114390-31-7Relevant articles and documents
Engineering graphene oxide with ultrasmall SPIONs and smart drug release for cancer theranostics
Luo, Yu,Tang, Yan,Liu, Tianzhi,Chen, Qian,Zhou, Xiaohan,Wang, Ning,Ma, Ming,Cheng, Yingsheng,Chen, Hangrong
, p. 1963 - 1966 (2019)
A smart nanotheranostics nanoplatform was constructed using engineered graphene oxide and the in situ growth of ultrasmall superparamagnetic iron oxide particles (SPIONs). The construction of such a novel theranostics nanoplatform shows great potential in tumor theranostics, especially for T1-weighted magnetic resonance (T1-MR) imaging guided, pH-sensitive chemotherapy.
In vitro and in vivo evaluation of stimuli-responsive vesicle from PEGylated hyperbranched PAMAM-doxorubicin conjugate for gastric cancer therapy
Nie, Jinshan,Wang, Yang,Wang, Wei
, p. 168 - 177 (2016)
Gastric Cancer is one of the major leading causes of death by cancer worldwide, but the chemotherapeutics, one of the preferred approaches, bring about extensive side effects when systemically injected. In our work, doxorubicin-loaded pH and redox responsive hyperbranched poly(amidoamine)(h-PAMAM)-based vesicle was prepared to enhance anti-tumor efficacy of chemotherapeutic compounds. The doxorubicin (DOX) molecules were attached to PEGylated h-PAMAM by acid sensitive cis-aconityl linkage to form pH sensitive conjugate (PPCD), which self-assembled in THF into micelles. The resulted micelles were then crosslinked by disulfide bonds and transferred from THF into water to form vesicles, which could be disassembled into small-sized conjugates under the redox condition. The drug release profiles showed that the PPCD vesicle presented stimuli-triggered drug release in acidic and reducing environment, and lower DOX leakage under neutral condition. The in vitro cell assay reflected the rapid DOX release and significant tumor-cytotoxic effect of the PPCD vesicle. The in vivo anticancer activity and systematic toxicity studies showed that the PPCD vesicles had lower tissue toxicity with good antitumor effect. In brief, h-PAMAM-based PPCD vesicle provides a safe and effective drug delivery system for the therapy of gastric cancer.
PEGylated PAMAM dendrimer-doxorubicin conjugates: In vitro evaluation and in vivo tumor accumulation
Zhu, Saijie,Hong, Minghuang,Zhang, Lihong,Tang, Guotao,Jiang, Yanyan,Pei, Yuanying
experimental part, p. 161 - 174 (2010/10/20)
Purpose: To investigate the effects of PEGylation degree and drug conjugation style on the in vitro and in vivo behavior of PEGylated polyamidoamine (PAMAM) dendrimers-based drug delivery system. Methods: Doxorubicin (DOX) was conjugated to differently PEGylated PAMAM dendrimers by acid-sensitive cis-aconityl linkage and acid-insensitive succinic linkage to produce the products of PPCD and PPSD conjugates, respectively. In vitro evaluations including pH-dependent DOX release, cytotoxicity, cellular uptake, cell internalization mechanism, and intracellular localization were performed. Tumor accumulation was also visualized by in vivo fluorescence imaging. Results: DOX release from PPCD conjugates followed an acid-triggered manner and increased with increasing PEGylation degree. In vitro cytotoxicity of PPCD conjugates against ovarian cancer (SKOV-3) cells increased, while cellular uptake decreased with increasing PEGylation degree. PPSD conjugates released negligible drug at any tested pH condition and were less cytotoxic. The conjugates were internalized by SKOV-3 cells via clathrin-mediated and adsorptive endocytosis, and were delivered to acidic lysosomes where DOX was released from PPCD conjugates and diffused into the nuclei. PPCD conjugates with highest PEGylation degree showed the highest tumor accumulation in mice inoculated with SKOV-3 cells. Conclusion: The obtained results suggested that PPCD conjugates with highest PEGylation degree would be a potential candidate for solid tumor treatment.
