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A common challenge in hydrogel-based delivery systems is the premature release of low molecular weight encapsulates through diffusion or swelling and reduced cell viability caused by the low pH in gastric conditions. A second biopolymer, such as chitosan, can be incorporated to overcome this. Chitosan is usually associated with colonic drug delivery systems. We intended to formulate chitosan-coated pectin beads for use in delaying premature release of the encapsulate under gastric conditions but allowing release through disintegration under intestinal conditions. The latter is of utmost importance in delivering most functional food ingredients. Therefore, this study investigated the impact of formulation and process conditions on the size, sphericity, and dissolution behavior of chitosan-coated hydrogel beads prepared by interfacial coacervation. The size and sphericity of the beads depend on the formulation and range from approximately 3 to 5 mm and 0.82 to 0.95, respectively. Process conditions during electro-dripping may be modulated to tailor bead size. Depending on the voltage, bead size ranged from 1.5 to 4 mm. Confocal laser scanning microscopy and scanning electron microscopy confirmed chitosan shell formation around the pectin bead. Chitosan-coated beads maintained their size and shape in simulated gastric fluid but experienced structural damage in simulated intestinal fluid. Therefore, they represent a novel delivery system for functional food ingredients.
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Amphiphilic copolymers (ACs) are versatile systems with self-assembling and aggregating properties, enabling the formation of nanomaterials (NMs) such as micelles, vesicles, nanocapsules, and nanogels. These materials have been extensively explored for the delivery of various drugs and active compounds, enhancing the solubility and permeation of poorly water-soluble drugs into skin tissue. This improvement facilitates the treatment of skin diseases, including chronic conditions like cancer, as well as infections caused by bacteria, fungi, and viruses. This review summarizes recent applications of ACs in skin treatment, with a particular focus on their use in anti-cancer drug therapy. It covers the synthesis, classification, and characterization of ACs using various experimental techniques. Additionally, it discusses recent research on different drug delivery pathways using ACs, including encapsulation efficiency, release behavior, characteristics, applications, and responses to various chemical and physical stimuli (both in vivo and in vitro). Furthermore, this review provides a comprehensive analysis of the effects of ACs NMs on several skin diseases, highlighting their potential as alternative treatments.
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Producing food in quantity and quality to meet the growing population demand is a challenge for the coming years. In addition to the need to improve the use and efficiency of conventional agricultural inputs, we face climate change and disparity in access to food. In this context, creating innovative, efficient, and ecologically approaches is necessary to transform this global scenario. Several delivery systems are being developed to encapsulate agrochemicals, aiming to improve the controlled release of active ingredients and protect them against environmental biotic and abiotic factors. Among these systems, hydrogel spheres are particularly notable for their ability to be fabricated from biodegradable materials, allowing the encapsulation of molecules, nanomaterials, and even organisms (e.g., bacteria and fungi). This review provides an overview of the latest progress in developing polysaccharide-based hydrogel spheres for agriculture. In addition, we describe methods for preparing hydrogel spheres and discuss the encapsulation and release of agricultural inputs in the field. Finally, we put hydrogel spheres into perspective and seek to highlight some current challenges in the field to spark new inspiration and improve the development of environmentally friendly and cost-effective delivery systems for the agricultural sector.
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Agricultura , Preparaciones de Acción Retardada , Hidrogeles , Polisacáridos , Hidrogeles/química , Agricultura/métodos , Polisacáridos/química , Agroquímicos/químicaRESUMEN
Novel thiomer/nanoclay nanocomposites based on a thiomer and montmorillonite (MMT) were prepared in order to obtain a mucoadhesive material with controlled release properties for its potential use as drug carrier. The thiomer was synthesized by immobilization of L-cysteine in alginate mediated by carbodiimide reaction and further characterized by FT-IR and Ellman's reaction. Nanocomposites with growing concentrations of thiomer and MMT were prepared and analyzed by XRD, TGA and TEM. Rheological behavior of nanocomposite in contact with mucin and intestinal mucus were studied as in vitro and in situ mucoadhesion approach, showing until â¼10-fold increasing in the complex viscosity and â¼27-fold in elastic modulus when the amount of thiomer is increased. Higuchi and Korsmeyer-Peppas kinetic models were evaluated in order to study the release of deltamethrin from nanocomposite films. Release profiles showed a retard in the migration of the drug influenced by the amount of MMT (P < 0.05). Diffusion coefficient (D) showed a significant decrease (P < 0.0001) when concentration of MMT is increased reaching D = 4.18 × 10-7 m2 h-1, which resulted â¼7-fold lower in comparison with formulation without MMT. This hybrid nanocomposite can be projected as a potential mucoadhesive drug carrier with controlled release properties.
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The treatment of recurrent genital herpes typically involves daily doses of acyclovir for extended periods. Additive manufacturing is an intriguing technique for creating personalised drug delivery systems, which can enhance the effectiveness of treatments for various diseases. The vaginal route offers a viable alternative for the systemic administration of drugs with low oral bioavailability. In this study, we produced different grades of thermoplastic polyurethane (TPU) filaments through hot-melt extrusion, with acyclovir concentrations of 0%, 10%, and 20% by weight. We used fused filament fabrication to manufacture matrix-based devices, including intrauterine devices and intravaginal rings. Our results, obtained through SEM, FTIR, and DSC analyses, confirm the successful incorporation of acyclovir into the matrix. Thermal analysis reveals that the manufacturing process alters the organization of the TPU chains, resulting in a slight reduction in crystallinity. In our in-vitro tests, we observed an initial burst release on the first day, followed by sustained release at reduced rates for up to 145 days, demonstrating their potential for long-term applications. Additionally, cytotoxicity analysis suggests the excellent biocompatibility of the printed devices, and biological assays show a remarkable 99% reduction in HSV-1 replication. In summary, TPU printed devices offer a promising alternative for long-term genital herpes treatment, with the results obtained potentially contributing to the advancement of pharmaceutical manufacturing.
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Simvastatin (SIM) is widely prescribed to treat hyperlipidemia, despite its limitations, such as a short half-life and low oral bioavailability. To overcome these drawbacks, the development of a controlled-release formulation is desirable. This study aims to develop a microparticulate system based on cellulose acetate (ACT) obtained from Agave sisalana Perrine to promote a controlled SIM release. SIM-loaded microparticles (SMP) were prepared using the solvent emulsification-evaporation method. Several parameters were evaluated, including particle size, surface charge, morphology, encapsulation efficiency, thermochemical characteristics, crystallinity, and in vitro release profile. ACT exhibited favorable flow properties after acetylation, with a degree of substitution values superior to 2.5, as confirmed by both the chemical route and H-NMR, indicating the formation of cellulose triacetate. The obtained SMP were spherical with an average size ranging from 1842 to 1857 nm, a zeta potential of -4.45 mV, and a high SIM incorporation efficiency (98%). Thermal and XRD analyses revealed that SIM was homogeneously dispersed into the polymeric matrix in its amorphous state. In vitro studies using dialysis bags revealed that the controlled SIM release from microparticles was higher under simulated intestinal conditions and followed the Higuchi kinetic model. Our results suggest that ACT-based microparticles are a promising system for SIM delivery, which can improve its bioavailability, and result in better patient compliance.
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Natural Rubber Latex (NRL) has shown to be a promising biomaterial for use as a drug delivery system to release various bioactive compounds. It is cost-effective, easy to handle, biocompatible, and exhibits pro-angiogenic and pro-healing properties for both soft and hard tissues. NRL releases compounds following burst and sustained release kinetics, exhibiting first-order release kinetics. Moreover, its pore density can be adjusted for tailored kinetics profiles. In addition, biotechnological applications of NRL in amblyopia, smart mattresses, and neovaginoplasty have demonstrated success. This comprehensive review explores NRL's diverse applications in biotechnology and biomedicine, addressing challenges in translating research into clinical practice. Organized into eight sections, the review emphasizes NRL's potential in wound healing, drug delivery, and metallic nanoparticle synthesis. It also addresses the challenges in enhancing NRL's physical properties and discusses its interactions with the human immune system. Furthermore, examines NRL's potential in creating wearable medical devices and biosensors for neurological disorders. To fully explore NRL's potential in addressing important medical conditions, we emphasize throughout this review the importance of interdisciplinary research and collaboration. In conclusion, this review advances our understanding of NRL's role in biomedical and biotechnological applications, offering insights into its diverse applications and promising opportunities for future development.
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Materiales Biocompatibles , Sistemas de Liberación de Medicamentos , Látex , Medicina Regenerativa , Goma , Humanos , Materiales Biocompatibles/química , Látex/química , Medicina Regenerativa/métodos , Goma/química , Cicatrización de Heridas/efectos de los fármacosRESUMEN
Probiotics have gained significant attention in recent years due to the growing awareness of physical health and well-being. However, maintaining high concentrations of probiotics throughout the product's shelf life and during the gastrointestinal tract is crucial for ensuring their health-promoting effects. After determining an optimal formulation through a fractional factorial model, this study optimizes probiotic Bacillus Clausii delivery through spray-drying microencapsulation using a novel maltodextrin-alginate-inulin (MDX-ALG-IN) formulation (optimized ratio: 7:2:1). Notably, this formulation exclusively comprises non-digestible carbohydrates, marking a novel approach in probiotic encapsulation. Achieving a high Product Yield (51.06 %) and Encapsulation Efficiency (80.53 %), the study employed SEM for morphological analysis, revealing an irregular form and extensive surface in dentations characteristic of maltodextrin involvement. With a low moisture content of 3.02 % (±0.23 %) and 90.52 % solubility, the powder displayed exceptional properties. Probiotic viability remained robust, surviving up to 60 % even after 180 days at 4 °C, 25 °C, and 37 °C. Thermal characterization unveiled microcapsule resilience, exhibiting a glass transition temperature (Tg) at 138.61 °C and a melting point of 177.28 °C. The study systematically addresses crucial aspects of microencapsulation, including formulation optimization, morphological characteristics, and powder properties. Notably, the MDX-ALG-IN microcapsules demonstrated stability in simulated gastrointestinal conditions, indicating potential application for supplements and complex food matrices. In summary, this research contributes to microencapsulation understanding, emphasizing the MDX-ALG-IN formulation's efficacy in preserving probiotic viability across production stages and simulated digestive processes.
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Favipiravir is currently approved for the treatment of the influenza virus and has shown encouraging results in terms of antiviral capacity in clinical studies against severe acute respiratory syndrome coronavirus 2. Favipiravir is a prodrug, where its favipiravir-ribofuranosyl-5B-triphosphate metabolite is capable of blocking RNA replication of the virus. However, the antiviral efficiency of favipiravir is limited by two factors: (i) low accumulation in plasma and rapid excretion/elimination post-administration and (ii) low conversion rate into the active metabolite. To tackle these problems, herein, we have designed new favipiravir analogues focusing on the replacement of the fluorine atom at the 6-position by halogen or hydrogen atoms and 3-O-functionalization with labile groups. The first type of functionalization seeks to increase the antiviral activity because of the better ability of the keto-tautomer as a function of the halogen, and it is hypothesized that the keto-tautomer tends to promote the formation of the ribofuranosyl-5B-triphosphate (RTP) metabolite. Meanwhile, the second type of functionalization seeks to promote lipophilicity and increase accumulation in cells. From the in vitro antiviral activity against two coronavirus models (bovine and human 229E), it was identified that the replacement did not improve the antiviral activity against both the models, which seems to be attributable to the low water solubility of these new 6-functionalized analogues. Meanwhile, with 3-O-functionalization, acetylation provided the most active compounds with higher half-maximal inhibitory concentration and selectivity than favipiravir, whereas benzylation/methanosulfonation yielded the least active compounds. In summary, acetylation is found to be a convenient functionalization to enhance the antiviral profile of favipiravir.
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Amidas , Antivirales , Animales , Bovinos , Humanos , Antivirales/farmacología , Acetilación , Relación Estructura-Actividad , Amidas/farmacología , HalógenosRESUMEN
Alginate is a biopolymer widely used on delivery systems when bioactive protection at acidic pH is required, while chitosan can enhance mucoadhesion and controlled release at alkaline pHs. In this work, alginate ionotropic gelation and electrostatic complexation to chitosan were evaluated concomitantly or in a two-step approach to improve the delivery properties of systems in different pHs. The effect of pH on alginate gelation and chitosan interactions were also evaluated. Alginate microspheres were prepared by ionotropic gelation in CaCl2 at different pH values (2.5 and 6.0) by extrusion. Complexation with chitosan was carried out during alginate ionotropic gelation (one-step approach) or after alginate gel formation (two-step approach). Alginate microparticles without chitosan showed larger pores and lower mechanical strength. Extruded microspheres at pH 6.0 were more stable to pH and showed smaller pores than the formed at pH 2.5. One-step production retained a large amount of bioactive at pH 7.0 and resulted in lower release at the pH of intestinal digestion. The two-step approach retained less amount of bioactive but confer more protection to the pH of the stomach phase and higher release in pH of the intestinal phase than one-step samples. These results indicate that the formation of alginate gels by ionotropic gelation followed by the complexation with chitosan (in two-step) is promising for the transport and delivery of bioactives into intestinal conditions, whereas the ionotropic gelation concomitantly to electrostatic complexation (one-step approach) is indicated to the delivery of bioactives into lower pH environments.
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Quitosano , Sistemas de Liberación de Medicamentos , Sistemas de Liberación de Medicamentos/métodos , Quitosano/química , Alginatos/química , Concentración de Iones de Hidrógeno , Tamaño de la PartículaRESUMEN
Controlled-release fertilizers have been increasingly used. This study aimed to evaluate and adapt new technologies applied via soil for sustainable coffee production, in order to generate information that contribute to the technical innovation of the crop for the Vale do Ribeira region. The experiment was set at UNESP, in Registro SP. The experimental design was in randomized blocks. The experiment consisted of eight treatments with four replications, with plots of six plants. Four doses (200, 300, 400 and 500 kg ha-1) of a mixed fertilizer 20-05-20 were used, with controlled release in six months, intended for coffee trees in formation and production, compared to the dose of 500 kg ha-1 of the conventional mixed fertilizer 20-05-20, ammonium sulfate and calcium nitrate with boron, in addition to a control treatment, which did not receive NPK fertilization. The cultivar used was 'Obatã IAC 1669' in 3.0 x 0.6 m spacing. The following characteristics were evaluated: number of plagiotropic branches, number of nodes of plagiotropic branches, stem diameter, plant height and yield, in two harvest periods, besides the surface chemical characteristic of the soil. Increasing the dose of the slow-release fertilizer leads to greater plant growth; the coffee plant presents a highly responsive behavior to the increase in fertilizer doses in relation to nitrogen, and the use of the slow-release fertilizer Agroblen (20-05-20) 100% and ammonium sulfate + SS + KCl allows greater yield.
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Background: Tarin, a lectin purified from Colocasia esculenta, promotes in vitro and in vivo immunomodulatory effects allied to promising anticancer and antimetastatic effects against human adenocarcinoma mammary cells. This makes this 47 kDa-protein a natural candidate against human breast cancer, a leading cause of death among women. Tarin encapsulated in pegylated nanoliposomes displays increased effectiveness in controlling the proliferation of a mammary adenocarcinoma lineage comprising MDA-MB-231 cells. Methods: The mechanisms enrolled in anticancer and antimetastatic responses were investigated by treating MDA-MB-231 cells with nano-encapsulated tarin at 72 µg/mL for up to 48h through flow cytometry and transmission electron microscopy (TEM). The safety of nano-encapsulated tarin towards healthy tissue was also assessed by the resazurin viability assay, and the effect of nanoencapsulated tarin on cell migration was evaluated by scratch assays. Results: Ultrastructural analyses of MDA-MB-231 cells exposed to nanoencapsulated tarin revealed the accumulation of autophagosomes and damaged organelles, compatible with autophagy-dependent cell death. On the other hand, the flow cytometry investigation detected the increased occurrence of acidic vacuolar organelles, a late autophagosome trait, along with the enhanced presence of apoptotic cells, activated caspase-3/7, and cell cycle arrest at G0/G1. No deleterious effects were observed in healthy fibroblast cells following tarin nanoencapsulated exposition, in contrast to reduced viability in cells exposed to free tarin. The migration of MDA-MB-231 cells was inhibited by nano-encapsulated tarin, with delayed movement by 24 h compared to free tarin. Conclusion: The nanoliposome formulation delivers tarin in a delayed and sustained manner, as evidenced by the belated and potent antitumoral and anti-migration effects on adenocarcinoma cells, with no toxicity to healthy cells. Although further investigations are required to fully understand antitumorigenic tarin mechanisms, the activation of both apoptotic and autophagic machineries along with the caspase-3/7 pathway, and cell cycle arrest may comprise a part of these mechanisms.
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Adenocarcinoma , Neoplasias de la Mama , Humanos , Femenino , Caspasa 3 , Línea Celular Tumoral , Apoptosis , Neoplasias de la Mama/patología , Adenocarcinoma/tratamiento farmacológico , Adenocarcinoma/metabolismo , AutofagiaRESUMEN
Agriculture will face the issue of ensuring food security for a growing global population without compromising environmental security as demand for the world's food systems increases in the next decades. To provide enough food and reduce the harmful effects of chemical fertilization and improper disposal or reusing of agricultural wastes on the environment, will be required to apply current technologies in agroecosystems. Combining biotechnology and nanotechnology has the potential to transform agricultural practices and offer answers to both immediate and long-term issues. This review study seeks to identify, categorize, and characterize the so-called smart fertilizers as the future frontier of sustainable agriculture. The conventional fertilizer and smart fertilizers in general are covered in the first section of this review. Another key barrier preventing the widespread use of smart fertilizers in agriculture is the high cost of materials. Nevertheless, smart fertilizers are widely represented on the world market and are actively used in farms that have already switched to sustainable technologies. The advantages and disadvantages of various raw materials used to create smart fertilizers, with a focus on inorganic and organic materials, synthetic and natural polymers, along with their physical and chemical preparation processes, are contrasted in the following sections. The rate and the mechanism of release are covered. The purpose of this study is to provide a deep understanding of the advancements in smart fertilizers during the last ten years. Trends are also recognized and studied to provide insight for upcoming agricultural research projects.
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The excessive application of pesticides and fertilizers has generated losses in biological diversity, environmental pollution, and harmful effects on human health. Under this context, nanotechnology constitutes an innovative tool to alleviate these problems. Notably, applying nanocarriers as controlled release systems (CRSs) for agrochemicals can overcome the limitations of conventional products. A CRS for agrochemicals is an eco-friendly strategy for the ecosystem and human health. Nanopesticides based on synthetic and natural polymers, nanoemulsions, lipid nanoparticles, and nanofibers reduce phytopathogens and plant diseases. Nanoproducts designed with an environmentally responsive, controlled release offer great potential to create formulations that respond to specific environmental stimuli. The formulation of nanofertilizers is focused on enhancing the action of nutrients and growth stimulators, which show an improved nutrient release with site-specific action using nanohydroxyapatite, nanoclays, chitosan nanoparticles, mesoporous silica nanoparticles, and amorphous calcium phosphate. However, despite the noticeable results for nanopesticides and nanofertilizers, research still needs to be improved. Here, we review the relevant antecedents in this topic and discuss limitations and future challenges.
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In recent years, polymeric materials have been gaining prominence in studies of controlled release systems to obtain improvements in drug administration. These systems present several advantages compared with conventional release systems, such as constant maintenance in the blood concentration of a given drug, greater bioavailability, reduction of adverse effects, and fewer dosages required, thus providing a higher patient compliance to treatment. Given the above, the present work aimed to synthesize polymeric matrices derived from polyethylene glycol (PEG) capable of promoting the controlled release of the drug ketoconazole in order to minimize its adverse effects. PEG 4000 is a widely used polymer due to its excellent properties such as hydrophilicity, biocompatibility, and non-toxic effects. In this work, PEG 4000 and derivatives were incorporated with ketoconazole. The morphology of polymeric films was observed by AFM and showed changes on the film organization after drug incorporation. In SEM, it was possible to notice spheres that formed in some incorporated polymers. The zeta potential of PEG 4000 and its derivatives was determined and suggested that the microparticle surfaces showed a low electrostatic charge. Regarding the controlled release, all the incorporated polymers obtained a controlled release profile at pH 7.3. The release kinetics of ketoconazole in the samples of PEG 4000 and its derivatives followed first order for PEG 4000 HYDR INCORP and Higuchi for the other samples. Cytotoxicity was determined and PEG 4000 and its derivatives were not cytotoxic.
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Controlled release devices (CRD) have been widely studied regarding their application in periodontal therapy. Therefore, the present study aims to evaluate the use and effectiveness of controlled-release devices in nonsurgical periodontal therapy through a systematic review. The research was carried out in six different databases, namely: Online Medical Literature Search and Analysis System (Medline-PubMed), Web of Science, Science Direct, Scopus, Scielo, and Google Scholar. The descriptors "Delayed-Action Preparation," "Therapeutics," and "Periodontitis," were used with their EntryTerms and connected through the Boolean operators AND and OR. A total of 2847 studies were found, and after applying the Preferred Reporting Items for Systematic Reviews and Meta-Analyses checklist flowchart, 34 were selected using the eligibility criteria. After that, the qualitative results were tabulated and the risk of bias in each of them was evaluated. It can be observed that the use of CRD presents itself as a successful alternative for adjuvant treatment to periodontal therapy, a fact due to its availability and local concentration in the crevicular fluid. However, further clinical research is still needed to develop devices that are effective, with an easy and quick application, as well as available at a good cost-benefit ratio.
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INTRODUCTION: Skin cancer is the most common form of cancer worldwide, with increasing incidence rates in recent years. Although conventional chemotherapy and radiation therapy have been used for its treatment, these therapies have several limitations such as lack of selectivity and significant side effects. Targeted nanocarriers have emerged as a promising approach for the treatment of skin cancer. AREAS COVERED: This review article provides an overview of targeted nanocarriers for skin cancer treatment. It covers the various types of targeted nanocarriers, including liposomes, polymeric nanoparticles, dendrimers, and inorganic nanoparticles. EXPERT OPINION: There are still several challenges that need to be addressed before the clinical translation of targeted nanoparticles, such as optimization of their properties, development of reliable and robust characterization methods, and evaluation of their safety and efficacy in clinical trials. Another key aspect for the advancement of these studies is the need to improve regulatory aspects related to the toxicity and regulation of nanomedicines targeting skin cancer. Overall, targeted nanocarriers hold great potential for the development of safe and effective treatments for skin cancer, which can contribute to a better prognosis and overall patients' life quality.
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Nanopartículas , Neoplasias Cutáneas , Humanos , Portadores de Fármacos , Sistemas de Liberación de Medicamentos , Neoplasias Cutáneas/tratamiento farmacológico , Piel , LiposomasRESUMEN
Aromatic plants represent about 0.7% of all medicinal plants. The most common are peppermint (main active ingredient: menthol) and chamomile (main active ingredient: luteolin), which are usually consumed in "tea bags" to make infusions or herbal teas. In this study, menthol and luteolin encapsulates using different hydrocolloids were obtained to replace the conventional preparation of these beverages. Encapsulation was carried out by feeding an infusion of peppermint and chamomile (83% aqueous phase = 75% water - 8% herbs in equal parts, and 17% dissolved solids = wall material in 2:1 ratio) into a spray dryer (180 °C-4 mL/min). A factorial experimental design was used to evaluate the effect of wall material on morphology (circularity and Feret's diameter) and texture properties of the powders using image analysis. Four formulations using different hydrocolloids were evaluated: (F1) maltodextrin-sodium caseinate (10 wt%), (F2) maltodextrin-soy protein (10 wt%), (F3) maltodextrin-sodium caseinate (15 wt%), and (F4) maltodextrin-soy protein (15 wt%). The moisture, solubility, bulk density, and bioavailability of menthol in the capsules were determined. The results showed that F1 and F2 presented the best combination of powder properties: higher circularity (0.927 ± 0.012, 0.926 ± 0.011), lower moisture (2.69 ± 0.53, 2.71 ± 0.21), adequate solubility (97.73 ± 0.76, 98.01 ± 0.50), and best texture properties. Those suggest the potential of these powders not only as an easy-to-consume and ecofriendly instant aromatic beverage but also as a functional one.
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Curcumin (CUR) is one natural bioactive compound acknowledged for diverse therapeutic activities, but its use is hindered by its poor bioavailability, fast metabolism, and susceptibility to pH variations and light exposure. Thus, the encapsulation in poly(lactic-co-glycolic acid), or PLGA, has been successfully used to protect and enhance CUR absorption in the organism, making CUR-loaded PLGA nanoparticles (NPs) promising drug delivery systems. However, few studies have focused beyond CUR bioavailability, on the environmental variables involved in the encapsulation process, and whether they could help obtain NPs of superior performance. Our study evaluated pH (3.0 or 7.0), temperature (15 or 35 °C), light exposure, and inert atmosphere (N2) incidence in the encapsulation of CUR. The best outcome was at pH 3.0, 15 °C, without light incidence, and without N2 usage. This best nanoformulation showed NP size, zeta potential, and encapsulation efficiency (EE) of 297 nm, -21 mV, and 72%, respectively. Moreover, the CUR in vitro release at pH values 5.5 and 7.4 suggested different potential applications for these NPs, one of which was demonstrated by the effective inhibition of multiple bacteria (i.e., Gram-negative, Gram-positive, and multi-resistant) in the minimal inhibition concentration assay. Besides, statistical analyses confirmed a significant impact of temperature on the NP size; in addition, temperature, light, and N2 affected the EE of CUR. Thus, the selection and control of process variables resulted in higher CUR encapsulation and customizable outcomes, ultimately enabling more economical processes and providing future scale-up guidelines.
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Curcumina , Nanopartículas , Curcumina/farmacología , Curcumina/química , Copolímero de Ácido Poliláctico-Ácido Poliglicólico , Glicoles , Sistemas de Liberación de Medicamentos , Nanopartículas/química , Tamaño de la Partícula , Portadores de Fármacos/químicaRESUMEN
Nifedipine (NIFE) is a calcium channel blocker drug used to treat cardiovascular diseases, angina, and hypertension. However, NIFE is photolabile, has a short biological half-life, low aqueous solubility, and undergoes an intense first-pass effect, compromising its oral bioavailability. Thus, this study aimed to develop NIFE-loaded nanocapsules for sublingual administration. Nanocapsule suspensions of Eudragit® RS100 and medium chain triglycerides containing NIFE were prepared by the interfacial deposition of preformed polymer technique. The developed formulations showed particle size around 170 nm, polydispersity index below 0.2, positive zeta potential, and acid pH. The NIFE content was 0.98 ± 0.03 mg/mL, and the encapsulation efficiency was 99.9%. The natural light photodegradation experiment showed that the nanocapsules were able to provide NIFE photoprotection. The nanocapsules reduced the cytotoxicity of NIFE and showed no genotoxic effects in the Allium cepa model. Through the HET-CAM test, the formulations were classified as non-irritating. The developed nanocapsule suspension demonstrated a controlled release of NIFE and mucoadhesive potential. The in vitro permeation assay showed that the nanocapsules favored the NIFE permeation to the receptor compartment. In addition, the nanocapsules provided greater drug retention in the mucosa. Thus, the development of polymeric nanocapsule suspensions showed that this system could be a promising platform for NIFE sublingual administration.