-27693709

RESUMEN

Given the impact of biofilms in health care environment and the increasing antibiotic resistance and/or tolerance, new strategies for preventing that occurrence in medical devices are obligatory. Thus, biomaterials surface functionalization with active compounds can be a valuable approach. In the present study the ability of the biosurfactants sophorolipids to prevent biofilms formation on silicone rubber aimed for medical catheters was investigated. Sophorolipids produced by Starmerella bombicola, identified by HPLC-MS/MS were used to cover silicone and surface characterization was evaluated through contact angle measurements and FTIR-ATR. Results revealed that sophorolipids presence on silicone surface decreased the hydrophobicity of the material and biofilm formation of Staphylococcus aureus ATCC 25923 and Escherichia coli ATCC 25922. Antibiofilm activity was evaluated through different methods and was more pronounced against S. aureus. Furthermore, biocompatibility of silicone specimens with HaCaT cells was also obtained. From this study it was possible to conclude that sophorolipids seem to be a favourable approach for coating silicone catheters. Such compounds may represent a novel source of antibiofilm agents for technological development passing through strategies of permanent functionalization of surfaces.


Asunto(s)
Biopelículas/efectos de los fármacos , Catéteres/microbiología , Lípidos/farmacología , Elastómeros de Silicona , Adsorción , Línea Celular , Supervivencia Celular/efectos de los fármacos , Escherichia coli/efectos de los fármacos , Escherichia coli/fisiología , Humanos , Lípidos/biosíntesis , Lípidos/química , Octoxinol/química , Saccharomycetales/metabolismo , Elastómeros de Silicona/química , Dodecil Sulfato de Sodio/química , Staphylococcus aureus/efectos de los fármacos , Staphylococcus aureus/fisiología , Tensoactivos/química
15.
Int J Nanomedicine ; 10: 4351-66, 2015.
Artículo en Inglés | MEDLINE | ID: mdl-26185439

RESUMEN

The aim of the present study was to develop novel daptomycin-loaded poly-epsilon-caprolactone (PCL) microparticles with enhanced antibiofilm activity against mature biofilms of clinically relevant bacteria, methicillin-resistant Staphylococcus aureus (MRSA) and polysaccharide intercellular adhesin-positive Staphylococcus epidermidis. Daptomycin was encapsulated into PCL microparticles by a double emulsion-solvent evaporation method. For comparison purposes, formulations containing vancomycin were also prepared. Particle morphology, size distribution, encapsulation efficiency, surface charge, thermal behavior, and in vitro release were assessed. All formulations exhibited a spherical morphology, micrometer size, and negative surface charge. From a very early time stage, the released concentrations of daptomycin and vancomycin were higher than the minimal inhibitory concentration and continued so up to 72 hours. Daptomycin presented a sustained release profile with increasing concentrations of the drug being released up to 72 hours, whereas the release of vancomycin stabilized at 24 hours. The antibacterial activity of the microparticles was assessed by isothermal microcalorimetry against planktonic and sessile MRSA and S. epidermidis. Regarding planktonic bacteria, daptomycin-loaded PCL microparticles presented the highest antibacterial activity against both strains. Isothermal microcalorimetry also revealed that lower concentrations of daptomycin-loaded microparticles were required to completely inhibit the recovery of mature MRSA and S. epidermidis biofilms. Further characterization of the effect of daptomycin-loaded PCL microparticles on mature biofilms was performed by fluorescence in situ hybridization. Fluorescence in situ hybridization showed an important reduction in MRSA biofilm, whereas S. epidermidis biofilms, although inhibited, were not eradicated. In addition, an important attachment of the microparticles to MRSA and S. epidermidis biofilms was observed. Finally, all formulations proved to be biocompatible with both ISO compliant L929 fibroblasts and human MG63 osteoblast-like cells.


Asunto(s)
Antibacterianos , Biopelículas/efectos de los fármacos , Caproatos/química , Daptomicina , Lactonas/química , Staphylococcus aureus Resistente a Meticilina/efectos de los fármacos , Vancomicina , Antibacterianos/química , Antibacterianos/farmacocinética , Antibacterianos/farmacología , Daptomicina/química , Daptomicina/farmacocinética , Daptomicina/farmacología , Pruebas de Sensibilidad Microbiana , Microesferas , Vancomicina/química , Vancomicina/farmacocinética , Vancomicina/farmacología
16.
Int J Pharm ; 490(1-2): 200-8, 2015 Jul 25.
Artículo en Inglés | MEDLINE | ID: mdl-26002570

RESUMEN

Antibiotic-loaded acrylic bone cements (ALABCs) are well-established and cost-effective materials to control the occurrence of bone and joint infections. However, the inexistence of alternative antibiotics other than those already commercially available and the poor ability to bind to bone tissue hampering its biological function are still major drawbacks of ALABCs clinical application. The concept of this research work is to develop a novel bone cement (BC) drug delivery system composed by Mg- and Sr-doped calcium phosphate (CaP) particles as drug carriers loaded into a lactose-modified acrylic BC, which, to the best of our knowledge, has never been reported. CaP particles are known to promote bone ingrowth and current research is focused on using these carriers as antibiotic delivery systems for the treatment of bone infections, like osteomyelitis. Levofloxacin is a fluoroquinolone with anti-staphylococcal activity and adequate penetration into osteoarticular tissues and increasingly being recommended to manage bone-related infections. Also, the lactose-modified BC matrix, with a more porous structure, has already proved to enhance antibiotic release from the BC inner matrix. This novel BC composite biomaterial has shown improved mechanical integrity, biocompatibility maintenance, and sustained release of levofloxacin, with concentrations over the minimum inhibitory concentration values after a 48h while maintaining antibacterial activity over an 8-week period against Staphyloccocus aureus and Staphyloccocus epidermidis, common pathogens associated with bone infections.


Asunto(s)
Antibacterianos/química , Materiales Biocompatibles/química , Cementos para Huesos/química , Fosfatos de Calcio/química , Levofloxacino/química , Polimetil Metacrilato/química , Antibacterianos/farmacología , Portadores de Fármacos/química , Sistemas de Liberación de Medicamentos/métodos , Levofloxacino/farmacología , Ensayo de Materiales/métodos , Pruebas de Sensibilidad Microbiana/métodos , Porosidad , Staphylococcus aureus/efectos de los fármacos , Staphylococcus epidermidis/efectos de los fármacos
17.
Int J Pharm ; 485(1-2): 317-28, 2015 May 15.
Artículo en Inglés | MEDLINE | ID: mdl-25797053

RESUMEN

Antibiotic-loaded acrylic bone cements (ALABCs) are widely used to decrease the occurrence of bone infections in cemented arthroplasties and actually being considered as a more cost-effective procedure when compared to cementless implants. However, ALABCs have a major drawback, which is the incomplete release of the antibiotics and, as a result, pathogens that commonly are responsible for those infections are becoming resistant. Consequently, it is of most relevance to find new antibacterial agents to load into BC with an effective mechanism against those microorganisms. This research work intended to load levofloxacin, a fluoroquinolone with anti-staphylococcal activity and adequate penetration into osteoarticular tissues, on lactose-modified commercial bone cement (BC). This modified BC matrix exhibited increased levofloxacin release and delayed Staphylococcus aureus biofilm formation. Further insights on material-drug interaction during BC setting were investigated by density functional theory calculations. The obtained results suggested that favorable covalent and non-covalent interactions could be established between levofloxacin and the BC. Moreover, BC mechanical and biocompatibility properties were maintained. These features justify the potential of levofloxacin-loaded modified-BC as a valuable approach for local antibiotic delivery in bone infections management.


Asunto(s)
Antibacterianos/farmacología , Biopelículas/efectos de los fármacos , Portadores de Fármacos , Levofloxacino/farmacología , Polimetil Metacrilato/farmacología , Staphylococcus aureus/efectos de los fármacos , Animales , Antibacterianos/administración & dosificación , Antibacterianos/química , Biopelículas/crecimiento & desarrollo , Línea Celular , Química Farmacéutica , Simulación por Computador , Preparaciones de Acción Retardada , Fibroblastos/efectos de los fármacos , Fibroblastos/metabolismo , Cinética , Lactosa/química , Levofloxacino/administración & dosificación , Levofloxacino/química , Ratones , Microscopía Electrónica de Rastreo , Modelos Químicos , Modelos Moleculares , Estructura Molecular , Osteoblastos/efectos de los fármacos , Osteoblastos/metabolismo , Polimetil Metacrilato/administración & dosificación , Polimetil Metacrilato/química , Solubilidad , Staphylococcus aureus/crecimiento & desarrollo , Propiedades de Superficie , Tecnología Farmacéutica/métodos
18.
Mater Sci Eng C Mater Biol Appl ; 38: 218-26, 2014 May 01.
Artículo en Inglés | MEDLINE | ID: mdl-24656372

RESUMEN

Currently the safe and responsible use of antibiotics is a world-wide concern as it promotes prevention of the increasing emergence of multiresistant bacterial strains. Considering that there is a noticeable decline of the available antibiotic pipeline able to combat emerging resistance in serious infection a major concern grows around the prosthetic joint infections once the available commercial antibiotic loaded polymethylmethacrylate bone cements (BC) are inadequate for local antibiotic treatment, especially against MRSA, the most commonly isolated and antibiotic-resistant pathogen in bone infections. In this paper a novel modified BC matrix loaded with minocycline is proposed. A renewed interest in this tetracycline arises due to its broad-spectrum of activity against the main organisms responsible for prosthetic joint infections, especially against MRSA. The modified BC matrices were evaluated concerning minocycline release profile, biomechanical properties, solid-state characterization, antimicrobial stability and biocompatibility under in vitro conditions. BC matrix loaded with 2.5% (w/wBC) of minocycline and 10.0% (w/wBC) of lactose presented the best properties since it completely released the loaded minocycline, maintained the mechanical properties and the antimicrobial activity against representative strains of orthopedic infections. In vitro biocompatibility was assessed for the elected matrix and neither minocycline nor lactose loading enhanced BC cytotoxicity.


Asunto(s)
Antibacterianos/farmacología , Antibacterianos/uso terapéutico , Sistemas de Liberación de Medicamentos , Farmacorresistencia Bacteriana Múltiple/efectos de los fármacos , Artropatías/tratamiento farmacológico , Polimetil Metacrilato/química , Infecciones Relacionadas con Prótesis/tratamiento farmacológico , Materiales Biocompatibles/farmacología , Fenómenos Biomecánicos/efectos de los fármacos , Rastreo Diferencial de Calorimetría , Línea Celular , Supervivencia Celular/efectos de los fármacos , Humanos , Artropatías/microbiología , Ensayo de Materiales , Pruebas de Sensibilidad Microbiana , Microscopía Electrónica de Rastreo , Minociclina/farmacología , Minociclina/uso terapéutico , Infecciones Relacionadas con Prótesis/microbiología , Espectroscopía Infrarroja por Transformada de Fourier , Difracción de Rayos X
19.
Biomed Res Int ; 2013: 485246, 2013.
Artículo en Inglés | MEDLINE | ID: mdl-23971038

RESUMEN

OBJECTIVE: To evaluate the effect of postpolymerization treatment based on ethanol-aqueous solutions on the residual monomer (RM) content, flexural strength, microhardness, and cytotoxicity of hard chairside reline resins (Kooliner, Ufi Gel Hard). METHODS: After polymerization, specimens were immersed in water, 20%, 50%, or 70% ethanol solutions at 23°C or 55°C for 10 minutes. Controls were left untreated. HPLC was used for the determination of RM content. Specimens were submitted to Vickers microhardness and 3-point loading flexural strength tests. Cytotoxicity of resin eluates was determined on human fibroblasts by assessing cellular mitochondrial function and lactate dehydrogenase release. RESULTS: Higher concentrations of ethanol promoted lower RM content at 55°C in both materials. The mechanical properties were maintained after 50% and 20% ethanol treatments in Kooliner and Ufi Gel Hard, respectively. Specimens submitted to those treatments showed significant reduction on cytotoxicity compared to immersion in hot water, the treatment of choice in the recent literature. SIGNIFICANCE: Immersion of relined dentures in specific ethanol solutions at 55°C for 10 minutes can be considered an effective postpolymerization treatment contributing to increase materials biocompatibility. The proposed protocol is expeditious and easy to achieve with simple equipment in a dental office.


Asunto(s)
Resinas Acrílicas/síntesis química , Resinas Acrílicas/farmacología , Rebasado de Dentaduras/métodos , Etanol/química , Fibroblastos/citología , Fibroblastos/efectos de los fármacos , Materiales Biocompatibles/síntesis química , Materiales Biocompatibles/farmacología , Línea Celular , Supervivencia Celular/efectos de los fármacos , Etanol/farmacología , Ensayo de Materiales , Polímeros/síntesis química , Polímeros/farmacología , Resinas Sintéticas/síntesis química , Resinas Sintéticas/farmacología
20.
Dent Mater ; 26(5): e171-80, 2010 May.
Artículo en Inglés | MEDLINE | ID: mdl-20189238

RESUMEN

OBJECTIVES: The development of different types of materials with application in dentistry is an area of intense growth and research, due to its importance in oral health. Among the different materials there are the acrylic based resins that have been extensively used either in restorations or in dentures. The objective of this manuscript was to review the acrylic based resins biodegradation phenomena. Specific attention was given to the causes and consequences of materials degradation under the oral environment. DATA AND SOURCES: Information from scientific full papers, reviews or abstracts published from 1963 to date were included in the review. Published material was searched in dental literature using general and specialist databases, like the PubMED database. STUDY SELECTION: Published studies regarding the description of biodegradation mechanisms, in vitro and in vivo release experiments and cell based studies conducted on acrylic based resins or their components were evaluated. Studies related to the effect of biodegradation on the physical and mechanical properties of the materials were also analyzed. CONCLUSIONS: Different factors such as saliva characteristics, chewing or thermal and chemical dietary changes may be responsible for the biodegradation of acrylic based resins. Release of potential toxic compounds from the material and change on their physical and mechanical properties are the major consequences of biodegradation. Increasing concern arises from potential toxic effects of biodegradation products under clinical application thus justifying an intensive research in this area.


Asunto(s)
Resinas Acrílicas/química , Resinas Acrílicas/metabolismo , Resinas Acrílicas/toxicidad , Animales , Biotransformación , Análisis del Estrés Dental , Humanos , Hidrólisis , Metilmetacrilatos/química
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