Fabrication of chlorambucil loaded graphene- oxide nanocarrier and its application for improved antitumor activity.

The present study aims at designing a biodegradable and biocompatible nanocarrier using gelatin and reduced graphene oxide nanosheets functionalized with folic acid, for release of chlorambucil drug in controlled manner and achieving high loading efficiency. From scanning electron microscopic studies small pore like structure with rough and thick morphology on the plane of graphene oxide is clearly visible indicating high loading of drug. Further, Drug loading and encapsulation efficiency, in vitro release studies of the drug from the nanocarrier at different concentrations of reduced graphene oxide, different pH were studied. The mean particle size, entrapment efficiency (%) of optimized folic acid functionalized gelatin-graphene oxide formulation was observed to be 300 nm and 56% respectively. From the release studies it is clear that, after 24 h the release rate of the drug was found to be higher at acidic conditions compared to neutral conditions. It was found that 62.1% and 82% of the total bound drug was released from the nanocarrier at pH 5.4 and pH 1.2 respectively. Besides, under neutral conditions (pH 7.4), 43.7% of the total bound drug was released from the nanocarrier in the first 24 h. The % cell viability of free drug, drug loaded nanocomposites against human cervical adenocarcinoma cell line was found to be 11.7% and 28% respectively at the dose of 500 µg mL-1 after 24 h. IC50 values also manifest the significantly lower cytotoxicity of drug loaded nanocarrier (IC50 = 125.9 µg/mL) as compared to free-drug (IC50 = 86 µg/mL). For FAGGO, CLB and CLB-FAGGO the values of mean ± std. deviation were found to be 71.80 ± 6.66; 48.71 ± 23.15; 55.48 ± 19.65 respectively. The unique properties exhibited by biodegradable polymer like gelatin and carbon based materials such as graphene offers an excellent applications in biomedical field.

Development of rGO encapsulated polymeric beads as drug delivery system for improved loading and controlled release of doxycycline drug.

Objective: The aim of this study was to design a biodegradable core-shell structure where in reduced graphene-oxide (rGO) and doxycycline (DXC) drug comprise the core while polymer such as chitosan (CS) and alginate (ALG) acts as shell for attaining high loading efficiency and sustained release of drug.Significance: Cytotoxic drug used in conventional chemotherapeutic methods usually suffer from poor site selectivity and this has been resolved by using targeted delivery of anticancer drug with controlled drug release property.Methods: The structural and morphological properties of as synthesized drug delivery carrier were characterized by a range of techniques. Drug encapsulation efficiency and the studies on, in vitro release of the drug from these nanocarriers at different concentrations of rGO were carried out.Results: Across all batches of rGO-polymeric beads, the highest loading capacity of 85% was noted for rGO of wt 5 mg/ml. Further, for the formulations of only rGO, highest LE of 90% was noticed in 1 h and 100% loading was noticed in 3 h. The interaction of DXC and its release from the nanocarriers were controlled by the pH changes. At pH 1.2 for rGO-polymeric beads + DXC, the DXC release was reached 27.4% after 2 h; and at pH 5.4, the same beads liberated 57% of the drug after 4 h; and at pH 7.4 after 8 h, 90% of DXC was released into the medium.Conclusions: rGO-polymeric beads supported long-lasting and continuous DXC release which is slower at acidic pH (endosomal pH) than at physiological.

Visible-light-driven photocatalytic degradation of safranin-T dye using functionalized graphene oxide nanosheet (FGS)/ZnO nanocomposites.

Photocatalysts suffer from a lack of separation of photogenerated excitons due to the fast recombination of charge carriers, so a strong synergistic effect exhibited by photocatalysts is promising for effective photocatalysis. Herein, we have synthesized efficient visible light functionalized graphene oxide nanosheet (FGS)/ZnO nanocomposite photocatalysts via a simple and economical approach with large scale production for practical applications. A series of nanocomposites (FGS/ZnO NCs) with different amounts by weight of graphene oxide (GO) have been synthesized via a facile solution route followed by calcination under environmental conditions. The phase, purity and morphological studies of the synthesized FGS/ZnO NCs were carried out using powder X-ray diffraction (XRD) and transmission electron microscopy (TEM). The optical properties were studied using UV-visible diffuse reflectance spectroscopy (DRS) and photoluminescence spectroscopy (PL). XRD results confirm the formation of a pure phase of ZnO in the FGS/ZnO NCs and TEM results show strongly adhered ZnO NPs on the surface of the FGS. DRS results confirm the extension of light absorption in the visible region while PL results confirm the effective separation of charge carriers in 0.09 wt% FGS/ZnO NCs. The synthesized photocatalyst efficiently degrades carcinogenic safranin-T dye under visible light illumination which is reported for the first time using FGS/ZnO nanocomposites. Photocatalytic studies confirm the higher photocatalytic activity of 0.09 wt% FGS/ZnO NCs (about 94.5%) towards the photodegradation of safranin-T dye in aqueous solution under visible light. The improved photocatalytic activity of 0.09 wt% FGS/ZnO NCs can be ascribed to the integrative synergistic effects of the enhanced adsorption capacity of safranin-T dye, effective separation of photogenerated excitons and effective interfacial hybridization of FGS and ZnO NCs. The generation of reactive oxygen species was confirmed using terephthalic acid as a probe molecule and a scavenger test was conducted in presence of histidine.

Correlation between defects in capped ZnO nanoparticles and their antibacterial activity.

Antibacterial activity of ZnO nanoparticles (NPs) triggered by generation of reactive oxygen species (ROS) depends on the fate of photoexcited charge carriers. Batches of wide band gap ZnO NPs of 7-9nm sizes, capped with polyethylene glycol (PEG), ascorbic acid (AsA), mercaptoacetic acid (MAA) and polysorbate 80 (T-80) were synthesized by precipitation method. These capped ZnO NPs exhibited ROS induced antibacterial activity, where the ROS was measured by TBARS assay. The PEG capped and AsA capped ZnO NPs exhibited weaker antibacterial activity and were correlated with strong and broad green emission peak owing to oxygen vacancies. The oxygen vacancies were trap sites of photoexcited electrons which inhibited interaction between the photoexcited electrons and oxygen on the surface of the ZnO NPs and accounted for lesser ROS generation and subsequently weaker antibacterial activity. Contrastingly MAA capped and T-80 capped ZnO NPs did not exhibit significant green emission peak, but exhibited 13% and 43% inhibition of growth of E. coli, respectively. The lack of oxygen vacancy defects in MAA capped and T-80 capped ZnO NPs perhaps led to lesser trapping of charge carriers, which is favorable for higher ROS generation and consequently higher antibacterial activity.

Antibacterial effect of chronic exposure of low concentration ZnO nanoparticles on E. coli.

The toxicity effect due to chronic exposure of ZnO nanoparticles (NPs) was systematically studied by repeatedly treating different lower concentrations of ZnO nanoparticles with culture media of E. coli strain. The chronic exposure of ZnO NPs of concentrations below minimum inhibitory concentration (MIC) exhibited higher toxicity than the single exposure of higher concentrations. Most striking result was 57% inhibition of growth corresponding to chronic exposure of 0.06 mg/mL of ZnO NPs which was two folds more than that exhibited by single exposure of 0.30 mg/mL ZnO NPs. The toxicity of ZnO NPs in E. coli was studied in the light of formation of reactive oxygen species (ROS), measured as malondialdehyde (MDA) equivalent by thiobarbituric acid-ROS (TBARS) assay, and effect of Zn dissolution from ZnO NPs. Higher inhibition of growth for the chronic exposure batches were correlated with higher ROS generation, which subsequently contributed to cause membrane lipid peroxidation, confirmed from observation of cell wall deformation by scanning electron microscopy study and energy dispersive X-ray analysis showed adherence of ZnO NPs on cell wall. The possibility of membrane lipid peroxidation was addressed by revealing in vitro oxidation of oleic acid, which is a monounsaturated fatty acid. Further in this study we have shown that the dissolution of ZnO NPs at pH 7.4 was not significant to cause Zn-induced toxicity.

Studies on antibacterial activity of ZnO nanoparticles by ROS induced lipid peroxidation.

Recent studies indicated the role of ROS toward antibacterial activity. In our study we report ROS mediated membrane lipid oxidation of Escherichia coli treated with ZnO nanoparticles (NPs) as supported by detection and spectrophotometric measurement of malondialdehyde (MDA) by TBARS (thiobarbituric acid-reactive species) assay. The antibacterial effects of ZnO NPs were studied by measuring the growth curve of E. coli, which showed concentration dependent bacteriostatic and bacteriocidal effects of ZnO NPs. The antibacterial effects were characterized by scanning electron microscopy (SEM) and transmission electron microscopy (TEM). Further, antibacterial effect of ZnO NPs was found to decrease by introducing histidine to the culture medium treated with ZnO NPs. The ROS scavenging action of histidine was confirmed by treating histidine to the batch of Escherichia coli+ZnO NPs at the end of the lag phase of the growth curve (Set-I) and during inoculation (Set-II). A moderate bacteriostatic effect (lag in the E. coli growth) was observed in Set-II batch while Set-I showed no bacteriostatic effect. From these evidences we confirmed that the antibacterial effect of bare as well as TG capped ZnO NPs were due to membrane lipid peroxidation caused by the ROS generated during ZnO NPs interaction in culture medium.