JOURNAL OF APPLIED POLYMER SCIENCE
·
2015
·Vol. 133
·期 9
·
IF 1.768
Xiangxiang Du,Guohua Jiang,Lei Li,Wentong Yang,Hua Chen,Yongkun Liu,Qin Huang
Glucose-sensitive and fluorescence copolymer micelles were designed and prepared via a combination of photoinitiated polymerization and enzymatic transesterification. The water-soluble photoinitiator and emulsifier 2-oxooctanoic acid self-polymerized dimer molecules under UV irradiation were characterized by mass spectrometry. The fluorescence dye (9-anthracene alcohol) and biocompatible hydrophilic chains [poly(ethylene glycol)] were introduced to the polymer chains during the photopolymerization and enzymatic transesterification processes. The as-prepared copolymers were confirmed by 1 H-NMR spectroscopy, Fourier transform infrared spectroscopy, transmission electron microscopy, and dynamic light scattering. The resulting copolymers exhibited excellent glucose sensitivity and stability against protein. The optical fluorescence properties of the copolymer micelles were investigated with fluorescence spectrophotometry, fluorescence microscopy, and confocal laser scanning microscopy. Because of the amphiphilic feature, the micelles could be self-assembled and used to load insulin. The controlled release of insulin was evaluated and was triggered by glucose in vitro . This study provided a new strategy for fabricating functional carriers as self-regulated insulin-release systems. © 2015 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2016 , 133 , 43026.
✓ 已验证
产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2015
·
IF 3.65
Lijuan Chen,Liwei Tan,Xiaoning Zhang,Jun Li,Zhiyong Qian,Mingli Xiang,Yuquan Wei
In this paper, we systemly compared the two kinds of VP16 (etoposide) loaded polymers micelles , monomethyl poly (ethylene glycol)-poly (lactic acid) (MPEG-PDLLA) and monomethyl poly (ethylene glycol)-poly (ϵ-caprolactone) (MPEG-PCL) in vitro and in vivo . Molecular modeling study was used as a novel means to compare the two formulations. In vitro , the micelle samples were fully characterized by TEM, XRD, drug loading (DL), Encapsulation efficiency (EE), stability and MTT. The stability study revealed that MPEG-PDLLA-VP16 had the significant advantage of 100% drug retention within 48 h compared to MPEG-PCL-VP16 with 40%, conform to the computer simulation model results. Cellular uptake figured that MPEG-PDLLA-VP16 had a 7 times larger uptake rate in the H460 cell line. In vivo , pharmacodynamics results showed MPEG-PDLLA-VP16 perform no significant difference with VP16 clinical formulations (10, 20 mg/kg). However, MPEG-PCL-VP16 had no difference between different dosages on anticancer activities. Plasma pharmacokinetics results showed that the two micelle formulations prolong the half-life of VP16 twice than that of VP16 clinical formulations. In conclusion, micelle were better choice for cancer treatment on reducing drug toxic. In this study, the results also indicated that MPEG-PDLLA was more suitable for VP16 than MPEG-PCL as a more promising formulation for clinical cancer treatment.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
RSC Advances
·
2015
·Vol. 5
·期 115
·94719-94731
·
IF 3.84
Lili Chen,Xiaohong Wang,Fangling Ji,Yongming Bao,Jingyun Wang,Xianwu Wang,Lianying Guo,Yachen Li
Combined treatment of drugs and therapeutic genes has emerged as a new modality of anticancer therapy. In this study, a new amphiphilic bifunctional pullulan derivative (named as PSP) containing stearic acid and low-molecular weight (1 kDa) branched polyethylenimine was prepared and evaluated as a nano-carrier for the co-delivery of a drug and gene for potential cancer therapy. The amphiphilic PSP could self-assemble into cationic core–shell nano-micelles in water, with a critical micelle concentration of around 58.9 mg L−1. PSP nanomicelles had an average size of 188.75 ± 3.18 nm, and a positive zeta potential of 17.83 ± 0.75 mV. The drug loading content and encapsulation efficiency of the PSP nanomicelles for doxorubicin (DOX), an anti-tumor drug, were about 5.10% and 56.07%, respectively, and DOX in PSP nanomicelles showed sustained release. The flow cytometry and confocal laser scanning microscopy showed that PSP/DOX nanomicelles could be successfully internalized by MCF-7 cells. The in vitro IC50 of PSP/DOX nanomicelles was slightly lower than that of free DOX against MCF-7 cells. Additionally, PSP nanomicelles condensed DNA efficiently to form compact structures, and induced comparable GFP gene expression level to Lipo2000 at N/P = 10 in gene transfection studies. In comparison with single DOX or p53 delivery, the co-delivery of DOX and therapy gene p53 using PSP micelles displayed higher cytotoxicity and induced a higher apoptosis rate of tumor cells in vitro. Moreover, PSP exhibited good blood compatibility and low cytotoxicity in the hemolysis and MTT assays, respectively. Altogether, PSP nanomicelles have a great potential in delivering hydrophobic anticancer drugs and therapeutic genes simultaneously for improved cancer therapy.
✓ 已验证
产品关联
DOI
高影响因子
Journal of Materials Chemistry B
·
2016
·Vol. 5
·期 5
·961-971
·
IF 4.872
Yan Wen,Fan Li,Chunge Li,Yuji Yin,Junjie Li
High mechanical strength hydrogels without burst release are known to be beneficial to deliver bioactive molecules including drugs and growth factors. Herein, chitosan-based hydrogels are fabricated by the covalent attachment of poly(ethylene glycol) diacrylate (PEGDA) to thiol groups of thiolated natural polymers via Michael addition reaction under physiological conditions. Poly(ethylene glycol-b-caprolactone-b-ethylene glycol) (PECL) micelles bearing double bonds act as both fillers and chemical cross-linkers to mechanically reinforce chitosan-based hydrogels, which is confirmed by the results of rheological behavior and compressive strength measurements. Indomethacin (IMC) and/or basic fibroblast growth factor (bFGF) are/is entrapped into the PECL micelle cross-linked hydrogel network primarily through hydrophobic interaction and specific affinity to thiolated heparin, respectively. After a relatively quick initial release, rather than an initial burst commonly occurring in conventional hydrogels based on drug delivery systems, IMC and/or bFGF are/is released from these PECL micelle cross-linked hydrogels at a slower rate until a steady state is reached. The release rate of IMC and/or bFGF could be readily tuned by varying the micelle amount and the thiolated heparin content in a polymer matrix.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2025
·
IF 8.5
Xiaobing Liang,Jiaxin Li,Zhihui Li,Yibin Lin,Hailiang Li,Duoqu Chen,Yonghui Xiao,Wenjing Lin,Chufen Yang,Guobin Yi
Photo redox atom transfer radical polymerization (ATRP) represents an excellent technique for forming multifunctional polymers. However, there was little report on photo redox ATRP of graphene quantum dots (GQDs). Herein, we reported that introduced GQDs to ATRP in DMF solvent for the first time, significantly reducing the amount of copper catalyst (<500 ppm) required for the synthesis of alkali lignin-poly( N -isopropylacrylamide)-poly( N , N -dimethylaminoethyl methacrylate)-poly(poly(ethylene glycol) methyl ether methacrylate) (AL-(PNIPAM-PDMAEMA-PPEGMA) 2 ). The copolymer had molecular weight of 46,884 and polydispersity index (PDI) of 1.07. The micelles self-assembled from AL-(PNIPAM-PDMAEMA-PPEGMA) 2 in aqueous solution served as an excellent template for the simultaneous in situ preparation of silver nanoparticles (AgNPs) and the encapsulation of the hydrophobic anticancer drug camptothecin (CPT). By adjusting the mole ratio of [DMAEMA]:[AgNO 3 ], a series of AgNPs with controllable sizes (2.5–20.6 nm) could be obtained. AL-(PNIPAM-PDMAEMA-PPEGMA) 2 @Ag@CPT exhibited temperature and pH-sensitive release properties, releasing 80 % of the drug in an acidic and 37 °C tumor environment within 120 h. Furthermore, 150 μg/mL AL-(PNIPAM-PDMAEMA-PPEGMA) 2 @Ag@CPT effectively killed 75 % of cells within 48 h. 800 μg/mL AL-(PNIPAM-PDMAEMA-PPEGMA) 2 @Ag@CPT demonstrated highly efficient antibacterial effects. All these results suggest its potential application value in synergistic antitumor and antibacterial treatment system.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
BIOMACROMOLECULES
·
2024
·
IF 5.5
Yuhan Yang,Yangyi Chen,Yue Wei,Wei Wu,Qing Wang,Tianyun Xue,Xiaoyan Zhang,Wei Chen,Wei Zhang
A drug delivery system based on silybin-conjugated chitosan (CS-SB) polymeric micelles was developed to improve the oral absorption of doxorubicin (DOX). SB was grafted to CS via succinic acid, and CS-SB was identified by 1H NMR and FT-IR. The DOX-loaded micelles were prepared by self-assembly, and the characteristics of micelles, including a small particle size of 167.8 ± 2.3 nm, a high drug loading capacity of 8.59%, and a low critical micelle concentration of 1.3 × 10–5 g/mL, were demonstrated. The micelles showed oral bioavailability of up to 193% versus DOX·HCl. The cytotoxicity test showed the biosafety of CS-SB and the potential of reductive DOX-induced cardiotoxicity. The inhibition of P-gp efflux and CYP3A4 enzyme in CS-SB micelles was confirmed by cellular uptake and enzyme activity inhibition tests. The endocytosis process of micelles was revealed by an endocytosis inhibition test. The findings exhibited the potential of CS-SB micelles in drug delivery.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
MOLECULAR PHARMACEUTICS
·
2018
·
IF 4.556
Shihong Shao,Yun Zhu,Tingting Meng,Yupeng Liu,Yun Hong,Ming Yuan,Hong Yuan,Fuqiang Hu
Liver metastasis is a leading death cause in colorectal cancer. The pathological differences between orthotopic tumors and metastatic lesions increased the therapeutic difficulty of metastasis. Herein, the α5β1 integrin receptor expression on metastatic cells was first measured, the result showed that metastatic cells expressed the α5β1 integrin higher than that of the original cells from orthotopic tumors. Afterward, RPM peptide-modified chitosan-stearic (RPM-CSOSA) was designed based on α5β1 integrin expression. The cytotoxicity and resistance to migration and the invasion ability of the targeting drug delivery system loading doxorubicin (DOX) and curcumin (CUR) were evaluated in vitro. The metastatic inhibition of the targeting drug delivery system was also investigated in HT29 liver metastatic models. The modified RPM peptide could increase the cellular internalization of CSOSA micelles in metastatic tumor cells and endothelial cells mediated by α5β1 integrin. The synergistic effects of RPM-CSOSA/DOX and RPM-CSOSA/CUR could obviously inhibit migratory and invasive abilities of HT29 cells and endothelial cells. Moreover, the RPM-CSOSA/DOX&RPM-CSOSA/CUR could obviously decrease the number of metastatic sites by 86.96%, while CSOSA/DOX&CSOSA/CUR decreased liver metastasis by 66.58% compared with that in the saline group. In conclusion, the RPM peptide-modified drug delivery system may provide insights into targeting the metastatic cells overexpressing the α5β1 integrin, and it has the potential to inhibit liver metastasis of colorectal cancer.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Pharmaceutics
·
2024
·Vol. 16
·期 10
·1327
·
IF 4.9
Huiping Zhang,Liang Li,Wei Li,Hongxia Yin,Huiyun Wang,Xue Ke
Background:CPT is a pentacyclic monoterpene alkaloid with a wide spectrum of antitumor activity. Its clinical application is restricted due to poor water solubility, instability, and high toxicity. We developed a new kind of multifunctional micelles to improve its solubility, reduce the side effecs, and obtain enhanced antitumor effects.Methods:We constructed HA-CPT nano-self-assembly prodrug micelles, which combined the advantages of pH-sensitivity, redox-sensitivity, and active targeting ability to CD44 receptor-overexpressing cancer cells. To synthesize dual sensitive HA-CPT conjugates, CPT was conjugated with HA by pH-sensitive histidine (His) and redox-sensitive 3,3′-dithiodipropionic acid (DTPA). In vitro, we studied the cellular uptake and antitumor effect for tumor cell lines. In vivo, we explored the bio-distribution and antitumor effects of the micelles in HCT 116 tumor bearing nude mice.Results:The dual-sensitive and active targeting HA-His-ss-CPT micelles was proved to be highly efficient in CPT delivery by the in vitro cellular uptake study. The HA-His-ss-CPT micelles escaped from endosomes of tumor cells within 4 h after cellular uptake due to the proton sponge effect of the conjugating His and then quickly released CPT in the cytosol by glutathione (GSH). In mice, HA-His-ss-CPT micelles displayed efficient tumor accumulation and conspicuous inhibition of tumor growth.Conclusions:The novel, dual-sensitive, active targeting nano-prodrug micelles exhibited high efficiency in drug delivery and cancer therapy. This “all in one” drug delivery system can be realized in an ingenious structure and avoid intricate synthesis. This construction strategy can illume the design of nanocarriers responding to endogenous stimuli in tumors.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Soft Matter
·
2012
·Vol. 8
·期 46
·11644-11653
·
IF 4.39
Zhangwei Wang,Hengjie Lai,Peiyi Wu
The assembly properties, thermal phase behavior and microdynamics of poly(NIPAM-b-BVImBr), poly(N-isopropylacrylamide)-b-poly(1-butyl-3-vinylimidazolium bromide), in aqueous solution are investigated by dynamic light scattering (DLS), turbidity measurements and FTIR spectroscopy in combination with two-dimensional correlation spectroscopy (2Dcos) and the perturbation correlation moving window (PCMW) technique. In particular, the influence of the introduction of the poly(BVImBr) segment on the solution properties of the block copolymer has attracted our attention: a core–shell micelle structure forms, consisting of a relatively hydrophobic core of poly(BVImBr) and a hydrophilic shell of PNIPAM; the phase transition temperature increases, due to one more step in the dehydration process originating from the alkyl side chains of the poly(1-butyl-3-vinylimidazolium bromide) (PIL) segment; what's more, a stronger hysteresis during the heating–cooling cycle, closely related to the recovery process, is observed. It reveals that the hydrogen bonds of CO⋯D–N among the micelles formed during heating are harder to remove, thus, the reconstruction of the CO⋯D–O–D hydrogen bonding and the recovery hydration process for the C–H groups during cooling are prevented due to the compact and regular micelle structure. More interestingly, the CO groups interact with the N–D groups at room temperature because of the existence of the micelle structure, which is regarded as intra-micelle hydrogen bonding; above the LCST, hydrogen bonds of the CO⋯D–N among the aggregated micelles called inter-micelle hydrogen bonding occur.
✓ 已验证
产品关联
DOI
高影响因子
Polymers
·
2025
·Vol. 17
·期 3
·349
·
IF 4.9
Jizheng Song,Yu Hu,Shiyu Yang,Dexue Liu,Yiider Tseng,Lingjun Li
Hydrophobic modification alters the properties of Pluronic F127 to form micelles more efficiently and enhances its drug-loading capacity. However, selecting the appropriate hydrophobic group for modification is laborious. In this paper, we propose an efficient approach for predicting key parameters to select hydrophobic groups for F127 modification prior to synthesis, in order to improve the formability and stability of the micelles. The results of nuclear magnetic resonance and isothermal titration calorimetry were utilized to establish a function for predicting the hydrophile–lipophile balance, critical micelle concentration, and Gibbs free energy of the products based on the structure of raw material. These predicted values can assist us in selecting suitable hydrophobic groups for F127 modification. Subsequently, we successfully tested our method and validated our work using pharmaceutical evaluation methods, such as appearance observation, particle size measurement, drug loading determination, equilibrium binding rate assessment, storage stability testing, and the plotting of accumulation release curves. Therefore, we suggest that our work could provide a model linking the molecular structure to properties, with the purpose of pre-selecting modification products that have advantages in micelle preparation. This can facilitate the application of F127 in preparing nano-micelles.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
CHEMICAL ENGINEERING RESEARCH & DESIGN
·
2024
·
IF 3.7
Zhirong Zhang,Linhui Sun,Xu Huo,Xianggui Liu,Xiuxiu Pan
Carbon Dioxide capture, oil displacement and Storage (CCUS-EOR) projects inject captured carbon dioxide into developed reservoirs suitable for gas displacement. However, due to the strong heterogeneity of the reservoir, the CO 2 channeling is seriously. In this study, using tung oil as renewable chemical raw material, environmentally friendly surfactants and hydrophobic nano-SiO 2 were synthesized as the main components of smart gel system. Fourier transform infrared (FT-IR), nuclear magnetic resonance spectrum (NMR) and thermogravimetric analysis (TGA) were used to characterize the chemical structure. The smart gel system was obtained through the CO 2 response experiment. The system can cycle back and forth between low and high viscosity multiple times, and a good temperature resistance and salt resistance. The results of rheological experiments and dynamic light scattering show that the nanoparticles promote the growth and entanglement of WLMs. The plugging capacity and auxiliary CO 2 -EOR performance of the system were evaluated through the laboratory displacement test. The intelligent response system has good gas channeling plugging ability, plugging efficiency reaches 97 %, and CO 2 flooding oil recovery efficiency increases by 22.2 %. In addition, in the acute toxicity assessment, the bio-based gel system from plants showed slightly toxic, which is expected to become a new generation of green oilfield chemicals.
✓ 已验证
产品关联
DOI
高影响因子
Pharmaceutics
·
2020
·Vol. 12
·期 2
·111
·
IF 4.421
Weinan Li,Jialin Sun,Xiaoyu Zhang,Li Jia,Mingxi Qiao,Xiuli Zhao,Haiyang Hu,Dawei Chen,Yanhong Wang
PEG-poly(β-amino ester) (PEG-PBAE), which is an effective pH-responsive copolymer, was mainly synthesized by Michael step polymerization. Thioridazine (Thz), which was reported to selectively eliminate cancer stem cells (CSCs), was loaded into PEG-PBAE micelles (PPM) prepared by self-assembly at low concentrations. The critical micelle concentrations (CMC) of PPM in water were 2.49 μg/mL. The pH-responsive PBAE segment was soluble due to protonated tertiary amine groups when the pH decreased below pH 6.8, but it was insoluble at pH 7.4. The Thz-loaded PEG-PBAE micelle (Thz/PPM) exhibited a spherical shape, and the drug loading was 15.5%. In vitro release of Thz/PPM showed that this pH-sensitivity triggered the rapid release of encapsulated Thz in a weakly acidic environment. The in vitro cytotoxicity and cellular uptake of various formulations at pH 7.4 and 5.5 were evaluated on the mammospheres (MS), which were sorted by MCF-7 human breast cancer cell lines and identified to be a CD44+/CD24−phenotype. The results of the cytotoxicity assay showed that blank micelles were nontoxic and Thz/PPM exhibited a similar anti-CSC effect on MS compared to Thz solution. Stronger fluorescence signal of Coumarin-6 (C6) was observed in MS treated by C6-loaded PPM (C6/PPM) at pH 5.5. The tumor inhibition rate and tumor weight of the free DOX and Thz/PPM groups were significantly different from those of the other groups, which free DOX and Thz/PPM effectively suppressed breast tumor growth in vivo. The above experimental results showed that Thz/PPM is an ideal and effective pH-responsive drug delivery carrier to a targeted therapy of CSCs.Keywords:poly(β-amino ester);polymeric micelles;pH-responsive;cancer stem cells;thioridazine
✓ 已验证
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）