Construction And Biological Efficacy Of Different Types Of MTX Nanocomposites

Synthesis of nanoparticles with good surface characteristics and regular morphology have always been the important and difficult part in the drug delivery system, which plays a key role to promote the development of nanomedicine. In order to improve the stability of drug molecules and reduce their side effects, research on the synthesis of those nanocarriers has became a hotspot. In this paper, we choose methotrexate (MTX) as the guest drug molecule and a series of MTX based nanocarriers are synthesized. The morphology, property and inhibition towards A549 cells are explored thoroughly. The main researches are as follows:1. We report a simple, one-pot, and hydrothermal growth route for the synthesis of Au-MTX conjugates. The reaction transformed nanochains into discrete nanoparticles by using Au-MTX complex as the precursor and adding various EDTMPA contents. Moreover, the morphology change, drug loading capacity, optical properties, colloidal stability, and anticancer effect of both nanostructures were explored thoroughly. The results indicated that the discrete nanoparticles showed almost equal drug loading capacity as the nanochains but better drug release control,colloidal stability, and in vitro anticancer activity than the nanochains did. Meanwhile,a possible formation mechanism was provided indicating that the surface selective adsorption of the MTX molecules induced the formation of specific gold nanospheres and that the strong interaction among the adsorptive MTX molecules induced the formation of nanochains while the existence of strong electrostatic effect of the negatively charged phosphonic acid groups led to the production of discrete nanoparticles.2. Au nanoassemblies with different morphologies was synthesized at a certain reaction time by using Au-MTX complex as the precursor and adding different kinds of saccharides. Moreover, the morphology change, drug loading capacity, optical properties, colloidal stability, and anticancer effect of the obtained nanoassemblies were explored thoroughly. The results indicated that the introduction of glucose molecules resulted in the production of peanut-like Au nanoparticles and nanochains with great colloidal stability in PBS solution. while the addition of dextran molecules and sucrose molecules led to the generation of Au nanoassemblies possessing good optical property in the near-infrared (NIR) region. Furthermore, in vitro anticancer test showed that sugars doped Au-MTX conjugates were more efficient than free MTX in the suppression of the cancer cells.3. Based on the self-assembly of polyelectrolyte,different morphologies of PAH-MTX nanoassemblies were successfully synthesized in the aqueous solution.Moreover, their morphology change, drug loading capacity and controlled release,and anticancer effect were explored thoroughly. The results showed that many factors,such as temperature, the amount of ascorbic acid and MTX, all had an important effect on the morphology change. Meanwhile, the obtained nanoassemblies possessed obviously different drug release profiles and the spherical nanoassemblies exhibited the best effect of controlled release. Furthermore, in vitro anticancer test showed that PAH-MTX nanostrips were more efficient than others in the suppression of cancer cells.