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COLLOIDS AND SURFACES B-BIOINTERFACES · 2018 · IF 3.997

A pH-sensitive prodrug strategy to co-deliver DOX and TOS in TPGS nanomicelles for tumor therapy

Shujuan Xiong,Zhe Wang,Juan Liu,Xiangping Deng,Runde Xiong,Xuan Cao,Zhizhong Xie,Xiaoyong Lei,Yanming Chen,Guotao Tang

This work has presented a novel strategy for designing pH-sensitive TOS-H-DOX prodrug-loaded TPGS nanomicelles for co-delivery TOS and DOX to enhance tumor therapy and reduce the toxic side effects. DOX was covalently conjugated to the vitamin E succinate through hydrazone bond to produce an pH-sensitive prodrug TOS-H-DOX (amido bond as a control, TOS-A-DOX), which was responsive to the acidic environment in tumor cells, and the prodrugs were subsequently encapsulated in the core of TPGS nanomicelles via hydrophobic effects with a significant drug loading capacity. The pH-sensitive prodrug nanomicelles TOS-H-DOX/TPGS exhibited potent release of DOX in acidic media relative to the pH-insensitive prodrug nanomicelles TOS-A-DOX/TPGS, and further studies of their intracellular uptake and intracellular localization demonstrated that TOS-H-DOX/TPGS nanomicelles can be effectively taken up by cells and drugs can be released. In vitro results confirmed that TOS-H-DOX/TPGS nanomicelles exhibited significant antitumor cell proliferation activity compared to TOS-A-DOX/TPGS and free DOX, TPGS. Furthermore, in vivo studies further confirmed an excellent synergistic antitumor efficacy in MCF-7 tumor-bearing nude mice model. More importantly, the H&E staining of the heart, liver, kidney tissue sections of experimental nude mice showed that TOS-H-DOX/TPGS nanomicelles can reduce damage to them.

研究领域: 药学 · 纳米技术 · 癌症治疗 · 药物递送系统
✓ 已验证 产品关联 DOI PubMed 高影响因子
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BIOMEDICAL CHROMATOGRAPHY · 2022 ·Vol. 37 ·期 2 ·e5535 · IF 1.911

The antitumor activity and pharmacokinetics research of PPD-Arg (Tos) using ultra-performance liquid chromatography-quadrupole-time-of-flight mass spectrometry

Jiayin Liu,Yang An,Jun Su,Qinghai Dong,Hongliu Xie,Jihua Liu

In this study, a new compound PPD-Arg (Tos) (PAT), an arginine derivative of 20(s)-PPD, was synthesized via Fmoc-Arg (Tos)-OH and 20(s)-PPD. The pharmacokinetic properties in rats, in vitro cytotoxicity, and cell apoptosis rates of protopanaxadiol (PPD) and PAT were determined. A sensitive bioanalytical method for pharmacokinetics using ultra-performance liquid chromatography coupled with time-of-flight mass spectrometry was developed and validated. The result showed that the T max and t 1/2 of PAT were significantly enhanced, indicating a long-lasting effect in vivo . Compared to the PPD group, the PAT group showed higher bioavailability. PAT also exhibited higher antitumor efficacy than PPD against three cancer cells, especially the strongest inhibitory activity against Huh-7, even more potent than the positive control of paclitaxel. Therefore, the apoptosis assay based on annexin V/propidium iodide–combined staining against Huh-7 further demonstrated that PAT could induce apoptosis of Huh-7 cells. Better pharmacokinetic properties and antitumor efficacy of the arginine derivative of 20(s)-PPD were important. These findings could provide references for further clinical research on amino acid derivatives of PPD as antitumor agents.

CAS / MDL: 33069-62-4
研究领域: 药理学 · 肿瘤学 · 分析化学
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INTERNATIONAL JOURNAL OF PHARMACEUTICS · 2025 · IF 5.2

Light-responsive α-TOS liposomal nanocarriers Co-delivering TiO2 and doxorubicin for the treatment of breast cancer

Kaixin Feng,Zhongkun Zhang,Jingjing Zhang,Xiaohan Xia,Siyu Yao,Yufei Wang,Min Wu

Doxorubicin (DOX) is limited by its clinical toxicity as a breast cancer therapy. Traditional liposomal formulations improve the tumor delivery of DOX but suffer from inadequate controlled release and low encapsulation efficiency of DOX. To address these, we developed a photo-responsive liposomal formulation DTTPL by co-encapsulating DOX and TiO 2 nanostructures (TiO 2 ) within D-α-tocopheryl succinate (α-TOS)-PEG liposomes. DTTPL successfully facilitated the release of DOX through the light-sensitive catalysis mechanism of TiO 2 , exhibiting 4.6 times greater cytotoxicity against MCF-7 cells compared to free DOX. Transcriptional analysis revealed synergistic DOX/DTTPL dysregulation of key genes (Brca1, Bcl-2, Bax, Caspase-3), aligning with cytotoxicity.   Eventually, light-triggered DOX/DTTPL formulation resulted in 70.09% of tumor growth inhibition (TGI) in mice with no significant organ toxicity. This photo-responsive nanoformulation enables efficient controlled release of DOX, offering an alternative strategy for small molecule delivery to treat triple negative breast cancer.

CAS / MDL: 13463-67-7 144-55-8
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ANALYTICAL BIOCHEMISTRY · 2017 · IF 2.334

Development of a paper-based microfluidic analytical device by a more facile hydrophobic substrate generation strategy

Yuan-Yuan Xue,Wen-Tao Zhang,Meng-Yue Zhang,Li-Zhi Liu,Wen-Xin Zhu,Ling-Zhi Yan,Jing Wang,Yan-Ru Wang,Jian-Long Wang,Dao-Hong Zhang

Microfluidic paper-based analytical devices (μPADs) have a significant potential in developing portable and disposable point-of-care testing (POCT). Herein, a facile, rapid, cost-effective and environment friendly strategy for μPADs fabrication is proposed. Specifically, the substrate paper was hydrophobized by coating with trimethoxysilane (TOS), and then the selected area was hydrophilized by treating with surfactant. The whole fabrication process was implemented within 7 min, with no need for complex pre-treatment, high-temperature and special equipment. As a proof-of-concept application, the as-prepared μPAD was applied to determination of the glucose content in human serum samples. The results agreed well with those obtained by a glucometer. We believe that the μPADs fabrication method proposed here could provide a facile, rapid and low-cost reference for other related studies.

研究领域: 分析化学 · 生物医学工程 · 即时诊断
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Nano Energy · 2021 · IF 17.881

Elastic aerogel thermoelectric generator with vertical temperature-difference architecture and compression-induced power enhancement

Xiaodong Wang,Lirong Liang,Haicai Lv,Yichuan Zhang,Guangming Chen

Despite the rapid development for thermoelectrics (TEs) and aerogels , elastic aerogel TE generators (TEGs) with vertical-type architectures have not been found to harvest heat utilizing vertical temperature difference. Herein, an elastic poly(3,4-ethylenedioxytiophene)-tosylate(PEDOT-Tos)/single-walled carbon nanotube (SWCNT) TE aerogel was fabricated via convenient chemical oxidative polymerization, physical mixing and subsequent freeze-drying process. Then, we report the first elastic TEGs consisting of vertical-type aerogel legs, which not only inherit the advantages of ultralight weight and compressibility of aerogels, but also display high TE performance. The output performance can be conveniently adjusted by the number of legs, the temperature difference and compressive strain . An optimum output power of 1967 nW (output power density of 30.73 mW m −2 ) is achieved for the TE generator using 10 unipolar aerogel legs at 50% strain and temperature difference of 50 K. Furthermore, the ultralight and compressible TEG displays excellent capability of harvesting heat under vertical temperature difference and mechanical deformation , such as on hot oil/plate or compression by human body. The results will greatly facilitate the development of TE aerogels and TEGs, and widen the versatile application scenarios.

CAS / MDL: 126213-50-1 2530-83-8
研究领域: 材料科学 · 热电学 · 纳米技术 · 能量收集
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