Tofacitinib is a novel, oral Janus kinase inhibitor. The objectives of this study were to summarize the pharmacokinetics and metabolism tofacitinib in humans, including clearance mechanisms. Following administration single 50-mg ¹⁴C-labeled dose healthy male subjects, mean (standard deviation) total percentage administered radioactive recovered was 93.9% (±3.6), with 80.1% (±3.6) urine (28.8% parent), 13.8% (±1.9) feces (0.9% parent). rapidly absorbed, plasma concentrations...

A superhydrophobic ZnAl–layered double hydroxide (LDH)–La film was prepared by a hydrothermal method and further modification laurate anions in this work. Comprehensive characterizations of were performed terms morphology, composition, structure, roughness, wettability scanning electronic microscopy, energy-dispersive X-ray spectroscopy, diffraction, three-dimensional laser confocal microscopy. The long-term corrosion protection effect investigated deeply monitoring the changes...

Purpose: Mastoparan-M (Mast-M) has cytotoxic effects on various tumor cells in vitro, including liver cancer and colorectal cancer. However, the anti-tumor mechanism of Mast-M remains unclear its potential for therapy not been investigated. Herein, we aimed to develop a novel phytosome formulation loaded with evaluate efficacy against breast both vitro vivo. Furthermore, investigated underlying mechanisms Mast-M. Methods: The synthesis Phy-Mast-M involved co-solvent technique, followed by...

A novel formulation system of phytosomes loaded with mitomycin C-soybean phosphatidylcholine (MMC-SPC) complex (MMC-loaded phytosomes) was prepared by a solvent evaporation method combined nanoprecipitation technique for the purpose development an MMC drug delivery system. The MMC-loaded were evaluated average particle size, zeta-potential, and residual drug-loading content as well in vitro release profile. Furthermore, stability tests vitro/vivo biological evaluations performed. DSC, FTIR,...

Tumor microenvironment responsive multimodal synergistic theranostic strategies can significantly improve the therapeutic efficacy while avoiding severe side effects. Inspired by fact that special morphology could enhance photothermal conversion efficiency (PCE) and cellular delivery, we developed an acidic tumor shape-reversal metal–organic virus-inspired nanodrug for enhancing near-infrared (NIR)-II PCE, increasing cell adhesion, activating targeting. First, a NIR-I fluorescence probe...

Multifunctional nanocomposites hold great potential to integrate therapeutic and diagnostic functions into a single nanoscale structure. In this paper, we prepared the MTX-PEG-CS-IONPs-Cy5.5 by functionalizing surface of chitosan-decorated iron oxide nanoparticles (CS-IONPs) with polyethylene glycolated methotraxate (MTX-PEG) near-infrared fluorescent cyanin dye (Cy5.5). A clinically useful PEGylated anticancer prodrug, MTX-PEG, was also developed as tumor cell-specific targeting ligand for...

“All-in-one” carrier-free-based nano-multi-drug self-delivery system could combine triple advantages of small molecules, nanoscale characteristics, and synergistic combination therapy together. Researches have showed that dual-acting small-molecular methotrexate (MTX) target kill the folate-receptor-overexpressing cancer cells. Inspired by this mechanism, a novel collaborative early-phase tumor-selective targeting late-phase anticancer approach was developed for self-assembly...

Ion-interference therapy, which utilizes ions to disturb intracellular biological processes, provides inspiration for tumor therapy. Artificially reversing osmotic pressure by transporting large amounts of physiological cells is a straightforward yet low-toxic strategy ion-interference However, it hard achieve due the serious limitations single-ion delivery. Herein, we skillfully deliver NaCl nanocrystals sites and sequentially realize explosive release Na+/Cl– inside utilizing...

Codelivery of multiple drugs with one kind drug carriers provided a promising strategy to suppress the resistance and achieve synergistic therapeutic effect in cancer treatment. In this paper, we successfully developed both methotrexate (MTX) mitomycin C (MMC) loaded PEGylated chitosan nanoparticles (CS-NPs) as delivery systems, which MTX, folic acid analogue, was also employed tumor-targeting ligand. The new systems can coordinate early phase targeting late-phase anticancer effect....

Most present drug-phospholipid delivery systems were based on a water-insoluble complex but rarely water-soluble complex. Mitomycin C (MMC) is anticancer drug extensively used in first-line chemotherapy limited by its poor aqueous stability vitro, rapid elimination from the body, and lack of target specificity. In this article, we report MMC-soybean phosphatidylcholine complex-loaded PEG-lipid-PLA hybrid nanoparticles (NPs) with Folate (FA) functionalization (FA-PEG-PE-PLA NPs@MMC-SPC) for...

Integrating advantages of mitomycin C (MMC)–phospholipid complex for increased drug encapsulation efficiency and reduced premature release, DSPE-PEG-folate (DSPE-PEG-FA) specific tumor targeting, we reported a simple one-pot self-assembly route to prepare the MMC–phospholipid complex-loaded DSPE-PEG-based nanoparticles (MP-PEG-FA NPs). Both confocal imaging flow cytometry demonstrated that MMC was distributed into nuclei after cellular uptake intracellular delivery. More importantly,...

Abstract Free radical‐based anticancer modality has been widely applied to cancer therapies. However, it still faces challenges of low delivery efficiency and poor selectivity free radical generation specifically toward tumors. Herein, a virus‐mimicking hollow mesoporous disulfide‐bridged organosilica is designed encapsulate •C precursor 2, 2'‐azobis[2‐(2‐imidazolin‐2‐yl) propane] dihydrochloride (AIPH), which then enclosed by tannic acid (TA)/Fe III photothermal assembly further cloaked...

Abstract Traditional tumour‐dynamic therapy still inevitably faces the critical challenge of limited reactive oxygen species (ROS)‐generating efficiency due to tumour hypoxia, extreme pH condition for Fenton reaction, and unsustainable mono‐catalytic reaction. To fight against these issues, we skilfully develop a tumour‐microenvironment‐driven yolk‐shell nanoreactor realize high‐efficiency persistent dynamic via cascade‐responsive dual cycling amplification •SO 4 − /•OH radicals. The with an...

Traditional chemotherapy has faced tough challenges of systemic toxicity, hypoxia resistance, and inadequacy monotherapy. Developing the tumor-specific O

We constructed 10-hydroxycamptothecin (CPT) "nanodrugs" with functionalization of lipid-PEG-methotrexate (MTX) to prepare high-drug-loaded, and sustained/controlled-release MTX-PEG-CPT nanorods (NRs), in which MTX drug itself can serve as a specific "targeting ligand". The self-targeted nanodrug codeliver both CPT drugs distinct anticancer mechanisms. Furthermore, NRs significantly reduced burst release, improved blood circulation tumor accumulation, enhanced cellular uptake, synergistically...

The design of nanoscale drug delivery systems for the targeted codelivery multiple therapeutic drugs still remains a formidable challenge (ACS Nano, 2013, 7, 9558–9570; ACS 9518–9525). In this article, both mitomycin C (MMC) and methotrexate (MTX) loaded DSPE-PEG micelles (MTX–M–MMC) were prepared by self-assembly using dialysis technique, in which MMC–soybean phosphatidylcholine complex (drug–phospholipid complex) was encapsulated within MTX-functionalized micelles. MTX–M–MMC could...

A mitomycin C (MMC)-soybean phosphatidyhlcholine complex loaded in phytosomes was previously reported for the purpose of developing a MMC drug delivery system (Mol. Pharmaceutics 2013, 10, 90-101), but this approach limited by rapid elimination from body and lack target specificity. In article, to overcome these limitations, MMC-soybean complex-loaded (MMC-loaded phytosomes) as carriers were surface-functionalized with folate-PEG (FA-PEG) achieve reduced toxicity superior MMC-mediated...

Nanoparticles (NPs) functionalized with targeting ligands have shown promise, but are still limited by their nonspecific uptake certain healthy tissues and cells that express low or even comparable levels of receptors. To increase accumulation at tumor sites while decreasing the unintended toxicity, a possible solution is involvement two separate tumor-specific in localization. In this study, dual tumor-targeting drug-loaded NP system was self-assembled amphiphilic conjugate...

The relation between college students' entrepreneurial intention and education has long been concerned. Entrepreneurial alertness is the psychological basis for entrepreneur to identify opportunities. are two key focuses in entrepreneurship research. It of great significance explore investigate role arousal process by education.However, there very few researches reported on among education, intention. was measured theBenefits from EntrepreneurialEducation Programes(BEEP). By collecting data...

Abstract Carrier-free nanodrug with exceptionally high drug payload has attracted increasing attentions. Herein, we construct a pH/ROS cascade-responsive which could achieve tumor acidity-triggered targeting activation followed by circularly amplified ROS-triggered release via positive-feedback loop. The di-selenide-bridged prodrug synthesized from vitamin E succinate and methotrexate (MTX) self-assembles into nanoparticles (VSeM); decorating acidity-cleavable PEG onto VSeM surface...

High oxidative stress plays a significant role in activating intracellular signaling pathways that govern immunogenic cell death (ICD). Nevertheless, immune response is often confined by limited reactive oxygen species (ROS) production, upregulated antioxidant defense, and an immunosuppressive tumor microenvironment. Herein, the GSH/pH-sensitive Mn2+/polydopamine-incorporated hollow mesoporous tetrasulfide-bridged organosilica nanoreactors loaded with l-arginine (l-Arg) were successfully...