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COLLOIDS AND SURFACES B-BIOINTERFACES · 2024 · IF 5.4

Ultrasound assisted enzymatic synthesis of OPO structured lipids by covalent organic framework immobilized lipase

Xia Jiaojiao,Feng Ting,Suo Hongbo,Yan Lishi,Zou Bin

In this study, the covalent organic framework immobilized Rhizomucor miehie lipase COF@RML as a novel biocatalyst was applied in the enzymatic synthesis of OPO structured lipids (1, 3-dioleoyl-2-palmitoylglycerol). The impact of reaction medium, substrate molar ratio, enzyme addition amount, reaction time and temperature on the enzymatic synthesis of OPO structured lipids were studied. Furthermore, the effects of ultrasonic power and ultrasonic time on the synthesis of OPO structural lipids were studied. The results showed that ultrasonication could increase the yeild of OPO structured lipids by improving substrate mass transfer and enzyme particle dispersion. The optimal process for the synthesis of OPO structured lipids was obtained. When the ultrasonic power was set at 90 W, ultrasonic time at 12 minutes, enzyme addition amount at 10 wt%, substrate molar ratio at 1:8, reaction temperature at 45 °C, and reaction time at 6 hours, the yield of OPO structured lipids reached a remarkable 51.27 %. Finally, the commercial lipase Lipozyme RM IM was compared with the COF@RML. The findings indicated that COF@RML immobilized enzyme had better application value in the synthesis of OPO structured lipids.

研究领域: 生物化学 · 食品科学 · 酶工程
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Food Bioscience · 2024 · IF 4.8

Bio-imprinted lipase-catalyzed production of medium- and long-chain structured lipids rich in n-3 polyunsaturated fatty acids by acidolysis

Xiaoqiang Zou,Mudassar Hussain,Imad Khan,Yanxi Wang,Bangzhi Jiang,Lei Zheng,Yuechao Pan,Jijie Hu,Azqa Ashraf

Medium- and long-chain structured lipids (MLSLs) rich in docosahexaenoic acid (DHA) and eicosapentaenoic acid (EPA) were synthesized by acidolysis of fish oil (Omax 1812, a mixture of sardine and anchovy oils) with caprylic acid (CA) using a lipase bio-imprinted with fatty acids as a catalyst. A bio-imprinted lipase for the acidolysis reaction was first prepared under optimal conditions, and its activity was 1.43 times higher than that of the non-bioimprinted. The bio-imprinted lipase was used as a catalyst to produce such MLSLs, and the reaction conditions were optimized. Under the optimal conditions, equilibrium was achieved in 8 h, and the total and the sn -1, 3 CA contents in the obtained product were 28.72% and 42.26%. Additionally, the total and the sn -2 DHA contents were 14.23% and 21.10%, respectively, and the total and the sn -2 EPA contents were 16.43% and 10.14%, respectively. These obtained MLSLs, rich in sn -1, 3 CA, and sn -2 DHA, EPA can deliver significant health benefits.

研究领域: 生物化学 · 食品科学
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Biomass Conversion and Biorefinery · 2024 · IF 3.5

Enzymatic synthesis of novel structured lipids with tiger nut oil: optimized by response surface methodology

Ijaz Hira,Sun Shangde

The objective of this work was to utilize tiger nut oil as a new raw material to produce advanced structured lipids that are beneficial for human health. Behenic acid was also used as another raw material to make novel structured lipids. Enzyme screening on the reaction was scrutinized. The effect of different conditions (time, temperature, substrate ratio, and enzyme load) on the yield of structured lipids was evaluated and optimized by response surface methodology. Authentication of the response surface model was confirmed by the excellent acquiescence between the experimental and the predicted values of structured lipids yield. Furthermore, the kinetic model was applied based on the Ping-Pong Bi Bi method. Results showed that the novel structured lipids were successfully prepared using tiger nut oil as raw material, and Lipozyme RMIM as a green cleaner catalyst showed good performance for this reaction. The maximum yield of the product (78.8%) was obtained at a temperature of 85℃; time, 1.25 h; substrate ratio, 1:6 (w/w); and enzyme load, 12.5%. In addition, the reaction’s calculated activation energy ( Ea ) was estimated to be 17.302 kJ/mol. This study also summarized that response surface methodology helps to optimize the reaction conditions. The optimized production process offers a scalable method for creating structured lipids with specific health benefits, potentially benefitting the food, and nutraceutical industries by providing new chances for making health-promoting products. Graphical Abstract

CAS / MDL: 929-77-1
研究领域: 食品科学 · 生物化学 · 营养学
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Pharmaceutics · 2022 ·Vol. 14 ·期 7 ·1330 · IF 6.525

Optimization of Maduramicin Ammonium-Loaded Nanostructured Lipid Carriers Using Box–Behnken Design for Enhanced Anticoccidial Effect against Eimeria tenella in Broiler Chickens

Yan Zhang,Runan Zuo,Xinhao Song,Jiahao Gong,Junqi Wang,Mengjuan Lin,Fengzhu Yang,Xingxing Cheng,Xiuge Gao,Lin Peng,Hui Ji,Xia Chen,Shanxiang Jiang,Dawei Guo

Maduramicin ammonium (MAD) is one of the most frequently used anticoccidial agents in broiler chickens. However, the high toxicity and low solubility of MAD limit its clinical application. In this study, MAD-loaded nanostructured lipid carriers (MAD–NLCs) were prepared to overcome the defects of MAD by using highly soluble nanostructured lipid carriers (NLCs). The formulation was optimized via a three-level, three-factor Box–Behnken response surface method. Then, the optimal MAD–NLCs were evaluated according to their hydrodynamic diameter (HD), zeta potential (ZP), crystal structure, encapsulation efficiency (EE), drug loading (DL), in vitro release, and anticoccidial effect. The optimal MAD–NLCs had an HD of 153.6 ± 3.044 nm and a ZP of −41.4 ± 1.10 mV. The X-ray diffraction and Fourier-transform infrared spectroscopy results indicated that the MAD was encapsulated in the NLCs in an amorphous state. The EE and DL were 90.49 ± 1.05% and 2.34 ± 0.04%, respectively, which indicated that the MAD was efficiently encapsulated in the NLCs. In the in vitro study, the MAD–NLCs demonstrated a slow and sustained drug release behavior. Notably, MAD–NLCs had an excellent anticoccidial effect againstEimeria tenellain broiler chickens. In summary, MAD–NLCs have huge potential to form a new preparation administered via drinking water with a powerful anticoccidial effect.Keywords:maduramicin ammonium;nanostructured lipid carriers;Box–Behnken design;anticoccidial effect

研究领域: 兽医学 · 药剂技术 · 动物健康
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JOURNAL OF THE AMERICAN OIL CHEMISTS SOCIETY · 2013 ·Vol. 91 ·期 1 ·55-62 · IF 1.592

Typoselectivity of Crude Geobacillus sp. T1 Lipase Fused with a Cellulose-Binding Domain and Its Use in the Synthesis of Structured Lipids

Qin Xiao-Li,Huang Hui-Hua,Lan Dong-Ming,Wang Yong-Hua,Yang Bo

Typoselectivity of crude CBD-T1 lipase ( Geobacillus sp. T1 lipase fused with a cellulose binding domain) was investigated. Multi-competitive reaction mixtures including a set of n -chain fatty acids (C8:0, C10:0, C12:0, C14:0, C18:1 n-9, C18:2 n-6 and C18:3 n-3) and tripalmitin-enriched triacylglycerols were studied in hexane. The crude CBD-T1 lipase discriminated strongly against C18:1 n-9 [competitive factor ( α ) = 0.23] and showed the highest preference for C8:0 ( α  = 1). Utilizing the catalytic properties of crude CBD-T1 lipase, acidolysis of soybean oil with C8:0 was selected as a model reaction to investigate the ability of the lipase to produce MLM-type (medium-long-medium) structured lipids. Several reaction parameters (added water amount, reaction temperature, substrate molar ratio and reaction time) examined for incorporating C8:0 into soybean oil, the optimum conditions were: 1:3 (soybean oil/C8:0) of molar ratio, 3 mL of hexane, 50 °C of temperature, 48 h of reaction time, 20 % of crude CBD-T1 lipase (w/w total substrates), and 7.5 % of water (w/w enzyme). Under these conditions, the incorporation of C8:0 was 29.6 mol%. The results suggest that crude CBD-T1 lipase, which showed different fatty acid specificity profiles, is a potential biocatalyst for the modification of fats and oils.

研究领域: 生物化学 · 食品科学
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INTERNATIONAL JOURNAL OF PHARMACEUTICS · 2013 · IF 3.458

Preparation and characterization of 4-dedimethylamino sancycline (CMT-3) loaded nanostructured lipid carrier (CMT-3/NLC) formulations

Xiaomin Yang,Lin Zhao,Laszlo Almasy,Vasil M. Garamus,Aihua Zou,Regine Willumeit,Saijun Fan

Chemically modified tetracyclines (CMTs) have been reported to strongly inhibit proliferation and metastasis of various cancers, but their efficacy is restricted by poor water solubility. In the present study, a hydrophilic 4-dedimethylamino sancycline (CMT-3) loaded nanostructured lipid carrier (CMT-3/NLC) was produced by high pressure homogenization (HPH). The physical properties of CMT-3/NLC formulations were characterized by dynamic light scattering (DLS), high efficiency liquid chromatography (HPLC), atomic force microscopy (AFM), scanning electron microscopy (SEM), small-angle neutron scattering (SANS), small-angle X-ray scattering (SAXS) and wide-angle X-ray powder diffraction (XRD). The lipid and surfactant ingredients, as well as drug/lipid concentrations (m/m) were optimized to produce stable and sustained NLC formulations. In vitro cytotoxicity of CMT-3/NLC against HeLa cells was evaluated by MTT assay. The diameter of CMT-3/NLC was found to increase from 153.1   ±   3.0   nm to a maximum of 168.5   ±   2.0   nm after 30 days of storage, while the entrapment efficiency remained constant at >90%. CMT-3/NLC demonstrated a burst-sustained release profile in release media with different pH, a property attributed to the 3-dimensional structure of CMT-3/NLC. Cell uptake and localization studies indicated that NLC reached the cytoplasm and could thereby facilitate CMT-3 entry into HeLa cells.

研究领域: 药剂学 · 肿瘤学 · 材料科学
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Applied Food Research · 2025 · IF 6.2

Production of one novel low-calorie structured lipid using tiger nut oil by enzymatic transesterification

Hira Ijaz,Shangde Sun,Gholamreza Abdi,Rana Muhammad Aadil

The objective of the present study was to produce one novel low-calorie structured lipids (SLs), that can be used as a healthy alternative of shortening fat. SLs were produced by the interesterification of tiger nut oil (TNO) and methyl behenate using Lipozyme RMIM at a temperature of 85 °C, an agitation speed of 300 rpm, and a reaction time of 1.25 hours. Resulting SLs characterized through a comprehensive set of advanced physicochemical analysis including AV, slip melting point, solid fat content, total fatty acid composition, x-ray diffraction, differential scanning calorimetry, and triacylglycerol composition were analyzed for both SLs and formulated blends. Results showed that novel SLs had high melting point and solid fat content, to further optimize functionality, unique blend formulations of SLs and TNO were prepared, and the best ratio was selected. This blend demonstrated reduced slip melting point and solid fat content than SLs, suggesting its potential for developing low-calorie, health-friendly shortening fats.

CAS / MDL: 929-77-1
研究领域: 食品科学 · 生物化学
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FOOD RESEARCH INTERNATIONAL · 2025 · IF 8

Limonene-loaded nanostructured lipid carriers incorporated in hydrogels: Enhanced acid stability and controlled release properties

Simin Feng,Yitong Tian,Jiahao Yu,Yang Lin,Alan Giovanini de Oliveira Sartori,Ping Shao

Improving the acid stability of nanostructured lipid carriers (NLCs) is critical for broadening their engineering applications. The integration of NLCs with hydrogels results in a more stable, multifunctional system that facilitates the effective and sustained release of bioactive ingredients. In this study, The chitosan/alginate hydrogel (CAH) exhibited minimal limonene release under combined high-temperature and acidic conditions when the degree of carboxyl substitution (DS) of chitosan reached 17.68 ± 0.14 % (NLC-CAH1). It exhibited the lowest release rate and superior stability under high-temperature and acidic conditions. The cumulative release rates of limonene in NLC and NLC-CAH1 within 3 h of acid solution were 35.24 ± 0.97 % and 22.41 ± 2.09 %, respectively. The hydrogels effectively delayed the release of NLCs, reducing the release rate of limonene and facilitating a prolonged release of bioactive ingredients. Consequently, the NLCs-hydrogel system represents a novel delivery mechanism, and offers innovative strategies for the administration of lipophilic bioactive compounds.

CAS / MDL: 9005-38-3 9012-76-4
研究领域: 药剂学 · 生物材料科学
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AAPS PHARMSCITECH · 2020 ·Vol. 21 ·期 8 ·1-12 · IF 2.401

Development and Evaluation of Astaxanthin as Nanostructure Lipid Carriers in Topical Delivery

Geng Qiang,Zhao Yuming,Wang Lu,Xu Lulu,Chen Xiong,Han Jing

The study is designed to formulate, optimize, and evaluate astaxanthin (ASTA)-loaded nanostructured lipid carrier (NLC) with an aim to improve its stability, water solubility, skin permeability and retention and reduce drug-related side effects. ASTA was extracted from Haematococcus pluvialis. ASTA-NLC was formulated by the technique of melt emulsification—ultrasonic and optimized taking solid:liquid lipid ratio, total lipid:drug ratio, drug concentration, emulsifier types, and amounts as independent variables with particle sizes (PS) and entrapment efficiency (EE) as dependent variables. The optimized formulation (N21) exhibited spherical surfaced stable nanoparticles of 67.4 ± 2.1 nm size and 94.3 ± 0.5% EE. Formulation N21 was then evaluated for its physiological properties, physicochemical properties, drug content, in vitro release and skin penetration, and retention analysis. The ASTA-NLC was found to be nonirritating, homogenous, and with excellent stability and water solubility. In vitro release studies showed the cumulative release rate of NLC was 83.0 ± 3.4% at 48 h. The skin penetration and retention studies indicated that cumulative permeability was 174.10 ± 4.38 μg/cm 2 and the retention was 8.00 ± 1.62 μg/cm 2 within 24 h. It can be concluded that NLC serves as a promising carrier for site specific targeting with better stability and skin penetration.

研究领域: 药剂学 · 生物技术 · 皮肤病学
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INTERNATIONAL JOURNAL OF PHARMACEUTICS · 2016 · IF 3.994

Design and evaluation of lipoprotein resembling curcumin-encapsulated protein-free nanostructured lipid carrier for brain targeting

Fanfei Meng,Sajid Asghar,Yurui Xu,Jianping Wang,Xin Jin,Zhilin Wang,Jing Wang,Qineng Ping,Jianping Zhou,Yanyu Xiao

Many nanoparticle matrixes have been demonstrated to be efficient in brain targeting, but there are still certain limitations for them. To overcome the shortcomings of the existing nanoparticulate systems for brain-targeted delivery, a lipoprotein resembling protein-free nanostructured lipid carrier (PS80-NLC) loaded with curcumin was constructed and assessed for in vitro and in vivo performance. Firstly, single factor at a time approach was employed to investigate the effects of various formulation factors. Mean particle sizes of ≤100   nm, high entrapment efficiency (EE, about 95%) and drug loading (DL, >3%) were obtained for the optimized formulations. In vitro release studies in the presence of plasma indicated stability of the formulation under physiological condition. Compared with NLC, PS80-NLC showed noticeably higher affinity for bEnd.3 cells (1.56 folds greater than NLC) but with lower uptake in macrophages. The brain coronal sections showed strong and widely distributed fluorescence intensity of PS80-NLC than that of NLC in the cortex. Ex vivo imaging studies further confirmed that PS80-NLC could effectively permeate BBB and preferentially accumulate in the brain (2.38 times greater than NLC). The considerable in vitro and in vivo performance of the safe and biocompatible PS80–NLC makes it a suitable option for further investigations in brain targeted drug delivery .

CAS / MDL: 458-37-7
研究领域: 药剂学 · 神经科学 · 生物医学工程
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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 Bioengineering · 2024 ·Vol. 3 ·期 3 ·323-336 · IF 0

Enhancing high-temperature stability of limonene-loaded nanostructured lipid carriers with various solid lipids

Simin Feng,Yitong Tian,Jialu Sheng,Jiahao Yu,Yang Lin,Kseniya Hileuskaya,Aliaksandr Kraskouski,Huiliang Li,Zhihong Lin,Ping Shao

In this research, nanostructured lipid carriers (NLCs) loaded with limonene were developed using various solid lipids. The impact of high temperatures on the characteristics of NLCs was investigated. NLCs exhibited zeta potential values exceeding |30| mV, indicating excellent homogeneity and stability. Increasing the carbon chain length of monoglycerides from C15 to C21 resulted in a corresponding increase in particle size of NLCs from 219.1 ± 1.1 to 243.3 ± 0.9 nm. However, the particle size remained relatively constant with an increase in the number of solid lipid carbon chains. Encapsulation efficiency of limonene increased from 66.0 ± 0.7% to 86.2 ± 0.8% with an increase in the number of solid lipid carbon chains. The result showed that more ester bonds facilitated the dissolution of the target and enhanced the interaction forces between solid lipids and the target. X-ray diffraction, Fourier transform-infra-red spectroscopy and differential scanning calorimetry analyses confirmed effective encapsulation of limonene in NLCs, resulting in good stability. NLCs prepared from various solid lipids exhibited varying properties. Glycerol triglyceride demonstrated superior stability and homogeneity of nanoparticles under high-temperature conditions compared to other solid lipids. This study provides enhancing the thermal stability of limonene-loaded NLCs and proposes a novel approach for their practical application.

研究领域: 药剂学 · 材料科学 · 食品化学
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