Adv Healthc Mater. 2020 Jul;9(13):e2000268. doi: 10.1002/adhm.202000268. Epub 2020 May 19. Lithium Loaded Octa-Poly(Ethylene Glycol) Based Adhesive Facilitates Axon Regeneration and Reconnection of Transected Peripheral Nerves Yazhong Bu, Xianghai Wang, Lixia Li, Xiaofang Hu, Dandan Tan, Zhenlin Li, Muhua Lai, Xiaozhong Qiu, Feifei Sun, Hufei Wang, Fei Yang, Decheng Wu, Jiasong Guo Abstract At present, reconnecting the transected nerve in clinic is still mainly reliant on surgery suture. This is a procedure that requires thorough training and is also time consuming. Here, an octa-poly(ethylene glycol) (PEG)-based adhesive for fast reconnecting of the transected peripheral nerve is reported. To enhance the therapeutic efficacy, a succinyl unit is applied to endow the controllably dissolvable property of the adhesive, and lithium is loaded in the adhesive to improve the axonal regeneration. Present data reveal that this adhesive possesses good cytocompatibility and can significantly shorten the reconnecting time of the transected nerve ends compared to that required for suture surgery. Histology, electrophysiological, and behavior assessments indicate that the adhesive reconnected nerves exhibit a low grade of fibrosis, inflammation response, and myoatrophy as well as robust axonal regeneration and functional recovery. Together, these results indicate that this octa-PEG adhesive can act as an alternative to traditional nerve suture in peripheral nerve injury. Keywords: adhesives; peripheral nerve repair; poly(ethylene glycol); succinyl unit. Related products Abbreviation: HO-PEG(8)-OH Name: Octa-ethylene glycol Abbreviation: H2N-PEG(8)-NH2 Name: alpha,omega-Bis-amino octa(ethylene glycol) 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

Polysaccharide-based polymers such as pSar and cationic surfactants such as DOTMA (1,2-dioleoyl-3-trimethylammonium-propane) are increasingly being utilized in the development of drug delivery systems. pSar is a biocompatible and biodegradable polymer that can be used to encapsulate drugs and other molecules, protecting them from degradation and increasing their solubility. DOTMA is a cationic surfactant that can be used to modify the surface properties of nanoparticles, making them more stable and increasing their solubility. Both polymers can be used to improve the delivery of drugs and other molecules to target sites in the body. pSar and DOTMA can be used in combination to create more effective drug delivery systems, as they can be used to increase the solubility of drugs and improve their absorption. Additionally, they can be used to modify the properties of proteins, lipids, and other molecules, making them more stable and increasing their solubility. In conclusion, pSar and DOTMA are two essential polymers that are being used in the development of drug delivery systems, and their combination can be used to create more effective drug delivery systems. 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 Aug 10;283:113-125. doi: 10.1016/j.jconrel.2018.05.032. Epub 2018 May 29. Vitamin A-decorated biocompatible micelles for chemogene therapy of liver fibrosis Jian-Bin Qiao, Qian-Qian Fan, Lei Xing, Peng-Fei Cui, Yu-Jing He, Jing-Cheng Zhu, Lirui Wang, Tao Pang, Yu-Kyoung Oh, Chaofeng Zhang, Hu-Lin Jiang Abstract Liver fibrosis refers to excessive accumulation of hepatic collagen, which is primarily produced by activated hepatic stellate cells (HSCs). No effective drugs are clinically available to treat this condition, reflecting the fact that antifibrotic drugs do not specifically target activated HSCs. Here, we report the synthesis and evaluation of poly (lactide-co-glycolide)-polyspermine-poly (ethylene glycol)-vitamin A (PLGA-PSPE-PEG-VA), and activated HSC-targeted, biocompatible amphiphilic polymers for co-delivery of chemical (silibinin) and genetic (siCol1α1) drugs that synergistically suppress collagen I accumulation in fibrogenesis. PLGA-PSPE-PEG-VA self-assembled into core-shell polymeric micelles (PVMs) at low concentrations. After loading with silibinin and siCol1α1, the resulting chemical/genetic drug-loaded PVMs (CGPVMs) exhibited a small particle size and a slightly positive surface. CGPVMs had very low cytotoxicity and hemolytic activity in vitro and were well tolerated in mice, with no liver toxicity or inflammation. Importantly, CGPVMs effectively accumulated in fibrotic livers and specifically targeted activated HSCs. As expected CGPVMs more efficiently decreased collagen I production and ameliorated liver fibrosis compared with chemical drug (silibinin)-loaded PVMs (CPVMs) or genetic drug (siCol1α1)-loaded PVMs (GPVMs) only. These results indicate that CGPVMs are a promising tool for targeted delivery of chemogenes to activated HSCs in the treatment of liver fibrosis. Keywords: Chemogene therapy; Liver fibrosis; Micelle; Silibinin; Vitamin A; siRNA. Related products Abbreviation: HOOC-PEG-COOH Name: α,ω-Dicarboxyl poly(ethylene glycol) 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 May 10;321:629-640. doi: 10.1016/j.jconrel.2020.02.049. Epub 2020 Mar 2. Hyperbranched lipoid-based lipid nanoparticles for bidirectional regulation of collagen accumulation in liver fibrosis Jian-Bin Qiao, Qian-Qian Fan, Cheng-Lu Zhang, Jaiwoo Lee, Junho Byun, Lei Xing, Xiang-Dong Gao, Yu-Kyoung Oh, Hu-Lin Jiang Abstract Liver fibrosis leads to over one million deaths annually worldwide. Hepatic stellate cells (HSCs) have been identified as the main executors of liver fibrosis. Unfortunately, no drug has yet been approved for clinical use against liver fibrosis, largely because the tested drugs have been unable to access HSCs and efficiently remove the collagen accumulation involved in fibrogenesis. Here, we designed an efficient HSC-targeting lipid delivery system that carried dual siRNAs intended to both inhibit collagen synthesis and promote collagen degradation, with the goal of realizing enhanced anti-liver fibrosis by bidirectional regulation of collagen accumulation. The delivery system was constructed by using amphiphilic cationic hyperbranched lipoids (C15-PA) for siRNA complexation and helper lipoids (cholesterol-polyethylene glycol-vitamin A, Chol-PEG-VA) for HSCs targeting. The generated vitamin A-decorated and hyperbranched lipoid-based lipid nanoparticles (VLNPs) showed excellent gene-binding ability and transfection efficiency, and enhanced the delivery of siRNAs to HSCs. Fibrotic mice treated with dual siRNA-loaded VLNPs showed a great reduction in the collagen accumulation seen in this model; the enhanced effect of bidirectional regulation reduced the collagen accumulation level in treated mice to almost that seen in normal mice. There was no notable sign of toxicity or tissue inflammation in mice exposed to repeated intravenous administration of the dual siRNA-loaded VLNPs. In conclusion, our results indicate that biocompatible VLNPs designed to exploit precise targeting and an effective bidirectional regulation strategy hold promise for treating liver fibrosis. Keywords: Bidirectional regulation; Collagen accumulation; Hepatic stellate cells; Lipoid-based lipid nanoparticles; Liver fibrosis; siRNA. Related products Abbreviation: HOOC-PEG-COOH Name: α,ω-Dicarboxyl poly(ethylene glycol) 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

ACS Nano. 2020 Feb 25;14(2):2063-2076. doi: 10.1021/acsnano.9b08667. Epub 2020 Feb 7. Ultrasound-Switchable Nanozyme Augments Sonodynamic Therapy against Multidrug-Resistant Bacterial Infection Duo Sun, Xin Pang, Yi Cheng, Jiang Ming, Sijin Xiang, Chang Zhang, Peng Lv, Chengchao Chu, Xiaolan Chen, Gang Liu, Nanfeng Zheng Abstract Ultrasound (US)-driven sonodynamic therapy (SDT) has demonstrated wide application prospects in the eradication of deep-seated bacterial infections due to its noninvasiveness, site-confined irradiation, and high-tissue-penetrating capability. However, the ineffective accumulation of sonosensitizers at the infection site, the hypoxic microenvironment, as well as rapid depletion of oxygen during SDT greatly hamper the therapeutic efficacy of SDT. Herein, an US-switchable nanozyme system was proposed for the controllable generation of catalytic oxygen and sonosensitizer-mediated reactive oxygen species during ultrasound activation, thereby alleviating the hypoxia-associated barrier and augmenting SDT efficacy. This nanoplatform (Pd@Pt-T790) was easily prepared by bridging enzyme-catalytic Pd@Pt nanoplates with the organic sonosensitizer meso-tetra(4-carboxyphenyl)porphine (T790). It was really interesting to find that the modification of T790 onto Pd@Pt could significantly block the catalase-like activity of Pd@Pt, whereas upon US irradiation, the nanozyme activity was effectively recovered to catalyze the decomposition of endogenous H2O2 into O2. Such "blocking and activating" enzyme activity was particularly important for decreasing the potential toxicity and side effects of nanozymes on normal tissues and has potential to realize active, controllable, and disease-loci-specific nanozyme catalytic behavior. Taking advantage of this US-switchable enzyme activity, outstanding accumulation in infection sites, as well as excellent biocompatibility, the Pd@Pt-T790-based SDT nanosystem was successfully applied to eradicate methicillin-resistant Staphylococcus aureus (MRSA)-induced myositis, and the sonodynamic therapeutic progression was noninvasively monitored by photoacoustic imaging and magnetic resonance imaging. The developed US-switchable nanoenzyme system provides a promising strategy for augmenting sonodynamic eradication of deep-seated bacterial infection actively, controllably, and precisely. Keywords: bacterial infection; multidrug-resistant; nanozyme; sonodynamic therapy; ultrasound-switchable. Related products Abbreviation: H2N-PEG-SH Name: α-Amino-ω-mercapto poly(ethylene glycol) 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

Nanoscale. 2016 Mar 14;8(10):5706-13. doi: 10.1039/c5nr09120a. Platinum(IV) prodrug conjugated Pd@Au nanoplates for chemotherapy and photothermal therapy Saige Shi, Xiaolan Chen, Jingping Wei, Yizhuan Huang, Jian Weng, Nanfeng Zheng Abstract Owing to the excellent near infrared (NIR) light absorption and efficient passive targeting toward tumor tissue, two-dimensional (2D) core-shell PEGylated Pd@Au nanoplates have great potential in both photothermal therapy and drug delivery systems. In this work, we successfully conjugate Pd@Au nanoplates with a platinum(IV) prodrug c,c,t-[Pt(NH3)2Cl2(O2CCH2CH2CO2H)2] to obtain a nanocomposite (Pd@Au-PEG-Pt) for combined photothermal-chemotherapy. The prepared Pd@Au-PEG-Pt nanocomposite showed excellent stability in physiological solutions and efficient Pt(IV) prodrug loading. Once injected into biological tissue, the Pt(IV) prodrug was easily reduced by physiological reductants (e.g. ascorbic acid or glutathione) into its cytotoxic and hydrophilic Pt(II) form and released from the original nanocomposite, and the NIR laser irradiation could accelerate the release of Pt(II) species. More importantly, Pd@Au-PEG-Pt has high tumor accumulation (29%ID per g), which makes excellent therapeutic efficiency at relatively low power density possible. The in vivo results suggested that, compared with single therapy the combined thermo-chemotherapy treatment with Pd@Au-PEG-Pt resulted in complete destruction of the tumor tissue without recurrence, while chemotherapy using Pd@Au-PEG-Pt without irradiation or photothermal treatment using Pd@Au-PEG alone did not. Our work highlights the prospects of a feasible drug delivery strategy of the Pt prodrug by using 2D Pd@Au nanoplates as drug delivery carriers for multimode cancer treatment. Related products Abbreviation: H2N-PEG-SH Name: α-Amino-ω-mercapto poly(ethylene glycol) 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 Drug Target. 2015;23(6):568-76. doi: 10.3109/1061186X.2015.1018910. Epub 2015 Mar 4. Effective photothermal chemotherapy with docetaxel-loaded gold nanospheres in advanced prostate cancer Yanfang Shen, Zhiya Ma, Fei Chen, Qingjian Dong, Qiran Hu, Lingyu Bai, Jing Chen Abstract Background: Multifunctional gold nanospheres (MGNs)-loaded with docetaxel (MGN@DTX) were prepared and evaluated for therapeutic efficacy in nude mice bearing human prostate cancer xenografts. Methods: MGNs were prepared from PEGylated hollow gold nanospheres (HGNs) coated with folic acid and DTPTT chelate. Then, the effect of radiolabelled MGNs ((99m)Tc-MGNs) on PC-3 cell apoptosis was assessed by flow cytometry, while their binding affinity to these cells was evaluated by cell binding assays. Next, biodistribution of (99m)Tc-MGNs in xenograft bearing mice was measured by SPECT imaging. Also, DTX loading and release rates were estimated in MGN@DTX. Finally, in vitro stability in human serum and cytotoxicity of MGN@DTX were assessed, as well as their antitumor effect in xenograft bearing mice. Results: (99m)Tc-MGNs (97.69% purity) showed good binding affinity to PC-3 cells, a specific recognition blocked by excess folic acid. Interestingly, MGN@DTX remained stable in human serum for 24 h, and exhibited higher mean cytotoxicity after NIR laser irradiation than free DTX. By day 28, tumor inhibition rates were higher in the MGN@DTX + NIR laser irradiation group compared with the DTX and MGNs + NIR laser irradiation groups. Conclusions: Loading chemotherapeutic drugs into MGNs can increase antitumor potency, reduce normal cell damage and decrease drug resistance, thus representing a promising approach for advanced prostate cancer treatment. Keywords: Docetaxel; gold nanospheres; near-infrared laser; prostate cancer. Related products Abbreviation: H2N-PEG-SH Name: α-Amino-ω-mercapto poly(ethylene glycol) 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

First published: 26 February 2018. https://doi.org/10.1002/adfm.201706310 A Novel Theranostic Nanoplatform Based on Pd@Pt-PEG-Ce6 for Enhanced Photodynamic Therapy by Modulating Tumor Hypoxia Microenvironment Jingping Wei, Jingchao Li, Duo Sun, Qi Li, Jinyuan Ma, Xiaolan Chen, Xuan Zhu, Nanfeng Zheng Abstract Photodynamic therapy (PDT), which utilizes reactive oxygen species to kill cancer cells, has found wide applications in cancer treatment. However, the hypoxic nature of most solid tumors can severely restrict the efficiency of PDT. Meanwhile, the hydrophobicity and limited tumor selectivity of some photosensitizers also reduce their PDT efficacy. Herein, a photosensitizer-Pd@Pt nanosystem (Pd@Pt-PEG-Ce6) is designed for highly efficient PDT by overcoming these limitations. In the nanofabrication, Pd@Pt nanoplates, exhibiting catalase-like activity to decompose H2O2 to generate oxygen, are first modified with bifunctional PEG (SH-PEG-NH2). Then the Pd@Pt-PEG is further covalently conjugated with the photosensitizer chlorin e6 (Ce6) to get Pd@Pt-PEG-Ce6 nanocomposite. The Pd@Pt-PEG-Ce6 exhibits good biocompatibility, long blood circulation half-life, efficient tumor accumulation, and outstanding imaging properties. Both in vitro and in vivo experimental results clearly indicate that Pd@Pt-PEG-Ce6 effectively delivers photosensitizers to cancer cells/tumor sites and triggers the decomposition of endogenous H2O2 to produce oxygen, resulting in a remarkably enhanced PDT efficacy. Moreover, the moderate photothermal effect of Pd@Pt nanoplates also strengthen the PDT of Pd@Pt-PEG-Ce6. Therefore, by integrating the merits of high tumor-specific accumulation, hypoxia modulation function, and mild photothermal effect into a single nanoagent, Pd@Pt-PEG-Ce6 readily acts as an ideal nanotherapeutic platform for enhanced cancer PDT. Related products Abbreviation: H2N-PEG-SH Name: α-Amino-ω-mercapto poly(ethylene glycol) 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