RESUMO
Inspired by the citrus oil gland and cuticular wax, a multifunctional material that stably and continuously released the carvacrol and provided physical defenses was developed to address issues of fresh-cut fruits to microbial infestation and moisture loss. The results confirmed that low molecular weight and loose structure of starch nanoparticles prepared by the ultrasound-assisted Fenton system were preferable for octenyl succinic anhydride modification compared to native starch, achieving a higher degree of substitution (increased by 18.59 %), utilizing in preparing nanoemulsions (NEs) for encapsulating carvacrol (at 5 % level: 81.58 %). Furthermore, the NEs-based gelatin (G) film improved with surface hydrophobic modification by myristic acid (MA) successfully replicated the citrus oil gland and cuticular wax, providing superior antioxidant (enhanced by 3-4 times) and antimicrobial properties (95.99 % and 84.97 % against Staphylococcus aureus and Escherichia coli respectively), as well as the exceptional UV shielding (nearly 0 transmittance in the UV region), mechanical (72 % increase in tensile strength), and hydrophobic (WCA 133.63°). Moreover, the 5%NE-G@MA film inhibited foodborne microbial growth (reduced by 50 %) and water loss (controlled below 15 %), extending the shelf life of fresh-cut navel orange and kiwi. Thus, the multifunctional film was a potential shield for preserving perishable fresh-cut products.
Assuntos
Citrus , Emulsões , Escherichia coli , Frutas , Gelatina , Nanopartículas , Staphylococcus aureus , Amido , Ceras , Gelatina/química , Nanopartículas/química , Citrus/química , Emulsões/química , Amido/química , Amido/análogos & derivados , Staphylococcus aureus/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Frutas/química , Ceras/química , Antioxidantes/química , Antioxidantes/farmacologia , Antibacterianos/farmacologia , Antibacterianos/química , Interações Hidrofóbicas e Hidrofílicas , Cimenos/química , Cimenos/farmacologia , Óleos de Plantas/química , Óleos de Plantas/farmacologia , Ácido Mirístico/química , Ácido Mirístico/farmacologia , Conservação de Alimentos/métodosRESUMO
Tablet disintegration is crucial for drug release and subsequent systemic absorption. Although factors affecting the disintegrant's functionality have been extensively studied, the impact of wet granulation on the performance of disintegrants in a poorly water-soluble matrix has received much less attention. In this study, the disintegrants, crospovidone (XPVP), croscarmellose sodium (CCS) and sodium starch glycolate (SSG), were wet-granulated with dibasic calcium phosphate dihydrate as the poorly water-soluble matrix and polyvinylpyrrolidone as the binder. The effect of wet granulation was studied by evaluating tablet tensile strength and disintegratability. Comparison between tablets with granulated or ungranulated disintegrants as well those without disintegrants were also made. Different formulations showed different degrees of sensitivity to changes in tablet tensile strength and disintegratability post-wet granulation. Tablet tensile strength decreased for tablets with granulated disintegrant XPVP or CCS, but to a smaller extent for SSG. While tablets with granulated XPVP or CCS had increased disintegration time, the increment was lesser than for SSG, suggesting that wet granulation impacted a swelling disintegrant more. The findings showed that tablets with wet-granulated disintegrant had altered the disintegrant's functionality. These findings could provide better insights into changes in the disintegrant's functionality after wet granulation.
Assuntos
Fosfatos de Cálcio , Carboximetilcelulose Sódica , Excipientes , Povidona , Solubilidade , Amido , Comprimidos , Resistência à Tração , Água , Carboximetilcelulose Sódica/química , Povidona/química , Amido/química , Amido/análogos & derivados , Excipientes/química , Água/química , Fosfatos de Cálcio/química , Composição de Medicamentos/métodos , Liberação Controlada de Fármacos , Química Farmacêutica/métodosRESUMO
Lubricants are essential for most tablet formulations as they assist powder flow, prevent adhesion to tableting tools and facilitate tablet ejection. Magnesium stearate (MgSt) is an effective lubricant but may compromise tablet strength and disintegratability. In the design of orodispersible tablets, tablet strength and disintegratability are critical attributes of the dosage form. Hence, this study aimed to conduct an in-depth comparative study of MgSt with alternative lubricants, namely sodium lauryl sulphate (SLS), stearic acid (SA) and hydrogenated castor oil (HCO), for their effects on the tableting process as well as tablet properties. Powder blends were prepared with lactose, sodium starch glycolate or crospovidone as the disintegrant, and a lubricant at different concentrations. Angle of repose was determined for the mixtures. Comparative evaluation was carried out based on the ejection force, tensile strength, liquid penetration and disintegratability of the tablets produced. As the lubricant concentration increased, powder flow and tablet ejection improved. The lubrication efficiency generally decreased as follows: MgSt > HCO > SA > SLS. Despite its superior lubrication efficacy, MgSt is the only lubricant of four evaluated that reduced tablet tensile strength. Tablet disintegration time was strongly determined by tensile strength and liquid penetration, which were in turn affected by the lubricant type and concentration. All the above factors should be taken into consideration when deciding the type and concentration of lubricant for an orodispersible tablet formulation.
Assuntos
Excipientes , Lubrificantes , Ácidos Esteáricos , Comprimidos , Resistência à Tração , Lubrificantes/química , Ácidos Esteáricos/química , Excipientes/química , Composição de Medicamentos/métodos , Pós/química , Dodecilsulfato de Sódio/química , Óleo de Rícino/química , Povidona/química , Amido/química , Amido/análogos & derivados , Lactose/química , Administração Oral , Solubilidade , Química Farmacêutica/métodosRESUMO
Global concerns over environmental damage caused by non-biodegradable single-use packaging have sparked interest in developing biomaterials. The food packaging industry is a major contributor to non-degradable plastic waste. This study investigates the impact of incorporating different concentrations of polyvinyl alcohol (PVA) and yerba mate extract as a natural antioxidant into carboxymethyl cassava starch films to possibly use as active degradable packaging to enhance food shelf life. Films with starch and PVA blends (SP) at different ratios (SP radios of 100:0, 90:10, 80:20 and 70:30) with and without yerba mate extract (Y) were successfully produced through extrusion and thermoforming. The incorporation of up to 20â¯wt% PVA improved starch extrusion processing and enhanced film transparency. PVA played a crucial role in improving the hydrophobicity, tensile strength and flexibility of the starch films but led to a slight deceleration in their degradation in compost. In contrast, yerba mate extract contributed to better compost degradation of the blend films. Additionally, it provided antioxidant activity, particularly in hydrophilic and lipophilic food simulants, suggesting its potential to extend the shelf life of food products. Starch-PVA blend films with yerba mate extract emerged as a promising alternative for mechanically resistant and active food packaging.
Assuntos
Antioxidantes , Embalagem de Alimentos , Manihot , Extratos Vegetais , Álcool de Polivinil , Amido , Embalagem de Alimentos/métodos , Álcool de Polivinil/química , Amido/química , Amido/análogos & derivados , Antioxidantes/química , Manihot/química , Extratos Vegetais/química , Ilex paraguariensis/química , Resistência à Tração , Interações Hidrofóbicas e Hidrofílicas , Fenômenos MecânicosRESUMO
Curcumin (Cur), a bioactive compound extracted from plants, has attracted widespread attention due to its multiple pharmacological activities. However, the low bioavailability due to the inherent limitations in water solubility, chemical stability, and permeability poses great challenges for realizing its clinical potentials. In the current study, octenyl succinic anhydride-modified starch (OSA-S), a renewable and biodegradable biopolymer, was employed to fabricate Cur amorphous composite nanoparticles (Cur/OSA-S NPs) through a solvent-free pH-driven method with the aim to enhance Cur's bioavailability by improving its solubility and stability. Cur/OSA-S NPs, with mean sizes of about 128.9 ± 8.6 nm, encapsulation efficiencies of about 90.0 %, and the drug loading capacities around 51.0 ± 0.2 %, were successfully prepared. Cur was found to be dispersed within the composite nanoparticles in amorphous state as confirmed by the XRD and DSC characterizations. In addition, Cur/OSA-S NPs offers excellent storage, thermal and light stability, excellent re-dispersibility, and approximately 92 times better solubility than the original Cur. Furthermore, studies of dissolution and the parallel artificial membrane permeability assay (PAMPA) confirmed enhanced dissolution rates and in vitro permeabilities of Cur/OSA-S NPs. Cancer cell viability and uptake experiments revealed that Cur/OSA-S NPs possessed more potent inhibitory effects on cancer cell proliferation compared to the raw Cur. The results obtained from the current study demonstrated the effectiveness of OSA-S for manufacturing Cur amorphous composite nanoparticles with enhanced solubility, stability, and permeability, which might be valuable for further development of Cur based products for treatment of various diseases.
Assuntos
Disponibilidade Biológica , Curcumina , Nanocompostos , Solubilidade , Amido , Curcumina/química , Curcumina/farmacocinética , Curcumina/farmacologia , Amido/química , Amido/análogos & derivados , Nanocompostos/química , Humanos , Química Verde , Portadores de Fármacos/química , PermeabilidadeRESUMO
Traditional submucosal filling materials frequently show insufficient lifting height and duration during clinical procedures. Here, the anionic polysaccharide polymer sodium carboxymethyl starch and cationic Laponite to prepare a hydrogel with excellent shear-thinning ability through physical cross-linking, so that it can achieve continuous improvement of the mucosal cushion through endoscopic injection. The results showed that the hydrogel (56.54 kPa) had a lower injection pressure compared to MucoUp (68.56 kPa). The height of submucosal lifting height produced by hydrogel was higher than MucoUp, and the height maintenance ability after 2 h was 3.20 times that of MucoUp. At the same time, the hydrogel also showed satisfactory degradability and biosafety, completely degrading within 200 h. The hemolysis rate is as low as 0.76 %, and the cell survival rate > 80 %. Subcutaneous implantation experiments confirmed that the hydrogel showed no obvious systemic toxicity. Animal experiments clearly demonstrated the in vivo feasibility of using hydrogels for submucosal uplift. Furthermore, successful endoscopic submucosal dissection was executed on a live pig stomach, affirming the capacity of hydrogel to safely and effectively facilitate submucosal dissection and mitigate adverse events, such as bleeding. These results indicate that shear-thinning hydrogels have a wide range applications as submucosal injection materials.
Assuntos
Hidrogéis , Amido , Amido/análogos & derivados , Animais , Hidrogéis/química , Hidrogéis/farmacologia , Amido/química , Suínos , Camundongos , Mucosa Gástrica/metabolismo , Ressecção Endoscópica de Mucosa/métodos , Injeções , Humanos , Hemólise/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Silicatos/químicaRESUMO
The utilization of naturally derived biodegradable polymers, including proteins, polysaccharides, and polyphenols, holds significant promise in addressing environmental concerns and reducing reliance on nonrenewable resources. This study aimed to develop films with enhanced UV resistance and antibacterial capabilities by covalently cross-linking soy protein isolate (SPI) with dialdehyde starch (DAS) through the incorporation of tannic acid (TA). The covalent crosslinking of TA with DAS and SPI was shown to establish a stable chemical cross-linking network. The tensile strength of the resulting SPI/DAS/15TA film exhibited a remarkable increase of 208.27 % compared to SPI alone and 52.99 % compared to SPI/DAS film. Notably, the UV absorption range of SPI/DAS/10TA films extended from 200 nm to 389 nm. This augmentation can be attributed to the oxidation of TA's phenolic hydroxyl groups to quinone under alkaline conditions, which then facilitated cross-linking with the SPI chain via Michael addition and Schiff base reactions. Furthermore, the film demonstrated robust antibacterial properties due to the incorporation of TA. Collectively, the observed properties highlight the significant potential of the SPI/DAS/10TA film for applications in food packaging, where its enhanced mechanical strength, UV resistance, and antibacterial characteristics can contribute to improved product preservation and safety.
Assuntos
Embalagem de Alimentos , Polifenóis , Proteínas de Soja , Amido/análogos & derivados , Proteínas de Soja/química , Antibacterianos/farmacologiaRESUMO
In this work, a multifunctional preservative film of ZnO/carboxymethyl starch/chitosan (ZnO/CMS/CS) with the unique "Steel Wire Mesh" structure is fabricated by the chemical crosslinked of ZnO NPs, CMS and CS. Unlike traditional nano-filled polymer film, the formation of the "Steel Wire Mesh" structure of ZnO/CMS/CS film is based on the synergistic effect of ZnO NPs filled CMS/CS and the coordination crosslinked between CMS/CS and Zn2+ derived from ZnO NPs. Thanks to the "Steel Wire Mesh" structure, the tensile strength and water vapor barrier of 2.5ZnO/10CMS/CS film are 2.47 and 1.73 times than that of CS film, respectively. Furthermore, the transmittance of 2.5ZnO/10CMS/CS film during antifogging test is close to 89 %, confirming its excellent antifogging effects. And the 2.5ZnO/10CMS/CS film also exhibits excellent long-acting antibacterial activity (up to 202 h), so it can maintain the freshness and appearance of strawberries at least 5 days. More importantly, the 2.5ZnO/10CMS/CS film is sensitive to humidity changes, which achieves real-time humidity monitoring of the fruit storage environment. Note that the preparation method of the film is safe, simple and environmentally friendly, and its excellent degradation performance will not bring any problems of food safety and environmental pollution.
Assuntos
Quitosana , Fragaria , Amido/análogos & derivados , Óxido de Zinco , Quitosana/química , Óxido de Zinco/farmacologia , Óxido de Zinco/química , Antibacterianos/farmacologia , Antibacterianos/química , Embalagem de AlimentosRESUMO
Implementing novel oral drug delivery systems with controlled drug release behavior is valuable in cancer therapy. Herein, a green synthetic approach based on the sol-gel technique was adopted to prepare MgFe2O4 nanoparticles at different calcination temperatures using citric acid as a chelating/combustion agent. In this context, pH-responsive and magnetic carboxymethyl starch/alginate hydrogel beads (CMCS-SA) containing the MgFe2O4 nanoparticles were developed as potential drug carriers for the anticancer drug (Doxorubicin, Dox) release in simulated gastrointestinal fluids. Furthermore, in vitro release behaviors validated that these beads illustrated excellent stability in the simulated stomach liquids. In contrast, the data in simulated intestinal fluids showed sustained release of Dox because of their pH-sensitive swelling characteristics. Notably, applying an external magnetic field (EMF) could accelerate drug release from the beads. The in vitro release of drugs from gel beads was mainly accomplished by a combination of diffusion, swelling and erosion. Moreover, the cell cytotoxicity test and laser confocal results showed no harmful effects on normal cells (3T3) but were significant cytotoxic to colon cancer cell lines (HCT116) by drug-loaded hydrogel beads. Therefore, the prepared gel beads could be qualified as latent platforms for controlling the release of anticancer drugs in cancer treatment.
Assuntos
Antineoplásicos , Manihot , Nanopartículas , Alginatos , Antineoplásicos/farmacologia , Ácido Cítrico , Preparações de Ação Retardada , Doxorrubicina/farmacologia , Portadores de Fármacos , Liberação Controlada de Fármacos , Ácido Glucurônico , Ácidos Hexurônicos , Hidrogéis , Concentração de Íons de Hidrogênio , Amido/análogos & derivadosRESUMO
BACKGROUND: Catechins, a member of the flavonoids, exist widely in teas, and have health benefits. However, catechins have poor stability, which greatly limits their application. In order to improve the stability of catechins, different catechins including (-)-epicatechin (EC), (-)-epicatechin gallate (ECG), (-)-epigallocatechin (EGC) and (-)-epigallocatechin gallate (EGCG) were conjugated onto dialdehyde starch by acid-mediated coupling method. The structure, stability and antioxidant activity of dialdehyde starch-catechin conjugates were determined. RESULTS: Thin-layer chromatography and ultraviolet-visible spectroscopy, fluorescence, nuclear magnetic resonance and infrared spectra revealed that catechins were successfully conjugated onto dialdehyde starch, coupling between 6-H/8-H of catechins' A ring and dialdehyde starch's aldehyde groups. The conjugates presented an amorphous structure and sheet-like and/or blocky morphologies. As compared to dialdehyde starch, the conjugates showed enhanced thermal stability. Furthermore, the stability of catechins in pH 7.4 phosphate-buffered saline was improved after conjugating onto dialdehyde starch. The conjugates exhibited significantly higher antioxidant activities than dialdehyde starch, decreasing in the following order: dialdehyde starch-ECG, dialdehyde starch-EGCG, dialdehyde starch-EC, dialdehyde starch-EGC and dialdehyde starch. CONCLUSION: Dialdehyde starch-catechin conjugates have great potential as stable antioxidant agents. © 2022 Society of Chemical Industry.
Assuntos
Catequina , Aldeídos/análise , Antioxidantes/análise , Catequina/análogos & derivados , Catequina/química , Flavonoides/análise , Fosfatos , Amido/análogos & derivados , Chá/químicaRESUMO
Achieving a new oral drug delivery system with controlled drug release behavior is valuable in cancer therapy. Therefore, for the first time, doxorubicin (DOX) and 5-fluorouracil (5-Fu) were simultaneously co-loaded on the as-synthesized layered double hydroxides LDH(MgAl). The resulted system was encapsulated with carboxymethyl starch to improve its efficiency for colon cancer therapy. Several characterization techniques were used to evaluate the successful synthesis of the CMS@LDH(MgAl)@DOX,5-Fu microspheres. The scanning electron microscopy result showed that the size of prepared microspheres is about 72 µm. Additionally, the presence of one broad peak at 2θ ~ 20 of the X-ray diffraction spectrum approved its amorph nature. The drug release study showed a controlled release profile with ~22% of DOX and 29% of 5-Fu. In addition, the cell viability test outcome confirmed the sustained drug release pattern from CMS@LDH(MgAl)@DOX,5-Fu against the colon cancer cell line. The results suggest that the prepared microspheres are capable to operate as an acceptable formulation for oral co-drug delivery.
Assuntos
Fluoruracila , Hidróxidos , Doxorrubicina/farmacologia , Sistemas de Liberação de Medicamentos , Liberação Controlada de Fármacos , Fluoruracila/química , Hidróxidos/química , Amido/análogos & derivadosRESUMO
A mild and efficient green protocol has been disclosed for selective oxidative esterification of various aldehydes over a novel Pd fabricated chitosan-starch polyplex encapsulated Kaolin (Kaolin@CS-starch-Pd) as a heterogeneous and reusable biocompatible nanocatalyst. Molecular oxygen was used as an oxidizing agent to generate water as the sole by-product. A wide variety of aldehydes was converted to their methyl esters in high yields. The process involved gentle reaction conditions to avoid any type of pre-activation. Structural features of the catalyst were determined through FT-IR, FE-SEM, TEM, EDX, elemental mapping, XRD and ICP-OES analyses. The material was found to be stable enough toward Pd leaching. Durability of Kaolin@CS-starch-Pd was further justified by retaining its catalytic activity through successful reusability for several times.
Assuntos
Quitosana/análogos & derivados , Caulim/análogos & derivados , Nanopartículas Metálicas/química , Paládio/química , Amido/análogos & derivados , Esterificação , Glutaral/química , OxirreduçãoRESUMO
Recently, food industries are directing on the promotion of innovative food matrices fortified with bioactive compounds in order to enhance the consumer's health. Octenyl succinic anhydride modified starches (OSA-MS) such as Hi-cap100 (HCP) and purity gum 2000 (PUG) were used to fabricate emulsions co-entrapped with borage seed oil (BSO), resveratrol (RES) and curcumin (CUR), which were further spray dried to obtain powders. The fabricated microcapsules loaded with BSO, RES, and CUR displayed excellent dissolution performance, high encapsulation efficiency (≈93.05%) as well as semi-spherical shape, revealed via scanning electron microscopy (SEM). We also evaluated the impact of storage time (4 weeks) and temperature (40 °C) on the physicochemical characterization of OSA-MS coated microcapsules. Microcapsules coated with HCP exhibited greater oxidative stability, lower water activity and moisture contents rather than PUG coated microcapsules during storage because of its good film-forming properties. Addition of CUR enhanced the oxidative stability and retention of bioactive compounds. HCP microcapsules loaded with BSO + RES + CUR presented supreme retention of RES (70.32%), CUR 81.6% and γ-linolenic acid (≈ 96%). Our findings showed that CUR acted as an antioxidant agent; also, lower molecular weight OSA-MS as wall material could be used for the entrapment of bioactive compounds and promotion of innovative food products.
Assuntos
Antioxidantes/química , Curcumina/química , Portadores de Fármacos , Nanopartículas , Óleos de Plantas/química , Resveratrol/química , Amido/química , Ácido gama-Linolênico/química , Composição de Medicamentos , Estabilidade de Medicamentos , Armazenamento de Medicamentos , Emulsões , Nanotecnologia , Oxirredução , Pós , Secagem por Atomização , Amido/análogos & derivados , Fatores de TempoRESUMO
In this study, carboxymethyl cassava starch (CMCS)-functionalized magnetic nanoparticles (CMCS@Fe3O4) were synthesized via a simple one-pot co-precipitation method using CMCS materials with varying degrees of substitution, and used for the adsorption/removal of doxorubicin hydrochloride (Dox; a clinically available anti-cancer drug) from aqueous solution. The adsorption of Dox was studied using experimental conditions with varied pH, temperature, initial Dox concentration, and CMCS@Fe3O4 dosage. The CMCS@Fe3O4 adsorbents were characterized by scanning electron microscopy, transmission electron microscopy, infrared spectroscopy, X-ray diffraction, thermogravimetric analysis, and vibrating sample magnetometry. Each CMCS@Fe3O4 adsorbent exhibited a cubic inverse spinel iron oxide phase, small particle size, favorable magnetic properties, and good thermal stability. Batch adsorption experiments showed that the Dox adsorption efficiency reached 85.46% at a CMCS@Fe3O4 concentration of 20 mg mL-1 at 303 K in pH 7.0. The adsorption experimental results indicated that the adsorption kinetics followed a pseudo-second-order model and the Langmuir equation. Considering the environmentally nontoxic nature of Fe3O4 and starch, the CMCS@Fe3O4 material demonstrated significant potential for removing Dox from aqueous solution and in magnetic targeted drug delivery systems for synergistic tumor treatments.
Assuntos
Antineoplásicos/análise , Doxorrubicina/análise , Manihot/química , Amido/análogos & derivados , Poluentes Químicos da Água/análise , Concentração de Íons de Hidrogênio , Fenômenos Magnéticos , Nanopartículas de Magnetita , Nanocompostos , Tamanho da Partícula , Amido/química , Temperatura , Difração de Raios XRESUMO
Corn starch (CS), octenyl succinic anhydride modified corn starch (OSCS) and shells (OSCs) microgels have been prepared using water-in-oil (W/O) inverse microemulsions for loading and releasing of epigallocatechin gallate (EGCG). The structural and morphological properties of CS, OSCS, and OSCs microgels were characterized by Fourier transform infrared (FTIR) spectroscopy, X-ray diffraction (XRD), Transmission electron microscopy (TEM), and Thermogravimetric analysis (TGA). The strong hydrogen bonds between starch molecules in the W/O system and interplay between hydroxyl groups of EGCG and oxygen atoms of starch microgels were formed. OSCs microgel showed low average particle size and weak thermal stability with an irregular shape and a typical V-type crystalline structure. Encapsulation efficiency (EE) and clearance rate of 2,2-diphenyl-1-picrylhydrazyl (DPPH) for EGCG were ranged between 41.78 and 63.89% and 75.53-85.37%, respectively, when absorbed into OSCS and OSCs microgels, the values which were higher than that of CS microgel. Further, OS starch microgels (particularly OSCs) modulated the slow release of EGCG into simulated gastrointestinal tract conditions and therefore could be proposed as an encapsulating agent for loading polyphenols.
Assuntos
Catequina/análogos & derivados , Portadores de Fármacos/química , Liberação Controlada de Fármacos , Microgéis/química , Óleos/química , Amido/análogos & derivados , Água/química , Catequina/química , Emulsões , Ligação de Hidrogênio , Tamanho da Partícula , Amido/químicaRESUMO
In this study, cassava starch aldehyde was functionalized with catechin through acid catalyzed condensation reaction. The structural characterization, stability and antioxidant activity of starch aldehyde-catechin conjugates were investigated. Thin layer chromatography revealed the conjugates did not contain free catechin. UV-vis spectra of the conjugates exhibited an absorption band at 280 nm, attributing to the B-ring of catechin moiety. Fourier-transform infrared and proton nuclear magnetic resonance spectroscopy demonstrated the conjugation occurred between the H-6/H-8 of catechin A-ring and the aldehyde groups of starch aldehyde. X-ray diffraction pattern indicated that the conjugates had an amorphous structure. Scanning electron microscopy showed the conjugates were fragmentary slices with rough surfaces. Notably, the conjugates were more stable than catechin in phosphate buffered saline (pH 7.4). In addition, the conjugates could not be digested in simulated saliva, gastric and small intestinal juices. The reducing power and free radical scavenging activity of starch aldehyde were remarkably elevated by conjugating with catechin. Meanwhile, the conjugates were non-cytotoxic to RAW264.7 mouse macrophage cells and possessed higher resistant starch contents than starch. Our results suggest starch aldehyde-catechin conjugates can be used as antioxidants in food industry.
Assuntos
Aldeídos/química , Antioxidantes/síntese química , Catequina/química , Glicoconjugados/síntese química , Manihot/química , Amido/análogos & derivados , Animais , Antioxidantes/farmacologia , Materiais Biomiméticos/química , Sobrevivência Celular/efeitos dos fármacos , Estabilidade de Medicamentos , Tecnologia de Alimentos , Suco Gástrico/química , Glicoconjugados/farmacologia , Humanos , Camundongos , Células RAW 264.7 , Saliva/química , Amido/isolamento & purificaçãoRESUMO
Controlled-release drug delivery systems are promising platforms in medicine. Among various types of material in drug delivery, hydrogels are interesting ones. They are water-soluble and tissue compatible polymers with a high capacity to carry and release drugs in a controllable manner. In this study, we introduce the synthesis, characterization, and application of an α-amylase responsive hydrogel in controlled drug delivery. The newly synthesized starch-based hydrogels structurally characterized by means of Fourier-transform infrared spectroscopy and scanning electron microscopy. A proapoptotic drug, doxorubicin, was loaded into the hydrogels and the controlled release of the drug was assessed in the presence of α-amylase and ultimately it was evaluated to controlled-drug release in vitro and subsequently in killing cancer cells. Our results highlight the effectiveness of temporal drug delivery using α-amylase responsive hydrogels in killing cancer cells.
Assuntos
Hidrogéis/síntese química , Amido/análogos & derivados , alfa-Amilases/metabolismo , Morte Celular , Linhagem Celular Tumoral , Reagentes de Ligações Cruzadas/química , Doxorrubicina/química , Doxorrubicina/farmacologia , Humanos , Espectroscopia de Infravermelho com Transformada de Fourier , Amido/metabolismoRESUMO
Starch nanoparticles are promising candidates for the delivery of active compounds or drugs. The purpose of this study was to prepare nanoparticles from debranched starch using an ionic gelation method. Negatively charged carboxymethyl debranched starch (CMDBS) was obtained by modification of debranched starch (DBS). The zeta potential value of CMDBS with a degree of substitution of 0.81 was approximately -26 mV. The starch nanoparticles formed from 2 mg mL-1 CMDBS and cationized DBS (CDBS) had particle sizes of 50 to 100 nm, as determined by transmission electron spectroscopy, and most nanoparticles were spherical in shape. Measurements with a quartz crystal microbalance with dissipation monitoring confirmed a successful adsorption interaction between the negatively charged CMDBS and positively charged CDBS. Epigallocatechin gallate (EGCG) was successfully incorporated into the nanoparticles with the highest encapsulation efficiency of 84.4%, and the resulting nanoparticles showed controlled release of EGCG into simulated gastric and intestinal fluids.
Assuntos
Catequina/análogos & derivados , Géis/química , Nanopartículas/química , Amido/análogos & derivados , Células CACO-2 , Catequina/química , Cátions/química , Linhagem Celular Tumoral , Preparações de Ação Retardada/química , Humanos , Tamanho da Partícula , Amido/químicaRESUMO
The control of blood flow from breached blood vessels during surgery or trauma is challenging. With the existing treatment options being either expensive or ineffective, the development of a haemostat that overcome such drawbacks would be beneficial. With an aim to develop an ideal haemostat, the potential of sodium starch glycolate (SSG), a commonly used pharmaceutical disintegrant was modified to obtain porous microparticles (pSSG). The biodegradability, cyto-compatibility and haemo-compatibility of the modified particles were confirmed using appropriate studies. In comparison to starch and SSG, the irregular shaped pSSG demonstrated spontaneous and significant fluid absorption (3500+500 %) and formed a physical barrier to blood flow. In addition, significant blood cells aggregation and platelet activation was observed in the modified micoparticles leading to rapid clot formation. In-vivo studies on liver and abdominal artery injury models in rats indicated the superior haemostatic potential of pSSG over SSG and starch. The results indicated that pSSG can be explored further in clinical evaluation as a hemostat.
Assuntos
Hemostáticos/farmacologia , Amido/análogos & derivados , Eritrócitos/efeitos dos fármacos , Hemostáticos/síntese química , Hemostáticos/química , Humanos , Tamanho da Partícula , Agregação Plaquetária/efeitos dos fármacos , Porosidade , Amido/síntese química , Amido/química , Amido/farmacologia , Propriedades de SuperfícieRESUMO
The presence of different excipient types/brands in solid oral dosage forms may affect product performance and drug bioavailability. Understanding the biopharmaceutical implications of superdisintegrant variability (changes in material properties), variation (changes in excipient amount) and interchangeability (use of different excipient types with the same intended functionality) in oral drug performance would be beneficial for the development of robust final dosage forms. The current study investigated the impact of superdisintegrants (sodium starch glycolate, croscarmellose sodium, crospovidone) on the apparent solubility of drugs with different physicochemical properties (drug ionisation, drug lipophilicity, drug aqueous solubility). Compendial and biorelevant media were used to assess the impact of gastrointestinal conditions on the effects of excipient on drug apparent solubility. For the majority of compounds, changes in drug apparent solubility were not observed in superdisintegrant presence, apart from the cases of highly ionised compounds (significant decrease in drug solubility) and/or compounds that aggregate/precipitate in solution (significant increase in drug solubility). Excipient variability did not greatly affect the impact of excipients on drug apparent solubility. The use of multivariate data analysis identified the biopharmaceutical factors affecting excipient performance. The construction of roadmaps revealed that superdisintegrants may be of low risk for the impact of excipients on oral drug performance based on drug solubility alone; superdisintegrants activity could still be a risk for oral bioavailability due to their effects on tablet disintegration.