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FOOD CHEMISTRY · 2021 · IF 7.514

Fabrication of Zein-Lecithin-EGCG complex nanoparticles: Characterization, controlled release in simulated gastrointestinal digestion

Hujun Xie,Chengzhi Liu,Jian Gao,Jieyu Shi,Fangfang Ni,Xin Luo,Ying He,Gerui Ren,Zisheng Luo

The Zein-Lecithin-Epigallocatechin gallate (EGCG) complex nanoparticles were fabricated by anti-solvent coprecipitation method. The Zein-Lecithin (Z-L) nanocomplexes exhibited great encapsulation efficiency of 68.5% for EGCG, and the encapsulated EGCG still had good antioxidative capacity. The cumulative release of EGCG in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) were 19% and 92%, respectively, and the release was closest to Fick release in SGF and First release in SIF. Fluorescence spectroscopy (FL), Fourier transform infrared spectroscopy (FTIR) and X-ray diffraction (XRD) experiments revealed that the EGCG was successfully encapsulated by Z-L nanocomplexes through electrostatic, hydrophobic and hydrogen bonding interactions. The Zein-Lecithin-EGCG complex nanoparticles exhibited excellent stability and great sustained-release performance, which will be the alternative for potential application in the food industry.

研究领域: 纳米技术 · 食品科学 · 药学
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FIBERS AND POLYMERS · 2021 ·Vol. 23 ·期 1 ·28-36 · IF 2.153

Controlled Release of Tetracycline Hydrochloride Loaded Highly Absorbent Alginate Submicron Fibers from Centrifugally Spinning

Lu Yishen,Li Xianglong,Hou Teng,Yang Bin

Highly absorbent alginate/polyethylene oxide submicron fibers containing the hydrophilic model drug tetracycline hydrochloride were prepared through centrifugal spinning. Pre-treatment with ethanol before crosslinking with calcium chloride solution maintained the structure of submicron fibers. The crosslinked submicron fibers could absorb phosphate buffer over 8 hours continuously, and they absorbed more phosphate buffer than commercial alginate dressing (Kaltostat and Algisite M). The morphology and chemical structures of submicron fibers were also investigated. In-vitro drug release tests revealed that more than 70 % (86 % 75 % and 73 % for drug loaded CA1, CA2 and CA3 fibers, respectively) of the loaded drug could be released continuously from the fibers in 24 hours, which matches well with the change frequency guidance of wound dressing for exuding wounds with heavy to moderate exudate. TCH loaded submicron fibers maintained the inhibition effect on Gram-positive S. aureus (31.25±0.71 mm (TCH-CA1), 30.85±0.27 mm (TCH-CA2) and 28.75±1.01 mm (TCH-CA3)) and Gram-negative E. coli . (29.8±0.35 mm (TCH-CA1), 29.28±0.87 mm (TCH-CA2) 27.38±0.64 mm (TCH-CA3)). These drug-loaded alginate submicron fibers may have application in wound dressing for exuding wounds.

研究领域: 材料科学 · 药学 · 生物医学工程
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Materials Science & Engineering C-Materials for Biological Applications · 2021 · IF 7.328

Controlled release of dopamine coatings on titanium bidirectionally regulate osteoclastic and osteogenic response behaviors

Mingyue Wang,Chenxi Wang,Yu Zhang,Ye Lin

Bone diseases, for example, osteoporosis, cause excessive differentiation of osteoclasts and decreased bone formation, resulting in imbalance of bone remodeling and poor osseointegration, which can be considered a relative contraindication for titanium implants. Dopamine (DA) might provide a solution to this problem by inhibiting osteoclasts and promoting osteoblasts at different concentrations. However, current commercial implants cannot load bone-active molecules, such as DA. Therefore, this study aimed to develop a surface modification method for implants to achieve a controlled release of DA and enhance the resistance of titanium implants to bone resorption and bone regeneration. DA-loaded alginate-arginine-glycine-aspartic acid (RGD) (AlgR) coatings on a vaterite-modified titanium surface were successfully assembled, which continuously and steadily released DA. In vitro studies have shown that materials showing good biocompatibility can not only inhibit receptor activator of nuclear factor-kappa B (NFκB) ligand (RANKL)-induced osteoclastogenesis but also enhance the adhesion and osteogenic differentiation of human bone marrow mesenchymal stem cells (hBMSCs). The optimal DA-loaded concentration of this bidirectional regulation is 100 μM. Interestingly, DA more effectively attenuated osteoclastogenesis when released in a sustained manner from titanium coatings than it did via traditional, free administration, and the alginate-RGD coating and DA clearly exhibited great synergy. This study provides a design of titanium implant surface modification to improve bone remodeling around implants.

研究领域: 生物材料 · 组织工程 · 骨科 · 生物医学工程 · 细胞生物学
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Journal of Materials Chemistry B · 2021 ·Vol. 9 ·期 41 ·8615-8625 · IF 6.331

A photo-responsive membrane for tailored drug delivery with spatially and temporally controlled release

Buyun Guo,Rong Fan,Shuwei Shen,Yue Xue,Zhiqiang Zhu,Ronald X. Xu

Accurate delivery of therapeutics to tumor regions and effective sparing of normal tissue structures are important principles for the treatment of widespread metastases or malignant lesions in close proximity to vital organs. However, the currently available drug delivery techniques do not support precise drug release within the identified disease margins. We propose a tailored drug delivery strategy that utilizes a photo-responsive material in combination with tumor margin imaging for automated and tailored release of therapeutics. As a proof of concept, a poly(ethylene oxide)-b-PSPA (PEO-b-PSPA) diblock copolymer is synthesized by spiropyran (SP) polymerization. A photo-responsive membrane (PRM) is formed and irradiated with light sources of different wavelengths. Switching irradiation between ultraviolet light (UV) and green light (Vis) controls the permeability of the PRM in coincidence with the programmed irradiation patterns. The dynamic process of photo-switchable drug permeation through the PRM is modeled and compared with the experimental results. The strategy of tailored drug release is verified using both regular geometric shapes and metastatic cancer images. The therapeutic effect of this tailored drug release strategy is demonstrated in vitro in human breast cancer cells. Our pilot study implies the technical potential of using photo-responsive carriers for image-guided chemotherapy with precisely controlled drug release patterns.

CAS / MDL: 9002-18-0 81-88-9
研究领域: 生物医学工程 · 药理学 · 肿瘤学
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2022 · IF 8.025

Structural and mechanistic insights into starch microgel/anthocyanin complex assembly and controlled release performance

Lei Chen,Die Zhang,Ling-Feng Wei,Wei-Jia Zhu,Xiao-Qin Yan,Rui Zhou,Zia-ud Din,Wen-Ping Ding,Tie-Zheng Ma,Jie Cai

We report a self-assembly method for the fabrication of multilayer-starch-based microgels used for anthocyanin encapsulation. Alcohol-heating treatment and ionization reactions were employed to reduce the crystallinity of starch and introduce ionic groups on the molecule to further cross-link it with sodium trimetaphosphate and produce a starch microgel. The molecular interactions between the starch and the anthocyanins facilitated the anthocyanin encapsulation and the starch-microgel/anthocyanin complexes with one, two, and three self-assembled layers were obtained. The Lay-1 microgel exhibited an encapsulation efficiency of 50.1% when the anthocyanin concentration, cross-linking starch concentration, contact time, and temperature were 0.25 mg/mL, 1.5 mg/mL, 3 h, and 40 °C, respectively. An increase in the number of layers resulted in a more compact microgel structure with the zeta potential presenting variations upon structural changes. Furthermore, the encapsulated anthocyanins presented a slow release from Lay-1, while the multilayered microgels (Lay-2 and Lay-3) displayed outstanding encapsulation stability. This study gives an insight on the encapsulation and release of anthocyanins by starch microgels, and provides a novel strategy for the design of starch-based encapsulation materials presenting great stability.

研究领域: 材料科学 · 食品科学 · 化学工程
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JOURNAL OF BIOMATERIALS SCIENCE-POLYMER EDITION · 2022 · IF 3.682

Synthesis and characterization of magnetic polymeric nanocomposites for pH-sensitive controlled release of methotrexate

Juan Wu,Xi Wang,Binglong Zhu,Qinting He,Yaheng Zhang,Wei Jiang

As one of the well-known anticancer drugs, methotrexate (MTX) has been limited in clinical application due to its side effects on normal tissues. This study focused on the one-step hydrothermal synthesis and in vitro evaluation of Fe3O4/RGO-PEI as MTX carriers for targeted anticancer therapy. In which, the Fe3O4 provided magnetic response properties; RGO acted as a stage for Fe3O4 loading and improved the dispersion of Fe3O4; polyethylenimine (PEI) was used as a surface modifier and a storehouse for MTX. The prepared Fe3O4/RGO-PEI nanocomposites exhibited a suitable size, good stability and magnetic responsibility. And the MTX loading content and loading efficiency were calculated to be 26.6% and 90.5%, respectively. What’s more, due to the diffusion and dissolution of PEI, the Fe3O4/RGO-PEI-MTX exhibited excellent pH-sensitivity, the values of MTX release rate (%) within 48 h at pH 5.8 and 4.0 were 64.3% and 87.4%, respectively. Furthermore, MTT assays in cancer cells (HepG2) and normal cells (HUVEC) demonstrated that Fe3O4/RGO-PEI-MTX exhibited high anticancer activity while low toxicity to normal cells, and also the Fe3O4/RGO-PEI composites were practically non-toxic. Thus, our results revealed that Fe3O4/RGO-PEI-MTX would be a competitive candidate for targeted delivery and controlled release of MTX.

研究领域: 材料科学 · 纳米技术 · 药学 · 癌症研究
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Foods · 2022 ·Vol. 11 ·期 23 ·3818 · IF 5.561

Controlled Release of Thymol by Cyclodextrin Metal-Organic Frameworks for Preservation of Cherry Tomatoes

Zhicheng Li,Yanan Sun,Xiaodan Pan,Tong Gao,Ting He,Chun Chen,Bin Zhang,Xiong Fu,Qiang Huang

Thymol is a phenol monoterpene with potential antifungal, antioxidant and antibacterial activities. Due to the low water solubility and high volatility of thymol, encapsulation serves as an effective tool during application. In the present study, cyclodextrin (CD)-based metal-organic-frameworks (MOFs) were synthesized using α-CD, β-CD, and γ-CD as organic building blocks, and further complexed with thymol to produce three CD-MOF-THY inclusion complexes (ICs). The encapsulation content, release kinetics and fruit preservation effect of ICs were analyzed. Results showed that thymol was well embedded in γ-CD-MOFs, with the highest encapsulation content of 286.7 ± 8.4 mg/g. Release kinetics revealed that CD-MOFs exhibited a controlled release effect toward thymol for 35 days. The release kinetics of three ICs fit the Rigter–Peppas model well, with γ-CD-MOF-THY showing the lowest release rate constant of 2.85 at 50 °C, RH 75%. Moreover, γ-CD-MOF-THY exhibited a remarkable preservation performance on cherry tomatoes with the lowest decay index (18.75%) and weight loss (5.17%) after 15 days of storage, suggesting this material as a potential fresh-keeping material for fruit and vegetable preservation.Keywords:CD-MOF;thymol;encapsulation;controlled release;cherry tomatoes

CAS / MDL: 17465-86-0 89-83-8
研究领域: 食品科学 · 材料科学 · 农业科学
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Molecular Systems Design & Engineering · 2023 ·Vol. 8 ·期 6 ·767-774 · IF 3.6

Substituent effect on controlled release of fragrant aldehydes from pH-triggered nicotinoylhydrazone-based precursors

Zuobing Xiao,Chengjing Wu,Xinyu Lu,Yunwei Niu,Peiran Yu,Xiaojie Ma

Fragrance precursors are an assorted class of pro-fragrances that could realize the controlled release of aromatic compounds. Herein, nicotinoylhydrazone-based pH-triggered fragrance precursors (NTA1–NTA4) have been prepared by reacting nicotinoylhydrazine with a series of aromatic benzaldehydes bearing different electron-donating groups. The chemical structures and substituent effects have been confirmed by FT-IR, NMR, mass and ultraviolet-visible (UV-vis) spectroscopies. Controlled release studies in an acidic environment revealed that a strong electron-donating substituent accelerates the release rate, while weak electron donor groups favor the deceleration of fragrance release. Surprisingly, intramolecular hydrogen bond formation (–OH⋯NC–) has a positive impact upon the stability of the hydrazone bridge in precursor NTA4, consistent with the simulation of the molecular electrostatic potential (MEP) results. In addition, the release kinetics were also investigated and the release rate constant could be estimated with a first-order kinetic model (R2 > 0.98). Furthermore, it was demonstrated that fragrance precursors on cotton fabrics could be an efficient controlled release strategy for fragrant aldehydes after exposure to an ambient atmosphere for several days, compared to a reference sample containing the raw aroma chemicals.

研究领域: 有机化学 · 材料科学 · 香料技术
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ACS Applied Polymer Materials · 2023 · IF 5

pH-Responsive Intelligent Antibacterial Coatings Based on 2D-COF for Controlled Release of Capsaicin

Zhipeng Zhao,Huimeng Feng,Dong Qin,Wen Li,Wei Wang,Shougang Chen

Herein, we designed and synthesized a two-dimensional covalent organic framework (2D-COF) of a Schiff base using a mechanical chemical grinding method. Moreover, capsaicin@chitosan (CAP@CS) microcapsules were loaded on a TpPa-1 COF by a physical adsorption method to prepare composites (CAP@CS/TpPa-1), which realized the pH-sensitive controlled release of the fungicide CAP, dispersed in fluorocarbon resin to prepare an intelligent coating with environmentally friendly long-term antifouling performance. TpPa-1 improves the antibacterial efficiency by increasing the dispersity of CAP@CS in the resin. Therefore, a CAP release amount of 2 wt % composite coating can meet the minimum bacteriostatic concentration of 37.5 μg/mL required for antifouling. Importantly, pH-responsive controlled release caused by the protonation of CS and the electrostatic interaction between CAP@CS and TpPa-1 COF and increased bacterial contact area by CAP@CS reunion inhibited by TpPa-1 COF improve the bactericidal efficiency of the composite. The composite coating has excellent corrosion resistance, mainly because COF extends the propagation path of the corrosive medium.

CAS / MDL: 9012-76-4
研究领域: 材料科学 · 化学 · 生物医学工程 · 环境科学
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Engineering · 2023 · IF 12.8

Ca-Alginate-Based Janus Capsules with a Pumping Effect for Intestinal-Targeted Controlled Release

Shuang Wen,Xiao-Jie Ju,Wen-Ying Liu,Yu-Qiong Liu,Xing-Qun Pu,Zhuang Liu,Wei Wang,Rui Xie,Yousef Faraj,Liang-Yin Chu

A novel intestinal-targeted θ-shaped capsule with a pumping effect for the controlled release of hydrophobic drugs is successfully developed. The proposed capsule is composed of a Ca-alginate–chitosan/protamine/silica (ACPSi) composite shell and two chambers forming a θ-shape (θ-ACPSi), which respectively encapsulate drugs and booster agents. Enteric hydroxypropyl methylcellulose phthalate (HPMCP) microspheres are embedded into the drug chamber shell. The θ-ACPSi composite shell offers improved protection for the encapsulated drug in the stomach environment and excellent intestinal-targeted drug release. Using indomethacin as the model drug and polyacrylic acid (PAA) as the booster agent, both the opening of “microchannels” in the drug chamber and the swelling of PAA in the booster chamber increase the release rate of high-concentration indomethacin and ensure a constant release of indomethacin in the small intestine. In the stomach (pH 2.5), less than 1% of the indomethacin is released. However, when the θ-ACPSi capsules enter the small intestine (pH 6.8), the HPMCP microspheres in the drug chamber shell dissolve to open the “microchannels,” while the PAA swells to provide pumping impetus. As a result, more than 60% of the indomethacin is released at a constant speed in the small intestine. The proposed θ-ACPSi capsules provide a potential and novel model for developing responsive pumping controlled-release systems and intestinal-targeted drug delivery systems.

CAS / MDL: 53-86-1
研究领域: 药剂学 · 生物材料学
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2023 · IF 8.2

Structural homeostasis and controlled release for anthocyanin in oral film via sulfated polysaccharides complexation

Yiwen Bao,Xi Yang,Jiaxin Li,Zhiying Li,Zhen Cheng,Mingshuang Wang,Zhongxia Li,Xu Si,Bin Li

Oral film is a novel functional carrier, which can provide a new pathway for the efficient absorption of anthocyanin . However, anthocyanin homeostasis in oral film is a prerequisite for achieving efficient absorption and utilization of anthocyanin. Herein, three sulfated polysaccharides , including chondroitin sulfate (CS), fucoidin (FU) and λ-carrageenan (λ-CG), were complexed with blueberry anthocyanin (BA) to prepare oral film formulations using hydroxypropyl methylcellulose (HPMC) as a film-forming matrix. The addition of three sulfated polysaccharides improved the stability of BA in content and color, which were associated with interactions between BA and polysaccharides. The BA retention rate of CS-BA/HPMC system increased 5.5-fold after 8 d of light-accelerated storage compared with the control group, showing the best homeostasis effect. CS and λ-CG enhanced the elongation at break and prolonged disintegration time of oral films. The addition of FU made the oral film denser and smoother, and had the highest BA release (75.72 %) in the simulated oral cavity system. In addition, the oral films of three sulfated polysaccharides complexed with BA showed superior antioxidant capacity. The present study provides new insights into the application of anthocyanin in film formulation carriers.

CAS / MDL: 9064-57-7
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Carbon Letters · 2023 · IF 4.5

Study on the controlled release properties of modified multi-walled carbon nanotubes on sulforaphane

Li Ronghua,Hu Xiucai,Shan Shiqiang,Li Yongbo,Cui Wenbin,Liu Lingling

Sulforaphane is a naturally occurring active substance found in vegetables that is known for its potential in preventing and treating cancer. This compound has demonstrated promising effects in inhibiting the growth of various types of cancer, including esophageal, lung, colon, breast, and liver cancer. However, its instability towards pH and heat limits its application in the medical and food industries. To address this challenge, novel drug delivery systems have been developed to improve the stability and efficacy of sulforaphane, making it a more suitable candidate for clinical use in cancer research. In this study, nanocomposite materials were prepared using multi-walled carbon nanotubes (MWCNTs) and chitosan (CS) as base materials, with polydopamine (PDA) acting as a bridge material. The synthesized composite materials were used as drug carriers for the release of sulforaphane. The results of the study showed that the drug loading increased with an increase in the concentration of sulforaphane, indicating that the nanocomposite materials were effective in delivering and releasing the drug. Moreover, a positive correlation was observed between the drug loading and the thickness of the PDA layer. These findings suggest that the use of MWCNTs, CS, and PDA in the development of drug delivery systems can enhance the stability and efficacy of sulforaphane, potentially leading to improved cancer treatment outcomes.

研究领域: 生物医学工程 · 药剂学 · 肿瘤学
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