JOURNAL OF APPLIED POLYMER SCIENCE
·
2015
·Vol. 132
·期 40
·
IF 1.768
Xiaofen Hu,Yuyan Zhang,Huifen Zhou,Haitong Wan
PEGylated chitosans with different degrees of grafting were synthesized, and the application potential of microspheres based on PEGylated chitosan as mucoadhesive drug-delivery carriers for puerarin was investigated. Compared with chitosan microspheres, PEGylated chitosan microspheres (PCMs) exhibited better physical stability and higher swelling capacity, and the amount of water uptake increased as the content of poly(ethylene glycol) methyl ether in the microspheres increased. PCMs showed obviously improved mucoadhesive behavior on a mucosa-like surface. Puerarin was incorporated into the microspheres, and the release experiments in vitro showed that the PEGylation of chitosan accelerated puerarin release from the particles and decreased the retention of the drug. The abilities of all of the tested microspheres to open tight junctions and improve the permeability of puerarin were demonstrated with a Caco-2 cell monolayer as an in vitro model. The amount of puerarin permeating across the Caco-2 cell monolayer was significantly increased by the incorporation of puerarin into the PCMs. © 2015 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2015 , 132 , 42623.
研究领域:
药剂学
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生物材料
·
药物传递系统
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DOI
高影响因子
Drug Research
·
2017
·Vol. 68
·期 05
·270-279
·
IF 0
Shuoye Yang
Long-circulating liposomal delivery systems of encapsulated Coenzyme Q10 (CoQ10), a ubiquinone anti-cataract agent, were developed with different molar ratios of PEGylated lipids and/or cholesterol. The resulting samples were contrasted through observation of morphology, analysis of particle size and Zeta potential, and in vivo pharmacokinetics. A protamine aggregation method with high selectivity was developed to determine the encapsulation efficiency (EE), after which the liposome formulation was further optimized by applying a Box Behnken design (BBD) using EE as the evaluation index. The results showed that liposomes had a large, unilamellar structure, and that particle sizes of cholesterol-containing liposomes increased along with the increase of cholesterol molar percentage, while the size of PEGylated vesicles decreased slightly as PEG-lipid contents increasing. The optimum formulation and optimal values of each influencing factor were quantitatively obtained, and the measured value was highly consistent with the predicted results. In vivo evaluation performed by liquid chromatography coupled with tandem mass spectrometry (LC-MS/MS) demonstrated that liposomal encapsulation largely prolonged half-lives and improved bioavailability for vectors prepared with either lipid component, and the liposomes composed of both cholesterol and PEG-lipid possessed the best pharmacokinetic properties. The results suggest that incorporating high contents of cholesterol and PEG modification could be a potentially useful method for enhancing the length of circulation and the sustained release effect for liposome-encapsulated chemicals.
研究领域:
药剂学
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生物医学工程
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药物代谢动力学
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DOI
PubMed
MACROMOLECULAR BIOSCIENCE
·
2021
·Vol. 21
·期 8
·2100077
·
IF 4.979
Yu Zhang,Xinming Liu,Xueping Wang,Pan He,Chunsheng Xiao,Haiyang Yu,Xuesi Chen
Chemotherapy using vascular targeting agents is an emerging new approach for cancer therapy. Combretastatin A4 (CA4) is a leading vascular-disrupting agent that targets the tumor blood vasculature for clinical tumor elimination. However, the extremely poor water solubility of CA4 hinders its biomedical applications. In this study, nanoparticles composed of novel PEGylated alternating copolymer-CA4 conjugates are designed to improve the therapeutic efficiency of CA4. First, an alternating copolymer with an alkene-pendant is synthesized by mPEG-OH-initiated ring-opening copolymerization. Then, side carboxyl groups are introduced by a thio-ene “click” chemical reaction, followed with CA4 conjugation through the Yamaguchi-reaction, resulting in the target copolymer, mPEG- b -P(PA- alt -GCA4). Interestingly, the polymer-drug conjugates can self-assemble into nanoparticles with an average diameter of 55.6 nm. The in vitro drug release and cytotoxicity of the obtained CA4-NPs toward 4T1 cells are investigated. Finally, the antitumor efficiency is evaluated in a 4T1-tumor bearing murine model. The in vivo test results demonstrate that CA4-NPs inhibited tumor growth much more efficiently at doses of 30 and 60 mg kg −1 , compared with the control group.
研究领域:
药学
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肿瘤学
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生物材料学
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产品关联
DOI
PubMed
高影响因子
COLLOIDS AND SURFACES B-BIOINTERFACES
·
2018
·
IF 3.997
Zichen Xie,Jianfeng Song,Heng Zhang,Yifei Zhuang,Shenqi Xie,Yongliang Li,Zhimin Li,Mei Liu,Keyu Sun
The prodrug strategy serves well in drug formulation and delivery. Two disulfide-based PEGylated prodrugs were developed and the drug reconversion upon different conditions were studied in detail. The reconversion-induced oversaturation phenomenon was firstly reported here. We found the prodrug can co-assemble with parent drug via π-π stacking into well-defined nanoparticles. The PEG layer of the self-assembled nanoparticles improved the stability of the PEGylated prodrug by reducing the contact with biological enzymes. The nanoparticles also show favorable antitumor efficacy, both in vitro and in vivo .
研究领域:
药物化学
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生物医学工程
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肿瘤学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
CHEMISTRY OF MATERIALS
·
2015
·
IF 8.354
Mingxia Jiao,Jianfeng Zeng,Lihong Jing,Chunyan Liu,Mingyuan Gao
PEGylated Fe3O4 nanoparticles were prepared through flow synthesis upon the pyrolysis of ferric acetylacetonate (Fe(acac)3) in anisole at 250 °C under pressure of 33 bar, in the presence of α,ω-dicarboxyl-terminated polyethylene glycol (HOOC–PEG–COOH) and oleylamine. In combination with theoretical analysis, the effects of linear velocity, residence time, and reactor dimension on particle size distribution were systematically investigated. In addition, the impact of Ostwald ripening on particle size distribution was also revealed. In particular, the impacts of monomer concentration distributions along both axial and radial directions of the tube reactor on the particle size distribution were carefully investigated. Under optimized conditions, PEGylated Fe3O4 nanoparticles with the relative standard deviation of particle size down to 10.6% were thus obtained. The resulting 4.6 nm particles exhibited excellent colloidal stability and high longitudinal relaxivity (r1) up to 11.1 mM–1·s–1, which manifested the reliability of flow synthesis in preparing PEGylated Fe3O4 nanoparticles as contrast agents for magnetic resonance imaging applications.
研究领域:
材料科学
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医学影像
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纳米技术
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产品关联
DOI
高影响因子
JOURNAL OF NANOSCIENCE AND NANOTECHNOLOGY
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2016
·Vol. 16
·期 7
·7530-7538
·
IF 1.338
Wang Yang,Nie Jinshan,Wang Wei,Gu Zhun
In this work, redox and pH responsive vesicles of PEGylated hyperbranched poly(amidoamine)-doxorubicin (PPCD) conjugates were prepared for the improvement of cancer therapy. The PPCD 3/1 and PPCD 6/1 conjugates were respectively prepared by the acid sensitive cis-aconityl linkage
between doxorubicin and differently PEGylated hPAMAM (PEG3-g-hPAMAM and PEG6-g-hPAMAM). The PPCD vesicles were prepared by disulfide-crosslinking the micelles formed in THF and then transferring them from THF into water. The crosslinked
PPCD vesicle with a higher PEGylated degree showed a measurable decrease in size and zeta potential. Both the crosslinked PPCD vesicles could be disassembled into small-sized conjugates under the redox condition. The drug release profiles showed that the both vesicles presented stimuli-triggered
drug release in acidic and reducing environment and lower DOX leakage under neutral condition. The cytotoxicity assay reflected that both the PPCD vesicles could effectively kill the gastric cancer MGC803 cells, and PPCD 6/1 vesicle with smaller size presented higher cytotoxicity than PPCD
3/1 vesicle. Considering the more applicable size (about 100 nm), higher capacity of killing tumor cells and better compatibility, the PPCD-6 vesicle with higher PEGylation degree is more favorable to promote the therapeutic effect of cancer, and will be more suitable as drug delivery system
for solid tumor treatment.
研究领域:
药剂学
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肿瘤学
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生物材料学
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DOI
高影响因子
RSC Advances
·
2020
·Vol. 10
·期 41
·24624-24630
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IF 3.119
Gaizhen Kuang,Qingfei Zhang,Shasha He,Ying Liu
Curcumin (Cur) can be used as a photosensitizer in the photodynamic therapy (PDT) of cancer, but its low bioavailability limits further clinical application. A mesoporous silica-based drug delivery system (PEGylated mesoporous silica nanoparticles, MSN-PEG@Cur) was designed to solve the problem. The successful preparation of MSN-PEG@Cur was characterized by several physico-chemistry techniques. The endocytosis, ROS generation and in vitro anti-cancer efficacy of MSN-PEG@Cur were evaluated in detail step by step. The results indicated that MSN-PEG@Cur could be effectively endocytosed into cells and release Cur, which can promptly generate ROS upon irradiation, achieving effective PDT in cancer treatment. This MSNs-based drug delivery system provides an alternative strategy for Cur loading and PDT of cancer.
研究领域:
药学
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纳米医学
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肿瘤学
✓ 已验证
DOI
高影响因子
JOURNAL OF BIOMATERIALS APPLICATIONS
·
2019
·
IF 2.442
Anlin Yin,Xiaorong Lan,Weihua Zhuang,Zhonglan Tang,Yan Li,Yunbing Wang
In this study, we fabricated native tissue mimicking a bilayered small-diameter vascular graft based on PEGylated chitosan (PEG–CS) and poly(l-lactic acid-co-ε-caprolactone) (PLCL). PEG–CS possesses good hemocompatibility, and as the inner layer of a vascular graft, it is more likely to swell and deform to debris, causing a blood clot, so the PLCL was added to stabilize it. In order to optimize the performance of the inner layer, PEG–CS blends with different ratios of PLCL (P/C:PLCL) casting films were fabricated, and endothelial cell compatibility and hemocompatibility were tested. The outer layer of the graft was fabricated via electrospinning with PLCL blends with different ratios of water-soluble polyethylene glycol. After water treatment, we tested smooth muscle cell penetration. Designing a two-layer vascular graft structure with an inner layer of P/C:PLCL = 1:6 and an outer layer being composed of a PLCL blend with 12% polyethylene glycol offers very good hemocompatibility and fast cell growth and also reserves well mechanical properties with good cell infiltration. Therefore, this kind of graft has a high potential to be used as an artificial blood vessel.
研究领域:
生物材料学
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组织工程学
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产品关联
DOI
PubMed
高影响因子
NEW JOURNAL OF CHEMISTRY
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2018
·Vol. 42
·期 14
·11565-11572
·
IF 3.201
Tao Wang,Guorong Jia,Chao Cheng,Qiuhu Wang,Xiao Li,Yanyan Liu,Chaofan He,Luguang Chen,Gaofeng Sun,Changjing Zuo
Multimodal imaging can improve the accuracy of cancer diagnosis by combining two or more imaging modalities into one system. In this study, PEGylated BaGdF5 nanoparticles (NPs) were synthesized by a hydrothermal method, and the formed PEG-BaGdF5 NPs showed good X-ray attenuation properties and positive MR contrast effects in vitro. Considering that the overexpression of integrin αvβ3 in the endothelial cells of angiogenic tumor vasculature is universal, RGD peptide, which can recognize and bind integrin αvβ3 specifically, was connected to the surface of PEG-BaGdF5 NPs. The resulting RGD-PEG-BaGdF5 NPs had good biocompatibility and a long half-life in vivo. In VX2 tumor-bearing mice, the HU values and MR signal enhancement of tumor sites in the targeted group were both higher than that in the non-targeted group after intravenous injection of RGD-PEG-BaGdF5 NPs or PEG-BaGdF5 NPs, respectively. Therefore, the RGD-PEG-BaGdF5 NPs may be used as dual-modal CT/MR contrast agents of different types of solid tumors via an active RGD-mediated vasculature targeting pathway.
研究领域:
医学影像
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纳米技术
·
肿瘤学
✓ 已验证
产品关联
DOI
高影响因子
BIOMACROMOLECULES
·
2020
·
IF 6.092
Shuyue Zhao,Wenjun Huang,Changrong Wang,Yaping Wang,YuFeng Zhang,Zhanpeng Ye,Jianhua Zhang,Liandong Deng,Anjie Dong
The amphiphilic cationic polymers that mimic antimicrobial peptides have received increasing attention due to their excellent antibacterial activity. However, the relationship between the structure of cationic polymers and its antibacterial effect remains unclear. In our current work, a series of PEG blocked amphiphilic cationic polymers composed of hydrophobic alkyl-modified and quaternary ammonium salt (QAS) moieties have been prepared. The structure–antibacterial activity relationship of these cationic polymers was investigated against E. coli and S. aureus, including PEGylation, random structure, molecular weights, and the content and lengths of the hydrophobic alkyl side chains. The results indicated that PEGylated random amphiphilic cationic copolymer (mPB35/T57) showed stronger antibacterial activity and better biocompatibility than the random copolymer without PEG (PB33/T56). Furthermore, mPB35/T57 with appropriate mole fraction of alkyl side chains (falkyl = 0.38), degree of polymerization (DP = 92), and four-carbon hydrophobic alkyl moieties was found to have the optimal structure that revealed the best antibacterial activities against both E. coli (MIC = 8 μg/mL, selectivity > 250) and S. aureus (MIC = 4 μg/mL, selectivity > 500). More importantly, mPB35/T57 could effectively eradicate E. coli biofilms by killing the bacteria embedded in the biofilms. Therefore, the structure of mPB35/T57 provided valuable information for improving the antibacterial activity of cationic polymers.
研究领域:
微生物学
·
材料科学
·
药理学
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产品关联
DOI
PubMed
高影响因子
RSC Advances
·
2015
·Vol. 5
·期 86
·70109-70116
·
IF 3.84
Gongyan Liu,Quanqing Luo,Haibo Wang,Weihua Zhuang,Yunbing Wang
To realize desirable functions in the rather complex biological systems, a suitable surface coating is desirable for gold nanoparticles, which plays an important role in their colloidal stability and biocompatibility. In this work, a novel multidentate PEGylated chitosan derivative was synthesized by conjugating PEG and dithiolane lipoic acid (LA) to the chitosan backbone. Under reduction conditions, gold nanoparticles (AuNPs) could be in situ formed by the electrostatic interaction between amino groups of the chitosan derivative and gold chloride ions (AuCl4−), with their surface covalently coated by the multidentate PEGylated chitosan via the disulfide bond from LA. After the surface modification, such AuNPs exhibited remarkable colloidal stabilities under extreme conditions, including high salt conditions and complex biological media containing serum. Moreover, the multidentate PEGylated chitosan also provided AuNPs with good biocompatibility and low cytotoxicity, resistance of protein adsorption and anti-phagocytosis by RAW 264.7 cells. This kind of AuNP was expected to be a promising platform for applications in nanomedicine.
研究领域:
材料科学
·
生物医学工程
·
纳米技术
✓ 已验证
产品关联
DOI
高影响因子
RSC Advances
·
2015
·Vol. 5
·期 130
·107949-107956
·
IF 3.84
Xuemin Yu,Zhu Xiong,Jinglong Li,Ziyang Wu,Yunze Wang,Fu Liu
Poly(lactic acid) (PLA) has attracted growing attention as a sustainable and environmentally benign membrane material. The good biocompatibility/hemocompatibility is essential for hemodialysis membranes. To circumvent the inadequate hydrophilicity/biocompatibility/hemocompatibility, we have developed a feasible strategy that enables the persistent PEGylation on PLA membranes via micro-swelling and subsequent UV-initiated crosslinking of poly(ethylene glycol)diacrylate (PEGDA). The content of DMSO and PEGDA in the reaction solution was crucial to control the surface PEGylation kinetics. Besides, the influence of PEGylation on membrane chemistry, morphology, hydrophilicity, water flux and dynamic fouling resistance to BSA was investigated. It was demonstrated that the biocompatibility/hemocompatibility was significantly improved by the surface PEGylation in terms of reduced BSA adsorption, extended APTT and alleviative platelet adhesion.
研究领域:
材料科学
·
生物医学工程
✓ 已验证
产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）