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PEG-b-PCL
IONICS · 2017 ·Vol. 24 ·期 3 ·787-795 · IF 2.062

A well-defined biodegradable 1,2,3-triazolium-functionalized PEG-b-PCL block copolymer: facile synthesis and its compatibilization for PLA/PCL blends

Wang Ping,Zhang Di,Zhou Yiyang,Li Yu,Fang Huagao,Wei Haibing,Ding Yunsheng

A novel biodegradable 1,2,3-triazolium-functionalized PEG- b -PCL copolymer (TAPEC) was synthesized by the “click” coupling of methoxypolyethylene glycol azide and α-propargyl-ω-hydroxyl-poly(ε-caprolactone), followed by the quaternization of the 1,2,3-triazole moiety with iodomethane. All the intermediates and TAPEC were characterized by 1 H NMR, FT-IR, and gel permeation chromatography (GPC). Taking advantage of the characteristics of ionic liquid and block copolymer, this ion-containing diblock copolymer is expected to be used as a novel compatibilizer in mixed biopolyester for regulating the interface and crystallization behaviors. Hence, the TAPEC was evaluated as a compatibilizer and an interface emulsifier in the blends of polylactic acid (PLA) and poly(ε-caprolactone) (PCL). Non-isothermal crystallization experimental results showed that the TAPEC with the higher amount of ε-caprolactone units induces a plasticization and nucleate effect that increased the crystallization ability of the PLA phase; meanwhile, in the PCL phase, the agminated ionic cluster acting as a nucleating agent significantly increased the crystalline of PCL.

研究领域: 材料科学 · 高分子化学
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CHEMICAL ENGINEERING JOURNAL · 2021 · IF 13.273

Polymeric micelles amplify tumor oxidative stresses through combining PDT and glutathione depletion for synergistic cancer chemotherapy

Ting Su,Furong Cheng,Yuji Pu,Jun Cao,Shuibin Lin,Guizhi Zhu,Bin He

Cancer has been one of the major healthcare burdens, which demands innovative therapeutic strategies to improve the treatment outcomes. Combination therapy hold great potential to leverage multiple synergistic pathways to improve cancer treatment. Cancer cells often exhibit an increased generation of reactive oxygen species (ROS) and antioxidant species compared with normal cells, and the levels of these species can be further elevated by common therapeutic modalities such as photodynamic therapy (PDT) or chemotherapy. Taking advantage that cancer cells are vulnerable to further oxidative stress, we aim to design a drug delivery system by simultaneously increasing the cellular ROS level, reducing antioxidative capacity, and inducing anticancer chemotherapy in cancer cells. Here, we designed a star-shape polymer, PEG(- b -PCL-Ce6)- b -PBEMA, based on the Passerini three-component reaction, which can both enhance ROS generation during PDT and decrease the GSH level in cancer cells. The polycaprolactone conjugated with photosensitizer Ce6 served as hydrophobic segments to promote micelle formation, and Ce6 was used for PDT. The H 2 O 2 -labile group of arylboronic esters pendent on the third segment was designed for H 2 O 2 -induced quinone methide (QM) release for GSH depletion. We thoroughly investigated the spectral properties of blank micelle during its assembling process, ROS generation, and H 2 O 2 -induced QM release in vitro . Moreover, this polymeric micelle could successfully load hydrophobic anti-cancer drug Doxorubicin (DOX) and efficiently deliver DOX into cancer cells. The triple combination of ROS generation, GSH elimination, and chemotherapy dramatically improved antitumor efficiency relative to each of them alone in vitro and in vivo .

CAS / MDL: 2052-01-9
研究领域: 癌症治疗 · 纳米医学 · 药物递送系统 · 生物医学工程
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INTERNATIONAL JOURNAL OF PHARMACEUTICS · 2020 · IF 4.845

Dopamine-modified poly(ε-caprolactone) micelles for pH controlled delivery of bortezomib

Lei Liu,Shuaichao Wang,Peilan Qi,Shiyong Song,Yanwei Yang,Jiahua Shi,Guang Han

Poly(ethylene glycol)-poly(ε-caprolactone) (PEG-b-PCL) micelles have been widely used as drug delivery vehicles for cancer therapies. Because of the lack of functional groups, the use of PEG-b-PCL in drug delivery system is greatly limited and structural modifications is needed. In this work, chemical modification at the terminus of PEG-b-PCL was performed via the “grafting from” polymerization method. A poly(dopamine methyl acrylamide) segment was introduced containing multiple catechol groups, which could attach bortezomib (BTZ) to the chain of the polymer through the formation of a pH-sensitive borate bond. This method greatly enhanced the loading capacity of BTZ into the micelles. Additionally, the controlled release of BTZ in response to the acidic environment of a tumor was realized. High loading capacity, stimuli-responsiveness, biodegradability, and compatibility were integrated in the PEG-b-PCL-based system. In vitro and in vivo studies demonstrated that superior tumor inhibition without obvious side effects can be achieved by the BTZ-loaded PEG-b-PCL-b-PDMA micelles.

CAS / MDL: 502-44-3
研究领域: 药学 · 材料科学 · 纳米技术 · 肿瘤学 · 生物医学工程
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Biomaterials Science · 2019 ·Vol. 8 ·期 5 ·1290-1297 · IF 5.251

Angiopep-2 conjugated nanoparticles loaded with doxorubicin for the treatment of primary central nervous system lymphoma

Xiao-Xiao Shi,Wei-Min Miao,Di-Wen Pang,Jia-Si Wu,Qi-Song Tong,Jia-Xian Li,Jia-Qi Luo,Wen-Yu Li,Jin-Zhi Du,Jun Wang

Primary central nervous system lymphoma (PCNSL) is a rare brain tumor. Its therapeutic efficacy is much lower than that of traditional lymphoma, largely due to the presence of the blood–brain barrier (BBB), which hinders the effective drug delivery and deposition on the disease site. Angiopep-2 (ANG) can target low-density lipoprotein receptor-related protein (LRP) on the surface of brain capillary endothelial cells (BCECs) and exhibits high BBB transport capability. In this study, we designed an ANG conjugated poly(ethylene glycol)-b-poly(ε-caprolactone) (PEG-b-PCL) (APP) nanoparticle to deliver doxorubicin (DOX) for the treatment of PCNSL. Our data indicated that the targeted APP nanoparticles showed significantly increased cellular uptake by BCECs compared with the control nanoparticles. In the intracranial SU-DHL-2-LUC lymphoma xenograft mice model, APP enhanced drug deposition in tumor tissues, and DOX-loaded APP (APP@DOX) exhibited a better therapeutic effect than free DOX and nontargeted PP@DOX, which significantly prolonged the survival time of mice.

CAS / MDL: 25316-40-9
研究领域: 肿瘤学 · 神经科学 · 药学 · 纳米技术
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