3261-86-7Relevant articles and documents
Redox-Sensitive Citronellol-Cabazitaxel Conjugate: Maintained in Vitro Cytotoxicity and Self-Assembled as Multifunctional Nanomedicine
Xue, Peng,Liu, Dan,Wang, Jing,Zhang, Na,Zhou, Jiahua,Li, Lin,Guo, Weiling,Sun, Mengchi,Han, Xiangfei,Wang, Yongjun
, p. 1360 - 1372 (2016)
Citronellol-cabazitaxel (CIT-ss-CTX) conjugate self-assembled nanoparticles (CSNPs) were designed and prepared by conjugating cabazitaxel with citronellol via the disulfide bond that is redox-sensitive to the high concentration of glutathione within tumor cells. Notably, the CSNPs maintained in the cell cytotoxicity. Moreover, the AUC0-t of CSNPs was 6.5-fold higher than that of cabazitaxel solutions and the t1/2 was prolonged 2.3 times. Furthermore, we found that CSNPs could be employed as an efficient carrier for other hydrophobic drugs or imaging agents. Thus, the in vivo targeting study was implemented via using 1,1-dioctadecyl-3,3,3,3-tetramethylindotricarbocyanine iodide (DiR)-loaded CSNPs as imaging agent, which showed CSNPs could effectively accumulate at the tumor site. Curcumin, a hydrophobic anticancer drug, was successfully loaded in CSNPs which exhibits good stability and synergistic antitumor effects. The citronellol-cabazitaxel conjugate therefore has a promising perspective as a multifunctional nanomedicine for combination therapy and theranostics attributed to its long-circulation property, redox-sensitive mechanism, and high drug coloading capability.
Amphiphilic Endomorphin-1 derivative functions as self-assembling nanomedicine for effective brain delivery
Liu, Hui,Zhao, Xiaoning,Liang, Shan,Fan, Linlan,Li, Zhaojun,Zhang, Yun,Ni, Jingman
, p. 977 - 984 (2019)
Endomorphin-1 (Tyr-Pro-Trp-Phe-NH2, EM-1), an endogenous μ-opioid receptor ligand with strong antinociceptive activity, is not in clinical use because of its limited metabolic stability and membrane permeability. In this study, we develop a short-peptide self-delivery system for brain targets with the capability to deliver EM-1 without vehicle. Two amphiphilic EM-1 derivatives, C18-SS-EM1 and C18-CONH-EM1, were synthesized by attaching a stearyl moiety to EM-1 via a disulfide and amide bond, respectively. The amphiphilicity of EM-1 derivatives enabled self-assembling into nanoparticles for brain delivery. The study assessed morphology, circular dichroism, and metabolic stability of the formulations, as well as their pharmacodynamics and in vivo distribution, directly monitored by near-IR fluorescence imaging in mouse brains. In aqueous solution, the C18-SS-EM1 derivative self-assembled into spherical nanostructures with a diameter of 10–20nm. Near-IR fluorescence analysis visualized the accumulation of the peptides in the brain. Importantly, the analgesic effect of C18-SS-EM1 nanoparticles was significantly stronger as compared to that of unmodified EM-1 or C18-CONH-EM1 nanoparticles. An in vitro release study demonstrated that self-assembled C18-SS-EM1 nanoparticles possessed reduction-responsive behavior. In summary, self-assembling C18SS-EM1 nanoparticles, which integrate the advantages of lipidization, nanoscale characteristics and, labile disulfide bonds, represent a promising strategy for brain delivery of short peptides.
Triglyceride-mimetic structure-gated prodrug nanoparticles for smart cancer therapy
Tian, Chutong,Guo, Jingjing,Miao, Yifan,Zheng, Shunzhe,Sun, Bingjun,Sun, Mengchi,Ye, Qing,Liu, Wenxue,Zhou, Shuang,Kamei, Ken-Ichiro,He, Zhonggui,Sun, Jin
, p. 15936 - 15948 (2021/11/18)
Off-target drug release and insufficient drug delivery are the main obstacles for effective anticancer chemotherapy. Prodrug-based self-assembled nanoparticles bioactivated under tumor-specific conditions are one of the effective strategies to achieve on-demand drug release and effective tumor accumulation. Herein, stimuli-activable prodrugs are designed yielding smart tumor delivery by combination of the triglyceride-mimic (TG-mimetic) prodrug structure and disulfide bond. Surprisingly, these prodrugs can self-assemble into uniform nanoparticles (NPs) with a high drug loading (over 40%) and accumulate in tumor sites specifically. The super hydrophobic TG structure can act as a gate that senses lipase to selectively control over NP dissociation and affect the glutathione-triggered prodrug activation. In addition, the impacts of the double bonds in the prodrug NPs on parent drug release and the following cytotoxicity, pharmacokinetics, and antitumor efficiency are further demonstrated. Our findings highlight the promising potential of TG-mimetic structure-gated prodrug nanoparticles for tumor-specific drug delivery.
Bridging molecules for bonding metal material and hydrogel and preparation method and application of bridging molecule
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Paragraph 0026; 0079-0080; 0082-0083; 0085-0086; 0088-0089, (2019/06/05)
The invention belongs to the field of functional organic molecule synthesis, and discloses bridging molecules for bonding a metal material and hydrogel and a preparation method and application of thebridging molecules. Functional groups capable of reacting with the surface of metal and the hydrogel are introduced in the bridging molecules, the bridging molecules are treated as molecule interfacelinks, chemical anchor points are connected into the surface of the metal by surface modifying methods of in-situ spraying, dip-coating and the like, through in-situ polymerization reaction, two end group functional groups of the bridging molecules are subjected to bonding with the hydrogel and the surface of the metal correspondingly, and high-intensity bonding between the hydrogel and the surface of the metal is achieved. When bridging molecules containing responsive radical groups are used, the bridging molecules can be rapidly disconnected through external stimulate response on the basis of high-intensity bonding, and the effect of on-demand separation is achieved. According to the bridging molecules for bonding the metal material and the hydrogel and the preparation method and application of the bridging molecules, synthesis is simple, the repeatability is good, amplified preparation can be achieved, the whole surface processing and bonding process is convenient, rapid and efficient, and the bridging molecules are expected to be applied to the relative field of biomedicine and have high clinic application value.
