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COLLOIDS AND SURFACES B-BIOINTERFACES · 2024 · IF 5.4

Different mesoporous carbon carriers for the improvement of solubility and physical stability of poorly soluble drugs

Wei Gu,Qinfu Zhao,Ye He,Shengyu Wang,Yuanqi Yang,Yian Li,Shuaipeng Feng,Siling Wang

Mesoporous carriers have gained significant attention for enhancing the solubility and bioavailability of Biopharmaceutics Classification System (BCS) Class II drugs. However, the contribution of mesoporous carriers with varying morphologies to the physical stability of these drugs is not well-defined. In this work, mesoporous carbon nanoparticles (MCN) and hollow carbon mesoporous nanoparticles (HMC) were prepared, while the weakly acidic Indomethacin (IMC) and alkaline Celecoxib (CXB) were incorporated into these carriers in the amorphous state by the solvent evaporation method. Notably, HMC demonstrated superior drug loading efficiencies (approximately 43 %) for both IMC and CXB owning to its hollow structure. The mesoporous drug loading systems significantly enhanced dissolution rates in comparison with both self-made amorphous drugs and raw drugs. Furthermore, under accelerated and long-term storage conditions, the mesoporous carriers effectively prevented drugs loaded from crystallization, maintaining constant dissolution profiles for over 12 months. Intriguingly, CXB exhibited a slower rate of crystallization after loading into the mesoporous carriers, likely due to the formation of hydrogen bonds between the carbonaceous carrier material and the amino groups of CXB. Compared with loaded drugs, the self-made amorphous drugs exhibited a crystallinity increase beyond 60 % within the initial month. Collectively, these findings highlighted the potential of mesoporous carbon carriers to elevate the dissolution behaviors of BCS Class II drugs while preserving the physical stability of the loaded amorphous drugs.

研究领域: 药剂学 · 材料科学
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COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS · 2022 · IF 5.518

Physicochemical properties and aroma release of gelatin-stabilized rapeseed oil-in-water emulsions as affected by pH

Ying Xu,Xiaofei Xie,Chuankang Jia,Huimin Yan,Yalin Peng,Jun Qi,Guoyuan Xiong,Haiyue Xing,Xinglian Xu,Chen Cao

The release of volatile compounds in food processing is inevitable, and controlling aroma release is an important means of improving flavor quality. Herein, the physical stability and aroma release of 50 wt% rapeseed oil-in-water emulsions stabilized by 1 wt% gelatin at various pH levels were investigated in this study. Results showed that the emulsion prepared at pH 10 had a lower creaming index (CI), a smaller droplet size, a higher zeta potential value, and greater elasticity than that prepared at pH 4 and 7. Isobutanol , dimethyl sulfide , dimethyl sulfoxide , dimethyl sulfone , and γ-butyrolactone were detected in rapeseed oil but not in all emulsions. When the aqueous phase pH increased, the ability of emulsions to bind hydrophobic compounds increased significantly, while its ability to bind hydrophilic compounds with a density greater than water or less than oil decreased. The enhancement of the aroma-retention ability was due to an increase in the binding area between hydrophobic odorants and oil droplets, while the decrease in the aroma-retention ability was due to the hydrophilic properties of odorants, thin protein films , and density difference. This work explained the flavor release mechanism from the perspective of the hydrophobicity and density of volatile compounds and the interfacial protein films, which can provide certain theoretical and practical values for improving the flavor quality of broth products.

研究领域: 食品科学 · 化学
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EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS · 2022 · IF 5.589

Identification and characterization of chemical and physical stability of insulin formulations utilizing degraded glycerol after repeated use and storage

Min-Fei Sun,Youfu Xu,Jun-Jie Yuan,Wei-Jie Fang

Insulin treatment is currently considered to be the main strategy for controlling diabetes. Although the recombinant insulin formulation is relatively mature, we found that a batch of insulin formulation exhibited an unusual degradation rate in the stability experiment. The main purposes of this article are to identify the root cause for this phenomenon and characterize of chemical and physical degradation products. We compared the chemical and physical stability of two batches of insulin formulations prepared separately with simulated repeated use and freshly opened glycerol. The chemical stability of insulin was identified by liquid chromatography coupled with tandem mass spectrometry (LC- MS/MS). Micro-flow imaging (MFI), far-ultraviolet circular dichroism (Far-UV CD) and Thioflavin T (ThT) fluorescent assays were used to reveal protein aggregation and fibrosis . The chemical and physical stability of the insulin formulation with newly opened glycerol was much better than that with degraded glycerol, and both groups of formulations were extremely sensitive to light. The results indicated that the original batch insulin formulation with abnormal stability was indeed caused by the excipient glycerol after long-term storage and repeated usage. More attention should be paid to the quality changes of excipients during repeated usage and storage of excipients for the practical purpose. Moreover, we have discovered a novel degradation pathway for insulin and peptides in general. In addition, LC-MS/MS results suggested that the N-terminus of insulin B-chain was prone to chemical degradation which enlightens that it could be potentially modified to improve the stability of insulin formulations.

CAS / MDL: 540-69-2 75-05-8
研究领域: 药学 · 生物化学
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RSC Advances · 2016 ·Vol. 6 ·期 93 ·91060-91067 · IF 3.289

Investigation into the physical stability of a eugenol nanoemulsion in the presence of a high content of triglyceride

Huanle Chen,Xing Jin,Yan Li,Jing Tian

The physical stability of a eugenol (Eu) nanoemulsion in the presence of long-chain and medium-chain triglycerides with a high incorporation ratio (30 wt% to 80 wt% in the lipid phase) was investigated. The stability of the nanoemulsion was evaluated by dynamic light scattering and a centrifugal-force-based LUMi-Sizer. With an increase in the content of triglycerides, the particle size of the nanoemulsions decreased first and then increased. The variation pattern of the particle size in the presence of different contents of triglycerides formed a V-type shape. The presence of 60 wt% triglycerides resulted in the smallest particle size, which continued increasing within 28 days of storage. LUMi-Sizer analyses demonstrated that the instability of the nanoemulsion caused by the addition of 30–50 wt% of triglyceride was due to sedimentation of emulsion droplets. On the other hand, the instability caused by 60–80 wt% of triglyceride was due to the floating of emulsion droplets. The interfacial tension variation had the same trend as the particle size variation at the corresponding content of triglycerides. Thus the interfacial tension might be responsible for the triglyceride-caused instability of the Eu nanoemulsion.

CAS / MDL: 97-53-0
研究领域: 食品科学 · 化学工程
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2025 · IF 8.5

Physical stability improvement and digestion behavior evaluation of yogurt by incorporating cinnamaldehyde-loaded whey protein microcapsules

Yan Hu,Yaping An,Qingfeng Zhao,Cuie Tang,Shilin Liu,Bin Li,Yan Li,Seid Mahdi Jafari

An alternative approach to improve the physical stability of yogurt was developed by introducing cinnamaldehyde (CA)-loaded whey protein concentrate microcapsules (CA microcapsules). The effects of CA microcapsules on the physicochemical properties of whey protein-enriched set-yogurt during fermentation and post-ripening and the gastric digestion behavior were evaluated. The results showed that CA microcapsules were effective in controlling pH reduction during fermentation, mitigating post-acidification and enhancing gel density in yogurt. Addition of CA microcapsules (CA level at 0.25 % in oil phase) significantly improved the water holding capacity by 19 %, enhanced storage stability and preserved the activity of lactic acid bacteria (LAB). Digestion studies using in vitro dynamic human stomach model indicated that CA microcapsules had no effect on pH changes or microstructure during gastric digestion, promoted protein gastric emptying rate (89.29 %), increased the protein hydrolysis rate and provided a protective effect on LAB. Therefore, incorporation of flavor CA microcapsules can be a promising strategy to enhance the physical stability of yogurt.

研究领域: 食品科学 · 生物技术 · 营养学
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EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS · 2024 · IF 4.4

Nucleotides as new co-formers in co-amorphous systems: Enhanced dissolution rate, water solubility and physical stability

Xianzhi Liu,Luyan Shen,Lin Zhou,Wencheng Wu,Guang Liang,Yunjie Zhao,Wenqi Wu

Developing co-amorphous systems is an attractive strategy to improve the dissolution rate of poorly water-soluble drugs. Various co-formers have been investigated. However, previous studies revealed that it is a challenge to develop satisfied acidic co-formers, e.g., acidic amino acids showed much poorer co-former properties than neutral and basic amino acids. Only a few acidic co-formers have been reported, such as aspartic acid , glutamic acid , and some other organic acids . Thus, this study aims to explore the possibility of adenosine monophosphate and adenosine diphosphate used as acidic co-formers. Mebendazole, celecoxib and tadalafil were used as the model drugs. The drug-co-former co-amorphous systems were prepared via ball milling and confirmed using XRPD. The dissolution study suggested that the solubility and dissolution rate of the drug-co-formers systems were increased significantly compared to the corresponding crystalline and amorphous drugs. The stability study revealed that using the two nucleotides as co-formers enhanced the physical stability of pure amorphous drugs. Molecular interactions were observed in MEB-co-former and TAD-co-former systems and positively affected the pharmaceutical performance of the investigated co-amorphous systems. In conclusion, the two nucleotides could be promising potential acidic co-formers for co-amorphous systems.

研究领域: 药剂学 · 药物化学
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2016 · IF 3.138

Physical stability of R-(+)-Limonene emulsions stabilized by Ulva fasciata algae polysaccharide

Ping Shao,Huiling Ma,Qiang Qiu,Weiping Jing

The physical stability of R-(+)-Limonene emulsions stabilized by Ulva fasciata polysaccharide (UFP) was investigated in this study. Emulsion physical stability was evaluated under different polysaccharide concentrations (1%–5%, wt/wt) and pH values (3.0–11.0). The stability of R-(+)-Limonene emulsions was demonstrated by droplet size distribution, rheological properties, zeta potential and visual phase separation. R-(+)-Limonene emulsions displayed monomodal droplet size distributions, high absolute values of zeta potential and good storage stability when 3% (wt/wt) UFP was used. The rheological properties and stability of R-(+)-Limonene emulsions appeared to be dependent on polysaccharide concentration. The emulsion stability was impacted by pH. Higher zeta potential (−52.6   mV) and smaller mean droplet diameter (2.45   μm) were achieved in neutral liquid environment (pH 7.0). Extreme acidity caused the flocculation of emulsions, which was manifested as phase separation, while emulsions were quite stable in an alkaline environment. Through comparing the stabilities of emulsions stabilized by different emulsifiers (i.e. UFP, GA and Gelatin), the result suggested that UFP was the best emulsifying agent among them.

CAS / MDL: 5989-27-5
研究领域: 食品科学 · 生物化学
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KEY ENGINEERING MATERIALS · 2020 · IF 0

Types of Solid Lipids on Physical Stability of Resveratrol-Loaded Nanostructured Lipid Carriers

Benchawan Chamsai,Wipada Samprasit,Praneet Opanasopit,Pontip Benjasirimongkol,Pornsak Sriamornsak

Resveratrol (Res) loaded nanostructured lipid carriers (NLCs) were prepared by high shear homogenization and ultrasonication technique. Caprylic/capric glyceride (IM) was used as a liquid lipid, while glyceryl monostearate (GMS), beeswax (BW), palmitic acid (PA) and myristic acid (MA) at various concentrations (5, 10, 15, and 20 %w/w) were solid lipids. Polyoxyethylene 20 sorbitan monooleate or polysorbate 80 (Tween® 80) was use as a surfactant. The results showed that all concentration of PA and MA can be prepared the smaller particle NLC than that using GMS and BW according to the small molecule of MA and PA. The zeta potential of Res loaded NLCs were negative charge (-24.30 to -37.80 mV), which could be considered as a stable system. The stability studies revealed that NLCs with MA and PA showed a - high stability in particle size and zeta potential after storage at 40 ± 2°C /75 %RH for 3 months. These results suggested the MA and PA were suitable solid lipids for the NLCs preparation which have potential to be a nanoparticulate carrier for Res delivery.

研究领域: 药剂学 · 生物医学工程
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FOOD CHEMISTRY · 2020 · IF 6.306

Tannic acid enhanced the physical and oxidative stability of chitin particles stabilized oil in water emulsion

Fang Yang,Jinchu Yang,Si Qiu,Wei Xu,Yuntao Wang

In this work, the stability of CP-TA complex stabilized emulsion was first characterized. It was found that the peak thickness, Turbiscan Stability Index (TSI) and droplet size of CP-TA complex stabilized emulsion gradually decreased with increasing content of TA, indicating the gradually enhanced physical stability of emulsion, which was attributed to the gradually decreased interfacial tension, zeta potential and increased viscosity of CP-TA complex. Moreover, the oxidative stability of CP-TA complex stabilized emulsion gradually enhanced with increasing of TA content due to the antioxidant activity of TA. XRD and FTIR results suggested that the interaction between CP and TA gradually enhanced with increasing content of TA in CP-TA complex, leading to the formation of larger CP-TA clusters shown in AFM results. In conclusion, the presence of tannic acid (TA) enhanced the physical and oxidative stability of chitin particles-tannic acid (CP-TA) complex stabilized oil in water emulsion.

研究领域: 食品科学 · 生物化学
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FOOD CHEMISTRY · 2020 · IF 6.306

Effect of enzymatic degraded polysaccharides from Enteromorpha prolifera on the physical and oxidative stability of fish oil-in-water emulsions

Mei-Jia Shi,Fan Wang,Hui Jiang,Wen-Wen Qian,Yuan-Yuan Xie,Xiao-Yi Wei,Tao Zhou

To explore the potential application of enzymatic degraded polysaccharides from Enteromorpha prolifra (EEP) as antioxidant in fish oils, a stable fish oil emulsion system incorporating EEP was established. Effects of emulsifier (Tween 80, gum arabic and lecithin) and EEP concentration on the physical characteristics of fish oil emulsions were investigated. The results indicated that Tween 80 was the best choice, and 1% (w/w) of EEP was the optimum concentration for the preparation of fish oil emulsions. Influence of EEP on the oxidative stability and physical stability of fish oil emulsions was compared with that of antioxidants V E and TBHQ by determining the physical properties, lipid hydroperoxide formation, secondary reaction products formation, pH and long chain polyunsaturated fatty acid content, during storage at 45 °C. The results indicated that the fish oil emulsion system (5% oil, 1% EEP and 1% Tween 80, w/w) possessed good physical and oxidative stabilities.

研究领域: 食品科学 · 生物化学
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Food Bioscience · 2022 · IF 5.318

Characterization of physically stable oleogels transporting active substances rich in resveratrol

Kexin Qu,Hongtu Qiu,Hua Zhang,Xingfu Yin

Oleogels, substances that have a liquid phase of continuous oil, are being explored as a potential substitute for trans fatty acids and saturated fatty acids in food. To develop more stable and nutritious alternative lipids using blueberry extract, oleogels loaded with resveratrol (R) and blueberry extract were prepared using soybean oil (SO) and peanut oil (PO) as base oils, and β-sitosterol and lecithin as low-molecular-weight complex oleogelators. Microstructural characterization of oleogels showed that R-loaded and R-enriched blueberry extracts maintained the degree of cross-linking between oleogel crystal units to a certain extent as well as maintained or improved the mouthfeel and hardness of the oleogels. Differential scanning calorimetry and rheometric results demonstrated that the R-loaded ternary oleogels had good thermal stability and strength. With prolonged storage, the physical stability of peanut oil oleogels (POO) was better than that of soybean oil oleogels (SOO). In addition, in vitro simulation experiments revealed that the oleogels could better serve as a carrier for R but could inhibit their bioavailability in R-loaded oleogels.

研究领域: 食品科学 · 营养学
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LWT-FOOD SCIENCE AND TECHNOLOGY · 2020 · IF 4.006

Physical and bloom stability of low-saturation chocolates with oleogels based on different gelation mechanisms

Linlin Li,Guoqin Liu,Yunwei Lin

Oleogels are being increasingly used as solid fat alternatives in food . Low-saturation chocolates (referring to chocolates with low content of saturated fat) were prepared by replacing 50 g/100 g cocoa butter with three oleogels (monoglyceric stearate, β-sitosterol +  lecithin , and ethyl cellulose oleogel), which were fabricated through different gelation mechanisms (crystalline particles, self-assembly fibers, and polymeric strands, respectively). The physical characteristics and microstructures of oleogel-based chocolates during isothermal (4 and 20 °C) and fluctuating (20 °C for 17 h and 29 °C for 7 h) storage conditions were evaluated for 60 d, including whiteness index, hardness, thermal behavior, and crystal polymorph. We found that oleogel-based chocolates exhibited bloom delaying property through assessing whiteness index and polarized light microscopy images, especially under fluctuating temperatures. Among three oleogel-based chocolates, β-sitosterol + lecithin oleogel-based chocolate maintained the lowest whiteness index. Differential scanning calorimetry and X-ray diffraction revealed that oleogel-based chocolates showed sustained thermal and polymorphic stability throughout the storage period. Crystal morphology of fat phase observed by polarized light microscopy confirmed the existence of stable β crystals in oleogel-based chocolates. Collectively, oleogel-based chocolates not only lower the degree of saturation but also exhibit high physical and bloom stability during isothermal and fluctuating storage.

研究领域: 食品科学 · 材料科学
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