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Atovaquone smart lipid system: Design, statistical optimization, and in-vitro evaluation 阿托伐酮智能脂质系统:设计,统计优化和体外评估
IF 1.9 Q1 CHEMISTRY, APPLIED Pub Date : 2023-07-22 DOI: 10.1016/j.fhfh.2023.100144
Hardik Rana, Drashti Patel, Vaishali Thakkar, Tejal Gandhi

The research was undertaken to design, develop and characterize the smart lipid system of an inadequate bioavailable Atovaquone (ATQ). The poor aqueous solubility and dissolution are the major constrain of inadequate bioavailability. The solubility study reveals that Labrasol-ALF (L-ALF), Tween 80, and Trancutol®P (TP) were screened as oil, surfactant, and co-surfactant, respectively. The pseudo ternary diagram was constructed to locate the appropriate amount of each ingredient, and a 1:3:1 ratio of l-ALF: Tween 80: TP was chosen. The effect of precipitation inhibitor was assessed using the parachute effect. Soluplus® (SP) was chosen as a precipitation inhibitor at 5%. Ishikawa diagram and qualitative risk assessment were performed to screen the critical material attributes (CMAs) and critical process parameters (CPPs). d-optimal mixture design was explored for the optimization of the formulation. The amount of oil, surfactant, and co-surfactant was screened as independent variables, whereas globule size, poly-dispersibility index (PDI), and solubility were designated dependent variables. The design batches were evaluated for the in-vitro dissolution rate, PDI, zeta potential, globule size, etc. The optimal region was located using an overlay plot. The optimized formulation has shown a 97.91% drug release within 1 h. The value of zeta potential (-27.43 mV) and PDI (0.468) indicates the stability of the formulation. The parachute effect had explored for the selection of precipitation inhibitors. SP was able to increase the solubility of ATQ and reduce the precipitation of the drug. The amount of l-ALF, Tween, 80and TP was significant for the formulation of SNEDDS. The formulation was novel, effective, patient-friendly, and industry oriented.

本研究旨在设计、开发和表征一种生物利用度不足的阿托伐醌(ATQ)的智能脂质系统。水溶性和溶解性差是生物利用度不足的主要制约因素。溶解度研究表明,Labrasol-ALF (L-ALF)、Tween 80和Trancutol®P (TP)分别被筛选为油脂、表面活性剂和助表面活性剂。通过拟三元图确定各成分的适宜用量,选择l-ALF: Tween 80: TP的比例为1:3:1。利用降落伞效应评价了沉淀抑制剂的效果。选择Soluplus®(SP)作为5%的沉淀抑制剂。采用石川图和定性风险评估筛选关键材料属性(cma)和关键工艺参数(CPPs)。采用d-最优配合比设计进行配方优化。将油量、表面活性剂和助表面活性剂作为自变量,而将球粒径、多分散性指数(PDI)和溶解度作为因变量。对设计批进行体外溶出度、PDI、zeta电位、微球大小等评价。利用叠加图确定最优区域。优化后的制剂在1 h内释药率为97.91%。zeta电位(-27.43 mV)和PDI(0.468)值表明该制剂具有较好的稳定性。探讨了降落伞效应对沉淀抑制剂选择的影响。SP能增加ATQ的溶解度,减少药物的沉淀。l-ALF、Tween、80和TP的添加量对SNEDDS的制备有显著影响。该配方新颖、有效、对患者友好、面向行业。
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引用次数: 0
Fabrication of rice bran oil nanoemulsion and conventional emulsion with Mustard Protein Isolate as a novel excipient: Focus on shelf-life stability, lipid digestibility and cellular bioavailability 以芥菜分离蛋白为辅料制备米糠油纳米乳和常规乳剂:研究其保质期稳定性、脂质消化率和细胞生物利用度
IF 1.9 Q1 CHEMISTRY, APPLIED Pub Date : 2023-07-20 DOI: 10.1016/j.fhfh.2023.100143
Trina Das , Niloy Chatterjee , Amrita Chakraborty , Arpita Banerjee , Sudip Baran Haiti , Sriparna Datta , Helen Chattopadhyay , Pubali Dhar

Proteins are one of the many effective biomolecules found in oilseed meals. In order to formulate an oil-in-water nanoemulsion based lipophilic nutraceutical delivery vehicle for Rice Bran oil (RBO) rich in γ-oryzanol, we used mustard seed meal protein isolate (MPI) as a novel natural surfactant together with a small molecular weight co-surfactant Tween 20 in various ratios (3:1, 1:1, 1:3) to stabilize the heterogeneous system. The oxidative stability, physico-chemical characterization in response to pH and ionic strength, shelf-life, and storage of the nanoemulsions containing 1% surfactant in total, comprising different ratios of MPI and Tween 20 were optimised to form an efficient biphasic surfactant system. The oil-in-water nanoemulsions fabricated utilizing high energy approach, i.e. high pressure homogenisation method was found to reduce dispersed phase particles size in the range of 150–160 nm. Minimal non-significant variation in droplet size and surface charge over the 8 weeks storage periods proves their excellent shelf-life stability. The use of MPI as surfactant for the delivery system also increased the lipid fraction digestibility releasing 70% of the fatty acids from dispersed phase oil droplets in simulated intestinal phase of three step in vitro digestion of nanoemulsion as compared to its conventional counterpart. The γ-oryzanol rich nanoemulsions improved prophylactic effectiveness against ROS in terms of overall cell survival and cell membrane integrity. The results will pave new domains to use MPI as surface active agents for delivery system formulation enriched with nutraceuticals and phytochemicals possessing superior functional advantages, bioavailability and antioxidative potentials.

蛋白质是油籽粕中发现的许多有效生物分子之一。为了制备富含γ-米甲醇的米糠油(RBO)的亲脂性水包油纳米乳剂,以芥菜粕分离蛋白(MPI)为新型天然表面活性剂,与小分子量助表面活性剂Tween 20按不同比例(3:1、1:1、1:3)稳定非均相体系。优化了表面活性剂含量为1%的纳米乳(MPI和Tween 20的不同配比)的氧化稳定性、理化性质对pH和离子强度的响应、保质期和储存期的影响,以形成高效的双相表面活性剂体系。利用高能方法,即高压均质法制备的水包油纳米乳液,在150-160 nm范围内减小了分散相颗粒尺寸。在8周的储存期内,液滴大小和表面电荷的变化极小,证明了它们具有良好的货架寿命稳定性。使用MPI作为表面活性剂的传递系统也提高了脂质部分的消化率,在模拟肠相三步体外消化纳米乳的分散相油滴中释放了70%的脂肪酸。富含γ-谷米醇的纳米乳在整体细胞存活和细胞膜完整性方面提高了对ROS的预防效果。研究结果将为MPI作为表面活性剂的应用开辟新的领域,这些表面活性剂富含营养药品和植物化学物质,具有优越的功能优势、生物利用度和抗氧化潜力。
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引用次数: 2
Acute and subacute in vivo safety assessment of developed chitosan derivatives for food applications 用于食品应用的壳聚糖衍生物的急性和亚急性体内安全性评估
IF 1.9 Q1 CHEMISTRY, APPLIED Pub Date : 2023-07-20 DOI: 10.1016/j.fhfh.2023.100145
T.P. Punarvasu, K.V. Harish Prashanth

The acute and subacute studies of two chitosan derivatives was conducted by oral administration on Swiss albino mice. Chitosan soluble derivatives were prepared by depolymerization method using potassium persulfate. 13C NMR data have revealed that Low Molecular Weight Chitosan (LMWC) has higher (∼70%) ‘acetylated’ residues and Self Assembled Chitosan Microparticles (SAMC) consists of ‘deacetylated’ residues. For acute toxicity study, a single dose of two concentrations 2000 and 5000 mg/kg bw of the chitosan derivatives (LMWC, or SAMC) was given orally to healthy mice. Results indicated that the LD50 value for chitosan derivatives was greater than 5000 mg/kg bw. In the sub-acute toxicity studies, administration of concentrations 1000 and 2000 mg/kg bw dose of chitosan derivatives (repeated daily dose for 28 days) also did not reveal any toxicological changes in clinical observations, viz. relative organs, body weight, food consumption, biochemical parameters studied, antioxidant markers, and histopathological studies has been compared with control group. Together, present systematic study supports the oral administration of non-viscous and soluble chitosan derivatives (LMWC & SAMC) will have no toxicity may be safe to use in food and pharma applications.

通过口服两种壳聚糖衍生物对瑞士白化小鼠的急性和亚急性作用研究。采用过硫酸钾解聚法制备壳聚糖可溶性衍生物。13C核磁共振数据表明,低分子量壳聚糖(LMWC)具有较高(~ 70%)的乙酰化残基,而自组装壳聚糖微粒(SAMC)由“去乙酰化”残基组成。在急性毒性研究中,健康小鼠口服两种浓度(2000和5000 mg/kg bw)的壳聚糖衍生物(LMWC或SAMC)。结果表明,壳聚糖衍生物的LD50值大于5000 mg/kg bw。在亚急性毒性研究中,给药浓度为1000和2000 mg/kg bw的壳聚糖衍生物(每天重复给药28天)在临床观察中也没有发现任何毒理学变化,即相对器官,体重,食物消耗,研究的生化参数,抗氧化标志物和组织病理学研究与对照组相比。总之,本系统研究支持口服无粘性和可溶性壳聚糖衍生物(LMWC &SAMC)将没有毒性,可安全用于食品和制药应用。
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引用次数: 0
Liposome mediated encapsulation and role of chitosan on modulating liposomal stability to deliver potential bioactives-A review 脂质体介导的包封及壳聚糖在调节脂质体稳定性传递潜在生物活性中的作用综述
IF 1.9 Q1 CHEMISTRY, APPLIED Pub Date : 2023-06-23 DOI: 10.1016/j.fhfh.2023.100142
Jean Mary Joy , Amruth P , Rosemol Jacob M , Pavan Kumar Dara , V. Renuka , R. Anandan

Liposomes are amphiphilic structures widely explored for the encapsulation of various active ingredients in the area of pharmaceutics, cosmetics and numerous others. Wherein, the conventional liposomal structure is found to possess certain drawbacks with regard to their stability and release kinetics of active ingredients. Chitosan is a natural polysaccharide that exhibits structural stability, excellent biocompatibility, biodegradability, flexibility, non-immunogenicity and targetability. Coating of chitosan to liposomes have found to modulate the bio functionality of liposome vesicles in terms of stability and release kinetics and therefore chitosan coated liposomes (chitosomes) remain as efficient carrier to transport potential bioactives to the targeted sites effectively. This review highlights the liposomal mediated encapsulation methods and induces insights to employ modulation of liposomal stability by chitosan coating to liposomes for the facile transport of active ingredients for multiple applications.

脂质体是两亲性结构,在制药、化妆品和许多其他领域被广泛探索用于封装各种活性成分。其中,发现常规脂质体结构在活性成分的稳定性和释放动力学方面具有某些缺点。壳聚糖是一种天然多糖,具有结构稳定性、良好的生物相容性、生物降解性、柔韧性、非免疫原性和靶向性。壳聚糖与脂质体的包被已发现在稳定性和释放动力学方面调节脂质体囊泡的生物功能,因此壳聚糖包被的脂质体(壳体)仍然是将潜在的生物活性物质有效转运到靶位点的有效载体。这篇综述强调了脂质体介导的包封方法,并引入了通过壳聚糖涂层调节脂质体稳定性的见解,以便于将活性成分运输到多种应用中。
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引用次数: 1
Real time microcalorimetric profiling of prebiotic inulin metabolism 益生元菊糖代谢的实时微热量分析
IF 1.9 Q1 CHEMISTRY, APPLIED Pub Date : 2023-06-10 DOI: 10.1016/j.fhfh.2023.100141
Mansa Fredua-Agyeman , Simon Gaisford

The in vitro assessment of prebiotics involves elaborate microbiological techniques or a combination of culture techniques and molecular methods. In this study, the isothermal microcalorimeter, an instrument which can monitor the real time growth of bacteria was applied to investigate the prebiotic effect of inulin in real time. Fresh and standardized frozen faecal slurries were prepared, placed and monitored in the isothermal microcalorimeter. The faecal samples and commercial probiotic strains Lactobacillus acidophilus LA-5®, Bifidobacterium lactis BB-12® were cultured in a mixed medium of cooked meat medium (CMM) and brain heart infusion (BHI) broth with and without supplementation with inulin and monitored in the microcalorimeter. The results showed power-time (p-t) curves that were characteristic for the samples. The p-t curves of the fresh and frozen faecal samples were similar. Augmented microbial activity was observed when the faecal sample was inoculated into CMM-BHI mixed broth with significant enhancement of microbial activity detected in the presence of inulin which was reproducible. Deconvoluted p-t curves showed multiple peaks with time and intensity variance depending on presence or absence of inulin suggesting possible differences in utilization of inulin by the different groups of bacteria in the polymicrobial sample. P-t curves of the pure species did not show any significant change when inulin was supplemented into the medium likely due to the inability of the bacteria to primarily utilize inulin.

益生元的体外评估涉及精细的微生物技术或培养技术与分子方法的结合。本研究采用可实时监测细菌生长的等温微量热量计,实时研究菊粉的益生元作用。制备新鲜和标准化的冷冻粪便浆,放置在等温微量热量计中并进行监测。将粪便样品和商业益生菌菌株嗜酸乳杆菌LA-5®、乳酸双歧杆菌BB-12®在添加和不添加菊粉的熟肉培养基(CMM)和脑心浸液(BHI)肉汤的混合培养基中培养,并在微量热量计中监测。结果显示了功率-时间(p-t)曲线,这是样品的特征。新鲜和冷冻粪便样品的p-t曲线相似。当将粪便样品接种到CMM-BHI混合肉汤中时,观察到微生物活性增强,在菊粉存在下检测到的微生物活性显著增强,这是可重复的。去卷积的p-t曲线显示出多个峰值,其随时间和强度的变化取决于菊粉的存在与否,这表明多微生物样品中不同细菌组对菊粉的利用可能存在差异。当菊粉被补充到培养基中时,纯物种的P-t曲线没有显示出任何显著的变化,这可能是由于细菌不能主要利用菊粉。
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引用次数: 0
Pairing physical and sensory properties of dysphagia thickeners to understand disliking 结合吞咽困难增稠剂的物理和感官特性来理解厌恶
IF 1.9 Q1 CHEMISTRY, APPLIED Pub Date : 2023-05-23 DOI: 10.1016/j.fhfh.2023.100140
R. Baixauli, A. Dobiašová, A. Tarrega, L. Laguna

Patients with dysphagia who adhere to drinking thickened water is still a challenge, as patients dislike it and it does not quench their thirst. The objective of this study was to relate the physical properties of six commercial thickeners based on gums, modified starch, or mixtures of modified starch and gums, to sensory characteristics and the liking and refreshing sensation. Therefore, viscosity, friction, adhesiveness, and firmness were obtained for all thickeners with and without artificial saliva. Sensory attributes for the six thickeners were obtained using the Flash Profile method; furthermore, acceptance and refreshing sensation were also studied. The results showed that high viscous thickeners without particle presence were preferred. These thickeners were gum-based and starch-dispersed, which were described as providing a viscous and smooth texture and being tasteless. Starch-based thickeners with starch granules with integrity had lower preference than gum-based or starch-dispersed thickeners, and were described as having a sandy and fluid texture, with an intense starch taste and aftertaste. Among the preferred thickeners (gum-based thickeners and starch-dispersed thickeners), a lower friction coefficient was related to a higher refreshing sensation, probably caused by a short oral residence.

吞咽困难的患者坚持喝加厚的水仍然是一个挑战,因为患者不喜欢它,而且它不能解渴。本研究的目的是将六种以胶、变性淀粉或变性淀粉与胶的混合物为基础的商用增稠剂的物理特性与感官特性、口感和爽口感联系起来。因此,所有增稠剂在有和没有人工唾液的情况下都获得了粘度、摩擦力、粘附性和硬度。利用Flash剖面法获得了6种增稠剂的感官属性;此外,还研究了接受感和新鲜感。结果表明,无颗粒存在的高粘性增稠剂是优选的。这些增稠剂是胶基和淀粉分散的,被描述为提供粘性和光滑的质地,无味。具有完整淀粉颗粒的淀粉基增稠剂比胶基或淀粉分散增稠剂更低,并且被描述为具有沙质和流体质地,具有强烈的淀粉味和余味。在首选的增稠剂(牙龈基增稠剂和淀粉分散增稠剂)中,摩擦系数越低,清爽感越高,这可能是由于口腔停留时间较短所致。
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引用次数: 2
Ovalbumin and sodium alginate complex coacervates as delivery system of β-carotene: Formation, characterization, and cookies fortification 卵清蛋白和海藻酸钠复合物凝聚作为β-胡萝卜素递送系统:形成、表征和饼干强化
IF 1.9 Q1 CHEMISTRY, APPLIED Pub Date : 2023-05-22 DOI: 10.1016/j.fhfh.2023.100139
Alan Marques Farias , Augusto Bene Tomé Constantino , Edwin Elard Garcia-Rojas

β-carotene (βC) is a liposoluble natural pigment important for human health due to their antioxidant and provitamin A activities but presents high chemistry instabilities which increases their oxidation in the presence of light, oxygen, high temperatures and low pHs. This research aimed to microencapsulate βC by complex coacervation of ovalbumin (OVA) and sodium alginate (NaAlg). The microencapsulation technique was employed at pH=4.0 and 8:1 OVA/NaAlg (w/w) ratio, after confirming their affinity with zeta potential, state diagram, turbidity, and isothermal trituration calorimetry analyses. The obtained microcapsules presented spherical morphology with well-defined core and high encapsulation efficiency (97.90%). The presence of OVA, NaAlg and βC in microcapsules was confirmed by the Fourier transformed infrared analyses. The in vitro simulation of the gastrointestinal digestion of the microcapsules revealed that 71.39% of microencapsulated βC was released in the intestines with 32.78% of bioaccessibility. The release kinetics of encapsulated βC demonstrated that the βC release mechanism occurs by Fickian diffusion. The addition of βC microcapsules in cookies improved by 2-fold the antioxidant activities compared to free βC microcapsules cookies. These results suggest that βC microcapsules formed by complex coacervation of OVA/NaAlg can be added efficiently in the fortification of cookies.

β-胡萝卜素(βC)是一种脂溶性天然色素,由于其抗氧化和维生素a原活性,对人类健康很重要,但具有很高的化学不稳定性,在光、氧、高温和低ph值存在下会增加其氧化。本研究旨在通过卵清蛋白(OVA)与海藻酸钠(NaAlg)的复合凝聚,实现βC的微胶囊化。在pH=4.0和OVA/NaAlg (w/w)比为8:1的条件下,通过zeta电位、状态图、浊度和等温营养量热分析证实了微胶囊技术的亲和力。所制得的微胶囊呈球形,芯部清晰,包封率高(97.90%)。傅里叶变换红外分析证实微胶囊中存在OVA、NaAlg和βC。体外胃肠消化模拟实验表明,微囊化βC在肠道内的释放量为71.39%,生物可及度为32.78%。包封βC的释放动力学表明βC的释放机制为菲克扩散。添加βC微胶囊后,饼干的抗氧化活性比未添加βC微胶囊的饼干提高2倍。上述结果表明,OVA/NaAlg复合凝聚形成的βC微胶囊可以有效地添加到饼干的强化中。
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引用次数: 1
Trends in starch-based edible films and coatings enriched with tropical fruits extracts: a review 富含热带水果提取物的淀粉基可食用薄膜和涂料的发展趋势
IF 1.9 Q1 CHEMISTRY, APPLIED Pub Date : 2023-05-20 DOI: 10.1016/j.fhfh.2023.100138
María Gabriela Kupervaser , Maria Victoria Traffano-Schiffo , María Luciana Dellamea , Silvia Karina Flores , Carola Andrea Sosa

Petroleum-based food packaging materials are non-degradable and considerably affect the environment. In this context, edible films and coatings for food preservation represent a feasible alternative that could potentially reduce conventional non-biodegradable materials. It has been shown the suitability of starch as a non-toxic, widely available, low-cost and adequate film-forming biopolymer. In addition, natural compounds contained in tropical fruits are of great interest due to their proven antioxidant and antimicrobial properties, which are beneficial for the health of consumers and for obtaining more stable and safe foods. This review focuses on the new trends and benefits of incorporating tropical fruit extracts into starch-based edible films and coatings formulations as a source of bioactive compounds. The starch and fruit resources, extraction techniques, filmmaking methods, assays for determining functional properties and the potential uses of edible films and coatings in the food industry were stated and described.

石油基食品包装材料是不可降解的,对环境影响很大。在这种情况下,用于食品保存的可食用薄膜和涂层代表了一种可行的替代方案,可以潜在地减少传统的不可生物降解材料。淀粉已被证明是一种无毒、广泛可用、低成本和适宜成膜的生物聚合物。此外,热带水果中所含的天然化合物因其经证实的抗氧化和抗菌特性而引起极大的兴趣,这有利于消费者的健康,并有助于获得更稳定和安全的食品。本文综述了将热带水果提取物加入淀粉基可食用薄膜和涂层中作为生物活性化合物来源的新趋势和益处。介绍了可食性薄膜和涂层的淀粉和果实资源、提取技术、成膜方法、功能特性测定方法以及在食品工业中的潜在用途。
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引用次数: 2
Designing biphasic gels from dietary fiber sterculia gum by green approach using high energy radiation for biomedical applications 利用高能辐射的绿色方法设计膳食纤维球藻胶双相凝胶用于生物医学应用
IF 1.9 Q1 CHEMISTRY, APPLIED Pub Date : 2023-05-06 DOI: 10.1016/j.fhfh.2023.100137
Baljit Singh, Vikrant Sharma, Rajender Kumar, Diwanshi Sharma

Polysaccharides have been applied in food and biomedical applications. Bioactive dietary fiber sterculia gum (SG) has been used for treatment of diarrhea. Therefore, in present research, SG has been used for development of drug delivery (DD) system for controlled release of metronidazole to improve its pharmacotherapy for amoebic dysentery. Co-polymers were characterized by Cryo-scanning electron microscopy (Cryo-SEM), atomic force microscopy (AFM), Fourier transform infrared (FTIR) spectroscopy, 13C nuclear magnetic resonance (NMR) spectroscopy,), X-ray diffraction (XRD), thermo gravimetric analysis (TGA) and differential scanning calorimetry (DSC). Haemolytic index values of grafted product was less than 5 percent and DPPH assay illustrated free radical scavenging of hydrogels and bigels 74.00 ± 0.003% and 47.00 ± 0.005% respectively. Mucoadhesion experiment demonstrated that both hydrogels and bigels exhibited adhesion with intestinal mucus membrane required 0.034 ± 0.004 and 0.037 ± 0.002 N detachment force during mucoadhesion test. Diffusion of metronidazole was slow in sustained manner with Fickian diffusion mechanism. Overall results revealed biocompatible, antioxidant, and mucoadhesive properties of sterculia gum based gels which may be useful for DD applications of gastrointestinal infections.

多糖已被应用于食品和生物医学领域。生物活性膳食纤维胆胶(SG)已被用于治疗腹泻。因此,本研究利用SG开发甲硝唑控释给药系统,以改善甲硝唑治疗阿米巴痢疾的药物治疗效果。采用低温扫描电镜(cro - sem)、原子力显微镜(AFM)、傅里叶变换红外(FTIR)光谱、13C核磁共振(NMR)光谱、x射线衍射(XRD)、热重分析(TGA)和差示扫描量热法(DSC)对共聚物进行了表征。接枝产物的溶血指数值小于5%,DPPH测定显示水凝胶和凝胶的自由基清除率分别为74.00±0.003%和47.00±0.005%。黏附实验表明,水凝胶和凝胶均与肠粘膜发生黏附,黏附试验时分别需要0.034±0.004和0.037±0.002 N的剥离力。甲硝唑的扩散持续缓慢,具有菲克扩散机制。结果表明,该凝胶具有生物相容性、抗氧化性和黏附性,可用于胃肠道感染的治疗。
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引用次数: 1
Evaluation of liposomal hydrocolloidal NPs loaded by tea tree oil as antifungal agent in vitro and in vivo investigations: Preclinical studies 茶树油负载的脂质体水胶体NPs作为体外和体内抗真菌剂的评价:临床前研究
IF 1.9 Q1 CHEMISTRY, APPLIED Pub Date : 2023-04-30 DOI: 10.1016/j.fhfh.2023.100136
Ahmed M. Abd El- Salam , Amin Tahoun , Nemany A.N. Hanafy

Fungi have a great ability and a wide variety of mechanisms to endure the toxicity of current antifungal agents. Researchers are working to find new therapeutic agents to combat the resistance ability of fungi. Almost all commercial antifungal agents have a wide variety of side effects on human health. This study aims to introduce tea tree oil nanoparticles as antifungal delivery termed TNSAD, which contains hybrid tea tree oil attached chitosan in a liposomal formulation, and assess its antifungal activity using in vitro and in vivo infection models. Tea tree oil was first coated by chitosan, then inserted inside liposomal bilayers, and finally functionalized by a layer of chitosan, forming the TNSAD. The antifungal activity was evaluated against four different invasive, opportunistic, and zoonotic fungal pathogens (Aspergillus flavus, Aspergillus fumigatus, Microsporum gypsum, and Fusarium oxysporum). The cytotoxicity of TNSAD was then tested against the HEp-2 cell line. Finally, the antifungal activity against Aspergillus fumigatus and Microsporum gypsum was assessed in vivo in a rat model. The in vitro results confirm the potency of TNSAD against fungi and its safety at a concentration of ≤ 5 mg/ml. In vivo results revealed that fungal cells were destroyed within the tissue when used systematically. we have described here a natural remarkable design that represents a potential antifungal agent and provided evidence for its efficiency and safety, which makes it a promising antifungal agent for the treatment of systemic and topical fungal infections.

真菌具有强大的能力和多种机制来承受当前抗真菌药物的毒性。研究人员正在努力寻找新的治疗药物来对抗真菌的抗药性。几乎所有的商业抗真菌剂对人体健康都有各种各样的副作用。本研究旨在引入茶树油纳米颗粒作为抗真菌递送剂,即TNSAD,该纳米颗粒在脂质体中含有混合茶树油和壳聚糖,并通过体外和体内感染模型评估其抗真菌活性。茶树油先被壳聚糖包被,然后插入到脂质体双层中,最后被一层壳聚糖功能化,形成TNSAD。对四种不同的侵袭性、机会性和人畜共患性真菌病原体(黄曲霉、烟曲霉、石膏小孢子菌和尖孢镰刀菌)的抗真菌活性进行了评估。然后检测TNSAD对HEp-2细胞株的细胞毒性。最后,在大鼠体内模型中评价其对烟曲霉和小孢子菌的抗真菌活性。体外实验结果证实了TNSAD对真菌的抑菌作用和浓度≤5 mg/ml时的安全性。体内实验结果显示,当系统使用时,真菌细胞在组织内被破坏。我们在这里描述了一种天然的显著设计,它代表了一种潜在的抗真菌药物,并为其有效性和安全性提供了证据,这使得它成为治疗全身和局部真菌感染的有前途的抗真菌药物。
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引用次数: 2
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Food Hydrocolloids for Health
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