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1.
Polymers (Basel) ; 16(13)2024 Jul 02.
Artigo em Inglês | MEDLINE | ID: mdl-39000753

RESUMO

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.

2.
Int J Biol Macromol ; 267(Pt 2): 131666, 2024 May.
Artigo em Inglês | MEDLINE | ID: mdl-38636755

RESUMO

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.


Assuntos
Materiais Biocompatíveis , Sistemas de Liberação de Medicamentos , Látex , Medicina Regenerativa , Borracha , Humanos , Materiais Biocompatíveis/química , Látex/química , Medicina Regenerativa/métodos , Borracha/química , Cicatrização/efeitos dos fármacos
3.
Heliyon ; 10(2): e24923, 2024 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-38304817

RESUMO

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.

4.
Arch Pharm (Weinheim) ; 357(1): e2300494, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-37853660

RESUMO

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.


Assuntos
Amidas , Antivirais , Animais , Bovinos , Humanos , Antivirais/farmacologia , Acetilação , Relação Estrutura-Atividade , Amidas/farmacologia , Halogênios
5.
Biosci. j. (Online) ; 40: e40004, 2024.
Artigo em Inglês | LILACS-Express | LILACS | ID: biblio-1567760

RESUMO

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.

6.
Food Res Int ; 175: 113737, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-38129047

RESUMO

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.


Assuntos
Quitosana , Sistemas de Liberação de Medicamentos , Sistemas de Liberação de Medicamentos/métodos , Quitosana/química , Alginatos/química , Concentração de Íons de Hidrogênio , Tamanho da Partícula
7.
Int J Nanomedicine ; 18: 6393-6408, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37954458

RESUMO

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.


Assuntos
Adenocarcinoma , Neoplasias da Mama , Humanos , Feminino , Caspase 3 , Linhagem Celular Tumoral , Apoptose , Neoplasias da Mama/patologia , Adenocarcinoma/tratamento farmacológico , Adenocarcinoma/metabolismo , Autofagia
8.
Sci Total Environ ; 904: 166729, 2023 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-37678530

RESUMO

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.

9.
Nanomaterials (Basel) ; 13(13)2023 Jun 29.
Artigo em Inglês | MEDLINE | ID: mdl-37446494

RESUMO

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.

10.
Polymers (Basel) ; 15(11)2023 May 30.
Artigo em Inglês | MEDLINE | ID: mdl-37299312

RESUMO

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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