Ionic gelation

离子凝胶化
  • 文章类型: Journal Article
    通过改变施用方法和递送系统,利用已经可用的抗生素可以容易地治疗胃肠道的大多数感染性疾病。环丙沙星(CIP)被用作许多细菌感染的首选药物;然而,长期治疗和异地药物蓄积会增加肌腱炎和周围神经病变的风险.为了克服这个问题,纳米技术正被用来将抗生素封装在聚合物结构中,这不仅有助于在感染部位维持剂量,而且限制了非现场副作用。这里,海藻酸钠(SA)和巯基锚定的壳聚糖(TC)用于通过氯化钙(CaCl2)交联剂包封CIP。为此,使用简单的技术将B-390封装器用于制备纳米珠。然后将水凝胶状样品冷冻干燥,使用海藻糖或甘露醇作为冻干保护剂,以获得精细的干粉。实验设计(DoE)用于优化纳米珠的生产,其中研究了不同独立变量对多分散指数(PDI)结果的影响,颗粒大小,zeta电位,和百分比封装效率(%EE)。在模拟唾液液中进行体外溶出研究,模拟胃液,和模拟肠液。还进行了抗菌和抗炎研究以及细胞毒性分析。总的来说,这项研究取得了积极的成果,证明了使用纳米技术在使用已经可用的抗生素制造新的递送方法中的优势。
    Most infectious diseases of the gastrointestinal tract can easily be treated by exploiting the already available antibiotics with the change in administration approach and delivery system. Ciprofloxacin (CIP) is used as a drug of choice for many bacterial infections; however, long-term therapy and off-site drug accumulation lead to an increased risk of tendinitis and peripheral neuropathy. To overcome this issue, nanotechnology is being exploited to encapsulate antibiotics within polymeric structures, which not only facilitates dose maintenance at the infection site but also limits off-site side effects. Here, sodium alginate (SA) and thiol-anchored chitosan (TC) were used to encapsulate CIP via a calcium chloride (CaCl2) cross-linker. For this purpose, the B-390 encapsulator was employed in the preparation of nanobeads using a simple technique. The hydrogel-like sample was then freeze-dried, using trehalose or mannitol as a lyoprotectant, to obtain a fine dry powder. Design of Experiment (DoE) was utilized to optimize the nanobead production, in which the influence of different independent variables was studied for their outcome on the polydispersity index (PDI), particle size, zeta potential, and percentage encapsulation efficiency (% EE). In vitro dissolution studies were performed in simulated saliva fluid, simulated gastric fluid, and simulated intestinal fluid. Antibacterial and anti-inflammatory studies were also performed along with cytotoxicity profiling. By and large, the study presented positive outcomes, proving the advantage of using nanotechnology in fabricating new delivery approaches using already available antibiotics.
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  • 文章类型: Journal Article
    已经在食物中使用,Pharmaceutical,化妆品,和农用化学工业,封装是用于保护活性成分免受外部降解因素影响并控制其释放动力学的策略。已经研究了各种封装技术,这两者都是为了优化相对于侵扰物的性质的保护水平,并且有利于活性化合物的扩散和阻隔材料的降解之间的释放机制。生物聚合物由于其生物相容性而作为壁材料特别感兴趣。生物降解性,和无毒。通过在药物周围形成稳定的水凝胶,它们提供了一个“智能”屏障,其行为可以随着环境条件而改变。在对封装的概念和实现封装的主要技术进行了全面的描述之后,包括微凝胶和纳米凝胶,介绍了活性化合物的控释机制。然后展示了天然聚合物作为墙体材料的全景,强调与每种聚合物相关的主要结果,并试图确定在包封药物方面最具成本效益和合适的方法。
    Already used in the food, pharmaceutical, cosmetic, and agrochemical industries, encapsulation is a strategy used to protect active ingredients from external degradation factors and to control their release kinetics. Various encapsulation techniques have been studied, both to optimise the level of protection with respect to the nature of the aggressor and to favour a release mechanism between diffusion of the active compounds and degradation of the barrier material. Biopolymers are of particular interest as wall materials because of their biocompatibility, biodegradability, and non-toxicity. By forming a stable hydrogel around the drug, they provide a \'smart\' barrier whose behaviour can change in response to environmental conditions. After a comprehensive description of the concept of encapsulation and the main technologies used to achieve encapsulation, including micro- and nano-gels, the mechanisms of controlled release of active compounds are presented. A panorama of natural polymers as wall materials is then presented, highlighting the main results associated with each polymer and attempting to identify the most cost-effective and suitable methods in terms of the encapsulated drug.
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  • 文章类型: Journal Article
    通过离子凝胶化制备载有丁香精油(CEO)的海藻酸盐封装物,随后冷冻干燥。目前工作的目标是开发一种能够保护首席执行官免受其容易波动和氧化的产品。以下技术用于表征制剂:丁香酚释放,肿胀程度,GC/MS,TGA/DSC,和SEM。将含有不同浓度的CEO(LF1:1.0%;LF2:0.5%;LF3:0.1%)的藻酸盐溶液(1.0%)滴入3.0%CaCl2溶液中。冻干后,封装的样品起皱且坚硬,具有高封装功率(LF3:76.9%±0.5)。确定了三种化学成分:丁香酚(主要的一种),石竹烯,还有腐殖质.抗氧化能力(LF1:DPPHIC5018.1µgmL-1)与苯酚含量(LF1:172.2mgGAEg-1)一致。封装的是热稳定的,如FTIR峰分析所示,丁香酚分子结构保持不变。溶胀度为19.2%(PBS)。丁香酚(92.5%)在PBS溶液中的释放比在酸性介质中的释放更快。结论是,所使用的低成本技术可以在所测试的三种浓度中保持CEO的含量和特征,为精油胶囊的进一步研究提供了基础。
    Alginate encapsulates loaded with clove essential oil (CEO) were prepared by ionic gelation, with subsequent freeze-drying. The objective of the present work was to develop a product with the ability to protect CEO against its easy volatility and oxidation. The following techniques were used to characterize the formulations: eugenol release, degree of swelling, GC/MS, TGA/DSC, and SEM. The alginate solution (1.0%) containing different concentrations of CEO (LF1: 1.0%; LF2: 0.5%; LF3: 0.1%) was dropped into a 3.0% CaCl2 solution. After lyophilization, the encapsulated samples were wrinkled and rigid, with high encapsulation power (LF3: 76.9% ± 0.5). Three chemical components were identified: eugenol (the major one), caryophyllene, and humulene. The antioxidant power (LF1: DPPH IC50 18.1 µg mL-1) was consistent with the phenol content (LF1: 172.2 mg GAE g-1). The encapsulated ones were thermally stable, as shown by analysis of FTIR peaks, eugenol molecular structure was kept unaltered. The degree of swelling was 19.2% (PBS). The release of eugenol (92.5%) in the PBS solution was faster than in the acidic medium. It was concluded that the low-cost technology used allows the maintenance of the content and characteristics of CEO in the three concentrations tested, offering a basis for further research with essential oil encapsulates.
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  • 文章类型: Journal Article
    药用植物马齿轮轴科在传统医学中有着悠久的使用历史。植物提取物具有几个令人感兴趣的药理作用,但具有一些可通过用壳聚糖包封来解决的缺点。这项工作旨在总结富含多酚的P.olerace提取物的抗氧化作用,并观察胶囊如何影响它们。采用回流提取法和响应面法(RSM)对苦参提取物中的酚类和黄酮含量进行优化。此外,高分辨率质谱法用于确定提取物中存在的次级代谢产物。用离子凝胶法制备了负载提取物的壳聚糖微胶囊,并对其大小进行了表征,封装效率(EE),和微胶囊的形态。傅里叶变换红外(FTIR)用于通过主成分分析(PCA)方法观察微胶囊的成功生产。采用自由基清除法建立了微胶囊的抗氧化活性。根据RSM,最高含量的TPC和TFC在72.894%乙醇时获得,2.031小时,和57.384°C。所述化合物来自包括酚类和类黄酮的优选的甘蓝科提取物。微胶囊的%EE为43.56±2.31%。根据PCA,微胶囊的特性被批准用于获得的产品的成功合成。微胶囊具有浓度依赖性的抗氧化活性(p<0.0001)。这项研究的结果强调了使用壳聚糖作为提取物纳米载体的好处,提供了一种有希望的方法来增强植物衍生疗法。
    The medicinal plant Portulaca oleraceae has a long history of usage in traditional medicine. Plant extracts have several interesting pharmacological effects but have some drawbacks that can be addressed via capsulation with chitosan. This work set out to do just that tally up the antioxidant effects of a polyphenol-rich P. olerace extract and see how capsulation affected them. The reflux extraction and response surface methodology (RSM) were carried out to optimize the phenolic and flavonoid content of P. oleraceae extract. Additionally, high-resolution mass spectrometry was employed to determine the secondary metabolite present in the extract. The microcapsules of extract-loaded chitosan were prepared using the ionic gelation method and characterized in terms of size, encapsulation efficiency (EE), and morphology of microcapsules. Fourier transform infrared (FTIR) was used to observe the successful production of microcapsules with a principal component analysis (PCA) approach. The antioxidant activity of microcapsules was established using the radical scavenging method. According to RSM, the highest amounts of TPC and TFC were obtained at 72.894 % ethanol, 2.031 h, and 57.384 °C. The compounds were employed from the optimized extract of P. oleraceae including phenolics and flavonoids. The microcapsules were secured with a %EE of 43.56 ± 2.31 %. The characteristics of microcapsules were approved for the obtained product\'s successful synthesis according to the PCA. The microcapsules have antioxidant activity in a concentration-dependent manner (p < 0.0001). The findings of this study underscored the benefits of employing chitosan as a nanocarrier for extract, offering a promising approach to enhance plant-derived therapies.
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  • 文章类型: Journal Article
    冻干的植物来源提取物富含高效的抗氧化多酚。为了将它们融入食品中,有必要保护这些植物化学物质免受大气因素的影响,如热量,光,水分,或pH,并由于其低溶解度而提高其生物利用度。为了应对这些挑战,最近的研究集中在聚合结构中的抗氧化剂化合物的封装技术的发展。在这项研究中,冻干的橄榄叶提取物被微囊化,目的是克服上述挑战。用于制备所研究的微粒的方法包括在室温下在水-油(W/O)乳液中进行的外部离子凝胶化。HPLC分析表明多酚含量高,90%的生物活性化合物被封装。同时,通过电感耦合等离子体发射光谱(ICP-OES)的定量表明,干燥的叶子,冻干提取物,和微胶囊形式含有令人满意的宏观和微观矿物质水平(钙,钾,钠)。微囊化技术可能是利用橄榄叶中的多酚和矿物质的新策略,从而丰富食品和利用在冻干提取物中发现的多酚化合物的抗氧化特性。
    Lyophilized plant-origin extracts are rich in highly potent antioxidant polyphenols. In order to incorporate them into food products, it is necessary to protect these phytochemicals from atmospheric factors such as heat, light, moisture, or pH, and to enhance their bioavailability due to their low solubility. To address these challenges, recent studies have focused on the development of encapsulation techniques for antioxidant compounds within polymeric structures. In this study, lyophilized olive leaf extracts were microencapsulated with the aim of overcoming the aforementioned challenges. The method used for the preparation of the studied microparticles involves external ionic gelation carried out within a water-oil (W/O) emulsion at room temperature. HPLC analysis demonstrates a high content of polyphenols, with 90% of the bioactive compounds encapsulated. Meanwhile, quantification by inductively coupled plasma optical emission spectroscopy (ICP-OES) reveals that the dried leaves, lyophilized extract, and microencapsulated form contain satisfactory levels of macro- and micro-minerals (calcium, potassium, sodium). The microencapsulation technique could be a novel strategy to harness the polyphenols and minerals of olive leaves, thus enriching food products and leveraging the antioxidant properties of the polyphenolic compounds found in the lyophilized extract.
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  • 文章类型: Journal Article
    两种类型的藻酸盐,AlgLF和AlgP,在这项研究中用于通过电振动挤出生产藻酸盐珠。如通过NMR和SEC-MALS测量的,AlgLF和AlgP表现出不同的甘露糖醛酸盐/古洛糖醛酸盐(M/G)比率和分子量。发现氯化钙浓度对珠子尺寸的影响最大。更高的浓度导致更小的珠。具有较高分子量和较低比例的G嵌段的AlgLF显示较小的珠。对于两种藻酸盐,珠的大小也受流速和振动频率的影响。藻酸盐溶液老化显示出最小的影响。使用数学方程对藻类网状物进行建模。该研究通过对影响珠子尺寸的主要因素进行光照,为不同应用中的海藻酸盐基材料的优化提供了见解。分子量的重要性,胶凝过程中的M/G比和钙离子浓度,通过现象学模型提供了定制藻酸盐材料的机会。
    Two types of alginates, AlgLF and AlgP, were used in this study to produce alginate beads by electro-vibratory extrusion. AlgLF and AlgP exhibited different Mannuronate/Guluronate (M/G) ratios and molecular weights as measured by NMR and SEC-MALS. The calcium chloride concentration was found to have the greatest effect on bead size. Higher concentrations resulted in smaller beads. AlgLF with a higher molecular weight and a lower proportion of G blocks showed smaller beads. For both alginates, the bead size was also influenced by the flow rate and vibration frequency. Alginate solution aging showed a minimal effect. Alginate reticulation was modeled using a mathematical equation. The study provides insights for the optimization of alginate-based materials in different applications by shedding light on the main factors influencing bead size. The importance of the molecular weight, M/G ratio and calcium ion concentration in the gelling process is highlighted, providing opportunities for the tailoring of alginate materials through a phenomenological model.
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  • 文章类型: Journal Article
    使用离子凝胶化然后喷雾干燥制备多糖/二氧化硅杂化微胶囊。壳聚糖和藻酸盐被用作生物聚合物基质,原位制备的二氧化硅用作结构化添加剂。制备的微粒用于两种非常不同的应用:亲水分子的封装,并作为钯纳米颗粒的载体,用作模型有机反应的催化剂,即硼氢化钠还原对硝基苯酚。在第一个应用程序中,赤霉素二钠盐,作为亲水物质的典范,在制备微粒期间原位包封。结果表明,二氧化硅纳米结构的存在,集成在聚合物基质中,影响颗粒的形态和稳定性,延缓被包封物质的释放。在第二个应用程序中,氯钯酸盐在壳聚糖微粒的表面上络合,和钯(II)随后还原为钯(0),以获得具有优异性能的非均相催化剂。
    Polysaccharide/silica hybrid microcapsules were prepared using ionic gelation followed by spray-drying. Chitosan and alginate were used as biopolymer matrices, and in situ prepared silica was used as a structuring additive. The prepared microparticles were used in two very different applications: the encapsulation of hydrophilic molecules, and as a support for palladium nanoparticles used as catalysts for a model organic reaction, namely the reduction of p-nitrophenol by sodium borhydride. In the first application, erioglaucine disodium salt, taken as a model hydrophilic substance, was encapsulated in situ during the preparation of the microparticles. The results indicate that the presence of silica nanostructures, integrated within the polymer matrix, affect the morphology and the stability of the particles, retarding the release of the encapsulated substance. In the second application, chloropalladate was complexed on the surface of chitosan microparticles, and palladium(II) was subsequently reduced to palladium(0) to obtain heterogeneous catalysts with an excellent performance.
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  • 文章类型: Journal Article
    纳米技术已经成为改善植物化学物质限制的可能解决方案。本研究的目的是将甜菜根提取物(BRExt)封装在壳聚糖(CS)基纳米凝胶(NG)中,该凝胶通过与三聚磷酸盐(TPP)的离子交联设计用于甜菜碱(Bet)递送,主要在眼科环境中。BRExt富含甜菜碱(Bet),根据薄层色谱(TLC),紫外可见光谱,和HPLC分析。NG呈现尺寸为166±6nm和低多分散性(0.30±0.03)的单分散分布。+28±1的ζ电位(ζ-Pot)指示胶体稳定的系统。BRExt包封效率(EE)为45±3%。TEM,使用各自的3D表面图和AFM,呈球形椭圆形NG。BRExt释放曲线是双相的,具有突释,然后是12小时的缓慢和持续阶段。粘膜粘附测定表明NG与粘蛋白之间的相互作用。此外,NG为BRExt提供光保护和pH稳定性。FRAP和ABTS测定证实BRExt保持了进入NG的抗氧化活性。此外,使用人视网膜细胞的体外测定显示不存在细胞毒性以及对损伤剂(LPS和H2O2)的有效保护。NG是BRExt封装的一个有前途的平台,发挥眼科用途的控释。
    Nanotechnology has emerged as a possible solution to improve phytochemicals\' limitations. The objective of the present study was to encapsulate beetroot extract (BR Ext) within a chitosan (CS)-based nanogel (NG) designed via ionic crosslinking with tripolyphosphate (TPP) for betanin (Bet) delivery, mainly in the ophthalmic environment. BR Ext is rich in betanin (Bet) according to thin layer chromatography (TLC), UV-visible spectroscopy, and HPLC analysis. NG presented a monodisperse profile with a size of 166 ± 6 nm and low polydispersity (0.30 ± 0.03). ζ potential (ζ-Pot) of +28 ± 1 is indicative of a colloidally stable system. BR Ext encapsulation efficiency (EE) was 45 ± 3%. TEM, with the respective 3D-surface plots and AFM, showed spherical-elliptical-shaped NG. The BR Ext release profile was biphasic with a burst release followed by slow and sustained phase over 12 h. Mucoadhesion assay demonstrated interactions between NG with mucin. Moreover, NG provided photoprotection and pH stability to BR Ext. FRAP and ABTS assays confirmed that BR Ext maintained antioxidant activity into NG. Furthermore, in vitro assays using human retinal cells displayed absence of cytotoxicity as well as an efficient protection against injury agents (LPS and H2O2). NGs are a promising platform for BR Ext encapsulation, exerting controlled release for ophthalmological use.
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  • 文章类型: Journal Article
    纳米封装被广泛认为是一种通过保护精油免受氧化变质和蒸发来增强精油稳定性的高效策略。本研究旨在优化和表征一种有效的Cinnamomum封装技术(C.)利用响应面法(RSM)将维生精油转化为壳聚糖纳米颗粒。此外,研究了优化的C.verumEO纳米颗粒的抗菌性(针对革兰氏阳性和革兰氏阴性细菌),抗真菌药(针对白色念珠菌),和抗寄生虫活性(对抗利什曼原虫寄生虫)。使用Plackett-Burman和Box-Behnken统计设计研究了五个参数:壳聚糖分子量,TPP浓度,C.VerumEO/壳聚糖比率,混合方法,以及反应的持续时间。封装效率和抗念珠菌活性被视为响应。抗菌,anticanddal,还使用标准微肉汤稀释测定法评估了抗利什曼虫活性,并针对巨噬细胞系RAW264.7评估了细胞毒性测定法。利用傅里叶变换红外光谱对优化后的纳米粒子进行了表征,Zeta电位,和扫描电子显微镜。研究结果表明,在最佳条件下,将C.verumEO纳米封装到壳聚糖纳米颗粒中导致92.58%的封装效率,有规律的分布,纳米颗粒尺寸为480±14.55nm,和35.64±1.37mV的良好Zeta电位。优化的C.verumEO/壳聚糖纳米颗粒对白色念珠菌病原体(CMI=125µgmL-1)具有很强的抗真菌活性,对革兰氏阳性和革兰氏阴性细菌具有显着的抗菌活性(范围为125至250µgmL-1),针对热带乳杆菌和主要乳杆菌的前鞭毛形式的高利什曼杀虫潜力(IC50分别为10.47和15.09µgmL-1),与未包封的精油相比,细胞毒性降低了四倍。这些结果表明,装载C.verumEO的壳聚糖纳米颗粒可能是用于治疗皮肤白色念珠菌感染的有前途的递送系统。
    Nanoencapsulation is widely considered as a highly effective strategy to enhance essential oils\' (EO) stability by protecting them from oxidative deterioration and evaporation. The present study aims to optimize and characterize an efficient technique for encapsulating Cinnamomum (C.) verum essential oil into chitosan nanoparticles using response surface methodology (RSM). Moreover, the optimized C. verum EO nanoparticle was investigated for its antibacterial (against Gram-positive and Gram-negative bacteria), antifungal (against Candida albicans), and antiparasitic activity (against Leishmania parasites). Five parameters were investigated using a Plackett-Burman and Box-Behnken statistical design: the chitosan molecular weight, TPP concentration, C. verum EO/chitosan ratio, mixing method, and the duration of the reaction. Encapsulation efficiency and anti-candida activity were considered as responses. The antibacterial, anticandidal, and anti-leishmanial activities were also assessed using a standard micro-broth dilution assay and the cytotoxicity assay was assessed against the macrophage cell line RAW 264.7. The optimized nanoparticles were characterized using Fourier transform infrared spectroscopy, Zeta potential, and scanning electron microscopy. The study results indicated that under optimal conditions, the nanoencapsulation of C. verum EO into chitosan nanoparticles resulted in an encapsulation efficiency of 92.58%, with a regular distribution, a nanoparticle size of 480 ± 14.55 nm, and a favorable Zeta potential of 35.64 ± 1.37 mV. The optimized C. verum EO/chitosan nanoparticles showed strong antifungal activity against C. albicans pathogens (CMI = 125 µg mL-1), notable antibacterial activity against both Gram-positive and Gram-negative bacteria (ranging from 125 to 250 µg mL-1), high leishmanicidal potential against the promastigotes form of L. tropica and L. major (IC50 = 10.47 and 15.09 µg mL-1, respectively), and a four-fold cytotoxicity reduction compared to non-encapsulated essential oil. These results suggest that C. verum EO-loaded chitosan nanoparticles could be a promising delivery system for the treatment of cutaneous Candida albicans infections.
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  • 文章类型: Journal Article
    葡萄果渣是酿酒的副产品,其特征是具有丰富的化学成分,酚类成分从中脱颖而出。酚类物质是健康促进剂,它们的有益效果取决于它们的生物可利用性,这是受胃肠道消化的影响。海藻酸钠(SA)包裹富含苯酚的葡萄果渣提取物(PRE)的效果,SA与明胶(SA-GEL)的混合物,研究了SA与壳聚糖(SA-CHIT)在体外模拟消化过程中对酚类物质的生物可及性指数(BI)的影响。通过UHPLC对总共27种单独的酚类化合物(IPC)进行定量。向SA中添加第二涂层提高了封装效率(EE),SA-CHIT微珠的EE最高(56.25%)。封装影响物理化学性质(尺寸,形状和纹理,形态学,结晶度)产生的微珠,这影响了酚类物质向肠道及其BI的递送。因此,SA-GEL微珠具有最大的尺寸参数,如扫描电子显微镜(SEM)所证实的,总酚类化合物和IPC的BI最高(没食子酸,3,4-二羟基苯甲酸和邻香豆酸,表儿茶素,和gallocatechin没食子酸酯)的范围为96.20至1011.3%。结果表明,封装的PRE具有很大的潜力,可用作口服产品的功能成分。
    Grape pomace is a by-product of winemaking characterized by a rich chemical composition from which phenolics stand out. Phenolics are health-promoting agents, and their beneficial effects depend on their bioaccessibility, which is influenced by gastrointestinal digestion. The effect of encapsulating phenol-rich grape pomace extract (PRE) with sodium alginate (SA), a mixture of SA with gelatin (SA-GEL), and SA with chitosan (SA-CHIT) on the bioaccessibility index (BI) of phenolics during simulated digestion in vitro was studied. A total of 27 individual phenolic compounds (IPCs) were quantified by UHPLC. The addition of a second coating to SA improved the encapsulation efficiency (EE), and the highest EE was obtained for SA-CHIT microbeads (56.25%). Encapsulation affected the physicochemical properties (size, shape and texture, morphology, crystallinity) of the produced microbeads, which influenced the delivery of phenolics to the intestine and their BI. Thus, SA-GEL microbeads had the largest size parameters, as confirmed by scanning electron microscopy (SEM), and the highest BI for total phenolic compounds and IPCs (gallic acid, 3,4-dihydroxybenzoic acid and o-coumaric acid, epicatechin, and gallocatechin gallate) ranged from 96.20 to 1011.3%. The results suggest that encapsulated PRE has great potential to be used as a functional ingredient in products for oral administration.
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