Synergistic effect of polymer functionalized graphene oxide system for breast cancer treatment.

The multifaceted drug carrier system is an emerging trend in delivering chemotherapeutic drugs and photosensitizers for the synergistic effect. In this work, we have designed a functionalized graphene oxide (GO) based carrier system for combined chemo-photodynamic therapeutic effects. Doxorubicin (DOX) and rose bengal (RB) were entrapped on the surface of GO via hydrophobic and π-π stacking interactions. The functional group determination, crystalline properties, surface morphology, and hydrodynamic size were evaluated using FT-IR, XRD, SEM, TEM, AFM, and DLS analysis. At 24 h, the entrapment efficiency was 65 % DOX and 40.92 % RB, and the loading capacities were 16.9 % DOX and 5.68 % RB observed at 30 min. The drug release percentage was higher in pH-2.6 rather than in pH-5.5, 6.8, and 7.4 pH environments. The in-vitro toxicity analysis using the LDH assay reveals that the DOX and RB co-loaded carriers had a significant cytotoxic effect on MCF-7 cells, indicating that the carrier could improve the therapeutic efficacy of DOX. Morphological changes were studied using inverted light microscopy; the cells were irradiated with a laser 525 nm 10 J/cm2 for 2 min 51 sec, and it was observed that the DOX and RB co-loaded carrier with laser-irradiated cells exposed the high-level morphological changes with the occurrence of apoptotic cell death. Compared to free DOX, the DOX/RB co-loaded carrier + laser had an efficient anticancer activity, as confirmed by DAPI staining cell uptake, flow cytometry, and intracellular ROS generation analysis. The DOX and RB co-loaded carrier clearly exhibits the RB-mediated photodynamic action on MCF-7 cells in response to external laser light irradiation. It permits an on-demand dual-payload release to trigger an instantaneous photodynamic and chemo treatment for cancer cell eradication. Finally, the ensuing dual-agent release is probable to successfully fight cancer via a synergistic effect.

Enhanced Doxorubicin Delivery in Folate-Overexpressed Breast Cancer Cells Using Mesoporous Carbon Nanospheres.

Nanoparticle-based drug delivery reveals the safety and effectiveness and avoids premature drug release from the nanocarrier. These nanoparticles improve the bioavailability and stability of the drug against chemical and enzymatic degradation and facilitate targeted drug delivery. Herein, targeted folic acid-conjugated oxidized mesoporous carbon nanospheres (Ox-MPCNPs) were successfully fabricated and developed as antitumoral doxorubicin delivery for targeted breast cancer therapy. Fourier transform infrared spectroscopy studies confirmed that the doxorubicin was successfully bound on the Ox-MPCNP through hydrogen bonding and π-π interactions. X-ray diffraction studies showed that the synthesized doxorubicin-loaded Ox-MPCNP is semi-crystalline. The surface morphology of the synthesized doxorubicin-loaded Ox-MPCNP (DOX/Ox-MPCNP-Cys-PAsp-FA) was studied by scanning electron microscopy and high-resolution transmission electron microscopy, which demonstrates a sphere-shaped morphology. The cytotoxic effects of DOX/Ox-MPCNP-Cys-PAsp-FA were studied in MCF-7 breast cancer cells using the CytoTox96 assay kit. The study confirmed the cytotoxic effects of the synthesized nanospheres in vitro. Moreover, DOX/Ox-MPCNP-Cys-PAsp-FA-treated cells displayed efficient cell apoptosis and cell death in flow cytometry analysis. The mitochondrial fragmentation and nucleus damages were further confirmed by fluorescence microscopy. Thus, the approach used to construct the DOX/Ox-MPCNP-Cys-PAsp-FA carrier provides excellent opportunities for the targeted treatment of breast cancer.

Combined photodynamic-chemotherapy investigation of cancer cells using carbon quantum dot-based drug carrier system.

The combined chemotherapy and photodynamic therapy have significant advantages for cancer treatments, which have higher therapeutic effects compared with other medicines. Herein, we focused on the synthesis of carbon quantum dot (CQD) based nanocarrier system. CQD and 5-aminolevulinic acid (5-ALA) were conjugated with mono-(5-BOC-protected-glutamine-6-deoxy) ß-cyclodextrin (CQD-Glu-ß-CD) moiety, and finally, the anticancer chemotherapy doxorubicin (DOX) drug was loaded in the 5-ALA-CQD-Glu-ß-CD system. The stepwise physicochemical changes for the preparation of the DOX loaded 5-ALA-CQD-Glu-ß-CD system were investigated by Fourier transform infrared (FT-IR) spectroscopy, X-ray diffraction (XRD), transmission electron microscopy (TEM), atomic force microscopy (AFM), and Raman fluorescence spectroscopy. The encapsulation efficiency of DOX in 5-ALA-CQD-Glu-ß-CD was observed at ∼83.0%, and the loading capacity of DOX is ∼20.37%. The in vitro releasing of DOX and 5-ALA was observed through the UV-vis spectroscopy by the λmax value of 487 nm and 253 nm, respectively. By the investigation against the breast MCF-7 cancer cells, the high cytotoxicity and morphological changes of cancer cells were observed by the treating of DOX/5-ALA-CQD-Glu-ß-CD. The generation of reactive oxygen species (ROS) upon 635 nm (25 mW cm-2) for 15 min laser irradiation-induced improved the therapeutic effects. In vitro cellular uptake studies recommend the synthesized DOX/5-ALA-CQD-Glu-ß-CD nanocarrier could significantly enhance the cell apoptosis and assist in the MCF-7 cell damages. The result suggests a multifunctional therapeutic system for chemo/photodynamic synergistic effects on cancer therapy.

Development of biotin molecule targeted cancer cell drug delivery of doxorubicin loaded κ-carrageenan grafted graphene oxide nanocarrier.

Cervical cancer is one of the most occurring cancers and the fourth leading occurrence of cancer in women, worldwide. In this study, we planned to synthesis κ-Carrageenan grafted graphene oxide nanocarrier conjugated with biotin (GO-κ-Car-biotin) for targeted cervical cancer. Doxorubicin (DOX) is a well-known anticancer drug for any type of cancer and it is used to entrap over on the graphene oxide surface via π-π stacking interaction. The chemical function and crystalline nature of the synthesized nanocarrier was characterized by Fourier Transformed Infrared Spectroscopy (FT-IR) and X-ray diffraction Analysis (XRD). The surface morphological study was carried out through Scanning Electron Microscopy (SEM), Transmission electron microscopy (TEM) and Atomic force microscopy (AFM). The in-vitro drug release profile of DOX was carried out by UV-Vis spectrometer at the λmax value of 480 nm. The entrapment of DOX on GO-κ-car-biotin has been observed at 94%. The hydrophilic DOX drug has excellent pH-sensitive drug released in an in-vitro study. The anticancer efficiency of the synthesized GO-based nanocarrier was examined using HeLa cell line in-vitro. Cell viability, proliferation, cytotoxicity, and nuclear chromatin condensation was studied by trypan blue assay, triphosphate assay (ATP), lactate dehydrogenase assay (LDH) and Hoechst staining respectively. Finally, biotin leading GO-κ-Car carrier demonstrated is a promising drug delivery system for cervical cancer treatment.

Folate receptor targeted delivery of paclitaxel to breast cancer cells via folic acid conjugated graphene oxide grafted methyl acrylate nanocarrier.

The adaptability, joint with a large surface area, electronic flexibility, high intrinsic mobility, high mechanical strength and supreme thermal conductivity have condensed graphene family materials attractive as technological tools of the drug delivery system. In this present study, investigate a modified graphene oxide-methyl acrylate (GO-g-MA) nanocarrier for targeted anti-cancer drug delivery in breast cancer cells and the GO-g-MA fascinated with folic acidas a targeting ligand to target the cancer cells. Paclitaxel (PTX) was assembled through π-π stacking, hydrophophic interaction on the surface of the GO-g-MA/FA carrier. Structural modification of GO-g-MA, functionalization of targeting ligands GO-g-MA/FA and drug loaded GO-g-MA/FA-PTX was characterized and confirmed through FTIR, XRD, SEM,TEM and AFM analysis. The in-vitro drug release pattern of PTX from the GO-g-MA/FA was examined in different pH ranges. An MTT assay was performed to evaluate the cytotoxicity behaviour of the carrier and PTX loaded nanocarrier in the human breast cancer cell line (MDA-MB-231). GO-g-MA/FA-PTX carrier showed that 39% of cytotoxic effect. Furthermore, the in-vivo (DMBA induced breast cancer rats) studies were carried out and treatment with PTX- loaded GO-g-MA/FA nanocarrier attenuates the levels of mitochondrial citric acids enzymes to near normal.