Chinese Chemical Letters. Volume 28, Issue 6, June 2017, Pages 1290-1299 https://doi.org/10.1016/j.cclet.2017.01.007 Polyethylene glycol phospholipids encapsulated silicon 2,3-naphthalocyanine dihydroxide nanoparticles (SiNcOH-DSPE-PEG(NH2) NPs) for single NIR laser induced cancer combination therapy Jing-Ping Wei, Xiao-Lan Chen, Xiao-Yong Wang, Jing-Chao Li, Sai-Ge Shi, Gang Liu, Nan-Feng Zheng Abstract Currently, the combination of photothermal therapy (PTT) and photodynamic therapy (PDT) has emerged as a powerful technique for cancer treatment. However, most examples of combined PTT and PDT reported use multi-component nanocomposites under excitation of separate wavelength, resulting in complex treatment process. In this work, a novel theranostic nanoplatform (SiNcOH-DSPE-PEG(NH2) NPs) has been successfully developed by coating silicon 2,3-naphthalocyanine dihydroxide (SiNcOH) with DSPE-PEG and DSPE-PEG-NH2 for photoacoustic (PA) imaging-guided PTT and PDT tumor ablation for the first time. The as-prepared single-agent SiNcOH-DSPE-PEG(NH2) NPs not only have good water solubility and biocompatibility, but also exhibit high photothermal conversion efficiency and singlet oxygen generation capability upon 808 nm NIR laser irradiation. In addition, owing to their high absorption at NIR region, the SiNcOH-DSPE-PEG(NH2) NPs can also be employed as an effective diagnostic nanoagent for photoacoustic (PA) imaging. In vitro and in vivo experimental results clearly indicated that the simultaneously combined PTT and PDT under the guidance of PA imaging with single NIR laser excitation can effectively kill cancer cells or eradicate tumor tissues. Taking facile synthesis and high efficiency in cancer treatment by SiNcOH-DSPE-PEG(NH2) NPs into consideration, our study provides a promising strategy to realize molecular imaging-guided combination therapy. Related products Abbreviation: mPEG-DSPE Name: 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxypoly(ethylene glycol)] Abbreviation: DSPE-PEG-NH2 Name: α-Amino-ω-distearoyl-sn-glycero-3-phosphoethanolamino 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

Drug Deliv. 2017 Nov;24(1):707-719. doi: 10.1080/10717544.2017.1303855. Design of a novel curcumin-soybean phosphatidylcholine complex-based targeted drug delivery systems Jiajiang Xie, Yanxiu Li, Liang Song, Zhou Pan, Shefang Ye, Zhenqing Hou Abstract Recently, the global trend in the field of nanomedicine has been toward the design of combination of nature active constituents and phospholipid (PC) to form a therapeutic drug-phospholipid complex. As a particular amphiphilic molecular complex, it can be a unique bridge of traditional dosage-form and novel drug delivery system. In thisarticle, on the basis of drug-phospholipid complex technique and self-assembly technique, we chose a pharmacologically safe and low toxic drug curcumin (CUR) to increase drug-loading ability, achieve controlled/sustained drug release and improve anticancer activity. A novel CUR-soybean phosphatidylcholine (SPC) complex and CUR-SPC complex self-assembled nanoparticles (CUR-SPC NPs) were prepared by a co-solvent method and a nanoprecipitation method. DSPE-PEG-FA was further functionalized on the surface of PEG-CUR-SPC NPs (designed as FA-PEG-CUR-SPC NPs) to specifically increase cellular uptake and targetability. The FA-PEG-CUR-SPC NPs showed a spherical shape, a mean diameter of about 180 nm, an excellent physiological stability and pH-triggered drug release. The drug entrapment efficiency and drug-loading content was up to 92.5 and 16.3%, respectively. In vitro cellular uptake and cytotoxicity studies demonstrated that FA-PEG-CUR-SPC NPs and CUR-SPC NPs presented significantly stronger cellular uptake efficacy and anticancer activity against HeLa cells and Caco-2 cells compared to free CUR, CUR-SPC NPs and PEG-CUR-SPC NPs. More importantly, FA-PEG-CUR-SPC NPs showed the prolonged systemic circulation lifetime and enhanced tumor accumulation compared with free CUR and PEG-CUR-SPC NPs. These results suggest that the FA targeted PEGylated CUR-SPC complex self-assembled NPs might be a promising candidate in cancer therapy. Keywords: Curcumin; anticancer drug-phospholipid complex; nanoparticles; self-assembly; targeting. Related products Abbreviation: mPEG-DSPE Name: 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxypoly(ethylene glycol)] Abbreviation: DSPE-PEG-FA Name: α-Folic acid-ω-distearoyl-sn-glycero-3-phosphoethanolamino 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. 2016 Apr 28;228:107-119. doi: 10.1016/j.jconrel.2016.02.044. Epub 2016 Mar 3. Sigma receptor-mediated targeted delivery of anti-angiogenic multifunctional nanodrugs for combination tumor therapy Yuanke Li, Yuanyuan Wu, Leaf Huang, Lei Miao, Jianping Zhou, Andrew Benson Satterlee, Jing Yao Abstract The potential of low molecular weight heparin (LMWH) in anti-angiogenic therapy has been tempered by poor in vivo delivery to the tumor cell and potentially harmful side effects, such as the risk of bleeding due to heparin's anticoagulant activity. In order to overcome these limitations and further improve the therapeutic effect of LMWH, we designed a novel combination nanosystem of LMWH and ursolic acid (UA), which is also an angiogenesis inhibitor for tumor therapy. In this system, an amphiphilic LMWH-UA (LHU) conjugate was synthesized and self-assembled into core/shell nanodrugs with combined anti-angiogenic activity and significantly reduced anticoagulant activity. Furthermore, DSPE-PEG-AA-modified LHU nanodrugs (A-LHU) were developed to facilitate the delivery of nanodrugs to the tumor. The anti-angiogenic activity of A-LHU was investigated both in vitro and in vivo. It was found that A-LHU significantly inhibited the tubular formation of human umbilical vein endothelial cells (HUVECs) (p<0.01) and the angiogenesis induced by basic fibroblast growth factor (bFGF) in a Matrigel plug assay (p<0.001). More importantly, A-LHU displayed significant inhibition on the tumor growth in B16F10-bearing mice in vivo. The level of CD31 and p-VEGFR-2 expression has demonstrated that the excellent efficacy of antitumor was associated with a decrease in angiogenesis. In conclusion, A-LHU nanodrugs are a promising multifunctional antitumor drug delivery system. Keywords: Anti-angiogenesis; Combination therapy; Low molecular weight heparin; Nanodrugs; Sigma receptor; Ursolic acid. Related products Abbreviation: mPEG-DSPE Name: 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxypoly(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

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