Formulation and performance evaluation of emulgel platform for combined skin delivery of curcumin and propolis.

The environment can modify the physiology and body protective function of the skin. Propolis (PRP) and curcumin (CUR) possess important antioxidant and antimicrobial properties, and they can be administered in a combined way and using photodynamic therapy (PDT). Emulgels can control drug release due to the physicochemical properties of the gel and the emulsion. They constitute a good strategy for achieving an improved platform for the combined delivery of PRP and CUR. There are no other studies of emulgels composed of PRP and CUR and their performance as antimicrobial and skin healing using or not PDT. This study aimed to investigate the effect of Carbopol 934 P (C934P), 974 P (C974P) or polycarbophil (PC) on physicochemical stability, antioxidant activity, drug release profile, antimicrobial activity, and ex vivo skin permeation and retention of emulgels containing PRP and CUR. Formulations containing C974P or PC displayed improved stability and antioxidant activity. They displayed activity against Staphylococcus aureus and modified (extended) drug release, governed mainly by non-Fickian anomalous transport. C974P and PC resulted in improved emulgels for combined CUR and PRP delivery, allowing the drugs to cross the stratum corneum, and permeate the epidermis, reaching the dermis. The selected emulgels are candidates for further studies to prove their action and benefits to skin health.

Nutrient intake, digestibility and ruminal characteristics of lambs supplemented with probiotic.

The aim of this study was to evaluate the inclusion of different levels of probiotic in the diets of lambs, on ruminal characteristics, intake and digestibility of nutrients. The treatments were 0 (control group), 2, 4 and 6 g/day of probiotic doses, supplied orally and individually to the lambs. Four crossbred Santa Inês X Texel lambs were used, and the experimental design was a Latin square, with four treatments and four periods. Samples of diet, orts, feces, and ruminal fluid were collected from each animal. Intake and apparent digestibility variables were not different (p > 0.05) among the levels of probiotic evaluated. The average daily feed intake of lambs ranged from 1.27 to 1.28 kg of DM/day, and no significant differences (p > 0.05) were obtained between the levels of probiotics used in the diet. The percentage distribution of protozoa was not significant according to the different doses of probiotics used. A positive linear effect was obtained between the pH of the rumen fluid and the probiotic used, indicating that the highest pH values were obtained when the animals received the higher dose of 6 g probiotic; indicative that its use provides a ruminal environment closer to neutrality. The methylene blue reduction test in ruminal fluid samples did not differ between the different doses of probiotics used. The increasing levels of the probiotic in the diet of lambs are related to an increase in ruminal pH, without changing the levels of intake and digestibility of nutrients.

Molecular and genetic characterization of a large Brazilian cohort presenting hearing loss.

Hearing loss is one of the most common sensory defects, affecting 5.5% of the worldwide population and significantly impacting health and social life. It is mainly attributed to genetic causes, but their relative contribution reflects the geographical region's socio-economic development. Extreme genetic heterogeneity with hundreds of deafness genes involved poses challenges for molecular diagnosis. Here we report the investigation of 542 hearing-impaired subjects from all Brazilian regions to search for genetic causes. Biallelic GJB2/GJB6 causative variants were identified in 12.9% (the lowest frequency was found in the Northern region, 7.7%), 0.4% carried GJB2 dominant variants, and 0.6% had the m.1555A > G variant (one aminoglycoside-related). In addition, other genetic screenings, employed in selected probands according to clinical presentation and presumptive inheritance patterns, identified causative variants in 2.4%. Ear malformations and auditory neuropathy were diagnosed in 10.8% and 3.5% of probands, respectively. In 3.8% of prelingual/perilingual cases, Waardenburg syndrome was clinically diagnosed, and in 71.4%, these diagnoses were confirmed with pathogenic variants revealed; seven out of them were novel, including one CNV. All these genetic screening strategies revealed causative variants in 16.2% of the cases. Based on causative variants in the molecular diagnosis and genealogy analyses, a probable genetic etiology was found in ~ 50% of the cases. The present study highlights the relevance of GJB2/GJB6 as a cause of hearing loss in all Brazilian regions and the importance of screening unselected samples for estimating frequencies. Moreover, when a comprehensive screening is not available, molecular diagnosis can be enhanced by selecting probands for specific screenings.

In vitro modulation of gilthead seabream (Sparus aurata L.) leukocytes by Bacillus spp. extracellular molecules upon bacterial challenge.

Stimulation of the fish immune system using immunostimulants is an environmentally friendly strategy to minimize bacterial outbreaks in aquaculture. Different biological and synthetic immunostimulants can enhance non-specific innate immune responses by directly activating immune cells. An example are Bacillus spp., known for their immunostimulatory effects, although the exact mechanisms by which Bacillus spp. offer protection against diseases remains to be elucidated. Furthermore, most studies have focused on Bacillus spp. cells, while the immunostimulant effect of their extracellular metabolome, known to harbour biologically important metabolites, including antimicrobial molecules, has been scarcely evaluated. Here, we evaluated the in vitro immune-modulatory properties of extracellular extracts of three Bacillus spp. strains (B. subtilis FI314, B. vezelensis FI436 and B. pumilus FI464), previously isolated from fish-guts and characterized for their in vitro and in vivo antimicrobial activity against a wide range of fish pathogens. Bacillus spp. extracellular extracts did not affect immune cells viability, but remarkably increased pathogens' phagocytosis when seabream head-kidney leukocytes were challenged with Vibrio anguillarum and Edwardsiella tarda. All extracts significantly increased the engulfment of bacterial pathogens 1 h post-infection. Cells stimulated with the extracellular extracts showed an up-regulation of the expression of immune-relevant genes associated with inflammation, including IL-1ß, IL-6, and COX-2. In cells challenged with E. tarda, FI314 extracellular extract significantly increased the expression of IL-1ß, IL-6, and COX-2, while FI436 and FI464 significantly increased IL-6 expression. The results of this study revealed that the extracellular molecules from Bacillus spp. fish isolates improved the in vitro response of gilthead seabream immune cells and are thus promising candidates to act as immunostimulants, helping fish fight diseases.

Promising effect of propolis and a by-product on planktonic cells and biofilm formation by the main agents of human fungal infections.

Few antifungals available today are effective in treating biofilms. Thus, it is urgent to discover new compounds, such as natural products, that provide improvements to existing treatments or the development of new antifungal therapies. This study aimed to perform a comparative analysis between the green propolis extract (PE) and its by-product, a waste of propolis extract (WPE) through a screening with Candida sp., Fusarium sp. and Trichophyton sp. The antifungal property of PE and WPE was assessed by the minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC) determination in planktonic cells. The influence of both extracts on the inhibition of biofilm formation in these fungi was also tested. The WPE MIC and MFC values (68.75 to 275.0 µg/mL) were three to twelve times lower than the values obtained for PE (214.06 to 1712.5 µg/mL). PE was more efficient than WPE in inhibiting the biofilm initial phase, especially in C. albicans. Meanwhile, WPE had dose-dependent behavior for the three fungi, being more effective on filamentous ones. Both PE and WPE showed excellent antifungal activity on planktonic cells and demonstrated great efficacy for inhibiting biofilm formation in the three fungi evaluated.

Design of Quercetin-Loaded Natural Oil-Based Nanostructured Lipid Carriers for the Treatment of Bacterial Skin Infections.

The biological activity of natural plant-oil-based nanostructured lipid carriers (NPO-NLCs) can be enhanced by the encapsulation of bioactive compounds, and they in turn can improve topical delivery of the drugs. Quercetin (QR), a vital plant flavonoid, expresses antibacterial properties, and we recently showed that empty NPO-NLCs also have antimicrobial activity. The main objective of this study was to evaluate the synergetic effect of loading natural plant-oil-based nanostructured lipid carriers with quercetin (QR-NPO-NLCs) as a topical delivery system for the treatment of bacterial skin infections. Five nanostructured lipid carrier systems containing different oils (sunflower, olive, corn, coconut, and castor) were engineered. The particles' stability, structural properties, bioavailability, and antimicrobial activity were studied. NLCs with an average size of <200 nm and Z-potential of −40 mV were developed. Stable QR-NPO-NLCs were obtained with high encapsulation efficiency (>99%). The encapsulation of QR decreased cytotoxicity and increased the antioxidant effect of nanocarriers. An increase in antibacterial activity of the systems containing QR was demonstrated against Staphylococcus aureus. QR-NPO-NLCs could transport QR to an intranuclear location within HaCaT cells, indicating that QR-NPO-NLCs are promising candidates for controlled topical drug delivery.

Improving nutritional quality of unripe tomato through fermentation by a consortium of yeast and lactic acid bacteria.

BACKGROUND: Portugal is one of the main producers of industrial tomato and tomato paste, an important intermediate ingredient used in many added-value foods. The tomato processing industry rigorously selects the fruits by colour during mechanical harvest, picking only completely ripe fruits to produce high quality tomato paste. The latest available data shows that about 1.12 × 108 kg yr-1 of non-red/not-ripe tomatoes are left in the field, representing a major side product/field residue with great impact on the environment and for tomato producers. RESULTS: The aim of the work was to use fermentation by a consortium of yeast and lactic acid bacteria to improve the nutritional quality of unripe tomato paste. A consortium of Lactobacillus plantarum, Leuconostoc mesenteroides and Kluyveromyces marxianus was selected, producing an acidic paste with olive-like flavours after 4 days of fermentation. Nutritional characterization revealed a significant improvement (P < 0.05) in the content of ascorbic acid and antioxidant potential. In addition, ultrahigh-performance liquid chromatography tandem mass spectrometry (UHPLC-MS/MS) analysis showed that the fermented green tomato paste content in glycoalkaloid α-tomatine represents no hazard to the consumer. CONCLUSION: Therefore, the obtained fermented green tomato paste can be further used to produce new food products, such as salad dressings and sauces. © 2021 Society of Chemical Industry.

Thermosensitive gel based on cellulose derivative for topical delivery of propolis in acne treatment.

Thermosensitive bioadhesive formulations can display increased retention time, skin permeation, and improve the topical therapy of many drugs. Acne is an inflammatory process triggered by several factors like the proliferation of the bacteria Propionibacterium acnes. Aiming for a new alternative treatment with a natural source, propolis displays great potential due to its antibiotic, anti-inflammatory, and healing properties. This study describes the development of bioadhesive thermoresponsive platform with cellulose derivatives and poloxamer 407 for propolis skin delivery. Propolis ethanolic extract (PES) was added to the formulations with sodium carboxymethylcellulose (CMC) or hydroxypropyl methylcellulose (HPMC) and poloxamer 407 (Polox). The formulations were characterized as rheology, bioadhesion, and mechanical analysis. The selected formulations were investigated as in vitro propolis release, cytotoxicity, ex vivo skin permeation by Fourier Transform Infrared Photoacoustic Spectroscopy, and the activity against P. acnes. Formulations showed suitable sol-gel transition temperature, shear-thinning behavior, and texture profile. CMC presence decreased the cohesiveness and adhesiveness of formulations. Polox/HPMC/PES system displayed less cytotoxicity, modified propolis release governed by anomalous transport, skin permeation, and activity against P. acnes. These results indicate important advantages in the topical treatment of acne and suggest a potential formulation for clinical evaluation.

Bacillus spp. Inhibit Edwardsiella tarda Quorum-Sensing and Fish Infection.

The disruption of pathogen communication or quorum-sensing (QS) via quorum-quenching (QQ) molecules has been proposed as a promising strategy to fight bacterial infections. Bacillus spp. have recognizable biotechnology applications, namely as probiotic health-promoting agents or as a source of natural antimicrobial molecules, including QQ molecules. This study characterized the QQ potential of 200 Bacillus spp., isolated from the gut of different aquaculture fish species, to suppress fish pathogens QS. Approximately 12% of the tested Bacillus spp. fish isolates (FI). were able to interfere with synthetic QS molecules. Ten isolates were further selected as producers of extracellular QQ-molecules and their QQ capacity was evaluated against the QS of important aquaculture bacterial pathogens, namely Aeromonas spp., Vibrio spp., Photobacterium damselae, Edwardsiela tarda, and Shigella sonnei. The results revealed that A. veronii and E. tarda produce QS molecules that are detectable by the Chr. violaceum biosensor, and which were degraded when exposed to the extracellular extracts of three FI isolates. Moreover, the same isolates, identified as B. subtilis, B. vezelensis, and B. pumilus, significantly reduced the pathogenicity of E. tarda in zebrafish larvae, increasing its survival by 50%. Taken together, these results identified three Bacillus spp. capable of extracellularly quenching aquaculture pathogen communication, and thus become a promising source of bioactive molecules for use in the biocontrol of aquaculture bacterial diseases.

Higher Frequency of Fruit Intake Is Associated With a Lower Risk of Constipation in Hemodialysis Patients: A Multicenter Study.

OBJECTIVES: Constipation is a multifactorial gastrointestinal disorder commonly found in hemodialysis (HD) patients. In this multicenter cross-sectional study, we aimed to evaluate the prevalence and factors associated with constipation, including the frequency of dietary fiber intake. METHODS: HD patients from 4 dialysis clinics were invited. Participants answered a questionnaire which included Roma IV criteria to assess constipation status, use of medications, and lifestyle habits. A food frequency questionnaire with 7 response options on the main dietary fiber sources (fruits, vegetables, legumes, whole grains, and seeds) was also applied. Answers were transformed into a score to estimate the weekly intake frequency, and every score point corresponded to one time per week. Demographical and laboratory data were obtained from medical records. Univariate analysis was used to compare participants according to constipation status, and variables with P < .20 were included in the regression analysis model. RESULTS: Three hundred five HD patients were included (male: 51%; age: 52.2 ± 14.7 years old; HD vintage: 46 (19-82) months). Ninety-three participants had constipation (30.5%). Median (interquartile) food frequency questionnaire scores were as follows: fruits: 6 (2-14); vegetables: 6 (3-10); legumes: 3 (1-7); whole grain: 0 (0-1); and seeds: 0 (0-0). In univariate analysis, participants with constipation were significantly older, had lower literacy, higher prevalence of diabetes, and lower total beverage intake. The logistic regression analysis model also included body mass index, wheelchair need, sedentarism, fruits score, and seeds score (all with P < .20 in the univariate analysis). The independent predictors of constipation were diabetes (odds ratio = 1.96, 95% confidence interval 1.07-3.6, P = .03) and fruits intake score (odds ratio = 0.95, 95% confidence interval 0.91-0.99, P = .04). CONCLUSIONS: Almost one-third of the participants had constipation. The independent determinants of constipation were diabetes and lower frequency of fruit intake. Nutritional counseling to increase fiber intake can potentially decrease the prevalence of constipation in this population.

Development and physicochemical characterization of a new grass pea (Lathyrus sativus L.) miso.

BACKGROUND: Western consumers interest in Eastern fermented foods has been growing, due to their nutritional and healthy properties. In this study, new sweet misos and salty misos were produced using grass pea (Lathyrus sativus L.) - traditional Portuguese legume from local producers - to promote its consumption and preservation. The evolution of the new misos was evaluated in comparison to traditional miso (made from soybean), through analysis of the chemical composition, colour, texture and linear viscoelastic behaviour. RESULTS: Throughout the fermentation process, the ascorbic acid and phenolic compounds content - with important nutritional value - increased in all misos, mainly in misos produced using grass pea, besides, grass pea sweet miso presented the fastest evolution and darkest colour. The texture parameters (firmness and adhesiveness) of misos decreased over time: grass pea sweet miso showed the highest firmness reduction (51.63 N to 6.52 N) and soybean sweet miso the highest adhesiveness reduction (27.76 N to 3.11 N). Viscoelastic moduli also decreased, reflecting a reduction in the degree of internal structuring for all misos. However, grass pea misos presented more structured internal systems with faster maturation kinetics than soybean misos, for which stabilization started earlier. CONCLUSION: Two innovative misos were developed from grass pea. After 4 months, the texture parameters and viscoelastic moduli for grass pea misos, were similar to the control misos made from soybean, showing that grass pea can be used as a raw material to produce a sustainable miso with potentially healthy properties. © 2020 Society of Chemical Industry.

Industrial sustainability of microbial keratinases: production and potential applications.

Keratinases are proteolytic enzymes with a particular ability to cleave peptide bonds in keratin, and in other proteins. Due to their broad-spectrum of activity, keratinases are considered viable substitutes for chemical and thermal treatments of protein-rich industrial by-products. Among these protein residues, special attention has been given to keratinous materials (feathers, hair, horns, etc.), which disposal through harsh conditions methods, such as acid/alkaline hydrolysis or incineration, is not considered ecologically safe. Microbial keratinolytic enzymes allow for keratin degradation under mild conditions, resulting in keratin hydrolysates containing undamaged amino acids and peptides. In this review article, we offer perspectives on the relevance of these unique biocatalysts and their revolutionary ascent in industries that generate keratin-rich wastes. Additionally, we share insights for applications of keratinases and protein hydrolysates in agriculture, animal feed, cosmetics, phamaceuticals, detergent additives, leather processing, and others. Due to the scientific importance of keratinases and their potential use in green technologies, searching for bacterial and fungal species that efficiently produce these enzymes may contribute to the sustainability of industries.

Involvement of the Hsp70/TLR4/IL-6 and TNF-α pathways in delayed-onset muscle soreness.

Delayed-onset muscle soreness (DOMS) is a very common condition in athletes and individuals not accustomed to physical activity that occurs after moderate/high-intensity exercise sessions. The activation of microglial Toll-like receptor 4 (TLR4) in the spinal cord has been described to be important for the induction and maintenance of persistent pain. Based on that, we hypothesize that 70 kilodalton heat-shock protein (Hsp70), a mediator released by exercise, could activate microglial TLR4 in the spinal cord, releasing proinflammatory cytokines and contributing to the start of DOMS. In fact, we found that the knockout of TLR4, myeloid differentiation primary response 88 (MyD88), interleukin-6 (IL-6), or both tumor necrosis factor-α (TNF-α) receptor 1 and TNF-α receptor 2 in mice prevented the development of DOMS following acute aerobic exercise in contrast to the findings in male C57BL/6 wild-type mice. Furthermore, DOMS in exercised wild-type mice was also prevented after pre-treatment with microglia inhibitor, TLR4 antagonist, and anti-Hsp70 antibody. During exercise-induced DOMS, Hsp70 mRNA, TLR4 mRNA, and protein levels, as well as Iba-1 (a microglial marker), IL-6, and TNF-α protein levels, were increased in the muscle and/or spinal cord. Together, these findings suggest that Hsp70 released during exercise-induced DOMS activates the microglial TLR4/IL-6/TNF-α pathway in the spinal cord. Thus, the blockade of TLR4 activation may be a new strategy to prevent the development of DOMS before intense exercise.

Design and characterization of an organogel system containing ascorbic acid microparticles produced with propolis by-product.

This study aimed to prepare and characterize organogels containing microparticles of ascorbic acid (AA) obtained from propolis by-product. The formulations F1 (5% of microparticles) and F2 (10% of microparticles) were evaluated regarding rheological and textural properties, antioxidant and radical scavenging activity, in vitro release and cellular studies. The organogels showed plastic flow behavior and rheopexy. The textural parameters were within acceptable values for semisolid formulations. The antioxidant capacity of organogels F1 and F2 by the DPPH assay demonstrated IC50 ranging from 1523.59 to 1166.97 µg/mL, respectively. For the FRAP assay, the values found were 842.88 and 956.14 µmol of FSE/g formulation, respectively. Good scavenging activity against nitrogen species was observed. The concentration of 63 µg/mL did not present toxicity on HaCaT and HFF-1 cells. In vitro release profile of AA from organogels showed a slow pattern of drug release, mainly for F2. Therefore, the proposed organogel containing AA microparticles with propolis by-product matrix represents a promising platform for topical drug delivery with antioxidant effect.

Emulgels Containing Carbopol 934P and Different Vegetable Oils for Topical Propolis Delivery: Bioadhesion, Drug Release Profile, and Ex Vivo Skin Permeation Studies.

Topical administration can enable a more efficient therapy based on the improved bioavailability and patient compliance. Wounds and infections can lead to modifications of skin physiology and body protective function. Propolis (PRP) is utilized for skin protection and treatment. However, PRP extracts do not show suitable rheological characteristics and can cause irritation, pain, ulceration, and healing difficulties when they are administered on the harmed skin. Emulgels composed of Carbopol 934P (C934P) and different vegetable oils have been proposed for propolis extract release and may be a good strategy for topical delivery. The aim of this study was to investigate the bioadhesive properties, PRP release profile, skin permeation, and retention, by Franz's diffusion cell and photoacoustic spectroscopy (PS), of these emulgels. Formulations were composed of C934P and passion fruit oil (PF), sweet almond oil (SA), or andiroba oil (AO). PRP or by-product extracts were added to the systems, drug release profile was investigated, and porcine ear skin was utilized for analyses of bioadhesive properties, skin permeation, and retention. All formulations displayed similar bioadhesive force (0.05-0.07 N); PRP release was modified (prolonged), dependent on formulation composition, and mainly governed by diffusion. PS and analysis using diffusion cell showed that the systems could provide dermal permeation and retention, which was more effective for formulations containing AO. Considering the importance of propolis for many skin therapies, the emulgels containing AO for PRP delivery are worthy of biological studies and further clinical evaluation.

Generating electrical energy through urban solid waste in Brazil: An economic and energy comparative analysis.

The search for alternative energy sources and increasing concerns over the generation of municipal solid waste are two widely discussed themes in contemporary academic literature. A possible alternative for solving both of these problems is through electrical energy generation through the use of this waste material. Although this practice is encouraged by the Brazilian National Solid Waste Policy, energy production through such methods still requires improvement. Given these considerations, this study aims to evaluate the generation of electric energy from solid waste in three different systems (biogas from sanitary landfills; methanization of organic fraction in anaerobic digesters; and combustion in incinerators) through economic and energy analysis. Economic analysis was performed with the parameters Net Present Value and Levelized Cost of Electricity. Economic viability was only seen in the cases which considered landfill biogas energy recovery, demonstrating a need for incentives and support policies to enable technologies that are environmentally more advantageous than landfills.

Exome Sequencing Identifies a Novel Nonsense Mutation of MYO6 as the Cause of Deafness in a Brazilian Family.

We investigated 313 unrelated subjects who presented with hearing loss to identify the novel genetic causes of this condition in Brazil. Causative GJB2/GJB6 mutations were found in 12.7% of the patients. Among the familial cases (100/313), four were selected for exome sequencing. In one case, two novel heterozygous variants were found and were predicted to be pathogenic based on bioinformatics tools, that is, p.Ser906* (MYO6) and p.Arg42Cys (GJB3). We confirmed that this nonsense MYO6 mutation segregated with deafness in this family. Only the proband and her unaffected mother exhibited the GJB3 mutation, which is in the same amino acid of a known Erythrokeratodermia variabilis mutation. None of the patients exhibited this skin disease, but the proband exhibited a more severe hearing loss. Hence, the GJB3 mutation was considered to be a variant of uncertain significance. In conclusion, we described a novel nonsense MYO6 mutation that was responsible for the hearing loss in a Brazilian family. This mutation resides in the neck domain of myosin-VI after the motor domain. Thus, our data give further support for genotype-phenotype correlations, which state that when the motor domain of the protein is functioning, the hearing loss is milder and has a later onset. The three remaining families without mutations in the known genes suggest that there are still deafness genes to be revealed.

Chronic Sleep Restriction Impairs the Antitumor Immune Response in Mice.

OBJECTIVES: Sleep regulates immune function reciprocally and can affect the parameters that are directly involved in the immune response. Sleep deprivation is considered to be a stress-causing factor and is associated with impaired immune activity. It causes increased glucocorticoid concentrations by activating the hypothalamic-pituitary-adrenal axis; this can lead to a series of disorders that are associated with the prolonged or increased secretion of these hormones. The aim of this study was to evaluate the effects of sleep restriction (SR) on the development of pulmonary experimental metastasis and the modulation of the tumor immune response. METHODS: The SR protocol was accomplished by depriving C57BL/6 male mice of sleep for 18 h/day for 2, 7, 14, and 21 days. The modified multiple-platforms method was used for SR. RESULTS: The results showed that cytotoxic cells (i.e., natural killer [NK] and CD8+ T cells) were reduced in number and regulatory T cells were predominant in the tumor microenvironment. Sleep-restricted mice also exhibited a reduced number of dendritic cells in their lymph nodes, which may have contributed to the ineffective activation of tumor-specific T cells. Peripheral CD4+ and CD8+ T cells were also reduced in the sleep-restricted mice, thus indicating an immunosuppressive status. CONCLUSIONS: Sleep dep-rivation induces failure in the activity of cells that are im-portant to the tumor immune response, both in the tumor microenvironment and on the periphery. This leads to the early onset and increased growth rate of lung metastasis.

Thermal Magnetic Field Activated Propolis Release From Liquid Crystalline System Based on Magnetic Nanoparticles.

Intra-periodontal pocket drug delivery systems, such as liquid crystalline systems, are widely utilized improving the drug release control and the therapy. Propolis is used in the treatment of periodontal diseases, reducing the inflammatory and infectious conditions. Iron oxide magnetic nanoparticles (MNPs) can improve the treatment when an alternating external magnetic field (AEMF) is applied, increasing the local temperature. The aim of this study was to develop a liquid crystalline system containing MNPs for intra-periodontal pocket propolis release. MNPs were prepared using iron salts and the morphological, size, thermal, x-ray diffraction, magnetometry, and Mössbauer spectroscopy analyses were performed. Cytotoxicity studies using Artemia salina and fibroblasts were also accomplished. The systems were prepared using polyoxyethylene (10) oleyl ether, isopropyl myristate, purified water, and characterized by polarized optical microscopy, rheometry, and in vitro drug release profile using a periodontal pocket simulator apparatus. The antifungal activity of the systems was investigated against Candida spp. using an AEMF. MNPs displayed nanometric size, were monodisperse, and they displayed very low cytotoxicity. Microscopically homogeneous formulations were obtained displaying important physicochemical and biological properties. The system displayed prolonged release of propolis and important in vitro fungicide activity, which was increased when the AEMF was applied, indicating a potentially alternative therapy for the treatment of the periodontal disease.

Development and characterization of multiple emulsions for controlled release of Trichilia catigua (Catuaba) extract.

Considering the antioxidant activity of the Trichilia catigua extract (TCE), the aim of the current study was to develop and characterize W/O/W multiple emulsions containing different vegetable oils as a platform to deliver a TCE. The extract displayed antioxidant activity (IC50) of 4.59 µg/mL and total phenol content (TPC) of 50.84%. Formulations were prepared by the phase-inversion emulsification method and analyzed for morphological appearance, pH, conductivity, droplet size and distribution, content of active, rheological properties, in vitro release, skin permeation, and stability. Formulations prepared with canola oil were selected and displayed regular morphology, mean diameter 2.77 µm (without TCE), 3.07 µm with 0.5% and 3.23 µm with 1.0% TCE. Rheometry (flow) showed pseudoplastic behavior with minimal thixotropy for both systems. TCE could be released from emulsions containing 1.0% and 0.5% TCE in a controlled manner for 16 and 23 h, respectively. The emulsions allowed good retention of TCE in the skin (stratum corneum, epidermis, and dermis). In a 180-d assessment of accelerated chemical stability, TPC was more reduced for the emulsions at 40 °C; other parameters remained stable. Multiple emulsions containing TCE were developed, exhibited good characteristics, and may be considered for future investigations as anti-aging formulations for the skin.