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POLYMERS FOR ADVANCED TECHNOLOGIES · 2023 · IF 3.4

Influence of PEG-PLGA nanoparticles on the pore structure of injectable and self-healing hydrogels based on carboxymethyl chitosan/aldehyde sodium hyaluronate for prolonged sustained release of valsartan

Chihao Gao,Lixia Pan,Jie Song,Min Wei,Haozhi Sun,Feng Su,Xin Shen,Suming Li

Valsartan is almost insoluble, resulting in very low bioavailability. Preparing prolonged sustained-release systems to achieve valsartan drug delivery is essential. Herein, two types of poly(ethylene glycol)-b-poly(lactide-co-glycolide) (PEG-PLGA) nanoparticles loading valsartan and carboxymethyl chitosan/aldehyde sodium hyaluronate hydrogels were prepared. The nanoparticles and hydrogel composites(NPs@Gel) were obtained by physical mixing. The NPs@Gel composites have swelling ratios within the scope from 157.87% to 206.51% and mass loss within the scope from 12.85% to 17.32%, influenced by incorporating PEG-PLGA nanoparticles. Moreover, the NPs@Gel composites had properties of self-healing and injection proven by rheological measurements. Importantly, adding nanoparticles could significantly reduce the swelling ratios of the hydrogels by shrinking the void fraction and enhancing the mechanical properties. Meanwhile, NPs@Gel composites also present excellent biocompatibility as evidenced by hemolysis test and MTT assay. Therefore, a potential prolonged sustained-release system of NPs@Gel for the delivery of valsartan was achieved.

CAS / MDL: 9002-89-5
研究领域: 药剂学 · 生物材料 · 药物递送
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JOURNAL OF MOLECULAR LIQUIDS · 2022 · IF 6.633

Enhancement of long alkyl-chained imidazolium ionic liquids for the formation and extraction behaviour of PEG 600/(NH4)2SO4 aqueous two-phase system by complexing with Triton X-100

Yanrong Cheng,Xia Guo,Delan Ge,Wenlin Xu,Yaqiong Wang

Broadening the polarity range of polymer-based aqueous two-phase systems (ATPSs) is of practical significance. Recently, ionic liquids have been used as adjuvants to modify the polarity and properties of PEG-rich phases in PEG/salt ATPSs. However, thus far, only short alkyl (containing less than 8 carbon atoms)-chained ionic liquids have been able to promote the extraction performance of ATPSs; long alkyl-chained ionic liquids have decreased the extraction performance significantly due to their distribution in the bottom phase. In the present study, we found that by complexing with Triton X-100 (TX-100), long alkyl-chained imidazolium ionic liquids [C n mim]Br (n = 10 and 12) as adjuvants were enriched in the top phase of PEG/salt ATPSs, and hence, the polarity difference of the two phases were increased. By extracting two model substances (S-mandelic acid (MA) and l -tryptophan (Trp)), it was concluded that, although the long alkyl-chained [C n mim]Br adjuvant decreased the extraction performance of the ATPS substantially, the long alkyl-chained [C n mim]Br/TX-100 complex as the adjuvant enhanced the extraction performance of the ATPS significantly. Compared with the case without an adjuvant, when the [C 12 mim]Br/TX-100 complex and the [C 10 mim]Br/TX-100 complex were used as the adjuvants, the partition coefficients of MA and Trp in the PEG 600/(NH 4 ) 2 SO 4 ATPS were increased up to 3 ∼ 4 times, much better than those with short alkyl-chained ionic liquid as the adjuvant. Moreover, the [C 12 mim]Br/TX-100 complex is more conductive to the transfer of MA into the PEG-rich phase, and the [C 10 mim]Br/TX-100 complex is more conductive to the transfer of Trp into the PEG-rich phase.

CAS / MDL: 85100-78-3 25322-68-3
研究领域: 生物化学 · 分离科学 · 工业化学
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RSC Advances · 2016 ·Vol. 6 ·期 87 ·84164-84176 · IF 3.289

Effects of surface hydrophilic properties of PEG-based mucus-penetrating nanostructured lipid carriers on oral drug delivery

Huipeng Li,Nida El Islem Guissi,Zhigui Su,Qineng Ping,Minjie Sun

Nano-structured lipid carriers (NLCs) have been widely used for oral drug delivery due to their remarkable biocompatibility and biodegradability. In addition to formulation and particle size, particle surface properties are important for overcoming gastrointestinal (GI) barriers to oral drug delivery by lipid-based nanoparticles. In this study, we describe polyethylene glycol (PEG)-based mucus-penetrating NLCs and we report the effect of surface hydrophilic properties on their oral delivery across the GI mucus and intestinal epithelium cells in vivo and in vitro. The solvent evaporation method was used to prepare PEG-modified NLCs (pNLCs) with three different levels of polyethylene glycol (100) monostearate (S100) as the hydrophilic coating material. The stability and cytotoxicity of pNLCs, as well as their uptake by Caco-2 cells and transport across Caco-2 monolayers and mucus-secreting Caco-2/HT29 coculture monolayers, were investigated to confirm the optimal PEG level for oral delivery. In situ single-pass perfusion experiments, in vivo imaging and in vivo oral pharmacokinetic studies were also performed in rodents to evaluate the oral absorption of pNLCs with different hydrophilic surface properties. Our results showed that the hydration layer thickness of the pNLCs increased with the increasing S100 content. NLC containing 20% S100 (pNLC-20%) showed the highest uptake by Caco-2 cells and the most effective permeation through Caco-2/HT29 coculture monolayers compared with unmodified NLC, pNLC-40% and pNLC-80%. In addition, pNLC-20% was the most stable during the process of oral administration and uptake into the blood circulation, as judged by fluorescence resonance energy transfer (FRET). Moreover, in situ single-pass perfusion experiments, ligated intestinal loops tests, in vivo imaging and pharmacokinetics studies also demonstrated that pNLC-20% most rapidly penetrated the intestinal epithelium and had the highest AUC and Cmax of all the NLCs. In conclusion, optimization of surface hydrophilic properties is essential for enhancing the absorption of drugs delivered by oral administration of lipid-based nanocarriers.

研究领域: 药剂学 · 纳米技术 · 药物递送系统
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Nanoscale · 2014 ·Vol. 6 ·期 8 ·4361-4370 · IF 6.739

Cu2−xSe@mSiO2–PEG core–shell nanoparticles: a low-toxic and efficient difunctional nanoplatform for chemo-photothermal therapy under near infrared light radiation with a safe power density

Xijian Liu,Qian Wang,Chun Li,Rujia Zou,Bo Li,Guosheng Song,Kaibing Xu,Yun Zheng,Junqing Hu

A low-toxic difunctional nanoplatform integrating both photothermal therapy and chemotherapy for killing cancer cells using Cu2−xSe@mSiO2–PEG core–shell nanoparticles is reported. Silica coating and further PEG modification improve the hydrophilicity and biocompatibility of copper selenide nanoparticles. As-prepared Cu2−xSe@mSiO2–PEG nanoparticles not only display strong near infrared (NIR) region absorption and good photothermal effect, but also exhibit excellent biocompatibility. The mesoporous silica shell is provided as the carrier for loading the anticancer drug, doxorubicin (DOX). Moreover, the release of DOX from Cu2−xSe@mSiO2–PEG core–shell nanoparticles can be triggered by pH and NIR light, resulting in a synergistic effect for killing cancer cells. Importantly, the combination of photothermal therapy and chemotherapy driven by NIR radiation with safe power density significantly improves the therapeutic efficacy, and demonstrates better therapeutic effects for cancer treatment than individual therapy.

研究领域: 纳米医学 · 肿瘤学 · 生物材料科学
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RSC Advances · 2018 ·Vol. 8 ·期 12 ·6373-6380 · IF 2.936

High voltage, solvent-free solid polymer electrolyte based on a star-comb PDLLA–PEG copolymer for lithium ion batteries

Bingbing Wang,Hongming Lou,Hongli Xu,Junpeng Zhao,Qiujun Wang,Qiao Shi,Yonghong Deng

In this work, a novel star-comb copolymer based on poly(d,L-lactide) (PDLLA) macromonomer and poly(ethylene glycol)methyl ether methacrylate (PEGMA) was prepared, and the electrochemical properties were studied, with the aim of using it as a solid polymer electrolyte in lithium ion batteries. The six-arm vinyl functionalized PDLLA macromonomer was synthesized by a ring-opening polymerization (ROP) of D,L-lactide and subsequently an acylation of the hydroxy end-groups. A series of free-standing solid polymer electrolyte membranes from different ratios of PDLLA, PEGMA and LiTFSI were prepared through solvent-free free radical polymerization under UV radiation. The chemical structure of the obtained polymers was confirmed by 1H NMR and FTIR. The as-prepared six-arm star-comb solid polymer electrolytes (PDLLA-SPEs) exhibit good thermal stability with Td5%s of ∼270 °C and low Tgs of −48 to −34 °C. The electrochemical characterization shows that the PDLLA-SPEs possess a wide electrochemical window up to 5.1 V with an optimal ionic conductivity of 9.7 × 10−5 S cm−1 at 60 °C at an EO/Li+ ratio of 16 : 1. Furthermore, the all-solid-state LiFePO4/Li cells display extraordinary cycling and rate performances at 60 °C by curing the PDLLA-SPEs directly on the cathode. These superior properties of the six-arm star-comb PDLLA-SPE make it a promising candidate solid electrolyte for lithium batteries.

研究领域: 材料科学 · 电化学 · 能源存储
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Journal of Pharmaceutical Investigation · 2024 · IF 5.3

Transferrin modified PEG–PLGA nanoparticles: highly effective notoginsenoside R1 formulations for the treatment of ulcerative colitis

Zhou Limei,Shang Yunxia,Wang Yaru,Wei Xiaohui

Purpose Ulcerative colitis (UC) is a chronic and non-specific inflammatory bowel disease that poses a serious threat to individuals' health and lives. Notoginsenoside R1 (R1) alleviates various symptoms caused by UC effectively. However, the application of R1 is somewhat restricted due to its low bioavailability and nontargeted delivery in vivo. Consequently, it is imperative to develop novel strategies to overcome the aforementioned limitations and enhance the efficacy of this drug. To enhance R1's efficacy and targeting ability, polyethylene glycol poly (lactic-co-glycolic acid) nanoparticles loaded with R1 (R1@PEG–PLGA NPs) modified by transferrin (Tf) were prepared in this study and named R1@Tf–PEG–PLGA NPs. Methods R1@PEG–PLGA NPs and R1@Tf–PEG–PLGA NPs were prepared through nanoprecipitation, and the characterization methods were as follows: First, the surface morphology of the NPs was studied through transmission electron microscopy. Second, particle size, polydispersity index (PDI), and zeta potential were measured with a Malvern particle size analyzer, and the Tf grafting rate on the surface of the NPs was determined by using a bicinchoninic acid protein quantification kit. Third, high-performance liquid chromatography was used in determining the drug load (DL), entrapment efficiency (EE), and in vitro release of the prepared preparation. In addition, the fluorescence intensities of fluorescent-labeled NPs absorbed and ingested in Caco-2 cells were observed through in vitro experiments using fluorescence microscopy; the effects of incubation time, incubation temperature, and endocytosis inhibitors on the uptake of nanoparticles were compared; and the uptake-transport mechanism was explored. Finally, in vivo experiments were performed using the oxazolone (OXZ)-induced UC model in Sprague–Dawley (SD) rats to assess the pharmacodynamic effects and tissue distribution of the prepared NPs. Results The experimentally prepared R1@Tf–PEG–PLGA NPs were round particles with particle size and PDI of 153.50 ± 2.01 and 0.11 ± 0.01, respectively. In addition, the DL of R1@Tf-PEG-PLGA NPs was 24.26% ± 0.18%, and the EE was 50.32% ± 0.86%. Furthermore, R1@Tf–PEG–PLGA NPs had a slower cumulative release rate in vitro than R1 and R1@PEG–PLGA NPs. Fluorescence results showed that under the same conditions, Caco-2 cells took up more Tf-PEG–PLGA NPs than they took up PEG–PLGA NPs. Studies on the cellular uptake mechanism of absorption and uptake determined that the PEG–PLGA NPs entered the cells mainly through fovea-mediated endocytosis, whereas the Tf–PEG–PLGA NPs entered the cells mainly through fovea-mediated and lattice protein-mediated endocytosis. In vivo intestinal tissue distribution results in OXZ-induced SD rats showed that R1@Tf–PEG–PLGA NPs were more enriched in the colon than R1 and R1@PEG–PLGA NPs, and pharmacodynamic evaluation showed that R1@Tf–PEG–PLGA NPs exhibited more pronounced effects in ameliorating colonic injury. Conclusion R1@Tf–PEG–PLGA NPs showed significant colonic targeting and anti-UC effect, showing promising applications.

CAS / MDL: 25952-53-8
研究领域: 药学 · 纳米技术 · 炎症性肠病 · 药物递送系统
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Journal of Materials Chemistry B · 2016 ·Vol. 4 ·期 7 ·1284-1295 · IF 4.872

Harnessing the PEG-cleavable strategy to balance cytotoxicity, intracellular release and the therapeutic effect of dendrigraft poly-L-lysine for cancer gene therapy

Min Tang,Haiqing Dong,Yongyong Li,Tianbin Ren

Dendrimer catiomers like dendrigraft poly-L-lysine (DGL) have been very popular vectors for gene delivery recently; however, they generally suffer from serious cytotoxicity for high density of positive charge. PEGylated DGL engineered using the PEG cleavable mechanism (DGL(R)-SS-mPEG) was first developed as a non-viral gene vector for cancer intervention. Cleavable PEGylation of the DGL catiomer in tumor relevant glutathione (GSH) conditions enables us to dramatically decrease the cytotoxicity as well as to promote the intracellular release and expression of the genetic payload. Like DGL, DGL(R)-SS-mPEG is capable of efficiently complexing with plasmid DNA (pDNA) to afford homogeneous compact nano-complexes. Those gene carrying nanostructures could be stably dispersed in the regular serum medium without GSH, but with fast PEG dis-assembly if subject to 10 mM GSH. Compared with the non-cleavable counterpart, PEG-cleavable dendrigraft poly-L-lysine exhibited significantly higher enhanced green fluorescence protein (EGFP) expression against 293T cells. By using small interfering RNA (siRNA-VEGF) as the therapeutic gene payload, the complex nanoparticles demonstrated the pronounced inhibition effect on cell growth in vitro and tumor growth in vivo. The promising results revealed a universal strategy to balance disadvantages and advantages of dendrimer catiomers for future non-viral gene delivery vector.

研究领域: 药学 · 生物技术 · 基因治疗 · 癌症研究
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NANOTECHNOLOGY · 2022 ·Vol. 33 ·期 27 ·275604 · IF 3.953

pH-responsive and CD44-targeting polymer micelles based on CD44p-conjugated amphiphilic block copolymer PEG-b-HES-b-PLA for delivery of emodin to breast cancer cells

Kai Cheng,Jie Zhou,Yujie Zhao,Yu Chen,Lan Ming,Da Huang,Rui Yang,Zhenyu Lin,Daozhen Chen

Herein, an amphiphilic block copolymer CD44-targeting peptide-conjugated polyethylene glycol-block-hydroxyethyl starch-block-poly (L-lactic acid) (CD44p-conjugated PEG-b-HES-b-PLA) are synthesized, which could self-assemble into the pH-responsive and CD44-targeting polymer micelles against breast cancer cells MDA-MB-231. Emodin (Emo) is a natural anthraquino with pharmacological activities in anti-tumor effects. However, Emo suffers from poor water solubility, low biocompatibility, rapid systemic elimination, and off-target side effects, resulting in unsatisfactory treatment outcomes. Nanotechnology-based drug delivery systems have proven great potential for cancer chemotherapy. The constructed polymeric micelles Emo@CD44p-PM have exhibited an average size of 154.5 ± 0.9 nm characterized by DLS and TEM. Further, the Emo@CD44p-PM have effective Emo-loading capacity, good thermal stability, and pH responsiveness. Intracellular uptake study shows the enhanced cellular internalization of Emo@CD44p-PM due to the increased exposure of CD44p enhances the cellular internalization of Emo@CD44p-PM effectively. Furthermore, the in vitro results showed Emo@CD44p-PM has been observed good biocompatibility and anti-tumor effects. Therefore, the polymeric micelles Emo@CD44p-PM provide a promising delivery strategy of targeted therapy for breast cancer.

研究领域: 纳米技术 · 药学 · 癌症研究 · 高分子化学
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JOURNAL OF NANOBIOTECHNOLOGY · 2024 ·Vol. 22 ·期 1 ·1-13 · IF 10.6

NK-92 cells labeled with Fe3O4-PEG-CD56/Avastin@Ce6 nanoprobes for the targeted treatment and noninvasive therapeutic evaluation of breast cancer

Lian Jingge,Li Meng,Duan Meng,Sun Yaqian,Wang Zilin,Guo Xinyu,Li Jingchao,Gao Guo,Li Kangan

Adoptive cellular immunotherapy as a promising and alternative cancer therapy platform is critical for future clinical applications. Natural killer (NK) cells have attracted attention as an important type of innate immune regulatory cells that can rapidly kill multiple adjacent cancer cells. However, these cells are significantly less effective in treating solid tumors than in treating hematological tumors. Herein, we report the synthesis of a Fe3O4-PEG-CD56/Avastin@Ce6 nanoprobe labeled with NK-92 cells that can be used for adoptive cellular immunotherapy, photodynamic therapy and dual-modality imaging-based in vivo fate tracking. The labeled NK-92 cells specifically target the tumor cells, which increases the amount of cancer cell apoptosis in vitro. Furthermore, the in vivo results indicate that the labeled NK-92 cells can be used for tumor magnetic resonance imaging and fluorescence imaging, adoptive cellular immunotherapy, and photodynamic therapy after tail vein injection. These data show that the developed multifunctional nanostructure is a promising platform for efficient innate immunotherapy, photodynamic treatment and noninvasive therapeutic evaluation of breast cancer.

研究领域: 癌症治疗 · 免疫学 · 纳米技术 · 医学成像
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BIOSENSORS & BIOELECTRONICS · 2018 · IF 8.173

The detection of brucellosis antibody in whole serum based on the low-fouling electrochemical immunosensor fabricated with magnetic Fe3O4@Au@PEG@HA nanoparticles

Shuli Lv,Jinliang Sheng,Shiyi Zhao,Mingchao Liu,Lihua Chen

It is a novel competitive challenge for electrochemical biosensor to directly, rapidly and ultrasensitively detect the disease markers in the whole serum due to biofouling caused by the complexity of actual samples. In this paper, poly (ethylene glycol) (PEG) and hyaluronic acid (HA) were utilized to modify Fe 3 O 4 @Au nanoparticles (NPs). Based on the successfully preparation and characterization of Fe 3 O 4 @ [email protected] @HA NPs with TEM , SEM, XRD, FTIR and EDS , respectively, a novel immunosensor of brucellosis with high selectivity , sensitivity and almost perfect protein-resistant properties in various external environments, especially, in complex biological systems was fabricated. More importantly, this immunosensor is capable of assaying brucellosis antibody in 100% serum without suffering from any significant biological interference. In addition, a wide linear response range from 10 –15 g mL −1 to 10 –11 g mL −1 towards antibody in 100% serum and a low limit of detection (LOD) of 0.36 fg mL −1 (3σ, n = 13) are demonstrated, which indicates that this immunosensor has a promising potential in clinical diagnosis.

CAS / MDL: 9048-46-8 27988-77-8
研究领域: 生物传感器 · 纳米技术 · 分析化学 · 临床诊断
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MOLECULAR PHARMACEUTICS · 2018 · IF 4.556

Sialic Acid-Functionalized PEG–PLGA Microspheres Loading Mitochondrial-Targeting-Modified Curcumin for Acute Lung Injury Therapy

Feiyang Jin,Di Liu,Hui Yu,Jing Qi,Yuchan You,Xiaoling Xu,Xuqi Kang,Xiaojuan Wang,Kongjun Lu,Xiaoying Ying,Jian You,Yongzhong Du,Jiansong Ji

Acute lung injury (ALI) is a serious illness without resultful therapeutic methods commonly. Recent studies indicate the importance of oxidative stress in the occurrence and development of ALI, and mitochondria targeted antioxidant has become a difficult and hot topic in the research of ALI. Therefore, a sialic acid (SA)-modified lung-targeted microsphere (MS) for ALI therapy are developed, with triphenylphosphonium cation (TPP)-modified curcumin (Cur-TPP) loaded, which could specifically target the mitochondria, increasing the effect of antioxidant. The results manifest that with the increase of microsphere, lung distribution of microsphere is also increased in murine mice, and after SA modification, the microsphere exhibits the ideal lung-targeted characteristic in ALI model mice, due to SA efficiently targeting to E-selectin expressed on inflammatory tissues. Further investigations indicate that SA/Cur-TPP/MS has better antioxidative capacity, decreases intracellular ROS generation, and increases mitochondrial membrane potential, contributing to a lower apoptosis rate in human umbilical vein endothelial cells (HUVECs) compared to H2O2 group. In vivo efficacy of SA/Cur-TPP/MS demonstrates that the inflammation has been alleviated markedly and the oxidative stress is ameliorated efficiently. Significant histological improvements by SA/Cur-TPP/MS are further proved via HE stains. In conclusion, SA/Cur-TPP/MS might act as a promising drug formulation for ALI therapy.

研究领域: 药学 · 生物医学工程 · 药理学 · 治疗学 · 药物递送系统 · 肺疾病
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Small · 2024 · IF 13

Hydrophobic Multilayered PEG@PAN/MXene/PVDF@SiO2 Composite Film with Excellent Thermal Management and Electromagnetic Interference Shielding for Electronic Devices

Jiahui Lin,Jintao Huang,Zhanhu Guo,Ben Bin Xu,Yan Cao,Juanna Ren,Hua Hou,Yongshuang Xiao,Mustafa Elashiry,Zeinhom M. El-Bahy,Yonggang Min

With the rapid development of electronic industry, it's pressing to develop multifunctional electromagnetic interference (EMI) shielding materials to ensure the stable operation of electronic devices. Herein, multilayered flexible PEG@PAN/MXene (Ti 3 C 2 T x )/PVDF@SiO 2 (PMF) composite film has been constructed from the level of microstructure design via coaxial electrospinning, coating spraying, and uniaxial electrospinning strategies. Benefiting from the effective encapsulation for PEG and high conductivity of MXene coating, PEG@PAN/MXene composite film with MXene coating loading density of 0.70 mg cm −2 exhibits high thermal energy storage density of 120.77 J g −1 and great EMI shielding performance (EMI SE of 34.409 dB and SSE of 49.086 dB cm 3 g −1 ) in X-band (8–12 GHz). Therefore, this advanced composite film can not only help electronic devices prevent the influence of electromagnetic pollution in the X-band but also play an important role in electronic device thermal management. Additionally, the deposition of nano PVDF@SiO 2 fibers (289 ± 128 nm) endowed the PMF composite film with great hydrophobic properties (water contact angle of 126.5°) to ensure the stable working of hydrophilic MXene coating, thereby breaks the limitation of humid application environments. The finding paves a new way for the development of novel multifunctional EMI shielding composite films for electronic devices.

CAS / MDL: 25322-68-3
研究领域: 材料科学 · 电气工程 · 纳米技术 · 高分子科学 · 热工程 · 电磁兼容
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