Biomaterials. 2018 Mar;157:107-124. doi: 10.1016/j.biomaterials.2017.12.003. Epub 2017 Dec 9. Tumor acidity activating multifunctional nanoplatform for NIR-mediated multiple enhanced photodynamic and photothermal tumor therapy Junjie Liu, Huining Liang, Menghuan Li, Zhong Luo, Jixi Zhang, Xingming Guo, Kaiyong Cai Abstract The study reports a multifunctional nanoplatform based on mesoporous silica coated gold nanorod (AuNR@MSN) to overcome biological barriers associating with nanocarrier for multiple enhanced photodynamic therapy (PDT) and photothermal therapy (PPT). Indocyanine green (ICG) was loaded into AuNR@MSN and end-capped with β-cyclodextrin (β-CD). Then, a peptide RLA ([RLARLAR]2) with plasma membrane permeability and mitochondria-targeting capacity was anchored to AuNR@MSN via host-gust interaction. Subsequently, a charge-reversible polymer was introduced to endow stealth property. When the nanoplatform extravasates to tumor tissue, the weak acidity in tumor microenvironment could induce the dissociation of charge-reversible polymer and re-exposure of RLA peptide. Such a pH-mediated transition could facilitate the targeted accumulation of the nanoplatform in mitochondria. Upon singular 808 nm laser irradiation, the nanoplatform displayed enhanced PDT effect through the generation of reactive oxygen species (ROS) mediated by the local electric field of AuNR, plasmonic photothermal effect, and leakage of endogenous ROS by mitochondrion-targeted PDT. Meanwhile, local hyperthermia was generated by both ICG and AuNR for PPT. The in vitro and in vivo experiments demonstrated that the composite nanoplatform had good antitumor effect with minimal side effect. This work provides new insight into the development of new phototherapeutics for oncotherapy. Keywords: Charge-reversal; Gold nanorod; Mitochondrial targeting; Photodynamic therapy; Photothermal therapy; Reactive oxygen species. Related products Abbreviation: mPEG-CM Name: Methoxypoly(ethylene glycol) carboxymethyl 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

Powder Technology. Volume 358, 15 December 2019, Pages 3-12 https://doi.org/10.1016/j.powtec.2018.08.045 Matrix metalloproteinases sensitive multifunctional micelles for inhibition of metastatic tumor growth and metastasis Chao Qin, Xin Yang, Yubing Wu, Yaqi Lv, Li Zhang, Xiaofei Xin, Lei Yang, Wei He, Xiaopeng Han, Lifang Yin, Chunyong Wu Abstract A matrix metalloproteinases (MMPs) triggered multifunctional micellar system loading traditional chemotherapeutic agent paclitaxel (PTX) and marimastat (MATT), an inhibition of matrix metalloproteinases, was established to prevent tumor growth and metastasis. The micelles were self-assembled by the conjugate synthesized with an MMPs sensitive peptide as the bridge between PTX and poly(ethylene glycol) (PEG). 4T1 cell line derived from a murine breast tumor was selected as the cell model due to its high metastasis. The cytotoxicity assay and cell apoptosis analysis revealed that the sensitive micelles increased the toxicity and cell apoptosis compared with the insensitive micelles. In addition, this system also exhibited high penetration ability in tumor spheroids and significant invasion inhibition with the method of Transwell invasion assay. In the BALB/c mice bearing 4T1 tumors, this system inhibited the growth of the metastatic tumor and prevented the incidence of lung metastasis with low systemic toxicity. And the expression of MMP-2 and MMP-9, which are important in the process of tumor metastasis, was down-regulated. Generally, the data obtained from the in vitro and in vivo studies confirmed that the codelivery of PTX and MATT by the MMPs sensitive micelles achieved not only significant antitumor effect but also obvious inhibition effect of tumor metastasis, which are the leading cause of cancer deaths. This functional particle system may provide a promising strategy for metastatic breast cancer therapy. Related products Abbreviation: mPEG-CM Name: Methoxypoly(ethylene glycol) carboxymethyl 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

Industrial Crops and Products. Volume 152, 15 September 2020, 112497 https://doi.org/10.1016/j.indcrop.2020.112497 Avermectin loaded carboxymethyl cellulose nanoparticles with stimuli-responsive and controlled release properties Huaxin Zhu, Yue Shen, Jianxia Cui, Anqi wang, Ningjun Li, Chong Wang, Bo Cui, Changjiao Sun, Xiang Zhao, Chunxin Wang, Fei Gao, Shenshan Zhan, Liang Guo, Liang Zhang, Zhanghua Zeng, Yan Wang, Haixin Cui Abstract Polyethylene glycol (PEG) was introduced into carboxymethyl cellulose (CMC) to form hydrophilic chain of PEG-CMC. Avermectin (Avm) was grafted on the long chain of PEG-CMC by use of N, N-dicyclohexylcarbodiimide (DCC) as the dehydrant and 4-dimethylaminopyridine (DMAP) as the catalyst to form the amphiphilic molecule. Then the avermectin nanoparticles was prepared with esterase-responsive sustained release successfully through self-assembly. The size of nanoparticles was less than 400 nm. Avermectin loading was 8% and the degradation rate was less than 50 % under the xenon arc lamp for 72 h. Compared with avermectin technical, it showed an obvious anti-photodegradation advantage. Compared with commercially available water-dispersible granules (WDG), the avermectin nanoparticles had a smaller contact angle on the cucumber leaf surface and there was a significant difference. The toxicity test showed that the nanoparticles have a certain insecticidal effect on the larva of Hyphantria cunea and the sensitivity increased gradually over time. Related products Abbreviation: mPEG-CM Name: Methoxypoly(ethylene glycol) carboxymethyl 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 Mater Chem B. 2016 May 21;4(19):3324-3330. doi: 10.1039/c6tb00278a. Epub 2016 Apr 26. Oligoethylenimine grafted PEGylated poly(aspartic acid) as a macromolecular contrast agent: properties and in vivo studies Bin Jiang, Min Liu, Kunchi Zhang, Guangyue Zu, Jingjin Dong, Yi Cao, Lan Zhang, Renjun Pei Abstract PEGylated poly(aspartate-g-OEI) was developed as a magnetic resonance imaging probe. The PEG-PBLA block copolymer was prepared by the ring-opening polymerization of β-benzyl-l-aspartate N-carboxy-anhydride (BLA-NCA) initiated by the terminal primary amino group of mPEG-NH2, followed by grafting with oligoethylenimine (OEI, Mw = 800) and Gd-DTPA. Compared to Gd-DTPA (4.42 mM-1 s-1), PEG-p(Asp-OEI-DTPA-Gd) exhibited much higher T1 relaxivity (19.03 mM-1 s-1), up to 4.3 times higher than Gd-DTPA. No obvious cytotoxicity was observed from the WST assay and H&E analysis, which illustrated that this macromolecular contrast agent (mCA) exhibited excellent biocompatibility. Folic acid (FA) was further labeled onto the mCA to endow the mCA with targeting ability. During in vivo animal studies, the FA labeled MRI probes showed a significant signal intensity enhancement in the tumor during different time intervals and provided a long and efficient window time for MR examination. These results suggest that such mCAs are excellent candidates as magnetic resonance imaging (MRI) probes with high efficiency and safety. Related products Abbreviation: MeO-PEG-NH2 Name: alpha-Methoxy-omega-amino 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

Int J Nanomedicine. 2018 Mar 9;13:1381-1398. doi: 10.2147/IJN.S152312. eCollection 2018. Design of pH-sensitive methotrexate prodrug-targeted curcumin nanoparticles for efficient dual-drug delivery and combination cancer therapy Jiajiang Xie, Zhongxiong Fan, Yang Li, Yinying Zhang, Fei Yu, Guanghao Su, Liya Xie, Zhenqing Hou Abstract Aim: We designed acid-labile methotrexate (MTX) targeting prodrug self-assembling nanoparticles loaded with curcumin (CUR) drug for simultaneous delivery of multi-chemotherapeutic drugs and combination cancer therapy. Methods: A dual-acting MTX, acting as both an anticancer drug and as a tumor-targeting ligand, was coupled to 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[aldehyde(polyethylene glycol)-2000] via Schiff's base reaction. The synthesized prodrug conjugate (DSPE-PEG-Imine-MTX) could be self-assembled into micellar nanoparticles (MTX-Imine-M) in aqueous solution, which encapsulated CUR into their core by hydrophobic interactions (MTX-Imine-M-CUR). Results: The prepared MTX-Imine-M-CUR nanoparticles were composed of an inner hydrophobic DSPE/CUR core and an outside hydrophilic bishydroxyl poly (ethyleneglycol) (PEG) shell with a self-targeting MTX prodrug corona. The imine linker between 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[aldehyde(polyethyleneglycol)-2000] and MTX, as a dynamic covalent bond, was strong enough to remain intact in physiological pH, even though it is rapidly cleaved in acidic pH. The MTX-Imine-M-CUR could codeliver MTX and CUR selectively and efficiently into the cancer cells via folate receptor-mediated endocytosis followed by the rapid intracellular release of CUR and the active form of MTX via the acidity of endosomes/lysosomes. Moreover, the MTX-Imine-M-CUR resulted in significantly higher in vitro and in vivo anticancer activity than pH-insensitive DSPE-PEGAmide-MTX assembling nanoparticles loaded with CUR (MTX-Amide-M-CUR), MTX unconjugated DSPE-PEG assembling micellar nanoparticles loaded with CUR (M-CUR), combination of both free drugs, and individual free drugs. Conclusion: The smart system provided a simple, yet feasible, drug delivery strategy for targeted combination chemotherapy. Keywords: combination therapy; nanoparticles; pH-sensitive prodrug; self-assembly; targeting. Related products Abbreviation: HO-PEG-OH Name: α,ω-Dihydroxyl 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

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