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Candida albicans can cause various types of oral infections, mainly associated with denture stomatitis. Conventional therapy has been linked to high recurrence, toxicity, and fungal resistance, necessitating the search for new drugs and delivery systems. In this study, caffeic acid phenethyl ester (CAPE) and gellan gum (GG) were studied as an antifungal agent and carrier system, respectively. First, we observed that different GG formulations (0.6 to 1.0% wt/vol) were able to incorporate and release CAPE, reaching a controlled and prolonged release over 180 min at 1.0% of GG. CAPE-GG formulations exhibited antifungal activity at CAPE concentrations ranging from 128 to >512 µg/mL. Furthermore, CAPE-GG formulations significantly decreased the fungal viability of C. albicans biofilms at short times (12 h), mainly at 1.0% of GG (p < 0.001). C. albicans protease activity was also reduced after 12 h of treatment with CAPE-GG formulations (p < 0.001). Importantly, CAPE was not cytotoxic to human keratinocytes, and CAPE-GG formulations at 1.0% decreased the fungal burden (p = 0.0087) and suppressed inflammation in a rat model of denture stomatitis. Altogether, these results indicate that GG is a promising delivery system for CAPE, showing effective activity against C. albicans and potential to be used in the treatment of denture stomatitis.

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Nanocomposite polymer electrolytes (NPEs) were obtained using gellan gum (GG) and 1 to 40 wt.% of montmorillonite (Na+SYN-1) clay. The NPEs were crosslinked with formaldehyde, plasticized with glycerol, and contained LiClO4. The samples were characterized by impedance spectroscopy, thermal analyses (TGA and DSC), UV-vis transmittance and reflectance, X-ray diffraction (XRD), and continuous-wave electron paramagnetic resonance (CW-EPR). The NPEs of GG and 40 wt.% LiClO4 showed the highest conductivity of 2.14 × 10-6 and 3.10 × 10-4 S/cm at 30 and 80 °C, respectively. The samples with 10 wt.% Na+SYN-1 had a conductivity of 1.86 × 10-5 and 3.74 × 10-4 S/cm at 30 and 80 °C, respectively. TGA analyses revealed that the samples are thermally stable up to 190 °C and this did not change with clay addition. The transparency of the samples decreased with the increase in the clay content and at the same time their reflectance increased. Finally, CW-EPR was performed to identify the coordination environment of Cu2+ ions in the GG NPEs. The samples doped with the lowest copper concentration exhibit the typical EPR spectra due to isolated Cu2+ ions in axially distorted sites. At high concentrations, the spectra become isotropic because of dipolar and exchange magnetic effects. In summary, GG/clay NPEs presented good ionic conductivity results, which qualifies them for electrochemical device applications.

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In this study a novel gellan gum/pullulan bilayer film containing silibinin-loaded nanocapsules was developed for topical treatment of atopic dermatitis (AD). The bilayer films were produced by applying a pullulan layer on a gellan gum layer incorporated with silibinin nanocapsules by two-step solvent casting method. The bilayer formation was confirmed by microscopic analysis. In vitro studies showed that pullulan imparts bioadhesitvity for the films and the presence of nanocapsules increased their occlusion factor almost 2-fold. Besides, the nano-based film presented a slow silibinin release and high affinity for cutaneous tissue. Moreover, this film presented high scavenger capacity and non-hemolytic property. In the in vivo study, interestingly, the treatments with vehicle film attenuated the scratching behavior and the ear edema in mice induced by 2,4-dinitrochlorobenzene (DNCB). However, the nano-based film containing silibinin modulated the inflammatory and oxidative parameters in a similar or more pronounced way than silibinin solution and vehicle film, as well as than hydrocortisone, a classical treatment of AD. In conclusion, these data suggest that itself gellan gum/pullulan bilayer film might attenuate the effects induced by DNCB, acting together with silibinin-loaded nanocapsules, which protected the skin from oxidative damage, improving the therapeutic effect in this AD-model.

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This study aimed to evaluate the antimicrobial and anti-biofilm activity of morin on polymicrobial biofilms and its cytotoxicity in controlled-release films and tablets based on gellan gum. Polymicrobial biofilms were formed from saliva for 48 h under an intermittent exposure regime to 1% sucrose and in contact with films or tablets of gellan gum containing 2 mg of morin each. Acidogenicity, bacterial viability, dry weight and insoluble extracellular polysaccharides from biofilms were evaluated. The cytotoxicity of morin was evaluated in oral keratinocytes. Morin released from the systems reduced the viability of all the microbial groups evaluated, as well as the dry weight and insoluble polysaccharide concentration in the matrix and promoted the control of acidogenicity when compared with the control group without the substance. Morin was cytotoxic only at the highest concentration evaluated. In conclusion, morin is an effective agent and shows antimicrobial and anti-biofilm activity against polymicrobial biofilms.

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Abstract This study aimed to develop promising and innovative mucoadhesive gel systems containing dexamethasone-loaded nanoparticle to increase the effectiveness of treatment for oral precancerous lesions and to reduce side effects. In this respect, a dexamethasone-loaded nanoparticle formulation was prepared by using emulsification/solvent evaporation method. The nanoparticle has high zeta potential (-10.3±0.5 mV), low particle size (218.42±2.1), low polydispersity index (0.070±0.014) and high encapsulation efficiency (95.018±2.982%). To improve the mucosal retention time, the dexamethasone-loaded nanoparticle was dispersed in mucoadhesive gel using gellan gum. The developed gels offered appropriate pH value, high drug content, suitable mechanical and mucoadhesive performance and appropriate viscosity for mucosal administration. All formulations exhibited plastic flow and typical gel-type mechanical spectra after the determined frequency value. The developed formulations exhibited extended drug release as intended for these systems. Cytotoxicity was tested by MTT assay in human epithelioid carcinoma cell (HeLa) in vitro. The MTT assay showed that the blank formulations were non-toxic to cells. It was observed that the bioactivity of the free dexamethasone was potentiated by mucoadhesive gels containing dexamethasone-loaded nanoparticle in HeLa cells. Results from this study indicate that mucoadhesive gels are effective for the local treatment of precancerous lesions. Our findings showed that the developed formulations were worthy of further studies.

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Os biofilmes orais possuem grande relevância clínica por estarem associados com o desenvolvimento de cárie dentária e candidose bucal, que são doenças infecciosas frequentemente encontradas na população. O presente trabalho foi dividido em dois estudos: Estudo 1 que teve como objetivo analisar os efeitos da terapia fotodinâmica antimicrobiana (TFDa), mediada por Fotoenticine (FTC) e Azul de Metileno (AM), sobre biofilmes microcosmos de cárie dentária; e Estudo 2 cujo objetivo foi avaliar o gellan gum como biomaterial para carreador do antifúngico Ester fenetil do ácido caféico (CAPE) contra Candida albicans. No estudo 1, amostras de dentina cariada foram coletadas de diferentes pacientes para formar biofilmes microcosmos in vitro. Os biofilmes foram tratados com FTC ou AM associado à irradiação LED a 660 nm (28,5 J/cm²). Os dados foram analisados pela contagem de Unidades Formadoras de Colônias (UFC/mL). Além disso, a biomassa, estrutura do biofilme e produção de ácidos pelos microrganismos foram determinadas por análises microscópicas ou espectrofotométricas. Os biofilmes de diferentes pacientes apresentaram variações na composição microbiana, sendo formados por estreptococos, lactobacilos e leveduras. No geral, a TFDa diminuiu 3,7 Log10 do total de microrganismos, 2,8 Log10 de estreptococos, 3,2 Log10 de lactobacilos e 3,2 Log10 de leveduras, e atingiu a erradicação de estreptococos do grupo mutans. A TFDa também foi capaz de reduzir a biomassa, desagregar os biofilmes e diminuir a concentração de ácidos em 1,1 a 1,9 mmol de lactato/L. Em relação ao estudo 2, inicialmente, foram preparadas formulações do CAPE em diferentes concentrações de gellan gum (0,6 a 1%). As formulações foram avaliadas em relação ao sistema de liberação e ação antifúngica contra C. albicans. Verificou-se que concentrações mais altas de gellan (0,9 e 1%) levaram a uma liberação mais prolongada do CAPE em relação as concentrações mais baixas. Os valores de concentração inibitória mínima do CAPE sobre C. albicans foram aumentados quando esse composto foi incorporado no gellan. As formulações de CAPE em gellan apresentaram atividade antifúngica tanto em culturas planctônicas como em biofilmes de C. albicans, sendo esses efeitos dependentes do tempo de tratamento. O CAPE e suas formulações em gellan também levaram a uma diminuição da atividade proteolítica de C. albicans. Concluiu-se que a TFDa mediada por Fotoenticine e o sistema carreador de gellan gum podem ser estratégias terapêuticas promissoras para o controle dos biofilmes na cavidade bucal, podendo ser usadas respectivamente no tratamento da cárie e candidose. (AU)

Dental caries and oral candidiasis are infectious diseases frequently found in the population. The present work is divided into two studies, study 1 time as objective: To analyze the effects of antimicrobial photodynamic therapy (aPDT), mediated by Fotoenticine (FTC) and Methylene Blue (MB), on dental caries microcosm biofilms. In study 2, the objective was to evaluate gellan gum as a biomaterial to carry the antifungal caffeic acid phenethyl ester (CAPE) on Candida albicans. To conduct study 1, carious dentin samples were collected from different patients to form in vitro microcosm biofilms. The biofilms were treated with FTC or MB associated with 660 nm red LED irradiation, with energy dose of 28.5 J/cm² and power dose of 40 mW/cm². The data were analyzed by the count of Colony Forming Units (CFU/mL). In addition, the biomass, biofilm structure and acid production of the microorganisms were determined by microscopic or spectrophotometric analysis. The biofilms from different patients showed variations in microbial composition, being formed by streptococci, lactobacilli, and yeasts. Overall, aPDT decreased 3.7 Log10 of total microorganisms, 2.8 Log10 of streptococci, 3.2 Log10 of lactobacilli and 3.2 Log10 of yeasts, and achieved eradication of mutans group streptococci. PDTa was also able to reduce biomass, disaggregate biofilms, and decrease acid concentration by 1.1 to 1.9 mmol lactate/L. For study 2 of this, first the standards of CAPE were determined, such as minimum inhibitory concentration, and absorption peak, then CAPE was incorporated into gellan gum, and then the standard curve test and analysis of CAPE release was performed, finally the formulations were tested on planktonic culture and biofilm of different strains of C. albicans, it was also analyzed the action of this drug on the production of Sap. The MIC found varied from 32 to 64 µg/mL, the release tests showed a gradual release in the higher formulations, finally in the CFU/mL count both in planktonic culture and biofilm the formulations were able to inhibit the fungus. With this it is concluded that both aPDT for oral microcosm and gellan gum as caregiver of CAPE for Candida albicans inhibition are promising. (AU)

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Polymer blends of gellan gum (GG)/retrograded starch(RS) and GG/pectin (P) were cross-linked with calcium, aluminum, or both to prepare mucoadhesive microparticles as oral carriers of drugs or nano systems. Cross-linking with different cations promoted different effects on each blend, which can potentially be explored as novel strategies for modulating physical-chemical and mucoadhesive properties of microparticles. Particles exhibited spherical shapes, diameters from 888 to 1764 µm, and span index values lower than 0.5. Blends of GG:P cross-linked with aluminum resulted in smaller particles than those obtained by calcium cross-linking. GG:RS particles exhibited larger sizes, but cross-linking this blend with calcium promoted diameter reduction. The uptake rates of acid medium were lower than phosphate buffer (pH 6.8), especially GG:RS based particles cross-linked with calcium. On the other hand, particles based on GG:P cross-linked with calcium absorbed the highest volume of acid medium. The percentage of systems erosion was higher in acid medium, but apparently occurred in the outermost layer of the particle. In pH 6.8, erosion was lower, but caused expressive swelling of the matrixes. Calcium cross-linking of GG:RS promoted a significantly reduction on enzymatic degradation at both pH 1.2 and 6.8, which is a promising feature that can provide drug protection against premature degradation in the stomach. In contrast, GG:P microparticles cross-linked with calcium suffered high degradation at both pH values, an advantageous feature for quickly releasing drugs at different sites of the gastrointestinal tract. The high mucoadhesive ability of the microparticles was evidenced at both pH values, and the Freundlich parameters indicated stronger particle-mucin interactions at pH 6.8.

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The use of controlled drug delivery systems represents an alternative and promising strategy for the use of antimicrobials in the oral cavity. Microparticles, films and oral tablets based on alginate and gellan gum were developed also as a strategy to overcome the low aqueous solubility of morin. The systems were characterized in terms of morphological characteristics, mucoadhesion and in vitro drug release. Antibiofilm activity was analyzed for acidogenicity, microbial viability and the composition of the extracellular matrix of single-species biofilms. Scanning Electron Microscopy demonstrated that the microparticles were spherical, rough and compact. The film and the tablet presented smooth and continuous surface and in the inner of the tablet was porous. These systems were more mucoadhesive compared to the microparticles. The in vitro morin release profiles in artificial saliva demonstrated that the microparticles controlled the release better (39.6%), followed by the film (41.1%) and the tablet (91.4%) after 20 h of testing. The morin released from the systems reduced the acidogenicity, microbial viability, concentration of insoluble extracellular polysaccharides and dry weight of biofilms, when compared to the control group. The findings of this study showed that the morin has antibiofilm activity against cariogenic microorganisms.

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This study evaluated the effect of some natural additives and the structure imparted by them on microbial growth and rheological characteristics in acidic model foods with reduced glycidic content. Systems were formulated using gellan gum, as gelling agent; xylitol, as aw depressor; and natamycin, as antimicrobial. Additive-free control systems were prepared. The pH was adjusted to 3.50 or 5.50 as required. Systems were inoculated with Zygosaccharomyces bailii. The effect of additives alone and combined on Z. bailii growth was studied. In some cases, the possible use of additives as yeast nutrients was evaluated. Furthermore, systems rheological characterization was performed. Additives and the structure given by gellan gum significantly affected yeast growth. Gellan gum initially slowed Z. bailii development, but as storage progressed, it acted as yeast carbon source, promoting its growth. A similar trend was observed when xylitol effect was studied. Natamycin inhibited yeast growth in all systems assayed. Additives modified the rheological characteristics of the gels and this effect depended on gellan gum concentration and pH. Obtained results emphasize the importance of considering the different effects that additives and their combinations can exert on the growth of deteriorating microorganisms and on the physical characteristics of gels.

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Probiotics might provide an alternative approach for the control of oral candidiasis. However, studies on the antifungal activity of probiotics in the oral cavity are based on the consumption of yogurt or other dietary products, and it is necessary to use appropriate biomaterials and specific strains to obtain probiotic formulations targeted for local oral administration. In this study, we impregnated gellan gum, a natural biopolymer used as a food additive, with a probiotic and investigated its antifungal activity against Candida albicansLactobacillus paracasei 28.4, a strain recently isolated from the oral cavity of a caries-free individual, was incorporated in several concentrations of gellan gum (0.6% to 1% [wt/vol]). All tested concentrations could incorporate L. paracasei cells while maintaining bacterial viability. Probiotic-gellan gum formulations were stable for 7 days when stored at room temperature or 4°C. Long-term storage of bacterium-impregnated gellan gum was achieved when L. paracasei 28.4 was lyophilized. The probiotic-gellan gum formulations provided a release of L. paracasei cells over 24 h that was sufficient to inhibit the growth of C. albicans, with effects dependent on the cell concentrations incorporated into gellan gum. The probiotic-gellan gum formulations also had inhibitory activity against Candida sp. biofilms by reducing the number of Candida sp. cells (P < 0.0001), decreasing the total biomass (P = 0.0003), and impairing hyphae formation (P = 0.0002), compared to the control group which received no treatment. Interestingly, a probiotic formulation of 1% (wt/vol) gellan gum provided an oral colonization of L. paracasei in mice with approximately 6 log CFU/ml after 10 days. This formulation inhibited C. albicans growth (P < 0.0001), prevented the development of candidiasis lesions (P = 0.0013), and suppressed inflammation (P = 0.0006) compared to the mice not treated in the microscopic analysis of the tongue dorsum. These results indicate that gellan gum is a promising biomaterial and can be used as a carrier system to promote oral colonization for probiotics that prevent oral candidiasis.

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High pressure homogenization has been used for preparation and stabilization of emulsions and suspensions, promoting physical changes in products, such as viscosity change. However, its use in model systems for fruit nectar is innovative. This study aimed to evaluate the effect of the processing in high pressure homogenizer on the rheological behavior and the sensory attributes in model system of gellan gum. Gellan gum (0.05%), organic acids (0.3%), and sucrose (10%) were used to prepare the solutions, which were subsequently homogenized (0-control, 25 and 50 MPa) at 25°C. Rheological and sensory analyses were performed. The samples presented pseudoplastic behavior without residual stress and were characterized by the Ostwald-de-Waele model. The homogenization pressure (PH ) altered the viscosity of the model systems, reduced the consistency index and apparent viscosity, and increased the flow behavior index. The stimuli sour taste and viscosity differed among the parameters evaluated in the time-intensity analysis. No differences were observed for the maximum intensity of viscosity between the treated samples (25 and 50 MPa), which exhibited a similar temporal profile. Therefore, studies on the rheological and sensory behavior are fundamental to product development and process optimization. The present study shows new trends on the use of the high pressure homogenizer and the sensory profile in model systems that can be used for fruit nectar. This study evaluated the sensory attributes through the time-intensity analysis. The sensory data indicate that the homogenization pressure altered the viscosity perception, but did not alter the perception of the acid taste for the same organic acid used. Sensory as well as rheological data present new alternatives for product development. These findings are interesting for future research, equipment design, and process optimization.

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In this work, we developed biopolymeric structures, based on electrostatic attraction, through dripping gellan gum into hydrolyzed collagen (HC), to deliver hydrophilic compounds. Moreover, we evaluated the influence of starch addition on the polymeric network as well as the coating effects promoted by an outer gellan layer. The lowest tested gellan gum concentration in the core (0.5% w/w) was the best one to build spherical beads, with high retention of bioactives (>84% for anthocyanin and >68% for HC). Moreover, the minimum HC concentration (2.5% w/w) in the gelling bath allowed the saturation of active sites of gellan gum presented in the core, as regardless of the HC concentration in the peptide bath, particles presented the same amount of adsorbed peptide. Starch disturbed the interactions between HC and gellan, increasing porosity and pore size, but it presented an important role in retaining anthocyanin in the particle's core. Finally, we demonstrated that addition of a gellan coating layer affected the structure of beads: Peptide molecules (positively charged), already adsorbed onto the beads, diffused out of the core, attracted by the negatively charged gellan coating layer. Consequently, it decreased particle size and increased pore size in the outer part of the particles, which was associated with a reduction in the retention of bioactives. These findings bring important contributions to particle engineering: A new process for particle production was proposed, in which hydrogels were produced by dripping the polysaccharide into the protein bath to be externally gelled, without previous crosslinking with salts.

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This work addresses the establishment and characterization of gellan gum:pectin (GG:P) biodegradable mucoadhesive beads intended for the colon-targeted delivery of resveratrol (RES). The impact of the polymer carrier system on the cytotoxicity and permeability of RES was evaluated. Beads of circular shape (circularity index of 0.81) with an average diameter of 914 µm, Span index of 0.29, and RES entrapment efficiency of 76% were developed. In vitro drug release demonstrated that beads were able to reduce release rates in gastric media and control release for up to 48 h at an intestinal pH of 6.8. Weibull's model correlated better with release data and b parameter (0.79) indicated that the release process was driven by a combination of Fickian diffusion and Case II transport, indicating that both diffusion and swelling/polymer chains relaxation are processes that contribute equally to control drug release rates. Beads and isolated polymers were observed to be safe for Caco-2 and HT29-MTX intestinal cell lines. RES encapsulation into the beads allowed for an expressive reduction of drug permeation in an in vitro triple intestinal model. This feature, associated with low RES release rates in acidic media, can favor targeted drug delivery from the beads in the colon, a promising behavior to improve the local activity of RES.

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El aguacate es uno de los frutos de importancia económica en Colombia que presenta pérdidas en post cosecha. El objetivo de esta investigación fue evaluar el efecto de un recubrimiento comestible a base de gelana de alto (GAA) y bajo acilo (GBA), sobre la calidad post cosecha del aguacate (Persea americana cv. "Hass"), almacenado durante nueve semanas. Para la elaboración de los recubrimientos, se utilizó un diseño factorial 2³, donde los factores fueron las concentraciones de GAA (0,30 y 0,60% p/v), GBA (0,30 y 0,60% p/v) y glicerol (GLI) (8,0 y 12% v/v); como agente antimicrobiano, se utilizó extracto acuoso de Toronjil (Melissa officinalis L), por ser un aditivo natural. Se evaluaron propiedades, como la firmeza, la pérdida de humedad, el pH y los sólidos solubles totales (SST), durante almacenamiento. Finalmente, para la estimación del periodo de vida útil, se empleó la ecuación de Monod Hinshelwood, previo modelado de los datos, con ayuda de la ecuación de Baranyi y Roberts. Los resultados indicaron que la aplicación de recubrimientos comestibles de goma gelana, conteniendo bajas concentraciones de glicerol, disminuye significativamente (P<0,05) la pérdida de firmeza, de humedad, de sólidos solubles y evitan grandes modificaciones del pH, manteniendo la calidad del aguacate, alargando la vida útil.

Avocado is one of the fruits of economic importance in Colombia. However, it presents losses mainly during the post-harvest period. The aim of this research was to evaluate the effect of an edible coating based on high acyl (HAG) and low acyl gellan (LAG) on post-harvest avocado quality (Persea americana cv. "Hass") stored during nine weeks. A factorial design 2³ was employed for the biofilm preparation, where the factors were concentrations of HAG (0.30 and 0.60% w/v), LAG (0.30 and 0.60% w/v) and glycerol (GLY v/v). As antimicrobial aqueous extract of lemon balm (Melissa officinalis L) was used. Properties such as firmness, moisture loss, pH, total soluble solids (TSS) during storage were evaluated. Finally, for the microbiological shelf life estimation the Hinshelwood Monod equation was applied previous data modeling using the Baranyi and Roberts model. The results indicated that the application of edible coatings based on gellan gum containing low concentrations of glycerol reduces the loss of firmness, moisture, soluble solids and prevent large changes in pH, maintaining the quality of avocado and extend its shelf life.

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The retrogradation of high amylose starch (5% or 10%), by isothermal cycles at 4°C (method 1) or by alternating thermal cycles (method 2) was efficient and promoted important structural modifications. Hydrogels of gellan gum and starch retrograded blends, containing or not ketoprofen, were prepared by ionic and dual cross-linking, at different concentrations of polymer and cross-linkers, and characterized by texture and rheological analysis, X-ray diffraction and morphological analysis. The ionic cross-linking and starch retrograded by method 1 contributed to the improvement of hardness and cohesiveness of hydrogels while the dual cross-linking and starch retrograded by method 2 favored the adhesiveness. The rising of polymer concentration lead to the improvement of all mechanical parameters. Rheological data demonstrated that non-cross-linked dispersions showed a behavior of weak gels and the cross-linked hydrogels presented a predominantly elastic behavior (G'≫G″), peculiar of strong gels. X-ray diffraction, rheological data and the scanning electron microscopy (FEG-SEM) revealed that the increase of polymers and cross-linkers concentration and the presence of drug resulted in stronger and more stable tridimensional structures. The suitable adhesiveness and high strength and elasticity of hydrogels H253IC-KT, H255IC-KT, H21053DC-KT and H21055DC-KT make them more promising materials for the design of mucoadhesive drug delivery systems.

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O tratamento farmacológico de patologias bucais é conduzido, geralmente, por via de adminis-tração local. No entanto, devido ao pouco tempo de permanência do fármaco no local de ação, esse tratamento pode ser bastante comprometido. Assim, este trabalho teve por objetivo o de-senvolvimento de formas farmacêuticas que proporcionem a liberação local de triancinolona na cavidade oral. Foram produzidos filmes e comprimidos mucoadesivos a partir de polímeros naturais como gelana e pectina. Os filmes bucais foram preparados por meio de evaporação do solvente (solvent casting) utilizando diferentes quantidades de polímeros. As matérias-primas e os filmes foram caracterizados fisico quimicamente utilizando espectroscopia vibracional (in-fravermelho com transformada de Fourier e Raman) e difração de raios X. As propiedades físicas e mecânicas dos filmes também foram avaliadas. Além disso, realizou-se os ensaios de mucoadesividade e de dissolução do fármaco. Os comprimidos foram preparados por com-pressão direta usando como base os polímeros naturais. Diferentes parâmetros em relação as misturas e as formulações foram avaliados tais como as propriedades de fluxo dos pós consti-tuintes, peso médio, dureza, friabilidade e desintegração. Em relação aos filmes bucais, estes foram obtidos com sucesso através de um método simples, sem a utilização de agentes reticu-lantes, ácidos ou solventes orgânicos. Todos apresentaram bons resultados nas propriedades avaliadas, no entanto as formulações com quantidades intermediarias de polímeros foram as melhores. Dentre as formulações de comprimidos preparadas, apenas 4 apresentaram boas ca-racterísticas, no entanto, os resultados dos ensaios de dissolução mostraram que estas formula-ções têm capacidade de agir como sistema de liberação controlada de fármacos.

Pharmacological treatment of oral pathologies is usually conducted by local administration. However, due to the short time the drug stays in the site of action, this treatment can be quite compromised. Thus, the objective of this work was to develop pharmaceutical forms that pro-vide the local release of triamcinolone in the oral cavity. Mucoadhesive films and tablets were made from natural polymers such as gellan and pectin. The buccal films were prepared by sol-vent casting using different amounts of polymers. The raw materials and films were characte-rized physically chemically using vibrational spectroscopy (FTIR and Raman) and X-ray diffraction. The physical and mechanical properties of the films were also evaluated. In addi-tion, the mucoadhesive and drug dissolution tests were performed. The tablets were prepared by direct pressing with the natural polymers. Different parameters in relation to mixtures and formulations were evaluated such as the flow properties of the constituent powders, average weight, hardness, friability and disintegration. In relation to oral films, these were successfully obtained by a simple method, without the use of crosslinking agents, acids or organic solvents. All presented good results in the evaluated properties, however the formulations with interme-diate amounts of polymers were the best. Among the tablet formulations prepared, only 4 sho-wed good characteristics, however, the dissolution test results showed that these formulations have the ability to act as a controlled drug delivery system.

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O tratamento farmacológico de patologias bucais é conduzido, geralmente, por via de administração local. No entanto, devido ao pouco tempo de permanência do fármaco no local de ação, esse tratamento pode ser bastante comprometido. Assim, este trabalho teve por objetivo o desenvolvimento de formas farmacêuticas que proporcionem a liberação local de triancinolona na cavidade oral. Foram produzidos filmes e comprimidos mucoadesivos a partir de polímeros naturais como gelana e pectina. Os filmes bucais foram preparados por meio de evaporação do solvente (solvent casting) utilizando diferentes quantidades de polímeros. As matérias-primas e os filmes foram caracterizados fisico quimicamente utilizando espectroscopia vibracional (in-infravermelho com transformada de Fourier e Raman) e difração de raios X. As propriedades físicas e mecânicas dos filmes também foram avaliadas. Além disso, realizou-se os ensaios de mucoadesividade e de dissolução do fármaco. Os comprimidos foram preparados por com-pressão direta usando como base os polímeros naturais. Diferentes parâmetros em relação as misturas e as formulações foram avaliados tais como as propriedades de fluxo dos pós constituintes, peso médio, dureza, friabilidade e desintegração. Em relação aos filmes bucais, estes foram obtidos com sucesso através de um método simples, sem a utilização de agentes reticulantes, ácidos ou solventes orgânicos. Todos apresentaram bons resultados nas propriedades avaliadas, no entanto as formulações com quantidades intermediarias de polímeros foram as melhores. Dentre as formulações de comprimidos preparadas, apenas 4 apresentaram boas características, no entanto, os resultados dos ensaios de dissolução mostraram que estas formulações têm capacidade de agir como sistema de liberação controlada de fármacos

Pharmacological treatment of oral pathologies is usually conducted by local administration. However, due to the short time the drug stays in the site of action, this treatment can be quite compromised. Thus, the objective of this work was to develop pharmaceutical forms that pro-vide the local release of triamcinolone in the oral cavity. Mucoadhesive films and tablets were made from natural polymers such as gellan and pectin. The buccal films were prepared by sol-vent casting using different amounts of polymers. The raw materials and films were characte-rized physically chemically using vibrational spectroscopy (FTIR and Raman) and X-ray diffraction. The physical and mechanical properties of the films were also evaluated. In addi-tion, the mucoadhesive and drug dissolution tests were performed. The tablets were prepared by direct pressing with the natural polymers. Different parameters in relation to mixtures and formulations were evaluated such as the flow properties of the constituent powders, average weight, hardness, friability and disintegration. In relation to oral films, these were successfully obtained by a simple method, without the use of crosslinking agents, acids or organic solvents. All presented good results in the evaluated properties, however the formulations with interme-diate amounts of polymers were the best. Among the tablet formulations prepared, only 4 sho-wed good characteristics, however, the dissolution test results showed that these formulations have the ability to act as a controlled drug delivery system

Assuntos

RESUMO

Mixtures of gellan gum (GL) and a xyloglucan (XGJ) extracted from Hymenaea courbaril seeds were prepared in a solution of 0.15 mol L(-1) NaCl. Rheology measurements revealed that 2.4 g L(-1) pure GL formed a brittle hydrogel, and GL-XGJ blends showed improved pseudoplastic character with higher XGJ contents. SAXS analyses showed that the Rg dimensions ranged from 1.3 to 4.9 nm, with larger values occurring as the amount of XGJ increased, and diffusion tests indicated that better diffusion of methylene blue dye was obtained in the network with a higher XGJ content. AFM topographic images of the films deposited onto mica revealed fewer heterogeneous surfaces with increased XGJ contents. The water contact angle revealed more hydrophobic character on all of the films, and the wettability decreased with increasing amounts of XGJ. Therefore, the demonstrated benefit of using XGJ blends is the production of a soft material with improved interface properties.

Assuntos

RESUMO

Sodium alginate (SA) at 2% (w/v) and low acylated gellan gum (LAG) at 0.2% (w/v) were used to microencapsulate Lactobacillus helveticus and Lactobacillus delbrueckii spp lactis by employing the internal ionic gelation technique through water-oil emulsions at three different stirring rates: 480, 800 and 1200 rpm. The flow behavior of the biopolymer dispersions, the activation energy of the emulsion, the microencapsulation efficiency, the size distribution, the microcapsules morphology and the effect of the stirring rate on the culture viability were analyzed. All of the dispersions exhibited a non-Newtonian shear-thinning flow behavior because the apparent viscosity decreased in value when the shear rate was increased. The activation energy was calculated using the Arrhenius-like equation; the value obtained for the emulsion was 32.59 kJ/mol. It was observed that at 400 rpm, the microencapsulation efficiency was 92.83%, whereas at 800 and 1200 rpm, the stirring rates reduced the efficiency to 15.83% and 4.56%, respectively, evidencing the sensitivity of the microorganisms to the shear rate (13.36 and 20.05 s(-1)). Both optical and scanning electron microscopy (SEM) showed spherical microcapsules with irregular topography due to the presence of holes on its surface. The obtained size distribution range was modified when the stirring rate was increased. At 400 rpm, bimodal behavior was observed in the range of 20-420 µm; at 800 and 1200 rpm, the behavior became unimodal and the range was from 20 to 200 µm and 20 to 160 µm, respectively.

Assuntos