Sci Total Environ. 2020 Apr 1;711:134493.   doi: 10.1016/j.scitotenv.2019.134493.   Epub 2019 Oct 4. RhB-encapsulating silica nanoparticles modified with PEG impact the vascular endothelial function in endothelial cells and zebrafish model Shuang Liang 1, Yueyue Chen 1, Shiming Zhang 2, Yuanyuan Cao 1, Junchao Duan 3, Yapei Wang 4, Zhiwei Sun 5 Abstract Silica nanoparticles (SiNPs) have been widely used in human health related products, such as food additives, cosmetics and even drug delivery, gene therapy or bioimaging.   Recently, a first-in-human clinical trial based on polyethylene glycol (PEG)-modified SiNPs had been approved by US FDA to trace melanoma.   However, as a nano-based drug delivery system, its biocompatibility and vascular toxicity are still largely unknown.   Thus, we synthesized the fluorescent SiNPs to explore the biocompatibility and vascular endothelial function, and compare different biological effects caused by PEG-modified and unmodified SiNPs in cells and zebrafish model.   The characterizations of SiNPs and PEG-modified SiNPs were analyzed by TEM, SEM, AFM and DLS, which exhibited relatively good stable and dispersive.   Compared with SiNPs, PEG-modified SiNPs had markedly reduced the inflammatory response and vascular damage in Tg (fli-1: EGFP) and Tg (mpo: GFP) transgenic zebrafish lines, respectively.   Consistent with the in vivo results, the PEG-modified SiNPs had been found to significantly decline the levels of ROS, inflammatory cytokines and mitochondrial-mediated apoptosis in vascular endothelial cells compared to SiNPs, and the ROS scavenger NAC could effectively alleviate the above adverse effects induced by nanoparticles.   Our results suggested that the PEG-modified SiNPs could become more safety via increasing the biocompatibility and decreasing cellular toxicities in living organisms. Keywords: Endothelial cells;   PEG modification;   RhB-encapsulating SiNPs;   Vascular function;   Zebrafish. Related products Abbreviation: mPEG-NH2 Name: Methoxypoly(ethylene glycol) amine For more product information, please contact us at: US Tel: 1-844-782-5734 US Tel: 1-844-QUAL-PEG CHN Tel: 400-918-9898 Email: sales@sinopeg.com

J Control Release. 2018 Mar 28;274:56-68. doi: 10.1016/j.jconrel.2018.01.034. Epub 2018 Feb 2. Reactive oxygen species-responsive nanoprodrug with quinone methides-mediated GSH depletion for improved chlorambucil breast cancers therapy Cheng-Qiong Luo 1, Yu-Xin Zhou 2, Tian-Jiao Zhou 3, Lei Xing 1, Peng-Fei Cui 3, Minjie Sun 3, Liang Jin 4, Na Lu 5, Hu-Lin Jiang 6 Abstract Prodrug-based stimuli-responsive vectors have emerged as highly promising platform. Inspired by the fact that antioxidant systems including glutathione (GSH) make cancer cells adapt to oxidative stress and play a role in the inactivation of alkylating agents like chlorambucil (CHL) inside tumor cells, while arylboronic acid could transform into GSH depleting agent quinone methide (QM) upon degradation by reactive oxygen species (ROS) over-expressed in tumor cells, a ROS-responsive nanoprodrug (denoted by PPAHC) of CHL was established by integrating CHL into diols-containing hydrophilic polymer with self-immolative linker 4-(hydroxymethyl)phenylboronic acid (HPBA). The prodrug could form core-shell nanoparticle and possess high stability during storage. Drug release profile of PPAHC nanoprodrug demonstrated that nature CHL could be quickly released from PPAHC nanoprodrug in the presence of hydrogen peroxide (H2O2). Moreover, PPAHC nanoprodrug showed improved therapeutic efficiency compared to CHL via anti-proliferative study and cell apoptosis assay. Further measurement of GSH content and ROS levels in tumor cells suggested that the synergistic impact resulted from QM-mediated GSH reduction and CHL-induced further oxidative stress insults to tumor cells. In vivo tumor suppression effect and biocompatibility indicated the superiorities of PPAHC nanoprodrug. Accordingly, PPAHC provides a new approach as a ROS-responsive CHL delivery system and has a great potential for cancer therapy. Keywords: Chlorambucil; Glutathione; Nanoprodrug; Quinone methide; Reactive oxygen species; Self-immolative linker. Related products Abbreviation: mPEG-NH2 Name: Methoxypoly(ethylene glycol) amine For more product information, please contact us at: US Tel: 1-844-782-5734 US Tel: 1-844-QUAL-PEG CHN Tel: 400-918-9898 Email: sales@sinopeg.com

Journal of Nanomaterials | Volume 2015 | Article ID 541763 | https://doi.org/10.1155/2015/541763 Preparation and In Vitro Evaluation of a Multifunctional Iron Silicate@Liposome Nanohybrid for pH-Sensitive Doxorubicin Delivery and Photoacoustic Imaging Zehua Liu, Shaoheng Tang, Zhiran Xu, Yingjun Wang, Xuan Zhu, Liang-cheng Li, Wanjin Hong, and Xiumin Wang Abstract For preventing premature drug release in neutral environment and avoiding them being trapped into the endosomal/lysosomal system, we developed a novel iron silicate@liposome hybrid (ILH) formulation, which can be used as a carrier to transport doxorubicin (DOX) in a pH-sensitive manner and to escape from endosomal/lysosomal trapping through “proton-sponge” effect.   The high intensity of photoacoustic signal from in vitro photoacoustic imaging (PAI) experiments suggests that it is a promising candidate for PAI agent, providing the potential for simultaneously bioimaging and cancer-targeting drug delivery.   Cytotoxicity of our formulation toward tumor cells was remarkably higher than free DOX (48.4±7.7% and 26.2±8.4%, P < 0.001).   Confocal laser scanning microscopy experiments showed the enhanced transportation and enrichment process of DOX in QSG-7703 cells.   Taking together, we developed an easy approach to construct a multifunctional anticancer drug delivery/imaging system with a potency as a PAI agent.   The strategy of combining drug carrier and imaging agent is an emerging platform for further construction of nanoparticle and may play a significant role in cancer therapy and diagnosis. Related products Abbreviation: mPEG-NH2 Name: Methoxypoly(ethylene glycol) amine For more product information, please contact us at: US Tel: 1-844-782-5734 US Tel: 1-844-QUAL-PEG CHN Tel: 400-918-9898 Email: sales@sinopeg.com

J Biomed Nanotechnol. 2019 Feb 1;15(2):373-381. doi: 10.1166/jbn.2019.2693. Polymeric Micelles with Endosome Escape and Redox-Responsive Functions for Enhanced Intracellular Drug Delivery Jing Liu, Xixi Ai, Huaping Zhang, Weiling Zhuo, Peng Mi Abstract Efficient intracellular delivery of bioactive compounds into cancer cells is critically important for treatment, as some compounds only validate for therapy after entering cancer cells. The boron neutron capture therapy (BNCT) applies thermal neutron irradiation to react with 10B-compounds that existed inside cancer cells to generate secondary killing irradiations to eradicate cancer cells. The effective distance of the emitted secondary killing irradiations is as long as a cellular diameter, which requires the cellular uptake of 10B-compounds for efficient tumor BNCT. However, current clinical approved 10B-compound of sodium borocaptate (BSH) exhibits low cellular uptake by cancer cells, which limits the therapeutic efficacy. Herein, the multifunctional polymeric micelles with endosome escape and redox-responsive functions have been developed by self-assembly from the BSH-conjugated block copolymers for enhanced delivery of BSH into cancer cells. The BSH-loaded polymeric micelles (BSH/micelle) showed a hydrodynamic diameter around 50 nm, and the size distribution was monodisperse. The BSH/micelle were stable in normal physiological environment, while the BSH could be released in responding to high level of redox-potential in cancer cells. Besides, intracellular delivery of BSH was highly promoted by BSH/micelle through the endosome escape function of micelles, which further increased the tumor therapeutic efficacy by BNCT. Related products Abbreviation: mPEG-NH2 Name: Methoxypoly(ethylene glycol) amine For more product information, please contact us at: US Tel: 1-844-782-5734 US Tel: 1-844-QUAL-PEG CHN Tel: 400-918-9898 Email: sales@sinopeg.com

Int J Nanomedicine. 2017 Aug 16;12:5863-5877.     doi: 10.2147/IJN.S141982.     eCollection 2017. pH-sensitive and folic acid-targeted MPEG-PHIS/FA-PEG-VE mixed micelles for the delivery of PTX-VE and their antitumor activity Yan Di 1, Ting Li 1, Zhihong Zhu 1, Fen Chen 2, Lianqun Jia 2, Wenbing Liu 3, Xiumei Gai 1, Yingying Wang 1, Weisan Pan 1, Xinggang Yang 1 Abstract The aim of this study was to simultaneously introduce pH sensitivity and folic acid (FA) targeting into a micelle system to achieve quick drug release and to enhance its accumulation in tumor cells.     Paclitaxel-(+)-α-tocopherol (PTX-VE)-loaded mixed micelles (PHIS/FA/PM) fabricated by poly(ethylene glycol) methyl ether-poly(histidine) (MPEG-PHIS) and folic acid-poly(ethylene glycol)-(+)-α-tocopherol (FA-PEG-VE) were characterized by dynamic light scattering and transmission electron microscopy (TEM).     The mixed micelles had a spherical morphology with an average diameter of 137.0±6.70 nm and a zeta potential of -48.7±4.25 mV.     The drug encapsulation and loading efficiencies were 91.06%±2.45% and 5.28%±0.30%, respectively.     The pH sensitivity was confirmed by changes in particle size, critical micelle concentration, and transmittance as a function of pH. MTT assay showed that PHIS/FA/PM had higher cytotoxicity at pH 6.0 than at pH 7.4, and lower cytotoxicity in the presence of free FA.     Confocal laser scanning microscope images demonstrated a time-dependent and FA-inhibited cellular uptake.     In vivo imaging confirmed that the mixed micelles targeted accumulation at tumor sites and the tumor inhibition rate was 85.97%.     The results proved that the mixed micelle system fabricated by MPEG-PHIS and FA-PEG-VE is a promising approach to improve antitumor efficacy. Keywords: drug delivery;     folic acid targeting;     in vivo antitumor activity;     mixed micelles;     pH sensitive. Related products Abbreviation: mPEG-NH2 Name: Methoxypoly(ethylene glycol) amine For more product information, please contact us at: US Tel: 1-844-782-5734 US Tel: 1-844-QUAL-PEG CHN Tel: 400-918-9898 Email: sales@sinopeg.com

Inorg Chem. 2016 Apr 18;55(8):3872-80.  doi: 10.1021/acs.inorgchem.6b00020.  Epub 2016 Apr 6. Multimodal Upconversion Nanoplatform with a Mitochondria-Targeted Property for Improved Photodynamic Therapy of Cancer Cells Xiaoman Zhang, Fujin Ai, Tianying Sun, Feng Wang, Guangyu Zhu Abstract Upconversion nanoparticles (UCNPs) with the capacity to emit high-energy visible or UV light under low-energy near-infrared excitation have been extensively explored for biomedical applications including imaging and photodynamic therapy (PDT) against cancer.  Enhanced cellular uptake and controlled subcellular localization of a UCNP-based PDT system are desired to broaden the biomedical applications of the system and to increase its PDT effect.  Herein, we build a multimodal nanoplatform with enhanced therapeutic efficiency based on 808 nm excited NaYbF4:Nd@NaGdF4:Yb/Er@NaGdF4 core-shell-shell nanoparticles that have a minimized overheating effect.  The photosensitizer pyropheophorbide a (Ppa) is loaded onto the nanoparticles capped with biocompatible polymers, and the nanoplatform is functionalized with transcriptional activator peptides as targeting moieties.  Significantly increased cellular uptake of the nanoparticles and dramatically elevated photocytotoxicity are achieved.  Remarkably, colocalization of Ppa with mitochondria, a crucial subcellular organelle as a target of PDT, is proven and quantified.  The subsequent damage to mitochondria caused by this colocalization is also confirmed to be significant.  Our work provides a comprehensively improved UCNP-based nanoplatform that maintains great biocompatibility but shows higher photocytotoxicity under irradiation and superior imaging capabilities, which increases the biomedical values of UCNPs as both nanoprobes and carriers of photosensitizers toward mitochondria for PDT. Related products Abbreviation: mPEG-NH2 Name: Methoxypoly(ethylene glycol) amine For more product information, please contact us at: US Tel: 1-844-782-5734 US Tel: 1-844-QUAL-PEG CHN Tel: 400-918-9898 Email: sales@sinopeg.com

J Control Release. 2020 Apr 10;320:314-327.  doi: 10.1016/j.jconrel.2020.01.026.  Epub 2020 Jan 16. Ligand-installed anti-VEGF genomic nanocarriers for effective gene therapy of primary and metastatic tumors Huaping Zhang, Jing Liu, Qixian Chen, Peng Mi Abstract The systemic dosage regimen exhibited low therapeutic efficacy and incurred severe adverse effect, thus, the development of tumor-targeted therapeutics is crucial important for tumor precision therapy.  Herein, the active targeted modulation of tumor microenvironments was schemed by developing hyaluronic acid-installed genomic nanocarriers (HA-NPs) for effectively ablation of both primary and metastatic tumors through anti-vascular endothelial growth factor (anti-VEGF) approach.  The anti-VEGF genomic payloads were strategically packaged into the well-defined synthetic nanocarriers by layer-by-layer preparation strategy, exhibiting high colloidal stability and much lower cell viability than the cationic gene carriers.  Besides, the HA-NPs could specifically and efficiently internalize with cancer cells for efficient intracellular gene delivery, leading to high gene transfection efficacy.  Moreover, it further demonstrated efficient extravasation, high accumulation and deep penetration in tumors, which markedly facilitated tumor-targeted expression of anti-VEGF genomic payloads for inhabitation of neo-vasculature, consecutively contributing to potent ablation of solid tumors.  In addition, the ligand-installed nanocarriers facilitated systemic treatment of melanoma lung metastasis by the expressed anti-VEGF proteins, which were extensively spread along blood circulation and metastatic niches to diminish the formation of neovasculature for tumorigenesis.  Therefore, the proposed anti-VEGF genomic nanocarriers could shed intriguing implication in effectively treatment of primary tumors and metastasis. Keywords: Anti-VEGF;  Gene delivery;  Layer-by-layer;  Metastasis;  Nanoparticles;  Tumor. Related products Abbreviation: mPEG-NH2 Name: Methoxypoly(ethylene glycol) amine For more product information, please contact us at: US Tel: 1-844-782-5734 US Tel: 1-844-QUAL-PEG CHN Tel: 400-918-9898 Email: sales@sinopeg.com

Published: 08 June 2016 Layered double hydroxide modified by PEGylated hyaluronic acid as a hybrid nanocarrier for targeted drug delivery Anjie Dong  (董岸杰), Xue Li  (李 雪), Weiwei Wang  (王伟伟), Shangcong Han  (韩尚聪), Jianfeng Liu  (刘鉴锋), Jinjian Liu  (刘金剑), Junqiang Zhao  (赵军强), Shuxin Xu  (许舒欣) & Liandong Deng  (邓联东) Transactions of Tianjin University volume 22, pages237–246 (2016) Abstract In recent years, organic-inorganic hybrid nanocarriers are explored for effective drug delivery and preferable disease treatments. In this study, using 5-fluorouracil(5-FU)as electronegative model drug, a new type of organic-inorganic hybrid drug delivery system(LDH/HA-PEG/5-FU)was conceived and manufactured by the adsorption of PEGylated hyaluronic acid(HA-PEG)on the surface of layered double hydroxide(LDH, prepared via hydrothermal method)and the intercalation of 5-FU in the interlamination of LDH via ion exchange strategy. The drug loading amount of LDH/HA-PEG/5-FU achieved as high as 34.2%. LDH, LDH/5-FU and LDH/HA-PEG/5- FU were characterized by FT-IR, XRD, TGA, laser particle size analyzer and SEM. With the benefit of pHdegradable feature of LDH and enzyme-degradable feature of HA, LDH/HA-PEG/5-FU showed pH-degradable and enzyme-degradable capacity in in vitro drug release. Moreover, the drug carrier LDH/HA-PEG contained biocompatible PEG and tumor-targeted HA, resulting in lower cytotoxicity and better endocytosis compared with LDH in vitro. It was suggested that the organic-inorganic hybrid drug delivery system, which was endowed with the properties of controlled release, low toxicity and tumor-targeting delivery for ameliorative cancer therapy, was advisable and might be applied further to fulfill other treatments. Related products Abbreviation: mPEG-NH2 Name: Methoxypoly(ethylene glycol) amine For more product information, please contact us at: US Tel: 1-844-782-5734 US Tel: 1-844-QUAL-PEG CHN Tel: 400-918-9898 Email: sales@sinopeg.com