Conjugation of Au Nanoparticles with Chlorambucil for Improved Anticancer Activity

Abstract

Gold nanoparticles (AuNPs) of 30-40 nm in size has been prepared using A. hirsutus leaves extract as reducing agent for Au 3? ions under microwave irradiation from 60 to 360 s. These biocapped AuNPs were effectively conjugated with activated folic acid (FA, receptor) and chlorambucil (CHL, anticancer drug) molecules. The formation of AuNPs-FA-CHL was confirmed from different characterization techniques such as XRD, UV-Visible spectra, FT-IR and TEM images. The anticancer activity of these bioconjugated AuNPs was tested against human cancer cell lines (HeLa, RKO and A549) in comparison with normal epithelial cells (Vero). Unlike AuNPs and CHL alone, AuNPs-FA-CHL showed high toxicity towards human cancer cells by significantly decreasing the percentage viability of cells. Furthermore, the amount of drug released was found to be maximum at an ideal tumor environment pH 5.3.

Red‐Light‐Controlled Release of Drug–Ru Complex Conjugates from Metallopolymer Micelles for Phototherapy in Hypoxic Tumor Environments

“…In contrast, irradiating (656 nm, 60 J cm −2 ) cancer cells incubated with PEG‐ b ‐P(CPH‐ co ‐RuCHL) micelles significantly decreased the cell viability (Figure b). The EC 50 of polymeric micelles was less than 25 µg mL −1 , which is much lower than that of CHL (150 µg mL −1 ) . Because light irradiation (656 nm, 60 J cm −2 ) on the micelles (100 µL, 200 µg mL −1 ) resulted in 90% conversion of the photoreaction (Figure S20b, Supporting Information), we interpret that the released [Ru(CHLtpy)(biq)(H 2 O)] 2+ from the micelles inhibited cancer cell growth.…”

“…HeLa cells were incubated with [Ru(CHLtpy)(biq)(H 2 O)](PF 6 ) 2 with a concentration from 1.25 to 50 µg mL −1 for 24 h. Cell viability decreased as the concentration of [Ru(CHLtpy)(biq)(H 2 O)] 2+ increased. The half maximal effective concentration (EC 50 ) of [Ru(CHLtpy)(biq)(H 2 O)] 2+ to HeLa cells was ≈13.7 µg mL −1 , much lower than those of both [Ru(CHLtpy)(biq)(H 2 O)] 2+ (≈30 µg mL −1 , Figure S24, Supporting Information) and CHL (≈150 µg mL −1 ) . The result indicated that the two anticancer moieties had synergistic effects and the conjugate [Ru(CHLtpy)(biq)(H 2 O)] 2+ had improved cytotoxicity toward cancer cells.…”

Hesperidin Loaded on Gold Nanoparticles as a Drug Delivery System for a Successful Biocompatible, Anti-Cancer, Anti-Inflammatory and Phagocytosis Inducer Model

“…Thus, the results show that Hsp-AuNPs were able to particularly stimulate the delivery of hesperidin to cancer cells 29 . Previous studies also reported rapid release of chemotherapeutic drug loaded on AuNPs in acidic conditions when compared to neutral conditions 30,31 .…”

“…And subjected to dilution with 800 μL of either physiological (pH 7.4) or acidic (pH 5.04). Incubation of the mixtures was performed at 37 °C for different periods of time (5,15,30,60,120,180,240,1440, and 2880 min). After each period, measurement of the absorbance of the solution was achieved by a UV-VIS spectrophotometer at 286 nm.…”

Redox-Responsive Heparin–Chlorambucil Conjugate Polymeric Prodrug for Improved Anti-Tumor Activity

“…As shown in Figure S2, the reduction and oxidation of disulfide bonds by GSH and H2O2 disrupted the nanoparticles that induced an increase in size and irregular shape. From the DLS measurements, the mean The conjugation of Hep-Cys with Chl was also confirmed by UV-vis spectrophotometry [30][31][32]. As presented in Figure 3a, Chl was successfully grafted onto the Hep backbone, as shown by the UV absorption peak around 304 nm.…”