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JOURNAL OF THE CHINESE CHEMICAL SOCIETY · 2020 ·Vol. 67 ·期 5 ·874-879 · IF 1.554

Preparation of galactosylated curcumol liposomes

Wenjie Li,Yan Lu,Yi Cheng,Hui Luo,Zhenbin Jia,Ning Li

Curcumol (Cur), which is the primary active anti-liver cancer component of Chinese traditional medicine Rhizoma zedoariae , was encapsulated in galactosylated liposomes to enhance its liver-targeting efficacy. In this study, we optimized the preparation methods, prescription, and process of galactosylated curcumol liposomes (Gal-Cur-L). The experimental results showed that the encapsulation efficiency, particle diameter, and stability coefficient of Gal-Cur-L obtained by the two-step emulsification method were improved compared with those of it obtained by other methods. Single-factor investigation showed that two factors, pH and the amount of triolein, contribute at least partly to the encapsulation efficiency and particle diameter of Gal-Cur-L. The best prescription and process were obtained through orthogonal test: the ratio of lecithin to cholesterol was 2:1, the ratio of drug to lipid was 1:2, and the amount of ether and Twain-80 were 4 ml and 1.6 g/L, respectively, 15 min for ultrasonic time, 100 W for ultrasonic power, and 20 min for homogeneous time. Using the best method, prescription, and process mentioned earlier, the basic test results of Gal-Cur-L were obtained, which demonstrated that our methods, prescription, and process of Gal-Cur-L were applicable. The encouraging results of this study provided references for the research of liver-targeting reagents of curcumol.

研究领域: 药剂学 · 肿瘤学
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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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INTERNATIONAL JOURNAL OF PHARMACEUTICS · 2015 · IF 3.65

Comparative studies on the properties of glycyrrhetinic acid-loaded PLGA microparticles prepared by emulsion and template methods

Hong Wang,Guangxing Zhang,Hong Sui,Yanhua Liu,Kinam Park,Wenping Wang

The O/W emulsion method has been widely used for the production of poly (lactide- co -glycolide) (PLGA) microparticles . Recently, a template method has been used to make homogeneous microparticles with predefined size and shape, and shown to be useful in encapsulating different types of active compounds. However, differences between the template method and emulsion method have not been examined. In the current study, PLGA microparticles were prepared by the two methods using glycyrrhetinic acid (GA) as a model drug. The properties of obtained microparticles were characterized and compared on drug distribution, in vitro release, and degradation. An encapsulation efficiency of over 70% and a mean particle size of about 40   μm were found for both methods. DSC thermograms and XRPD diffractograms indicated that GA was highly dispersed or in the amorphous state in the matrix of microparticles. The emulsion method produced microparticles of a broad size distribution with a core–shell type structure and many drug-rich domains inside each microparticle. Its drug release and matrix degradation was slow before Day 50 and then accelerated. In contrast, the template method formed microparticles with narrow size distribution and drug distribution without apparent drug-rich domains. The template microparticles with a loading efficiency of 85% exhibited a zero-order release profile for 3 months after the initial burst release of 26.7%, and a steady surface erosion process as well. The same microparticles made by two different methods showed two distinguished drug release profiles. The two different methods can be supplementary with each other in optimization of drug formulation for achieving predetermined drug release patterns.

CAS / MDL: 9002-89-5
研究领域: 药剂学 · 生物材料学
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PROGRESS IN ORGANIC COATINGS · 2015 · IF 2.358

A new method to synthesize high solid content waterborne polyurethanes by strict control of bimodal particle size distribution

Shao-Jun Peng,Yong Jin,Xin-Feng Cheng,Tong-Bing Sun,Rui Qi,Bao-Zhu Fan

A new method named two-step emulsification process was developed to synthesize high solid content waterborne polyurethanes by strict control of the bimodal particle size distribution. In the first step, a series of 40% solid content polyester-based (WPU-1) with low content of hydrophilic group and large particle size were firstly synthesized. In the second step, polyether-based prepolymers (WPU-2 prepolymers) with high content of hydrophilic group were firstly prepared and WPU-1 emulsions were used to emulsify WPU-2 prepolymers to obtain the final emulsions with high solid content (WPU-3). The particle size of WPU-3 present bimodal distribution and the diameter ratio and volume percentage of large particles to small particles in WPU-3 were able to be strictly controlled by this method. The viscosity of WPU-3 with 55% solid content was only 489.1   mPa   s −1 when the diameter ratio of large particles to small particles was 9.2 and the volume percentage of large particles was 74%.

研究领域: 材料科学 · 化学工程
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BMC BIOTECHNOLOGY · 2019 ·Vol. 19 ·期 1 ·1-11 · IF 2.303

Formulation and evaluation of norcanthridin nanoemulsions against the Plutella xylostella (Lepidotera: Plutellidae)

Zeng Liya,Liu Yongchang,Pan Jun,Liu Xiaowen

Background Norcantharidin (NCTD), a demethylated derivative of cantharidin (defensive toxin of blister beetles), has been reported to exhibit insecticidal activity against various types of agricultural pests. However, NCTD applications are limited by its poor water solubility and high dosage requirement. Nanoemulsions have attracted much attentions due to the transparent or translucence appearance, physical stability, high bioavailability and non-irritant in nature. In general, nanoemulsions with small droplet size can enhance the bioavailability of drugs, whereas this phenomenon is likely system dependent. In present study, NCTD nanoemulsions were developed and optimized to evaluate and improve the insecticidal activity of NCTD against Plutella xylostella (Lepidotera: Plutellidae) by a spontaneous emulsification method.Results Triacetin, Cremophor EL and butanol were selected as the constituents of NCTD nanoemulsions via solubility determination, emulsification efficiency and ternary phase diagram construction. Insecticidal activity of NCTD nanoemulsion was associated with the content of surfactant and cosurfactant: (1) Higher effective toxicity exhibited at Smix (surfactant to cosurfactant mass ratio) = 3:1 that may be associated with the changes in interfacial tension; (2) NCTD nanoemulsion at 3:7 < SOR (surfactant to oil mass ratio) < 6:4 was more effective at lower surfactant level, which was attributed to the relatively slow diffusion rate of NCTD hindering by excess surfactant. Interestingly, nanoemulsions with smaller droplets were not found to be more effective in our study.Conclusion sThe optimized NCTD nanoemulsion (triacetin/Cremophor EL/butanol (60/20/20, w/w)) exhibited effective insecticidal activity (LC50 60.414 mg/l, LC90 185.530 mg/l, 48 h) than the NCTD acetone solution (LC50 175.602 mg/L, LC90 303.050 mg/L, 48 h). Spontaneous emulsifying nanoemulsion employed to formulate this poor water-soluble pesticide is a potential system for agriculture application.

研究领域: 农业科学 · 昆虫学 · 药剂学
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LANGMUIR · 2011 · IF 4.269

“Two-in-One” Fabrication of Fe3O4/MePEG-PLA Composite Nanocapsules as a Potential Ultrasonic/MRI Dual Contrast Agent

Bin Xu,Hongjing Dou,Ke Tao,Kang Sun,Jing Ding,Weibin Shi,Xiasheng Guo,Jiyu Li,Dong Zhang,Kun Sun

A new method for the fabrication of Fe3O4 nanoparticles enveloped by polymeric nanocapsules is proposed. This method is characterized by combining a double emulsification with the interfacial coprecipitation of iron salts to form Fe3O4/polymer composite nanocapsules in a single step. To demonstrate the viability of this approach, methoxy poly(ethylene glycol)-poly(lactide) (MePLEG) was chosen as the shell material for Fe3O4/MePLEG nanocapsules. In addition to the versatility offered for fabricating nanocapsules with different shell materials, the method was found to be convenient for adjusting the magnetite content of the nanocapsules from 0 to 43%. In addition to their confirmed T2-weighted magnetic resonance imaging (MRI) enhancement, the resultant composite nanocapsules display much more obvious acoustic responses than MePLEG nanocapsules in an acoustic investigation. Furthermore, the low toxicity of these composite nanocapsules, as confirmed by our study, combined with their magnetic and acoustic properties ensure that these composite nanocapsules have great potential in acting as ultrasonic/MRI dual contrast agents.

CAS / MDL: 12036-10-1 7790-28-5
研究领域: 材料科学 · 医学影像学 · 纳米医学
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NEW JOURNAL OF CHEMISTRY · 2023 ·Vol. 47 ·期 24 ·11669-11674 · IF 3.3

Preparation of nano dumbbell-shaped silver bismuth iodide perovskite hybrids and their enhanced photocurrent properties

Sellan Premkumar,Thankappan Thrupthika,Maheswari Palanivel,Dan Liu,Devaraj Nataraj,Wei Lei,Jianzhou Gui

Dumbbell-like silver bismuth iodide perovskite heterostructures were fabricated via the growth of heterogeneous silver using a modified emulsion method. Owing to the immiscibility between DMF and hexane, the silver bismuth iodide precursors in DMF could be dispersed as microscopic droplets in hexane under vigorous stirring. Subsequently, the addition of acetone as a demulsifier provided the driving force for crystallization to form dumbbell-shaped silver bismuth iodide perovskite heterostructures. In this synthesis, we added a high concentration of Ag precursors to DMF, which influenced the morphology changes to form a silver-metal-head dumbbell-shaped silver bismuth iodide perovskite hybrid system. However, in the dumbbell heterostructure, a large silver domain was exclusively grown on a single side of the AgBi2I7 system. Further, the as-prepared dumbbell-shaped AgBi2I7 heterostructure sample was used to fabricate a photo-sensitive device and its time-dependent photocurrent properties were analysed. The dumbbell-shaped metal-perovskite heterostructure sample exhibited a higher photocurrent magnitude of ∼21 and 70 μA for 0.1 and 0.2 V bias voltage, with a high ON–OFF ratio of 3.1 × 104 and 3.2 × 104, respectively. The improved photocurrent indicates that the transfer of photogenerated electrons was facilitated from the perovskite system to the metal head.

研究领域: 材料科学 · 纳米技术 · 光化学 · 半导体物理
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Molecular Medicine Reports · 2020 ·Vol. 22 ·期 6 ·4531-4540 · IF 2.1

Preparation and quality evaluation of a volatile oil microemulsion from Flos magnoliae and Centipeda minima

Yulin Liang,Junbo Zou,Xiaofei Zhang,Yajun Shi,Jia Tai,Yu Wang,Dongyan Guo,Ming Yang

In order to improve the water solubility of the volatile oils extracted from Flos magnoliae (FM) and Centipeda minima (CM), they were prepared as a microemulsion (ME), which were then used in the development of an FM and CM volatile oil ME for the treatment of allergic rhinitis (AR). ME was prepared by phase inversion emulsification, and the prescription factors such as emulsifier, co‑emulsifier, oil phase, Km, which represents the ratio of the mass of emulsifier to that of the co‑emulsifier, and preparation factors such as temperature affecting the formation of the ME were selected according to the formation area of ME in a pseudo‑ternary phase diagram. The quality of the ME was evaluated based on its appearance, particle size, Zeta potential and stability. The content of eucalyptol in ME was determined by gas chromatography‑mass spectrometry (GC‑MS). The cumulative permeability of the ME within 24 h was measured with a transdermal diffusion tester. The results revealed that the best formula for preparation of the ME was as follows: Castor oil polyoxyethylene ether (EL‑40) was the emulsifier; the co‑emulsifier was anhydrous ethanol; the Km was 2:1; the mixed phase of volatile oil and isopropyl myristate with mass ratio of 1:1 was used as oil phase; and the preparation temperature was 25˚C. The content of eucalyptol in the ME was 2.57 mg/g, and the cumulative permeability of the ME in 24 h was significantly increased compared with that of the reference oil solution. The appearance of the ME was uniform, and the solution was transparent. In conclusion, compared with traditional preparations, FM and CM volatile oil ME is a novel, improved and more effective preparation for the treatment of AR.

CAS / MDL: 470-82-6
研究领域: 药学 · 药物递送系统 · 中药 · 分析化学
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FOOD CHEMISTRY · 2024 · IF 8.5

Physical stability of oil-in-water multi-layered coenzyme Q10 nano-emulsions

Zhili Xu,Fan Zhang,Dewei Cheng,Qianyun Ma,Wenxiu Wang,Jie Wang,Jianfeng Sun

As a lipophilic antioxidant, coenzyme Q10 (CoQ10) has limited application owing to its low water solubility and instability. In the present study, potato protein (PP) and soybean soluble polysaccharide (SSPS) were used as carriers to prepare a multilayer SSPS-PP-CoQ10 nano-emulsion using the reversed-phase emulsification method; further, the water solubility, stability, and formation mechanism of the nano-emulsion were analyzed. The results showed that the particle size of SSPS-PP-CoQ10 nano-emulsions was 253–422 nm with good polydispersity. The encapsulation efficiency (EE) could reach up to 88.87 %. When the concentration of SSPS was 0.1 wt%, the decrease in interfacial tension and increase in viscoelasticity indicated that nano-emulsion improved CoQ10 physical stability. SSPS incorporation altered the microscopic environment of the hydrophobic residues, rendering them more hydrophilic and enhancing their water solubility. According to molecular docking results, hydrogen bonds promote binding among SSPS, PP, and CoQ10, and increase emulsion stability.

CAS / MDL: 303-98-0
研究领域: 食品科学 · 胶体与表面化学 · 药剂学
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INTERNATIONAL JOURNAL OF PHARMACEUTICS · 2019 · IF 4.213

Highly bioactive, bevacizumab-loaded, sustained-release PLGA/PCADK microspheres for intravitreal therapy in ocular diseases

Jiaxin Liu,Shuang Li,Ge Li,Xiang Li,Changhui Yu,Zhijiang Fu,Xiangyu Li,Lesheng Teng,Youxin Li,Fengying Sun

Bevacizumab, a vascular endothelial growth factor (VEGF)-targeting drug, is widely used as an off-label therapeutic for age-related macular degeneration (AMD). To reduce the monthly administration frequency, this study investigated microspheres comprising a poly( d , l -lactide-co-glycolide)/poly(cyclohexane-1,4-diyl acetone dimethylene ketal) (PLGA/PCADK) blend that could be loaded with bevacizumab-dextran particles using solid-in-oil-in-water (S/O/W) emulsification. Control microspheres were also prepared through water-in-oil-in-water (W/O/W) emulsification. The structural stability of bevacizumab in the polymer monomers was analyzed using dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE), size exclusion chromatography (SEC-HPLC), circular dichroism (CD) and fluorescence spectroscopy. Subsequently, microspheres were prepared and evaluated in terms of their morphology, encapsulation efficiency and release behavior. PLGA/PCADK microspheres prepared by the S/O/W method with <20% PCADK showed a smooth spherical structure with a uniform distribution of bevacizumab. The microspheres exhibited a release behavior comprising a slight initial burst and an increasing total release over 50 days both in vitro and in vivo . Additionally, the microspheres were well tolerated by ocular tissue. Finally, a chorioallantoic membrane (CAM) assay revealed that the bioactivity of bevacizumab was retained by PCADK. In conclusion, these results suggest the potential for bevacizumab-loaded PLGA/PCADK microspheres prepared by the S/O/W method as a means of intravitreal therapy for ocular diseases.

研究领域: 药物学 · 眼科学 · 药物递送系统
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FOOD HYDROCOLLOIDS · 2025 · IF 12.4

Precise control of biphasic droplet symmetry: Nanoparticle-mediated 2D interfacial engineering modulates 3D spatial configuration

Xiaolong Li,Changhu Xue,Zihao Wei

Differences in the spatial arrangement of two immiscible phases lead to variations in the symmetry of biphasic droplets, thereby endowing them with diversified 3D spatial configurations. Symmetric core-shell droplets and asymmetric Janus droplets play crucial roles in the food field, including applications in protective encapsulation, controlled release, autonomous motion, particle synthesis, and more. However, comprehending and elucidating the control mechanism of biphasic droplet symmetry in one-step emulsification process remains a daunting challenge. The collision and coalescence behaviors of zein droplets and sodium alginate droplets in 3D space, similar to phagocytosis, create opportunities for the formation of biphasic droplets and the precise control of their symmetry. The interactions between immiscible droplets are closely linked to their 2D interfacial structure. Nanoparticles are utilized as an effective tool to control integrity of 2D interface in monophasic droplets. Therefore, the protein–polysaccharide nanoparticles, fabricated through deamidation and the Maillard reaction, are utilized to regulate the properties of the sodium alginate droplet 2D interface. Variations in the 2D interface structure of the sodium alginate droplets lead to the complete or incomplete engulfment of the sodium alginate droplets by the zein droplets. Ultimately, the nanoparticle-mediated 2D interface engineering modulates 3D spatial configuration of biphasic droplets. This work employs dimensionality reduction theory, using a 2D interface as an anchor point, to achieve symmetry control of biphasic droplets through nanoparticles. It not only lays theoretical foundations for applications of biphasic droplets but also introduces a new research paradigm for the design of functional food colloid structures.

CAS / MDL: 81-88-9
研究领域: 胶体与界面化学 · 食品科学 · 生物材料 · 功能食品 · 分子自组装 · 软物质物理 · 纳米技术
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POLYMER BULLETIN · 2022 ·Vol. 80 ·期 3 ·2697-2711 · IF 2.843

Magnetic polyvinyl alcohol microspheres with self-regulating temperature hyperthermia and CT/MR imaging for arterial embolization

Yin Peinan,Wei Chengxiong,Jin Xin,Yu Xiaogang,Wu Chengwei,Zhang Wei

Trans-catheter arterial embolization, as a minimally invasive therapy strategy, has become a choice for treating liver cancer. Development of embolic agents integrated with therapy and imagining functions is desired. Herein, magnetic polyvinyl alcohol (PVA) microspheres as embolic agents are prepared by emulsification method. The diameter of the magnetic PVA microspheres ranges from 10 to 110 μm, and the required size can be obtained by sieving. The temperature of magnetic PVA microspheres suspension could stabilize at 49 °C under the applied magnetic field, which indicates the microspheres have self-regulating temperature hyperthermia characteristic due to the application of magnetic nanoparticles with low Curie point. In addition, magnetic PVA microspheres possess obvious contrast effects on CT and T2-weighted imaging due to the existence of magnetic nanoparticles. Cytotoxicity assay indicates the survival rate of cells cultured with leach liquor of 30 mg/mL PVA/MNPs microspheres is 97.4%, which shows the magnetic microspheres have good cell biocompatibility. The developed magnetic microspheres have the potential to realize embolization, self-regulating temperature hyperthermia, and CT/MR imaging simultaneously in interventional therapy.

研究领域: 医学成像 · 癌症治疗 · 生物医学工程 · 材料科学
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