Biomaterials Science
·
2015
·Vol. 4
·期 1
·167-182
·
IF 3.831
Fengqian Chen,Jinming Zhang,Yao He,Xiefan Fang,Yitao Wang,Meiwan Chen
It remains a challenge to increase drug tumor-specific accumulation as well as to achieve intracellular-controlled drug release for hepatocellular carcinoma (HCC) chemotherapy. Herein, we developed a dual-functional biodegradable micellar system constituted by glycyrrhetinic acid coupling poly(ethylene glycol)-disulfide linkage-poly(lactic-co-glycolic acid) (GA-PEG-SS-PLGA) to achieve both hepatoma-targeting and redox-responsive intracellular drug release. Tanshinone IIA (TAN IIA), an effective anti-HCC drug, was encapsulated. Notably, it exhibited rapid aggregation and faster drug release in 10 mM dithiothreitol compared with the redox-insensitive control. Furthermore, GA-decorated micelles revealed HCC-specific cellular uptake in human liver cancer HepG2 cells with an energy-dependent manner, in which micropinocytosis and caveolae-mediated endocytosis were demonstrated as the major cellular pathways. The enhanced cytotoxicity and pro-apoptotic effects against HepG2 cells in vitro were observed, mediated by up-regulation of the intracellular ROS level, the increased cell cycle arrest at S phase, enhanced necrocytosis and up-regulation of caspase 3/7, P38 protein expression. In addition, TAN IIA-loaded micelles had a significantly prolonged circulation time, improved bioavailability, and resulted in an increased accumulation of TAN IIA in the liver. With the synergistic effects of HCC-targeting and controlled drug release, TAN IIA-loaded GA-PEG-SS-PLGA micelles significantly inhibited tumor growth and increased survival time in a mouse HCC-xenograft model. Collectively, the GA-PEG-SS-PLGA micelles with HCC-targeting and redox-sensitive characters would provide a novel strategy to deliver TAN IIA effectively for HCC therapy.
✓ 已验证
DOI
PubMed
高影响因子
Journal of Macromolecular Science Part B-Physics
·
2012
·
IF 0.739
Dong Li,Xiaohui Wang,Yanzhu Guo,Haifei Huang,Runcang Sun
Controllable synthesis of self-associating lauroyl-grafted chitosan with high molecular weight was realized in ionic liquid reacting media. The obtained lauroyl chitosan with different grafting degrees was characterized by FT-IR and 1H-NMR spectra. The chitosan derivatives were able to self-assemble into spherical polymeric micelles in water. The onset of micellization or critical micelle concentration (CMC) was estimated by fluorescence spectroscopy. The hydrodynamic diameters of various lauroyl chitosan micelles, determined by dynamic light scattering, were in the range of 122–295 nm. The morphology of the micelles was observed by scanning electron microscopy. The self-assembly behavior and the size of the assembled micelles of lauroyl chitosan were affected by the grafting degree of lauroyl groups. Generally, higher grafting degree resulted in lower CMC and smaller micelle size. These lauroyl chitosan nano-micelles may have potential applications in biological and medical fields.
✓ 已验证
DOI
高影响因子
PLoS One
·
2014
·Vol. 9
·期 7
·e102539
·
IF 3.534
Caili Dai,Zhihu Yan,Qing You,Mingyong Du,Mingwei Zhao
Through the descriptive and rheological characterization of worm-like micelles formed by N -hexadecyl- N -methylpyrrolidinium bromide and sodium laurate, the formation and properties of the worm-like micelles were affected by the concentrations of sodium laurate and temperature. Additionally, cryogenic transmission electron microscopy images further validated the formation of worm-like micelles.
✓ 已验证
DOI
高影响因子
Bioengineering-Basel
·
2026
·Vol. 13
·期 8
·908
·
IF 4.4
Dandan Zhang,Zhigang Zhang,Dingxing Huang,Zhuoran Sun,Jiamin Huang,Chi Zhang,Qingyang Zeng,Qiling Liu,Wenzhuo Chen
Osteoarthritis is an irreversible degenerative joint disease driven by sustained NF-κB-mediated inflammatory responses, and conventional intra-articular hyaluronic acid or small-molecule NF-κB inhibitors cannot achieve targeted on-demand treatment due to poor solubility, rapid clearance and lack of lesion microenvironment responsiveness. OA with inherent anti-chondrolytic activity can self-assemble into nanocarriers in water, yet it lacks stimuli-responsive capacity. Herein, we rationally designed and synthesized an OA-Der by covalently conjugating o-phenylenediamine fragments to the OA backbone.1H NMR and HRESI-MS spectra fully verified the accurate chemical structures of intermediate and final OA-Der. Blank OA-Der micelles exhibited uniform spherical core–shell nanostructures (50–150 nm) under TEM and AFM, while pathological high NO triggered complete disassembly of micellar assemblies. We further co-assembled OA-Der with NF-κB inhibitor BAY 11-7082 to construct NO-responsive BAY@OA-Der supramolecular micelles. In vitro experiments using human C28/I2 chondrocytes with LPS-induced inflammatory injury demonstrated that BAY@OA-Der significantly improved cell viability and reduced apoptotic chondrocyte proportion. At mRNA and protein levels, the supramolecular micelle formulation remarkably suppressed NF-κB p65 phosphorylation, downregulated cartilage-degrading ADAMTS5, and upregulated ACAN compared with free BAY or blank OA-Der. Collectively, this natural bioactive self-assembled NO-responsive delivery platform achieves synergistic anti-inflammatory and matrix-protective effects by precisely releasing drugs at NO-overexpressed osteoarthritis inflammatory sites and offers an in vitro design strategy for osteoarthritis responsive delivery systems.
✓ 已验证
产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2026
·
IF 6
Yue Wei,Yangyi Chen,Huajing Zhang,Qiao Li,Huajuan He,Xiao Liang,Shiyuan Lin,Hui Chen,Wei Wu,Wei Zhang
A kind of purine nucleoside-chitosan-silybin (PN-CS-SB) polymeric micelles were developed for enhancing the oral absorption of doxorubicin (DOX) by intestinal nucleoside transporter mediation, the inhibition of P-glycoprotein (P-gp) efflux and CYP3A4 metabolism. The four types of PN, including adenosine, deoxyadenosine, guanosine and deoxyguanosine, respectively, and silybin, were conjugated to chitosan via the linker succinic acid. The synthesized PN-CS-SB were identified by 1 H NMR and FT-IR, and the doxorubicin (DOX)-loaded micelles were prepared by ultrasonication. The micelles demonstrated a series of the excellent properties, including the high drug loading capacity of above 8.2%, the regular spherical shapes with the small particle sizes of below 150 nm, and the low critical micelle concentration of below 5.82 × 10⁻⁶ g/mL. The oral bioavailability of the DOX-loaded micelles against DOX solution achieved to as high as 453.28%. The rapid and tremendous absorption of micelles was visually demonstrated by in vivo imaging. The micelle absorption mechanism was proved to be nucleoside transporter-mediation as well as the dual inhibition of P-gp and CYP3A4 by the cellular uptake, enzyme inhibition and immunofluorescence location test. The cellular endocytosis and transportation pathway of micelles across intestinal epithelial cells involved nucleoside transporter target, caveolin mediation or macropinocytosis with energy consumption. Download: Download high-res image (234KB) Download: Download full-size image
✓ 已验证
DOI
PubMed
高影响因子
FOOD CHEMISTRY
·
2026
·
IF 10.4
Ying Lu,Qiang Yin,Xiangzhou Li,Jun Zhou,Yanhong Yang,Bowen Fu,Yuqing Wang
To meet consumer demand for the application of natural ingredients such as essential oils in food systems, this study developed a chitosan-g-poly(lactic acid) (CS-g-PLA) micellar system for fir essential oil (FEO) delivery. The research focused on investigating the regulatory effects of PLA side-chain parameters on micellar properties. Results demonstrated that increasing parameters enhanced hydrophobic interactions, forming compact micelles with a minimal particle size (229.7 nm) and critical micelle concentration (0.012 mg/mL). The hydrophobic core enabled efficient FEO loading (30.99%) with stable sustained release. FEO@CS-g-PLA micelles also showed broad-spectrum antimicrobial activity by disrupting cell membranes. Molecular dynamics simulations visualized the self-assembly of CS-g-PLA and the FEO loading process, providing theoretical support for experimental observations. In summary, this work offers microscopic insights into the micellization of modified CS-g-PLA and FEO loading mechanisms, providing a feasible strategy for applying essential oils in food preservation.
✓ 已验证
DOI
PubMed
高影响因子
CARBOHYDRATE POLYMERS
·
2026
·
IF 13.2
Haiqi Zhang,Jinze Wang,Hongtao Hu,Weiqiang Tan,Lie Ma
The management of chronic diabetic wounds remains a great clinical challenge due to heightened oxidative stress and persistent inflammation. Although antioxidant hydrogels have shown promising therapeutic potential, many suffer from inadequate mechanical performance. Here, a natural rosmarinic acid-derived micelles potentiated dextran hydrogel was designed for chronic diabetic wound treatment. The hydrogel was crosslinked by acrylate-polyethylene glycol-modified rosmarinic acid (AR) micelles, double bonds and phenylboronic acid-modified dextran (DMP), acrylamide (AM), and polyvinyl alcohol (PVA). AR micelles not only imparted antioxidant properties to the hydrogel but also improved the mechanical performance by acting as crosslinkers and energy dissipation points. In addition, the dynamic phenylborate bonds formed by the phenylboronic acid groups on dextran and the cis -diols on PVA further enhanced the antioxidant and mechanical properties of the hydrogel. The AR/PAM/DMP/PVA (APDP) hydrogel exhibited good biocompatibility, ROS scavenging capacity, and anti-inflammatory property in vitro . More importantly, the APDP2 hydrogel effectively accelerated chronic diabetic wound healing by promoting macrophage polarization to the anti-inflammatory M2 phenotype, boosting anti-inflammatory cytokine secretion, as well as facilitating angiogenesis and collagen deposition. Thus, the rosmarinic acid-derived micelles crosslinked hydrogel presents a promising strategy for the treatment of diabetic wounds and provides new insights for developing herbal functionalized hydrogel materials.
✓ 已验证
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2026
·
IF 8.7
Wei Guo,Yingying Liang,Xuge Wang,Lei Nie
An asymmetric adhesive hydrogel is developed. • The sprayable and biodegradable hydrogel possesses antibacterial and antioxidant properties. • The hydrogel possesses excellent hemocompatibility and cytocompatibility, and can promote cell migration. Injectable hydrogel adhesives with asymmetric adhesion properties are of great significance in reducing the risk of postoperative tissue adhesion. In this study, a sprayable, in situ–forming hydrogel was synthesized by grafting 2-aminoethyl methacrylate (AEMA) and dopamine (DA) onto a sodium alginate (SA) backbone, followed by loading curcumin-PF127 micelles (Cur-PF127) and ultraviolet (UV)- initiated free-radical crosslinking. The prepared hydrogel exhibited porous microstructure, sprayability, degradability, and suitable swelling properties (>1000%). Rheological analysis revealed that the hydrogel exhibited stable storage and loss moduli. In addition, the hydrogel exhibited good adhesion to diverse substrates, including glass, rubber, plastic, porcine skin, and various mouse organs (liver, lung, stomach, spleen, kidney, and heart). Notably, the adhesive performance of the hydrogel could be reduced after UV exposure, enabling controllable adhesion behavior. Furthermore, the hydrogel exhibited antibacterial efficacy against Escherichia coli ( E. coli ) and Staphylococcus aureus ( S. aureus ), potent antioxidant activity (scavenging over 80% of free radicals), and good in vitro cytocompatibility, as validated by the CCK-8 assay, cell staining, the cell scratch test, and hemocompatibility analysis. Owing to its combination of controllable adhesion, sprayability, antioxidant and antibacterial properties, and cytocompatibility, this hydrogel shows potential as a multifunctional biomedical adhesive. Download: Download high-res image (134KB) Download: Download full-size image
✓ 已验证
DOI
PubMed
高影响因子
Regenerative Biomaterials
·
2022
·
IF 5.763
Jiang Linrui,Zheng Rong,Zeng Ni,Wu Changqiang,Su Hongying
Polymeric micelles have long been considered as promising nanocarrier for hydrophobic drugs and imaging probes, due to their nanoscale particle size, biocompatibility and ability to loading reasonable amount of cargoes. Herein, a facile method for dextran micelles preparation was developed and their performance as carriers of superparamagnetic iron oxide (SPIO) nanocrystals was evaluated. Amphiphilic dextran (Dex-g-OA) was synthesized via the Schiff base reactions between oxidized dextran and oleylamine, and self-assembled in situ into nano-size micelles in the reaction systems. The self-assembling behaviors of the amphiphilic dextran were identified using fluorescence resonance energy transfer technique by detection the energy transfer signal between the fluorophore pairs, Cy5 and Cy5.5. Hydrophobic SPIO nanoparticles (Fe3O4 NPs) were successfully loaded into the dextran micelles via the in situ self-assembly process, leading to a series of Fe3O4 NPs-loaded micelle nanocomposites (Fe3O4@Dex-g-OA) with good biocompatibility, superparamagnetism and strongly enhanced T2 relaxivity. At the magnetic field of 0.5 T, the Fe3O4@Dex-g-OA nanocomposite with particle size of 116.2 ± 53.7 nm presented a higher T2 relaxivity of 327.9 mM−1Fe·s−1. The prepared magnetic nanocomposites hold the promise to be used as contrast agents in magnetic resonance imaging.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Fundamental Research
·
2022
·
IF 0
Junyu Ma,Chen Ma,Xiaoyu Huang,Pedro Henrique Hermes de Araujo,Amit Kumal Goyal,Guolin Lu,Chun Feng
Fragmentation/disassembly of fiber-like micelles generated by living crystalline-driven self-assembly (CDSA) is usually encountered in aqueous media, which hinders the applications of micelles. Herein, we report the generation of uniform fiber-like micelles consisting of a π-conjugated oligo( p -phenylenevinylene) core and a cross-linking silica shell with grafted poly(ethylene glycol) (PEG) chains by the combination of living CDSA, silica chemistry and surface grafting-onto strategy. Owing to the presence of crosslinking silica shell and the outmost PEG chains, the resulting micelles exhibit excellent dispersity and colloidal stability in PBS buffer, BSA aqueous solution and upon heating at 80 °C for 2 h without micellar fragmentation/disassembly. The micelles also show negligible cytotoxicity toward both HeLa cervical cancer and HEK239T human embryonic kidney cell lines. Interestingly, micelles with L n of 156 nm show the “stealth” property with no significant uptake by HeLa cells, whereas some certain amounts of micelles with L n of 535 nm can penetrate into HeLa cells, showing length-dependent cellular uptake behaviors. These results provide a route to prepare uniform, colloidally stable fiber-like nanostructures with tunable length and functions derived for biomedical applications.
✓ 已验证
产品关联
DOI
CHINESE JOURNAL OF POLYMER SCIENCE
·
2022
·Vol. 41
·期 1
·84-94
·
IF 3.815
Zheng Ying-Ying,Zhu Han,Tan Yi,Liu Feng-Yi-Qi,Wu Yi-Xian
Liquid trimethoxy silane-functionalized cis-polybutadiene ( cis -PB-Si(OMe) 3 ), possessing number-average molecular weights of cis -PB segments ( M n,PB ) ranging from 1800 g/mol to 5400 g/mol, with cis -1,4 content of ca. 80% and high functionality (>96%) could be synthesized by coordination copolymerization of living cis -PB chain ends with ethenyltrimethoxy-silane with neodymium-based catalytic system. The silicon hydroxyl-functionalized cis-polybutadiene ( cis -PB-Si(OH) 3 )-based micelles in water have been achieved by in situ hydrolysis of cis -PB-Si(OMe) 3 in hexane/water mixture (pH=6.8) at 70 °C and by sequential removal of residue hexane. The size of the above micelles with soft elastic cis -PB cores could be remarkably enlarged by loading SiO 2 nanoparticles on their surfaces via hydrogen bonding interaction. Giant supramolecular long chain aggregates or networks formed by hydrogen bonding interaction and possible O—Si—O chemical bonds between cis -PB-Si(OH) 3 -based micellar surfaces had relatively large size and thus precipitated from water after several months of storage, leading to production of cis -PB-Si(OH) 3 solid elastomer with extremely low T g at −107.0 °C. The left cis -PB-Si(OH) 3 -based micelles in water with relatively small size gradually formed the water-insoluble cis -PB-Si(OH) 3 -based supramolecular aggregates or networks. The cis -PB-Si(OH) 3 -based supramolecular elastomer exhibited excellent self-healing property within 60 s at 25 °C. The elastomer (20 mg) in a joint of 25 mm × 30 mm (2.7 mg/cm 2 ) provided very strong adhesion for two pieces of glass and the bound glass keep unchanged at room temperature for 98 h even hung with 100 g of steel column below. The cis -PB-Si(OH) 3 -based supramolecular elastomer would have potential applications in adhesives, self-healing materials, damping materials and elastic materials.
✓ 已验证
产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2020
·
IF 4.845
Fangyuan Wang,Zhuanzhuan Yang,Mengli Liu,Yaotian Tao,Zhenbao Li,Zonghao Wu,Shuangying Gui
A rotigotine (ROT)-loaded polymer micelles thermosensitive gel (ROT-PM-TSG) delivery system was engineered to enhance the solubility of the drug, prolong the residence time, and increase the concentration of the drug in the brain tissue. First, ROT-loaded polymer micelles (ROT-PM) were tailored and optimized. The average particle size, encapsulation efficiency, and drug loading of the ROT-PM were (88.62 ± 1.47) nm , (93.5 ± 0.79) %, and (19.9 ± 0.60) %. The optimal ROT-PM-TSG formulation contained 22% P407 and 2% P188 with a gelation temperature of about 32.3 °C and a pH of 5.186. In vivo , the MRT of ROT-PM and ROT-PM-TSG nasal administration was 1.43 and 1.79 times extended than that of the intravenous. In comparison with the intravenous group, the distribution of ROT in olfactory bulb, cerebrum , cerebellum and striatum was 276.6%, 170.5%, 166.5% and 184.4%, respectively. In conclusion, the ROT-PM-TSG system has proven to be a potential application prospect as a ROT nose-to-brain delivery system.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）