Persson. Nguyen, T.V., M. Yao, and C.J. YG and YY designed and directed all the experiments and article writing. 2014;2:1362–70.Xu Z, Zhu S, Wang M, Li Y, Shi P, Huang X. You can also search for this author in To achieve an optimal therapeutic response, at intervals of 2 to 3 days the dosage may be increased 5 mg … You can also search for this author in Select one or more newsletters to continue. As shown in Fig. Vogelzang NJ. Based on these results, it is recommended to avoid enzalutamide co-administration with strong CYP2C8 inhibitors. J Nanobiotechnology. Ahn, S.O. 2010;10:3318–23.Li H, Flerens K, Zhang Z, Vanparijs N, Schuijs MJ, Van Steendam K, et al. The ultraviolet (UV) spectra and Fourier transform infrared (FT-IR) spectra were carried out to verify each step of preparation of the TP-GQDss. (2002). 2015;14:239–47.Chen J, Wu Z, Ding W, Xiao C, Zhang Y, Gao S, et al. Goodman. Watson, V. Arora, J. Wongvipat, P.M. Smith-Jones, D. Yoo, A. Kwon, et al. Blumenstein, M.A. Similarly, the bioavailability of enzalutamide in rats is 89.7%. 2009. TP-GQDss/DIR was prepared using the same method as TP-GQDss/Enz. Increased survival with enzalutamide in prostate cancer after chemotherapy. 3. Hepatic clearance of drugs. Small EJ, Halabi S, Dawson NA et al. Enz was loaded into TP-GQDss for in vitro and in vivo study.The results showed that high drug-loading efficiency was achieved by TP-GQDss via π–π electron interaction. Abdulla A, Kapoor A. Solid tumours were induced in nude mice by subcutaneously injecting C4-2B cells (5 × 10All values are presented as the mean ± SD. 2016;904:58–64.Yu X, Cheng H, Zhang M, Zhao Y, Qu L, Shi G. Graphene-based smart materials. Cells were seeded into 96-well plates at a density of 8 × 10For cell apoptosis analysis, cells were seeded into 12-well plates at a density of 1.5 × 10A near-infrared fluorescence substance DIR was entrapped in TP-GQDss for the in vivo biodistribution assay. 2019;17:83.Xia Q, Gong C, Gu F, Wang Z, Hu C, Zhang L, et al. 2014;6:11882–90.Pan Y, Sahoo NG, Li L. The application of graphene oxide in drug delivery. Mutation of the androgen-receptor gene in metastatic androgen-independent prostate cancer. The enzalutamide mean terminal elimination half-fife (T1/2), in patients with metastatic CRPC, following a single oral dose is 5.8 days (range 2.8 to 10.2 days). Medically reviewed by Drugs.com. Scher HI, Beer TM, Higano CS et al. The advancing uses of nano-graphene in drug delivery. Graphene-based nanosheets for delivery of chemotherapeutics and biological drugs. Therefore, this TP-GQDss nano-platform has the potential to provide Enz-based intravenous injection therapy for CRPC.Enz, aminated GQDs, MAL-PEG-SCM (PEG molecular size: 2000), Targeting peptide (TP, sequence: CKQFSALPFNFYT) was synthesized using the Fmoc-solid-phase peptide synthesis method by Ontores Biotech, Zhejiang, China. 2015;7:1355–63.Yang K, Zhang S, Zhang G, Sun X, Lee ST, Liu Z. Graphene in mice: ultrahigh in vivo tumor uptake and efficient photothermal therapy. LSD1 demethylates repressive histone marks to promote androgen-receptor-dependent transcription. TP-GQDss could be rapidly internalized by CRPC cells via endocytosis. Enzalutamide--a major advance in the treatment of metastatic prostate cancer. ACS Appl Mater Inter. FDA U. Ha, M. Baek, and H. Moon. Chem Soc Rev. 5. Application number 203415Orig1s000: Clinical pharmacology and biopharmaceutics review(s). The drug is rapidly absorbed after oral administration, with a mean bioavailability of 3.9%. Taplin ME, Bubley GJ, Shuster TD et al. Improvement in therapeutic efficacy and reduction in cellular toxicity: introduction of a novel anti-PSMA-conjugated hybrid antiandrogen nanoparticle. You can also search for this author in Afterward, the GQDss solution was dialyzed against DD water (3500 MWCO) to remove free GQDs and DTSSP.To increase biocompatibility and hydrophilicity, we introduced the MAL-PEG-SCM moiety to GQDss with carboxyl groups via the catalyst The zeta potential of GQDs, GQDss, PEG-GQDss and TP-GQDss (1 mg/mL) was measured by a dynamic light scattering system (DLS) (Zetasizer Nano ZS90, Malvern) at RT. 2018;14:1613–26.Feeney OM, Crum MF, McEvoy CL, Trevaskis NL, Williams HD, Pouton CW, et al. Fast PLiang RP, Qiu WB, Zhao HF, Xiang CY, Qiu JD. Graphene oxide (GO) has shown great potential as a drug delivery system due to its sheet-like structure and π–π stacking interaction, and the drug-loading efficiency of GO is extremely high compared to other nanocarriers [In this study, Enz could be effectively loaded into TP-GQDss due to the cross-linking of GQDs, with a DL of 60% and an EE of 96%, which was much higher than in the reported study [In conclusion, we designed a redox-sensitive nano-platform (TP-GQDss) based on graphene dots with high drug-loading efficiency for intravenous delivery of Enz against CRPC. Pang, K.S., and M. Rowland. To investigate the in vivo biodistribution of TP-GQDss/Enz, a red fluorescence dye 1,1′-dioctadecyl-3,3,3′,3′-tetramethylindotricarbocyanine iodide (DIR) was used as a model drug of Enz. 2015;38:2076–82.Krauwinkel W, Noukens J, Van Dijk J, Popa S, Ouatas T, De Vries M, et al.