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1.
Molecules ; 28(2)2023 Jan 04.
Artigo em Inglês | MEDLINE | ID: mdl-36677556

RESUMO

A study was conducted on selected physicochemical properties of blackberry jelly-like desserts (kissel) prepared from physically modified starches (with various degrees of inhibition) and chemically modified starches (with various degrees of cross-linking). The desserts were conventionally sweetened with saccharose (S) or, as a dietary alternative, xylitol (X). The characteristics of changes in the viscosity of the kissels as a function of temperature and time were determined. It was noted that regardless of the sweetener used, the viscosity of the kissels increased with the decreasing degree of inhibition (high < medium < low). Regardless of the kind of modification of the starch used for the preparation of the kissels and of the kind of sweetener, thixotropy was observed. Desserts prepared from inhibited starch with xylitol (CL + X) were characterised by the biggest range of their hysteresis loop. Progressing retrogradation was noted with the decrease in the temperature of the experiment (+20 °C and +4 °C). After 7 days of storage, kissels sweetened with saccharose were characterised by a low transparency, which may indicate retarded retrogradation; however, on day 28, the transparency significantly increased, exceeding the values of transmittance for samples sweetened with xylitol. The tendency towards syneresis was tested at +4 °C and -22 °C. The substitution of saccharose with xylitol only caused a slight modification of viscosity. Regardless of the sweetener used and of the level of starch inhibition, lower ranges of the hysteresis loop were noted (apart from CL + X) than in the case of kissels obtained from chemically modified starches. Distinctly lower values of kissel "aging" indices were noted in the case of samples obtained from inhibited starches, and their colour did not significantly differ in relation to the dessert prepared from native starch.


Assuntos
Rubus , Amido , Amido/química , Zea mays/química , Edulcorantes , Xilitol , Excipientes , Viscosidade , Sacarose
2.
Molecules ; 28(2)2023 Jan 13.
Artigo em Inglês | MEDLINE | ID: mdl-36677855

RESUMO

With the advent of nanotechnology, DNA molecules have been transformed from solely genetic information carriers to multifunctional materials, showing a tremendous potential for drug delivery and disease diagnosis. In drug delivery systems, DNA is used as a building material to construct drug carriers through a variety of DNA self-assembly methods, which can integrate multiple functions to complete in vivo and in situ tasks. In this study, ladder-shaped drug carriers are developed for drug delivery on the basis of a DNA nanoladder. We first demonstrate the overall structure of the nanoladder, in which a nick is added into each rung of the nanoladder to endow the nanoladder with the ability to incorporate a drug loading site. The structure is designed to counteract the decrement of stability caused by the nick and investigated in different conditions to gain insight into the properties of the nicked DNA nanoladders. As a proof of concept, we fix the biotin in every other nick as a loading site and assemble the protein (streptavidin) on the loading site to demonstrate the feasibility of the drug-carrying function. The protein can be fixed stably and can be extended to different biological and chemical drugs by altering the drug loading site. We believe this design approach will be a novel addition to the toolbox of DNA nanotechnology, and it will be useful for versatile applications such as in bioimaging, biosensing, and targeted therapy.


Assuntos
Nanoestruturas , Nanoestruturas/química , DNA/química , Nanotecnologia/métodos , Sistemas de Liberação de Medicamentos , Excipientes , Portadores de Fármacos
3.
PLoS One ; 18(1): e0279036, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-36656875

RESUMO

By forcing selection into response execution processes, the present mouse-tracking study investigated whether the ongoing process of response selection in the colour-word Stroop task is influenced by conflict and facilitation at both the level of response and stimulus. Mouse-tracking measures including partial errors provided credible evidence that both response and semantic conflict (i.e., distinct constituents of interference) contribute to the overall Stroop interference effect even after a response has been initiated. This contribution was also observed for the overall facilitation effect (that was credibly decomposed into response and semantic components in response times but not in mouse deviation measures). These results run counter to the dominant single-stage response competition models that currently fail to explain: 1) the expression of Stroop effects in measures of response execution and; 2) the composite nature of both interference and facilitation. By showing that Stroop effects-originating from multiple levels of processing-can cascade into movement parameters, the present study revealed the potential overlap between selection and execution process. It therefore calls for further theoretical efforts to account for when, where and under what conditions Stroop effects originating from different loci are controlled.


Assuntos
Excipientes , Semântica , Teste de Stroop , Tempo de Reação/fisiologia , Movimento
4.
Molecules ; 28(1)2023 Jan 02.
Artigo em Inglês | MEDLINE | ID: mdl-36615562

RESUMO

Photodetectors based on organic materials are attractive due to their tunable spectral response and biocompatibility, meaning that they are a promising platform for an artificial human eye. To mimic the photoelectric response of the human eye, narrowband spectrally-selective organic photodetectors are in great demand, and single-component organic photodetectors based on donor-acceptor conjugated molecules are a noteworthy candidate. In this work, we present single-component selective full-color organic photodetectors based on donor-acceptor conjugated molecules synthetized to mimic the spectral response of the cones and rods of a human eye. The photodetectors demonstrated a high responsivity (up to 70 mA/W) with a response time of less than 1 µs, which is three orders of magnitude faster than that of human eye photoreceptors. Our results demonstrate the possibility of the creation of an artificial eye or photoactive eye "prostheses".


Assuntos
Excipientes , Doadores de Tecidos , Humanos , Tempo de Reação
5.
Carbohydr Polym ; 302: 120394, 2023 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-36604072

RESUMO

The development of double encryption system enables information to switch reversibly between "False" and "True", which helps to ensure information security in the transmission process. Herein, a biomimetic cellulose nanofibre-based double information encryption sensor (CNF-DIES) with an excellent pH response and fluorescence colour-switching performance was prepared with fluorescein isothiocyanate and protoporphyrin IX modified acetylated cellulose nanofibres (ACNF) as the pH response switch and background, respectively. Interestingly, with the addition of cellulose, CNF-DIES can be regarded as both a dye and an ink binder, which can realize direct writing function. The fluorescein grafted to ACNF guaranteed the stability of writing and avoided the "coffee ring" phenomenon. The handwriting written by CNF-DIES processes excellent light/pH double encryption performance. Besides, the film prepared by CNF-DIES can realize high resolution fingerprint imaging. This work demonstrated a strategy for pH-responsive colour-tunable materials for sensors and double information encryption.


Assuntos
Celulose , Nanofibras , Biomimética , Diagnóstico por Imagem , Excipientes , Fluoresceína
6.
Food Res Int ; 163: 112118, 2023 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-36596087

RESUMO

Roasting is an important operation to produce attractive colors and distinctive flavors during the production of sesame oil. To investigate the contributions of macromolecules to the color and flavor during roasting sesame seeds, water-soluble polysaccharides (WSP) and chelator-soluble polysaccharides (CSP) sequentially extracted from sesame hull were mixed with sesame protein isolate (SPI) at different ratios (1:1, 1:2, and 2:1, w/w), then the mixtures were roasted at 180 °C for 35 min. Results showed that WSP, CSP, and SPI degraded approximately at 150 °C and SPI had the highest thermal stability. According to monosaccharide/amino acid analysis, glucose and galacturonic acid showed the highest reduction rates, as well as lysine and arginine. CSP + SPI mixtures showed greater reactivity than WSP + SPI mixtures, resulting in a darker color and many more Maillard reaction products. The predominant volatiles of roasted WSP/CSP + SPI mixtures were aldehydes and heterocyclic compounds identified by headspace solid-phase microextraction coupled with gas chromatography-mass spectrometry (HS-SPME/GC-MS). This work provides some new information about flavor and color development during roasting sesame seeds.


Assuntos
Sesamum , Sesamum/química , Sementes/química , Cromatografia Gasosa-Espectrometria de Massas , Excipientes , Óleo de Gergelim/química
7.
Food Res Int ; 163: 112123, 2023 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-36596089

RESUMO

This study fabricated a novel excipient emulsion by adding dark tea polysaccharides to improve the bioaccessibility of lycopene from tomatoes. Results indicated that addition of tea polysaccharides greatly increased the antioxidant activity of excipient emulsions. Additionally, tea polysaccharides markedly improved the physical stability of excipient emulsion when being mixed with tomato puree and passing through a simulated gastrointestinal tract, contributing to an increase in electrostatic and steric repulsion between the droplets. Besides, certain amount of tea polysaccharides (0.05 - 0.2 wt%) could increase the rate and extent of lipid digestion in tomato-emulsion mixtures. Finally, lycopene bioaccessibility was significantly increased (from 16.95 % to 26.21 %) when 0.1 wt% tea polysaccharides were included, which was mainly ascribed to the ability of tea polysaccharides to increase lipid digestion and reduce carotenoid oxidation within the gastrointestinal tract. These results suggest that well-designed excipient emulsions may increase carotenoids bioavailability in the complex food matrices.


Assuntos
Licopeno , Emulsões , Excipientes , Carotenoides , Suplementos Nutricionais/análise , Lipídeos , Chá
8.
Drug Deliv ; 30(1): 2162162, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-36587627

RESUMO

To design and evaluate hyaluronan-based cubosomes loaded with bromfenac sodium (BS) for ocular application to enhance the corneal permeation and retention in pterygium and cataract treatment. BS-loaded cubosomes were prepared by the emulsification method, employing 23 full factorial design using Design-Expert® software. Glycerol monoolein (GMO) and poloxamer 407 (P407) as lipid phase and polyvinyl alcohol (PVA) as stabilizer were the used ingredients. The optimized formulation (OBC; containing GMO (7% w/w), P407 (0.7% w/w) and PVA (2.5% w/w)) was further evaluated. OBC had an entrapment efficiency of 61.66 ± 1.01%, a zeta potential of -30.80 ± 0.61 mV, a mean particle size of 149.30 ± 15.24 nm and a polydispersity index of 0.21 ± 0.02. Transmission electron microscopy confirmed its cubic shape and excellent dispersibility. OBC exhibited high stability and no ocular irritation that was ensured by histopathology. Ex vivo permeation study showed a significant increase in drug deposition and permeability parameters through goat cornea, besides, confocal laser microscopy established the superior permeation capability of OBC, as compared to drug solution. In vivo pharmacokinetics in aqueous humor indicated higher AUC0-tlast (18.88 µg.h/mL) and mean residence time (3.16 h) of OBC when compared to the marketed eye drops (7.93 µg.h/mL and 1.97 h, respectively). Accordingly, hyaluronan-enriched cubosomes can be regarded as a promising carrier for safe and effective topical ocular delivery.


Assuntos
Córnea , Ácido Hialurônico , Benzofenonas , Bromobenzenos , Excipientes , Poloxâmero , Álcool de Polivinil , Tamanho da Partícula , Portadores de Fármacos
9.
J Indian Prosthodont Soc ; 23(1): 38-44, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-36588373

RESUMO

Aim: This study evaluated the color aging of two computer aided design/computer aided manufacturing (CAD/CAM) provisional materials of different compositions (polymethyl methacrylate and composite resin) after exposure to thermal aging and immersion in coffee for 3, 6, and 12 intraoral months. Setting and Design: The current in vitro study was conducted from September to December 2021 at the Craniofacial laboratory at the Saint Joseph University in Beirut, Lebanon. Materials and Methods: The shades of 2.0 mm thick, 10.0 mm in diameter disk shaped specimens of VITA CAD Temp® and Ceramill® TEMP were measured using the VITA Linearguide 3D MASTER® and a conversion table to extract the CIE LFNx01aFNx01bFNx01 values on a white background (n = 30). Statistical Analysis Used: The color differences ΔE at 3, 6, and 12 months were calculated and analyzed by repeated measures ANOVA followed by Bonferroni multiple comparisons, univariate analyses, and one sample t tests. Results: The mean ΔET1/T0, ΔET2/T0, and ΔET3/T0 values were significantly higher than the cutoff values for acceptability and perceptibility for the VITA CAD Temp® and the Ceramill® TEMP groups. In addition, the increase in ΔE overtime was significantly greater in the Ceramill® TEMP group compared to the VITA CAD Temp® group. Conclusions: The Ceramill® TEMP changed color more and faster than the VITA CAD Temp®. In addition, whether at 3, 6, or 12 months, the color variations of both materials are not only perceptible but also unacceptable compared to the initial shade.


Assuntos
Porcelana Dentária , Polimetil Metacrilato , Humanos , Teste de Materiais , Desenho Assistido por Computador , Excipientes
10.
J Mater Sci Mater Med ; 34(1): 8, 2023 Jan 11.
Artigo em Inglês | MEDLINE | ID: mdl-36630012

RESUMO

Mg-based biomaterials are commonly used as biodegradable orthopedic implants (e.g., bone regeneration applications). However, achieving high biocompatibility and corrosion resistance has remained a challenge to be tackled. In this work, to investigate various fabricated coatings (with and without pre- anodizing), five categories of samples are considered: (a) bare Mg alloy (Mg), (b) Anodized Mg alloy (Mg-A), (c) CS-coated Mg alloy (Mg-C), (d) CS-coated anodized Mg alloy (Mg-AC), and (e) CS-CNT-coated anodized Mg alloy (Mg-ACC). These samples were characterized by using Field Emission Scanning Electron Microscopes (FE-SEM), Energy Dispersive Spectroscopy (EDS), Fourier Transform Infrared Spectroscopy (FT-IR), and Raman Spectroscopy. The adhesion within the coated samples was compared. Then, the effects of the coatings were evaluated by comparing wettability, corrosion behavior, and biocompatibility for bare and coated samples. The adhesion test showed that the coatings exhibited higher adhesion for Mg-AC and Mg-ACC compared to Mg-C. Desired wettability was achieved as the contact angles of coated samples were in the range of 55°- 65°. Electrochemical impedance and polarization as well as immersion tests showed higher corrosion resistance for coated samples. The composite coated sample showed improved cell adhesion since the osteoblast cells covered almost the entire surface of the sample. Moreover, osteoblast cell viability for the sample was around 40% higher than that of the bare sample.


Assuntos
Quitosana , Nanotubos de Carbono , Espectroscopia de Infravermelho com Transformada de Fourier , Magnésio/química , Materiais Revestidos Biocompatíveis/química , Excipientes , Ligas/química , Corrosão
11.
Sci Rep ; 13(1): 571, 2023 Jan 11.
Artigo em Inglês | MEDLINE | ID: mdl-36631519

RESUMO

Recently, biocompatible optical sources have been surfacing for new-rising biomedical applications, allowing them to be used for multi-purpose technologies such as biological sensing, optogenetic modulation, and phototherapy. Especially, vertical-cavity surface-emitting laser (VCSEL) is in the spotlight as a prospective candidate for optical sources owing to its low-driving current performance, low-cost, and package easiness in accordance with two-dimensional (2D) arrays structure. In this study, we successfully demonstrated the actualization of biocompatible thin-film 930 nm VCSELs transferred onto a Polydimethylsiloxane (PDMS) carrier. The PDMS feature with biocompatibility as well as biostability makes the thin-film VCSELs well-suited for biomedical applications. In order to integrate the conventional VCSEL onto the PDMS carrier, we utilized a double-transfer technique that transferred the thin-film VCSELs onto foreign substrates twice, enabling it to maintain the p-on-n polarity of the conventional VCSEL. Additionally, we employed a surface modification-assisted bonding (SMB) using an oxygen plasma in conjunction with silane treatment when bonding the PDMS carrier with the substrate-removed conventional VCSELs. The threshold current and maximum output power of the fabricated 930 nm thin-film VCSELs are 1.08 mA and 7.52 mW at an injection current of 13.9 mA, respectively.


Assuntos
Condução de Veículo , Dimetilpolisiloxanos , Fototerapia , Excipientes , Lasers
12.
Sci Rep ; 13(1): 244, 2023 Jan 05.
Artigo em Inglês | MEDLINE | ID: mdl-36604562

RESUMO

Recent advances in deep learning realized accurate, robust detection of various types of objects including pedestrians on the road, defect regions in the manufacturing process, human organs in medical images, and dangerous materials passing through the airport checkpoint. Specifically, small object detection implemented as an embedded system is gaining increasing attention for autonomous vehicles, drone reconnaissance, and microscopic imagery. In this paper, we present a light-weight small object detection model using two plug-in modules: (1) high-resolution processing module (HRPM ) and (2) sigmoid fusion module (SFM). The HRPM efficiently learns multi-scale features of small objects using a significantly reduced computational cost, and the SFM alleviates mis-classification errors due to spatial noise by adjusting weights on the lost small object information. Combination of HRPM and SFM significantly improved the detection accuracy with a low amount of computation. Compared with the original YOLOX-s model, the proposed model takes a two-times higher-resolution input image for higher mean average precision (mAP) using 57% model parameters and 71% computation in Gflops. The proposed model was tested using real drone reconnaissance images, and provided significant improvement in detecting small vehicles.


Assuntos
Aeroportos , Veículos Autônomos , Humanos , Colo Sigmoide , Comércio , Excipientes
13.
Sci Rep ; 13(1): 511, 2023 Jan 10.
Artigo em Inglês | MEDLINE | ID: mdl-36627326

RESUMO

Tongue cracks refer to fissures with different depth and shapes on the tongue's surface, which can characterize the pathological characteristics of spleen and stomach. Tongue cracks are of great significance to the objective study of tongue diagnosis. However, tongue cracks are small and complex, existing methods are difficult to extract them effectively. In order to achieve more accurate extraction and identification of tongue crack, this paper proposes to apply a deep learning network based on image segmentation (Segmentation-Based Deep-Learning, SBDL) to extract and identify tongue crack. In addition, we have studied the quantitative description of tongue crack features. Firstly, the pre-processed tongue crack samples were amplified by using adding salt and pepper noise, changing the contrast and horizontal mirroring; secondly, the annotation tool Crack-Tongue was used to label tongue crack; thirdly, the tongue crack extraction model was trained by using SBDL; fourthly, the cracks on the tongue surface were detected and located by the segmentation network, and then the output and features of the segmentation network were put into the decision network for the classification of crack tongue images; finally, the tongue crack segmentation and identification results were quantitatively evaluated. The experimental results showed that the tongue crack extraction and recognition results based on SBDL were better than Mask Region-based Convolutional Neural Network (Mask R-CNN), DeeplabV3+, U-Net, UNet++ and Semantic Segmentation with Adversarial Learning (SegAN). This method effectively solved the inaccurate tongue crack extraction caused by the tongue crack's color being close to the surrounding tongue coating's color. This method can achieve better tongue crack extraction and recognition results on a small tongue crack data set and provides a new idea for tongue crack recognition, which is of practical value for tongue diagnosis objectification.


Assuntos
Aprendizado Profundo , Língua/diagnóstico por imagem , Excipientes , Alimentos , Redes Neurais de Computação , Processamento de Imagem Assistida por Computador
14.
J Ethnopharmacol ; 305: 116126, 2023 Apr 06.
Artigo em Inglês | MEDLINE | ID: mdl-36610672

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Various toxic medicinal materials have been used by different ethnic minorities in China for thousands of years because of their extraordinary pharmacological activities. However, the improper use and complex toxicity-efficacy relationship could cause poisoning and even death. Therefore, the study of toxicity-attenuating methods and mechanisms is necessary. AIM OF THE STUDY: This review aims to summarize commonly used toxic ethnomedicines and their processing methods as well as the underlying mechanisms to potentially reduce toxicity and even enhance or preserve efficacy. Prospective for possible future investigations is also discussed. MATERIALS AND METHODS: Processing methods and mechanisms are investigated mainly through literature review. RESULTS: Processing methods with heating (boiling, stir frying, and steaming, etc.) and without heating (soaking) are usually used by Chinese ethnic minorities to attenuate the toxicity of ethnomedicines. Wheat bran, vinegar, wine, and herbal decoction are commonly used processing excipients. The mechanisms of detoxification by processing can be briefly summarized into three major categories: (1) direct elimination of impurities or reduction of toxic constituents' contents of ethnomedicines by cutting, washing, soaking or frosting; (2) chemical structure transformation of toxic constituents, such as alkaloids, glycosides, toxic proteins, animal toxicants, and mineral components, during heating and/or soaking; and (3) biological synergism or antagonism effects between the chemical constituents of processing excipients and ethnomedicines in vivo, to reduce toxicity and protect target organs. CONCLUSION: Toxic ethnomedicines have long been used in China, and detoxification by processing is the prerequisite for their safe clinical application. However, understanding on the special processing methods and detoxification mechanisms of ethnomedicines in China remains insufficient. Investigations on quality control of toxic ethnomedicines, as well as evaluation of processing methods and studies of the corresponding mechanisms should be further strengthened for safe and effective clinical application.


Assuntos
Medicamentos de Ervas Chinesas , Minorias Étnicas e Raciais , Animais , Excipientes , Estudos Prospectivos , Medicina Tradicional , China , Medicamentos de Ervas Chinesas/uso terapêutico , Medicamentos de Ervas Chinesas/toxicidade , Medicamentos de Ervas Chinesas/química
15.
Chemosphere ; 315: 137777, 2023 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-36621692

RESUMO

A hot research topic in visible-light-driven photoelectrocatalytic (PEC) oxidation technology is the development of superior photoanode materials. The design of the photoanode system with a direct Z-scheme charge transfer mechanism is crucial to achieving effective charge separation for sustainable photoelectrocatalysis. Here, a novel Bi/Bi2S3/α-MoO3 heterostructure was successfully assembled by a simple and feasible strategy. The direct Z-scheme heterogeneous formed between Bi2S3 and α-MoO3 has the advantages of low resistance, high optical response current and the surface plasmon resonance (SPR) effect of Bi nanoparticles (Bi NPs). Thus, the efficiency of photogenerated carrier separation and transfer is further enhanced, and the catalytic activity is significantly improved. It is impressive that the unique photoanode has achieved a maximum removal efficiency of 85.8% of tetracycline (TC) pollutants under visible light irradiation within 60 min and has excellent stability, which is expected to degrade antibiotics efficiently and environmentally in harsh environments. These characteristics give Bi/Bi2S3/α-MoO3 promising candidates for practical applications in antibiotic degradation.


Assuntos
Poluentes Ambientais , Compostos Heterocíclicos , Tetraciclina , Antibacterianos , Luz , Excipientes
16.
Int J Mol Sci ; 24(2)2023 Jan 06.
Artigo em Inglês | MEDLINE | ID: mdl-36674627

RESUMO

Here, to develop new topical antibacterial formulations to treat staphylococcal infections, two pyrazoles (3c and 4b) previously reported as antibacterial agents, especially against staphylococci, were formulated as hydrogels (R1-HG-3c and R1HG-4b) using a cationic polystyrene-based resin (R1) and here synthetized and characterized as gelling agents. Thanks to the high hydrophilicity, high-level porosity, and excellent swelling capabilities of R1, R1HG-3c and R1HG-4b were achieved with an equilibrium degree of swelling (EDS) of 765% (R1HG-3c) and 675% (R1HG-4b) and equilibrium water content (EWC) of 88% and 87%, respectively. The chemical structure of soaked and dried gels was investigated by PCA-assisted attenuated total reflectance (ATR) Fourier transform infrared (FTIR) spectroscopy, while their morphology was investigated by optical microscopy. Weight loss studies were carried out with R1HG-3c and R1HG-4b to investigate their water release profiles and the related kinetics, while their stability was evaluated over time both by monitoring their inversion properties to detect possible impairments of the 3D network and by PCA-assisted ATR-FTIR spectroscopy to detect possible structural changes. The flow and dynamic rheological characterization of the gels was assessed by determining their viscosity vs. shear rate, applying the Cross rheological equation to achieve the curves of shear stress vs. shear rate, and carrying out amplitude and frequency sweep experiments. Finally, their content in NH3+ groups was determined by potentiometric titrations. Due to their favorable physicochemical characteristic and the antibacterial effects of 3c and 4b possibly improved by the cationic R1, the pyrazole-enriched gels reported here could represent new weapons to treat severe skin and wound infections sustained by MDR bacteria of staphylococcal species.


Assuntos
Hidrogéis , Poliestirenos , Hidrogéis/química , Antibacterianos/farmacologia , Antibacterianos/química , Excipientes , Composição de Medicamentos , Espectroscopia de Infravermelho com Transformada de Fourier
17.
Int J Mol Sci ; 24(2)2023 Jan 12.
Artigo em Inglês | MEDLINE | ID: mdl-36675021

RESUMO

Electrospun systems are becoming promising devices usable for topical treatments. They are eligible to deliver different therapies, from anti-inflammatory to antitumoral. In the current research, polycaprolactone electrospun membranes loaded with synthetic and commercial antitumoral active substances were produced, underlining how the matrix-filler affinity is a crucial parameter for designing drug delivery devices. Nanofibrous membranes loaded with different percentages of Dacarbazine (the drug of choice for melanoma) and a synthetic derivative of Dacarbazine were produced and compared to membranes loaded with AuM1, a highly active Au-complex with low affinity to the matrix. AFM morphologies showed that the surface profile of nanofibers loaded with affine substances is similar to one of the unloaded systems, thanks to the nature of the matrix-filler interaction. FTIR analyses proved the efficacy of the interaction between the amidic group of the Dacarbazine and the polycaprolactone. In AuM1-loaded membranes, because of the weak matrix-filler interaction, the complex is mainly aggregated in nanometric domains on the nanofiber surface, which manifests a nanometric roughness. Consequently, the release profiles follow a Fickian behavior for the Dacarbazine-based systems, whereas a two-step with a highly prominent burst effect was observed for AuM1 systems. The performed antitumoral tests evidence the high-cytotoxic activity of the electrospun systems against melanoma cell lines, proving that the synthetic substances are more active than the commercial dacarbazine.


Assuntos
Melanoma , Nanofibras , Humanos , Preparações Farmacêuticas , Sistemas de Liberação de Medicamentos , Anti-Inflamatórios , Excipientes , Dacarbazina/farmacologia , Melanoma/tratamento farmacológico , Liberação Controlada de Fármacos
18.
ACS Appl Mater Interfaces ; 15(1): 591-598, 2023 Jan 11.
Artigo em Inglês | MEDLINE | ID: mdl-36542734

RESUMO

Encoded microparticles (EMPs) have shown demonstrative value for multiplexed high-throughput bioassays such as drug discovery and diagnostics. Herein, we propose for the first time the incorporation of thermally activated delayed fluorescence (TADF) dyes with low-cost, heavy metal-free, and long-lived luminescence properties into polymer matrices via a microfluidic droplet-facilitated assembly technique. Benefiting from the uniform droplet template sizes and polymer-encapsulated structures, the resulting composite EMPs are highly monodispersed, efficiently shield TADF dyes from singlet oxygen, well preserve TADF emission, and greatly increase the delayed fluorescence lifetime. Furthermore, by combining with phase separation of polymer blends in the drying droplets, TADF dyes with distinct luminescent colors can be spatially separated within each EMP. It eliminates optical signal interference and generates multiple fluorescence colors in a compact system. Additionally, in vitro studies reveal that the resulting EMPs show good biocompatibility and allow cells to adhere and grow on the surface, thereby making them promising optically EMPs for biolabeling.


Assuntos
Micropartículas Derivadas de Células , Excipientes , Luminescência , Corantes Fluorescentes , Polímeros
19.
Int J Pharm ; 631: 122532, 2023 Jan 25.
Artigo em Inglês | MEDLINE | ID: mdl-36565771

RESUMO

Levonorgestrel intrauterine systems (LNG-IUSs) are polydimethylsiloxane (PDMS) based non-biodegradable complex drug-device combination products providing efficacy for up to several years based on the strength. A large amount of LNG (e.g., 52 mg in Mirena and Liletta) must be loaded in the LNG-IUS products to maintain the long-acting effect even though LNG is a potent hormone. However, the high amount of LNG not only poses the potential risk of dose dumping, but also leads to drug waste due to incomplete drug utilization close to the end of usage. It has been unclear whether the duration of usage of these products should be extended for full drug utilization or products with lower drug loading should be developed. Therefore, it is critical to understand the impact of strength (or drug loading) on drug release from LNG-IUSs. In the current study, drug reservoirs with a broad range of drug loading (from 0.5% w/w to 50% w/w) were prepared and assembled into LNG-IUSs. Different accelerated release conditions were used to perform release testing of LNG-IUSs with different drug loading. 5% to 10% variation in excipient of the LNG-IUSs did not significantly alter the drug release profiles of the LNG-IUSs. The release rate of LNG-IUSs is inversely proportional to their drug loading at high drug loading (10% w/w, 25% w/w and 50% w/w). Drug release was incomplete for LNG-IUS with low drug loading (2.5% w/w and 1% w/w) and no drug release could be detected for the LNG-IUS with 0.5% w/w drug loading. In addition, the burst effect of the LNG-IUSs with different drug loading was investigated. This is the first research report covering ultra-long duration (more than four years) of real-time drug release from LNG-IUSs with different drug loading (0.5%-50% w/w). The amount of excipient (PDMS) used in the reservoir of LNG-IUSs was determined to be not a critical quality parameter in the formulation design since LNG-IUSs (50% w/w drug loading) with up to 10% variation in excipient did not show significant differences in their release profiles. The drug release kinetics/mechanism remained the same for LNG-IUSs with drug loading ranging from 1% to 50%. In addition, the accelerated release testing methods were confirmed to be representative of the real-time release profiles and this can give confidence in extending the duration of usage for these products provided that the device remains physically intact (no tearing or damage in the outer membrane) and the release rate is within the therapeutic window. It is recommended to perform both real-time and accelerated release testing simultaneously for LNG-IUSs to understand the burst effect as well as the complete release characteristics. Lastly, drug/polymer interaction may play a role when designing LNG-IUS formulations with low drug loading (<5% w/w) since drug/polymer interaction is significant when only a small amount of drug present.


Assuntos
Anticoncepcionais Femininos , Dispositivos Intrauterinos Medicados , Feminino , Humanos , Levanogestrel , Excipientes , Liberação Controlada de Fármacos
20.
Int J Pharm ; 631: 122540, 2023 Jan 25.
Artigo em Inglês | MEDLINE | ID: mdl-36566828

RESUMO

The additive nature and versatility of 3D printing show great promise in the rapid prototyping of solid dosage forms for clinical trials and mass customization for personalized medicine applications. This paper reports the formulation and process development of sustained release solid dosage forms, termed "printlets", using a pilot-scale binder jetting (BJT) 3D printer and acetaminophen (APAP) as the model drug. With the inclusion of hydroxypropyl methylcellulose (HPMC) as a release retardant polymer in the print powder, the drug release time of APAP increased considerably from minutes to hours. However, given the swelling propensity of HPMC, a thicker layer of powder must be laid down during printing to avoid any shape distortion of the printlets. For a fixed print volume, the level of binder saturation (i.e., ratio between the liquid binder and powder in the as-printed sample) is inversely proportional to the thickness of the spread powder layer. An increase in the spread powder layer inadvertently resulted in a lower level of binder saturation and consequently weaker printlets. By increasing the level of binder saturation with jetting from more print heads, the mechanical strength of printlets containing 18% HPMC was successfully restored. The resultant printlets have a drug release time of 3.5 h and a breaking force of 12.5 kgf that is comparable to the fast-disintegrating printlets containing no HPMC and surpasses manually pressed tablets with the same HPMC content.


Assuntos
Acetaminofen , Tecnologia Farmacêutica , Tecnologia Farmacêutica/métodos , Preparações de Ação Retardada , Pós , Impressão Tridimensional , Comprimidos , Excipientes , Derivados da Hipromelose , Liberação Controlada de Fármacos
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