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BIOLOGICAL & PHARMACEUTICAL BULLETIN · 2015 ·Vol. 38 ·期 10 ·1658-1662 · IF 1.828

Pomegranate Seed Oil Exerts Synergistic Effects with trans-Resveratrol in a Self-nanoemulsifying Drug Delivery System

Lu-yang Lu,Yuan Liu,Zhi-feng Zhang,Xiao-jun Gou,Jun-hao Jiang,Ji-zhong Zhang,Qian Yao

Pomegranate seed oil (PSO) has diverse bioactivities. It was hyphothesized that if PSO were employed to construct a trans-resveratrol-loaded self-nanoemulsifying drug delivery system (RES SNEDDS-PSO), not only could PSO serve as an oil phase but also exert synergistic effects with resveratrol to yield better therapeutic outcomes. In this study, we prepared RES SNEDDS-PSO for the first time to validate that hypothesis. The anti-inflammatory and anticancer activities of RES SNEDDS-PSO were compared with another SNEDDS composed of oil phase isopropyl palmitate (RES SNEDDS-IP). The results showed that upon exposure to a 10-fold amount of water, RES SNEDDS-PSO was converted into nanoemulsions with a mean size of 44 nm. Nanoemulsions enhanced the water solubility of resveratrol by 20-fold, significantly improved resveratrol stability in intestinal fluid, and slowed the decomposition of resveratrol in water by 1-fold. An in vivo anti-infection test showed that the degree of inflammatory swelling in mice given RES SNEDDS-PSO was only 60 and 76% that of the group fed with RES SNEDDS-IP at doses of 10 and 20 mg/kg, respectively. An in vitro anticancer study showed that the inhibitory rate of RES SNEDDS-PSO against MCF-7 breast cancer cells was 2.03- and 1.24-fold that of RES SNEDDS-IP at a concentration of 12.5 and 25 µg/mL, respectively. This study demonstrated that the newly developed SNEDDS may be a prospective formulation in the functional food and clinical fields.

研究领域: 药剂学 · 生物医学 · 食品科学
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Nanomaterials · 2020 ·Vol. 10 ·期 10 ·2058 · IF 4.324

Perfluoropolyether Nanoemulsion Encapsulating Chlorin e6 for Sonodynamic and Photodynamic Therapy of Hypoxic Tumor

Liang Hong,Artem M. Pliss,Ye Zhan,Wenhan Zheng,Jun Xia,Liwei Liu,Junle Qu,Paras N. Prasad

Sonodynamic therapy (SDT) has emerged as an important modality for cancer treatment. SDT utilizes ultrasound excitation, which overcomes the limitations of light penetration in deep tumors, as encountered by photodynamic therapy (PDT) which uses optical excitations. A comparative study of these modalities using the same sensitizer drug can provide an assessment of their effects. However, the efficiency of SDT and PDT is low in a hypoxic tumor environment, which limits their applications. In this study, we report a hierarchical nanoformulation which contains a Food and Drug Administration (FDA) approved sensitizer chlorin, e6, and a uniquely stable high loading capacity oxygen carrier, perfluoropolyether. This oxygen carrier possesses no measurable cytotoxicity. It delivers oxygen to overcome hypoxia, and at the same time, boosts the efficiency of both SDT and PDT. Moreover, we comparatively analyzed the efficiency of SDT and PDT for tumor treatment throughout the depth of the tissue. Our study demonstrates that the strengths of PDT and SDT could be combined into a single multifunctional nanoplatform, which works well in the hypoxia environment and overcomes the limitations of each modality. The combination of deep tissue penetration by ultrasound and high spatial activation by light for selective treatment of single cells will significantly enhance the scope for therapeutic applications.Keywords:photodynamic;sonodynamic;hypoxia;nanoemulsion;delivery;tumor

研究领域: 肿瘤学 · 药剂学 · 生物医学工程
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COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS · 2024 · IF 4.9

A clay-based Pickering nanoemulsion with antibacterial activity

Yuetong Kang,Yonghui Zan,Yujie Cong,Xiaoyu Wang,Yufeng Luo,Lidong Li

Non-biotic antibacterial materials have drawn increasing attention. Some natural clays are able to promote the generation of reactive oxygen species , rendering them as promising candidates in combination with their abundant reserves, low cost and biosafety. However, the antibacterial performance of raw clay is usually below satisfaction due to poor solubility and restricted surface area . Hence, the modulation on dispersion form and the surface modification are essential for the design and practical application of natural clays as antibacterial materials. Herein, we developed a facile method to prepare a Pickering nanoemulsion with chitosan-coated montmorillonite (MMT) nanosheet . The addition of chitosan benefited the exfoliation of raw MMT and the stabilization of resultant colloidal MMT nanosheets, which were subsequently employed for preparing Pickering emulsion . The emulsion exhibited good stability and small size endowing them with good diffusion ability to interact with bacteria. Furthermore, the Pickering emulsion inherited the MMT nanosheet peroxidase-like property and displayed good antibacterial activity .

CAS / MDL: 9012-76-4
研究领域: 材料科学 · 生物学
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Frontiers in Bioengineering and Biotechnology · 2025 · IF 4.8

Nanotechnology-driven nanoemulsion gel for enhanced transdermal delivery of Sophora alopecuroides L. empyreumatic oil: formulation optimization, and anti-biofilm efficacy

Xiuli Cheng,Xiangyu Zhou,Wenping Wang,Jing Chen,Yikun Cao,Jia Wen,Jin Hu

Sophora alopecuroides L. empyreumatic oil (SoA oil) exhibits therapeutic potential for psoriasis and eczema but suffers from poor skin permeability and formulation challenges. To overcome these limitations, a nanoemulsion (NE) gel was developed. The NE was optimized using pseudo-ternary phase diagrams and characterized for droplet size, polydispersity index (PDI), zeta potential, and rheological properties. Skin permeability and retention were assessed in vitro using Franz diffusion cells, with oxymatrine quantified by HPLC. In vivo skin irritation was tested on rabbit dorsal skin, and anti-biofilm activity was evaluated against Staphylococcus aureus (S. aureus) and methicillin-resistant S. aureus (MRSA). A final concentration of 5% SoA oil in the NE formulation was used for subsequent studies. The optimized SoA oil NE (the NE) had a mean droplet size of 53.27 nm, PDI of 0.236, and zeta potential of −38.13 mV. Adding 2% carbomer 940 (CP940) to the gel enhanced viscoelasticity. The NE showed superior skin permeability and higher cutaneous retention of oxymatrine. SoA oil caused moderate irritation to the skin of rabbits, while the other two formulations did not. The NE demonstrated enhanced biofilm inhibition against S. aureus at 0.09766 mg/mL, with an 8.9% rate surpassing SoA oil (2.0%) and SoA oil NE gel (the gel, 4.0%). At 12.50 mg/mL, the NE and the gel achieved slightly higher inhibition rates (81.7% and 82.1%, respectively) than SoA oil (78.3%). Notably, the NE showed significantly greater anti-biofilm effects against MRSA within the concentration range from 0.09766 to 3.12 mg/mL (P < 0.001). In mature biofilm clearance against S. aureus, the NE demonstrated a clearance rate of 4.9% at 0.09766 mg/mL, while SoA oil and the NE gel achieved clearance rates of 2.3% and 0.8%, respectively. At a higher concentration of 12.50 mg/mL, the clearance rate for the NE increased to 38.1%, significantly outperforming SoA oil (29.1%) and the NE gel (36.4%). Against MRSA, the NE and the gel displayed significantly improved clearance at 12.50 mg/mL (42.7% and 43.9%, respectively) compared to SoA oil (31.9%) (P < 0.0001). These findings highlight the potential of nanotechnology-driven delivery systems to improve the clinical application of herbal extracts for treating biofilm-associated dermatological infections.

CAS / MDL: 9003-01-4
研究领域: 药剂学 · 皮肤病学 · 微生物学
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COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS · 2016 · IF 2.76

Impact of short-chain alcohols on the formation and stability of nano-emulsions prepared by the spontaneous emulsification method

Liya Zeng,Yalin Zhang

The principles of formation and stability of nano-emulsions have been extensively investigated in previous research. In this study, we focus on the impact of short-chain alcohols (C   <   5) on the formation and stability of oil-in-water nano-emulsions prepared by the spontaneous emulsification method. Due to its smaller droplet size and excellent optical transparency, the nano-emulsion stabilized by Cremophor EL was selected for further study. Addition of alcohol facilitated the nano-emulsion formation, moreover, the droplet size decreased with increasing alcohol chain length (C   >   2) and hydroxyl groups. Nevertheless, the droplet size then increased further with the addition of alcohols, which we ascribed to the effect of alcohols on droplet flocculation. An optimum Cremophor EL-to-1-butanol ratio of 2:1 was employed to construct the ternary phase diagram. It was found that the fine droplets (r   <   100   nm, PDI   <   0.2) were obtained only when converting the initial oil drops completely into the lamellar liquid crystalline phase and/or bicontinuous phase and then this phase became supersaturated in oil, so that the nucleation of oil drops occurred spontaneously. According to the dynamic light scattering results, coalescence and Ostwald ripening were the main destabilization mechanisms in our systems. Notably, nano-emulsion stability was greatly improved with ethanol in comparison to 1-propanol and 1-butanol.

研究领域: 化学工程 · 材料科学
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RSC Advances · 2017 ·Vol. 7 ·期 32 ·19815-19827 · IF 3.108

Development and characterization of promising Cremophor EL-stabilized o/w nanoemulsions containing short-chain alcohols as a cosurfactant

Liya Zeng,Xin Xin,Yalin Zhang

Nanoemulsions have attracted much attention due to their wide application in commercial industries such as pharmaceutics, food, beverages and skin care. Cremophor EL has been extensively used for emulsification, protection and solubilization of various lipophilic bioactive agents. However, their anaphylactoid hypersensitivity reactions are still challenging. Therefore, the aim of this study was to develop and characterize a promising, low-level Cremophor EL-stabilized o/w nanoemulsion using the spontaneous emulsification method for oral administration. From comparing the physicochemical properties (particle size and size distribution) of their emulsions, Cremophor has better emulsifying capacity than Tween and the droplet radius of emulsions can be reduced by increasing the surfactant concentration in current systems. The impact of various short-chain alcohols (C–OH < 5) on the formation and stability of nanoemulsions was also investigated to optimize the formulations. And there is a good correlation between nanoemulsion droplet size and the surfactant packing parameter (p). The smallest droplet size with the narrowest size distribution was produced by the system containing ethylene glycol as a cosurfactant. However, preparation of nanoemulsions with ethylene glycol was a time-consuming process since it was difficult to emulsify the water-induced gel-structure. Surfactant-to-oil mass ratio and surfactant-to-cosurfactant levels had to be optimized to produce fine droplets. Moreover, there was a linear relationship between the viscosity/log P value of alcohols and droplet size. Ostwald ripening was the dominant breakdown process of nanoemulsions obtained in the ethyl oleate/Cremophor EL–butanol (3 : 2)/water system. Ostwald ripening rate was increased with increasing surfactant concentration. Dilution (100×) of this system considerably improved their stability against droplet growth. This study demonstrated that alcohol addition might be a useful tool for preparing Cremophor EL-stabilized nanoemulsions for pharmaceutical applications.

研究领域: 药剂学 · 化学工程 · 生物医学工程
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LWT-FOOD SCIENCE AND TECHNOLOGY · 2020 · IF 4.006

Improvement of storage quality of strawberries by pullulan coatings incorporated with cinnamon essential oil nanoemulsion

Yifu Chu,ChengCheng Gao,Xiaoya Liu,Ni Zhang,Tian Xu,Xiao Feng,Yuling Yang,Xinchun Shen,Xiaozhi Tang

This study was aimed at evaluating the effect of pullulan coating incorporated with cinnamon essential oil (CEO) nanoemulsion on the shelf life and senescence of fresh strawberries during room storage. Pullulan-CEO nanoemulsion prepared using ultrasound treatment had smaller particle size (162.1 nm) and more uniform distribution of oil droplets. After six days of storage, pullulan-CEO nanoemulsion coating remarkably lowered the loss in fruit mass, firmness, total soluble solids and titratable acidity of strawberries. In addition, pullulan-based nanoemulsion coated strawberries showed the strongest antimicrobial activity against bacteria and molds (2.544 and 1.958 log CFU/g, respectively) compared to control and pure pullulan coating groups. It is mainly due to the antimicrobial activities of CEO dispersed in nano size in pullulan matrix. This study revealed that pullulan-CEO nanoemulsion coating showed great potential to prolong the shelf life of fresh strawberries during room storage.

CAS / MDL: 7385-67-3
研究领域: 食品科学 · 植物病理学
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DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY · 2019 · IF 2.367

Study on the transdermal penetration mechanism of ibuprofen nanoemulsions

Li Zhengguang,Huang Jie,Zhang Yong,Cao Jiaojiao,Wang Xingqi,Chu Xiaoqin

Objective: The purpose of this study was to research the mechanism of percutaneous penetration of Ibuprofen (IBU) nanoemulsion.Method: Transdermal penetration mechanism of IBU nanoemulsion was investigated by using Fourier transform infra-red spectral analysis (FTIR), differential scanning calorimeter thermogram (DSC), and activation energy (Ea) measurement. The in vivo skin penetration test of rats was carried out using Rhodamine B nanoemulsion to simulate the process of drug penetration into the skin, and the frozen section of the skin was observed by confocal laser scanning microscopy (CLSM).Result: FTIR spectra and DSC thermogram of rat skin treated with IBU nanoemulsion showed that infiltration occurred due to disruption of the stratum corneum (SC) protein–lipid structure and increasing of fluidity, hydration, and disruption of the lipid bilayer structure of the SC. The significant reduce in Ea (1.255 kcal/mol) for IBU permeating rat skin suggested crucial disruption of the SC lipid bilayers (P < 0.05), which is speculated that nanoemulsion may create new pathways to promote drug penetration. CLSM revealed that Rhodamine B penetrated into the SC in a shorter period of time and it accumulated around the sebaceous glands.Conclusion: The study of skin penetration mechanism indicated that nanoemulsion can be perfectly well used as the transdermal penetration of poorly soluble drugs.

研究领域: 药剂学 · 皮肤科学 · 生物医学工程
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BIOMEDICAL CHROMATOGRAPHY · 2024 ·Vol. 39 ·期 1 ·e6055 · IF 1.8

Development of a UPLC-MS/MS Method for Bioanalysis of Ethoxysanguinarine and Its Application in Pharmacokinetic Study of Ethoxysanguinarine Nanoemulsion

Jianhui Luo,Songshen Chen,WenYang Song,Yongtong Huang,Song Gao,Jiu Wang

Ethoxysanguinarine (ETSG), a benzophenanthridine alkaloid, exhibits diverse biological activities, including antibacterial, antifungal, anti-inflammatory, antioxidant, and anti-tumor effects. Despite these properties, limited research exists on ETSG in vivo pharmacokinetics due to its poor solubility and low bioavailability. In this study, we developed a rapid and specific UPLC-MS/MS method for ETSG bioanalysis. Sample preparation involved one-step protein precipitation using methanol and phellodendrine as an internal standard (IS). The Waters HSS T3 column (2.1 * 50 mm, 1.8 μM) employed a gradient elution with mobile phases A (2 mmol/L ammonium formate aqueous solution-formic acid [99.8:0.2, v/v]) and B (methanol-formic acid [99.8:0.2, v/v]). Mass analysis via Waters Q-mass spectrometer utilized positive scan mode and multiple reaction monitoring. ETSG and IS were detected at m/z 332.0 → 274.0 and 342.0 → 177.0, respectively, within 7.0 min. The method demonstrated excellent precision, accuracy, recovery, and stability, with a linear calibration curve (1.1–560 ng/mL) and strong correlation coefficient (0.9984). Successful pharmacokinetic evaluation in Sprague–Dawley rats included intravenous ETSG administration and intragastric ETSG nanoemulsion/suspension. This method enables steroidal saponin analysis from ETSG in biological samples.

CAS / MDL: 67-68-5 25322-68-3
研究领域: 药物分析 · 生物化学 · 药理学
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Food Packaging and Shelf Life · 2025 · IF 10.6

Encapsulation of cinnamaldehyde with protein-based nanoemulsions for strawberry preservation: Influence of protein types

Jiayan Lu,Yunyan Hua,Mengjia Guo,Laixue Ni,Yuling Cai,Yungang Cao,Longfeng Wang,Weiwei Li

This study investigated the encapsulation of cinnamaldehyde with three types proteins (soy 7S, whey protein and sodium caseinate) for strawberry preservation, and illustrated the related mechanism of the sustained release ability of CA-loaded nanoemulsions from the perspective of protein-cinnamaldehyde interactions. The results of FTIR, intrinsic fluorescence, and molecular docking indicated that the dominant interactions between the protein and cinnamaldehyde were mainly hydrophobic interaction and hydrogen bonds, of which, the interaction between cinnamaldehyde and SC was the strongest with the highest binding energy. The particle size of CA-loaded nanoemulsion formed by SC was the smallest (296 nm), but its release rate of cinnamaldehyde was the slowest. These results indicated that the exchange rate of bioactive compounds in nanoemulsion with the external environment was not only affected by the size of droplets, but also strongly affected by the interaction between bioactive compounds and interfacial proteins. A slowly release rate of cinnamaldehyde represented sustained antimicrobial activity. However, in practical preservation applications, not only the type of antibacterial agent and wall material should be considered, but also the influence of the concentration of antibacterial agent released in the environment should be taken into consideration.

研究领域: 食品科学 · 生物化学 · 材料科学
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Food & Function · 2019 ·Vol. 10 ·期 6 ·3344-3355 · IF 3.241

Impact of plant extract on the gastrointestinal fate of nutraceutical-loaded nanoemulsions: phytic acid inhibits lipid digestion but enhances curcumin bioaccessibility

Yaqiong Pei,Tingyang Ai,Ziyu Deng,Di Wu,Hongshan Liang,David Julian McClements,Bin Li

The impact of phytic acid on lipid digestion and curcumin bioaccessibility in oil-in-water nanoemulsions was investigated using a simulated gastrointestinal tract (GIT). The size, charge, and structural organization of the colloidal particles in the system were measured as the curcumin-loaded emulsions (7 mg curcumin per g lipid) were passed through simulated mouth (pH 6.8, 2 min), stomach (pH 2.5, 2 hours), and small intestine (pH 7.0, 2 hours) stages. After the small intestine stage, the level of free fatty acids (FFAs) generated and the bioaccessibility of curcumin were measured. The total amount of FFAs released significantly decreased with increasing phytic acid level, from 105.7 ± 5.9% (control) to 78.4 ± 6.4% (0.5% phytic acid). Conversely, curcumin bioaccessibility significantly increased from 39.4 ± 3.5% (control) to 74.7 ± 2.6% (0.5% phytic acid). The inverse relationship between lipolysis and curcumin bioaccessibility was ascribed to the impact of phytic acid on droplet flocculation and the level of free calcium ions present, which affected the production of mixed micelles capable of solubilizing the nutraceutical. The knowledge obtained here might prove beneficial for the employment of phytic acid as a multifunctional ingredient that inhibits lipid digestion while boosting nutraceutical bioavailability.

CAS / MDL: 458-37-7
研究领域: 食品科学 · 营养学 · 胃肠生理学
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International Journal of Food Engineering · 2017 ·Vol. 13 ·期 1 · IF 0.685

Stability and Bioaccessibility of Fucoxanthin in Nanoemulsions Prepared from Pinolenic Acid-contained Structured Lipid

Zhenghua Huang,Liqing Xu,Xuemei Zhu,Jiangning Hu,Hailong Peng,Zheling Zeng,Hua Xiong

Fucoxanthin intake has been correlated with the functions of anti-obesity and anti-oxidation, but applications of it in functional food or dietary supplements are still challenging due to its poor water-solubility, chemical instability, and low bioavailability. In this work, to study physicochemical and biological properties of fucoxanthin nanoemulsions, we investigated the influence of emulsion particle diameter on the stability of fucoxanthin during storage time and bioaccessibility in-vitro digestion. The structured lipid that enriched pinolenic acid at sn-2 position was chosen as the oil phase and the fucoxanthin oil-in-water nanoemulsions with droplet diameters of 344, 173, and 98 nm were prepared through a high-pressure microfluidizer. Then fucoxanthin emulsions were stored for 28 days at 4, 37, and 55 °C. Results showed that the physical stabilities of droplets were decreased with increases in the initial size and storage temperature, while the change of fucoxanthin retention indicated that fucoxanthin chemical stability was improved with increasing emulsion particle size. The augmentation of lipolysis and the value of free fatty acids (FFA) released in vitro digestion proved that digestion stability of fucoxanthin emulsion reduced with decreasing initial particle diameter, which was probably attributed to the increased surface area interacting with pancreatic lipase with decreasing droplet size. In addition, the concentrations of fucoxanthin in micelle phase were appreciable increased as droplet size decreased. Therefore, the bioaccessibility of fucoxanthin was improved. These results may benefit the optimization of an emulsion-based delivery system for fucoxanthin in food applications.

CAS / MDL: 9005-65-6
研究领域: 食品科学 · 营养学
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