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Frontiers in Chemistry · 2022 · IF 5.545

A peptide-DNA hybrid bio-nanomicelle and its application for detection of caspase-3 activity

Fan Zhang,Changqing Mao,Siyu Cao,Runchi Zhang,Yi Guo,Guifang Chen,Chang Feng

Bio-nanomicelles based on biomaterials such as nucleic acids, peptides, glycans, and lipids have developed rapidly in the field of bioanalysis. Although DNA and peptides have unique advantages, unfortunately, there are few bio-nanomicelles integrating DNA with peptides. Here, we designed a peptide-DNA hybrid bio-nanomicelle for the activity detection of caspase-3. The detection mechanism is based on caspase-3 specific recognition and cleavage of peptide substrates, which owns high sensitivity and selectivity. Under optimal conditions, the detection of caspase-3 activity can be achieved using our designed bio-nanomicelles and the detection limit is 0.72 nM. Furthermore, the proposed method was also successfully applied for the detection of caspase-3 in cell lysate samples after apoptosis-inducing.

研究领域: 生物分析 · 纳米技术 · 生物医学工程
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Regenerative Biomaterials · 2021 ·Vol. 8 ·期 3 · IF 6.353

Cisplatin and paclitaxel co-delivery nanosystem for ovarian cancer chemotherapy

Wang Qiaoying,Wu Changqiang,Li Xiaoting,Yang Dixiao,Shi Liangjun

We have designed and developed an effective drug delivery system using biocompatible polymer of poly (ethylene glycol)-polyaspartic acid (mPEG-PAsp) for co-loading the chemotherapy drugs paclitaxel (PTX) and cisplatin (CP) in one nano-vehicle. This study aimed to improve the anti-cancer efficacy of combinations of chemotherapy drugs and reduce their side effects. mPEG-PAsp-(PTX/Pt) nano-micelles disperse well in aqueous solution and have a narrow size distribution (37.8 ± 3.2 nm) in dynamic light scattering (DLS). Drug release profiles found that CP released at pH 5.5 was significantly faster than that at pH 7.4. MPEG-PAsp-(PTX/Pt) nano-micelles displayed a significantly higher tumor inhibitory effect than mPEG-PAsp-PTX nano-micelles when the polymer concentrations reached 50 μg/mL. Our data indicated that polymer micelles of mPEG-PAsp loaded with the combined drug exert synergistic anti-tumor efficacy on SKOV3 ovarian cells via different action mechanisms. Results from our studies suggested that mPEG-PAsp-(PTX/Pt) nano-micelles are promising alternatives for carrying and improving the delivery of therapeutic drugs with different water solubilities.

CAS / MDL: 33069-62-4 14913-33-8
研究领域: 药学 · 肿瘤学
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PEST MANAGEMENT SCIENCE · 2022 ·Vol. 78 ·期 10 ·4407-4416 · IF 4.462

Preparation and characterization of emamectin benzoate nanocapsules based on the dual role of polydopamine

Liyin Shi,Weiyao Yan,Li Sun,Chaoqun Hou,Nuo Wei,Zhiyang Chen,Jianguo Feng

Background Developing pesticide-controlled release formulations with foliage adhesion has become the focus of current research in the field of crop protection. In this study, an excellent adhesive nanocapsule loaded with emamectin benzoate (Eb@PDA) was prepared via emulsion interfacial polymerization based on the self-polymerization ability and adhesion properties of polydopamine (PDA). Results The physicochemical properties of the Eb@PDA were characterized by scanning electron microscopy, transmission electron microscopy, particle size statistics, Fourier transform infrared spectroscopy and X-ray diffraction. The Eb@PDA presented a regular spherical shape, with an average particle size of 163.8 nm. Compared with conventional formulations, it had higher pesticide-loading content (34%) and excellent adhesion onto corn leaf. In addition, Eb@PDA showed sustained-release characteristics, facilitating the release of Eb at low pH and high temperature. Eb@PDA could effectively protect Eb against photodegradation and had a longer effective period for controlling Spodoptera frugiperda and Spodoptera exigua . Furthermore, acute toxicity tests showed that the 50% lethal concentration (LC 50 ) was 80.91 and 57.91 mg kg −1 at 7 and 14 days, respectively, indicating a lower toxicity of the Eb@PDA to earthworms. The cells (L02) treated with Eb@PDA showed a higher cell viability but a lower apoptosis rate (only 5.75%), demonstrating the lower cytotoxicity of the Eb@PDA. Conclusion The self-prepared Eb@PDA could be used as a formulation with the advantages of slow release, UV shielding, strong leaf adhesion, superior insecticidal properties, sustained effectiveness and biosafety. It will also facilitate the development of an efficient and safe pesticide delivery system. © 2022 Society of Chemical Industry.

研究领域: 农药科学 · 材料科学 · 植物保护
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INTERNATIONAL JOURNAL OF PHARMACEUTICS · 2018 · IF 3.862

Glutathione-sensitive PEGylated curcumin prodrug nanomicelles: Preparation, characterization, cellular uptake and bioavailability evaluation

Hui-Yun Zhang,Cong-yong Sun,Michael Adu-Frimpong,Jiang-nan Yu,Xi-ming Xu

The anti-tumor efficacy of curcumin can be markedly improved by nano-drug self-delivery systems with high drug loading capacity and smart stimulus-triggered drug release in tumor cells. Herein, a type of novel, glutathione (GSH)-responsive, PEGylated prodrug nano-micelles (PPNMs) was prepared by self-assembly of curcumin-s-s-vitamin E/mPEG2k-DSPE mixture. The PPNMs (entrapment efficiency: 96.7%) was acceptably stable in water with a mean particle size of 29.84 nm. Compared with curcumin-loaded mPEG2k-DSPE nano-micelles (CUR-NMs), PPNMs showed a higher drug loading (1.68% vs 27.3%) and remarkably improved the chemical stability of curcumin in phosphate buffer saline (PBS) (pH = 7.4), 10% FBS culture medium, and rat plasma. In vitro release study showed that PPNMs could redox responsively control the release of curcumin from the prodrug. Moreover, PPNMs showed a cytotoxicity in HepG2 cells similar to that of the free curcumin; however, when the HepG2 cells were pretreated with 1 mM GSH, PPNMs displayed a markedly enhanced cytotoxicity and cellular uptake than the free curcumin. After intravenous injection, PPNMs showed an increased half-life in blood circulation (10.6-fold) and bioavailability (107-fold) compared with the free curcumin injection. Altogether, the prodrug nano-micelles represent a promising preparation for sustained and controlled delivery of curcumin with enhanced antitumor activity.

CAS / MDL: 505-73-7
研究领域: 药学 · 肿瘤学 · 纳米医学
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JOURNAL OF COLLOID AND INTERFACE SCIENCE · 2012 · IF 3.07

Formation and characterization of natural polysaccharide hollow nanocapsules via template layer-by-layer self-assembly

Yuxi Liu,Jing Yang,Ziqi Zhao,Junjie Li,Rui Zhang,Fanglian Yao

With natural polysaccharides carrageenan (Car) and chitosan (Cs) as the polyanion and polycation, respectively, multilayer hollow nanocapsules have been fabricated via sequential layer-by-layer (LbL) electrostatic self-assembly from the sacrificed templates nanospheres (SiO 2 –NH 2 ). The LbL assembly process with the polysaccharides on SiO 2 –NH 2 core was followed by ζ -potential and size analysis. The fabrication of (Car/Cs) x nanocapsules and the removing of the SiO 2 –NH 2 core templates were confirmed by TGA and EDS analysis. The morphology of SiO 2 (Car/Cs) x nanospheres and (Car/Cs) x nanocapsules were observed by TEM analysis. The size analysis of (Car/Cs) x nanocapsules indicated that the cyst wall thickness and cavity volume of the nanocapsules are pH and ionic strength dual responsive. Due to the biocompatibility of the natural polysaccharides carrageenan and chitosan and the responsiveness of nanocapsules to pH and ionic strength, the (Car/Cs) x multilayer nanocapsules are expected to be used as nanoreactors or nanocontainers to control the synthesis, encapsulation, and releasing behaviors of bioactive molecules.

CAS / MDL: 919-30-2
研究领域: 材料科学 · 生物医学工程
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MATERIALS & DESIGN · 2021 · IF 7.991

Design of crown ether based micelles and their anti-tumor properties by perturbing potassium ion homeostasis

Long Pang,Haohui Feng,Wei Zhong,Haonan Dong,Youqing Shen,Bing Yu,Hailin Cong

Chemotherapy is one of the most used method for cancer therapy, however, brings huge pain to patients as the drugs commonly causes side effects. Inducing tumor cells apoptosis by perturbing ion homeostasis is a novel approach to replace chemotherapy in recent years. Crown ether has been widely used since it was discovered in the last century and has shown its potential in biological applications. The aim of this paper is to design a series of novel nanometer micelles with crown ether on their surface. Crown ether was connected to a commonly used amphiphilic polymeric carrier, PEG-PCL, through ester bond (CPMs). Micelles about 120 nm in diameter were formed in aqueous solution. The micelles could capture potassium ions prominently in both aqueous solution and tumor cells. In vitro and in vivo experiments showed that the CPMs had certain anti-tumor activity, indicating that the CPMs had anti-tumor potential.

CAS / MDL: 301-10-0
研究领域: 药学 · 生物化学 · 肿瘤学
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COMPOSITES PART B-ENGINEERING · 2025 · IF 14.2

Bioactive nanocapsules based on lychee-like bilayer structure for synovitis treatment

Wenwen Chai,Pengfei Tian,Mengke Fan,Xiaochen Chen,Liyan Zhang,Muyan Qin,Yingbo Wang,Yansong Wang,Wei Chen,Qiang Yang,Honglong Li,Xu Cui,Deping Wang,Haobo Pan

Osteoarthritis (OA), as a degenerative disease, often necessitates intra-articular administration to alleviate pain. Synovial inflammation represents an important pathological factor in the development of OA. ZIF-8 (a type of Zeolitic imidazolate frameworks), a newly developed drug carrier, has garnered significant attention due to its high drug loading capacity and favorable biocompatibility. However, pH-sensitive burst drug release in inflammatory environments hampered its clinical application. To overcome this limitation, we have engineered a novel lychee-like double-layered bioactive nanocapsule, with ZIF-8 serving as the core and a bioactive amorphous sol as the outer shell, facilitated by Zn ion and Si–O coordination. The amorphous sol not only inhibits the rapid degradation of ZIF-8 in inflammatory conditions, preventing quick drug release, but also enhances the immunomodulatory capabilities of the functional carrier. Remarkably, our studies reveal that, in addition to sustained drug release, the synergistic effect of the functional carrier and anti-inflammatory drugs can regulate inflammation-induced lymphatic abnormalities. This is manifested by the suppression of macrophage secretion of excessive VEGF-C and iNOS, thereby modulating lymphatic density and restoring normal lymphatic rhythmic function. These findings indicate that such pathology-adaptive functional carriers possess superior drug release control and immunomodulatory potential compared to traditional carriers, presenting a promising innovative material for synovitis treatment.

研究领域: 药剂学 · 骨科 · 生物材料学
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Journal of Manufacturing Processes · 2024 · IF 6.1

Self-lubricating performance of a grinding wheel filled with CNTs@T304 nano-capsules

Jiju Guan,Zhengya Xu,Lanyu Yang,Zhiqiang Luan,Xuefeng Xu

This paper introduces a new grinding wheel which lubricates the grinding area directly. This is achieved by filling a resin grinding wheel with nano-capsules comprised of carbon nanotubes (CNTs) and di-n-butyl phosphite (T304) (CNTs@T304). The CNTs@T304 nano-capsules filled grinding wheel reduces the grinding force, lowers the grinding temperature, and improves the workpiece surface quality. The T304 lubricant is first filled into the CNT cavity to prepare nano-capsules, which exhibit better friction and wear quality than CNTs. Then the paper analyzes the configuration of the nano-capsules in the grinding wheel, together with the investigation of how the filling content impacts the mechanical properties. Additionally, the effects of nano-capsule filling content and grinding parameters on grinding force, grinding temperature, grinding ratio, as well as workpiece surface roughness are studied and the self-lubricating mechanism of the nano-capsules is assessed. According to the experimental results, nano-capsules maintain stable under thermal condition and resist the curing temperature. Moreover, the tensile strength and hardness exhibited by the grinding wheel still meet the application requirements at a filling content <16 wt%. Compared with the grinding wheel without fillers, the nano-capsule filled wheel exhibits superior grinding performance, with a 33 % reduction in the grinding force. Also, the grinding temperature is 28 % lower, there is a 30 % improvement in the grinding ratio, and the workpiece surface quality increases by 35 % under the same conditions. The T304 in the nano-capsules is continually released onto the grinding interface with the wear of the wheel in the grinding process, which forms a self-lubricating layer along with the friction products of the CNTs. This exerts an outstanding anti-friction and anti-wear effect, thereby improving the grinding performance.

CAS / MDL: 308068-56-6
研究领域: 材料科学 · 机械工程
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Asian Journal of Pharmaceutical Sciences · 2025 · IF 11.9

All-in-one peptide with sequential pH gradient sensing capabilities for the targeted delivery and deep penetration of nanomicelles against breast cancer

Qinying Chen,Xinao Liu,Zijin Tan,Zhihao Liu,Zijie Qiu,Yerong Xiong,Jiasheng Tu,Yanping Wu,Chunmeng Sun

Antitumor nanomedicines are usually decorated with ligands to achieve multiple functions, such as focused targeting, tissue penetration, and enhanced cellular uptake. However, a single ligand with multiple functions is generally preferred for use in practice. Herein, a versatile peptide, (HE) 10 G 5 R 6 GDK (HE-RK), was engineered by integrating several motifs in a single sequence, including a masking segment (HE), a flexible linker (G 5 ), and a tumor-penetrating head (RK), which comprised a cell-penetrating peptide (R 6 ) and a C-end Rule peptide (RGDK). The RK moiety in HE-RK was sequentially activated following the gradual charge reversal of HE to facilitate the accumulation of its cargos in deep tumor tissue and the cytosol of cancer cells. Moreover, in our study, polymer micelles conjugated with the HE-RK peptide (PM-HE-RK) showed superior cellular internalization at pH 6.5 compared to pH 7.4 in vitro , as well as extended blood circulation time and improved tumor targeting and penetration in vivo . Furthermore, the paclitaxel (PTX)-loaded micelles (PTX/PM-HE-RK) demonstrated considerable antitumor efficacy, that is, an 81.48% tumor inhibition rate in the 4T1 mouse model. Overall, the construction of this all-in-one multisegment peptide presents a synergistic and complementary approach to advancing multifunctional peptide ligand design.

研究领域: 生物医学工程 · 癌症治疗学 · 分子生物学
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BIOMACROMOLECULES · 2025 · IF 5.4

Polyphenylalanine-Baicalein Nanomicelles Reduce Nerve Cell Apoptosis and Inflammation to Enhance Neuroprotection and Poststroke Rehabilitation

Ling-Kun Zhang,Li Liu,Ziqing Li,Yiquan Zhang,Limin Zhai,Luna Zhang,Chu-Hua Li,Yan-Qing Guan

Cerebral ischemic stroke, neuronal death, and inflammation bring difficulties in neuroprotection and rehabilitation. In this study, we developed and designed the ability of natural lactoferrin-polyethylene glycol-polyphenylalanine-baicalein nanomicelles (LF-PEG-PPhe-Bai) to target and reduce these pathological processes, such as neurological damage and cognitive impairment in the stages of poststroke. Nanomicelles made from biocompatible materials have improved bioavailability and targeted distribution to afflicted brain areas. The results showed that LF-PEG-PPhe-Bai greatly improved the antioxidation, antiapoptosis, and anti-inflammation activity in vitro. Meanwhile, LF-PEG-PPhe-Bai improved the behavioral and cognitive impairment of 2-VO model mice, protected nerve cells in the hippocampus, and reduced inflammation at the brain injury site in vivo. In conclusion, LF-PEG-PPhe-Bai nanomicelles are employed for enhancing neuroprotection and poststroke rehabilitation. The development of this technology might provide a new technique for neural repair after ischemia in the future.

研究领域: 神经科学 · 药学 · 生物材料学
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Polymer Chemistry · 2018 ·Vol. 9 ·期 11 ·1337-1347 · IF 4.927

Diblock copolymer glyco-nanomicelles constructed by a maltoheptaose-based amphiphile for reduction- and pH-mediated intracellular drug delivery

Lulu Cheng,Tingting Luan,Di Liu,Ju Cheng,Hongping Li,Hua Wei,Lifen Zhang,Jingfeng Lan,Yali Liu,Guanghui Zhao

A new type of reduction- and pH-mediated glyco-polymeric micelles was synthesized for the antitumor drug doxorubicin (DOX) delivery in this study. The micelles were constructed by a diblock copolymer (MH-S-S-AcMH) with a disulfide linkage between hydrophilic block maltoheptaose (MH) and hydrophobic block acetalated maltoheptaose (AcMH). The experimental results showed that the amphiphilic MH-S-S-AcMH with 20 nm average size could self-assemble into micelles under physiological conditions and rapidly release the conjugated drug DOX when exposed to weakly acidic (pH = 5) and reductive (10 mM DTT) environment. Fluorescence microscopy detection indicated that drug carriers can be endocytosed effectively, making the anticancer agents flow into cells and suppress the growth of HeLa tumor cells. Compared with DOX at higher dosage and MH-S-S-AcMH micelles which are non-toxic to tumor cells, cytotoxicity assays manifested that the DOX-loaded MH-S-S-AcMH micelles exhibited better toxicity to HeLa tumor cells. According to these results, the copolymer mentioned above as practically non-toxic, highly stable, novel reduction- and pH-mediated glyco-polymeric micelles could be employed in improving drug delivery efficiency and enhancing anticancer efficacy.

研究领域: 药物递送 · 肿瘤学 · 生物材料
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International Journal of Nanomedicine · 2020 · IF 5.115

Enhanced Percutaneous Delivery of Methotrexate Using Micelles Prepared with Novel Cationic Amphipathic Material

Yun-Chun Zhao,Hai-Li Zheng,Xiao-Rong Wang,Xiao-Ling Zheng,Yue Chen,Wei-Dong Fei,Yong-Quan Zheng,Wen-Xi Wang,Cai-Hong Zheng

Background Methotrexate (MTX) is an antiproliferative drug widely used to treat inflammatory diseases and autoimmune diseases. The application of percutaneous administration is hindered due to its poor transdermal penetration. To reduce side effects and enhanced percutaneous delivery of MTX, novel methotrexate (MTX)-loaded micelles prepared with a amphiphilic cationic material, N,N-dimethyl-(N′,N′-di-stearoyl-1-ethyl)1,3-diaminopropane (DMSAP), was designed.Materials and Methods DMSAP was synthesized via three steps using simple chemical agents. H nuclear magnetic resonance and mass spectroscopy were used to confirm the successful synthesis of DMSAP. A safe and non-toxic phosphatidylcholine, soybean phosphatidylcholine (SPC), was added to DMSAP at different ratios to form P/D-micelles. Then, MTX-entrapped micelles (M/P/D-micelles) were prepared by electrostatic adsorption. The physicochemical properties and blood stability of micelles were examined thoroughly. In addition, the transdermal potential of the micelles was evaluated by permeation experiments.Results In aqueous environments, DMSAP conjugates could self-assemble spontaneously into micelles with a low critical micelle concentration (CMC) of 0.056 mg/mL. Stable, spherical MTX-entrapped micelles (M/P/D-micelles) with a size of 100–120 nm and high zeta potential of +36.26 mV were prepared. In vitro permeation studies showed that M/P/D-micelles exhibited superior skin permeability and deposition of MTX in the epidermis and dermis compared with that of free MTX.Conclusion These special novel cationic M/P/D-micelles can enhance the permeability of MTX and are expected to be a promising percutaneous delivery system for therapy skin diseases.

研究领域: 药剂学 · 皮肤病学 · 生物材料
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