Preparation And Characterization Of Matrine-loaded Magnetic Chitosan Microspheres

The objective of this study was using magnetic targeted drugs delivery system (MTDDS) to target matrine to the site of action through magnetic chitosan microspheres for sustaining drug delivery and targeting. Magnetic microspheres were used as carrier of anticancer drugs extensively in recent years. These magnetic microspheres consist of magnetite (Fe₃O₄) particles, which are responsible for magnetic property, and a therapeutic agent entrapped in the biodegradable polymer matrix. These magnetic microspheres can improve chemotherapy target tropism of medicine to a certain extent, reduce chemotherapy medicines malicious side effect of medicine by a large margin, raise chemotherapy treatment index of medicine from several ways, compared with other form of an anticancer drug at present.In this study, spherical shaped magnetic chitosan microspheres were produced by a very convenient method of ionic gelation. The complexation between oppositely charged macromolecules to prepare magnetic chitosan microspheres has attracted much attention for the simple and mild process. In addition, reversible physical cross-linking by electrostatic interaction, instead of chemical cross-linking, has been applied to avoid the possible toxicity of reagents and other undesirable effects.To overcome the toxicity produced by matrine and to get prolonged therapeutic effect, in the present study, magnetic chitosan microspheres are formulated to target matrine at its site of action. The ionic gelation process of tripolyphosphate (TPP) and chitosan was used for the production of magnetic chitosan microspheres. Line-up competition algorithm was used to optimize the parameters. The formulated magnetic fluid and microspheres were characterized by X-ray diffraction, loading efficiency, encapsulation efficiency, size and the size distribution, magnetic properties, fourier transform infra red(FTIR), scanning electron microscopy (SEM) and in vitro release studies.The average particle size of magnetic fluid was found to be 98.1nm. The chitosan magnetic microspheres loaded with 9.43% w/w of matrine and 20.34% w/w of magnetite. The average particle size of magnetic chitosan microspheres, matrine-loaded chitosan magnetic microspheres were found to be 538.2nm, 682.4nm, respectively and spherical in nature as evidenced by the SEM photographs. The size and size distribution were well below the size that can be injected through intravenous injection. FTIR studies revealed the absence of drug-polymer interaction. Encapsulated matrine released cumulatively about 79.6% for 24h. Further studies are required to improve the targeting efficiency of magnetic chitosan microspheres by modifying surface properties to overcome phagocytosis and by selecting suitable particle size to avoid the entrapment of microspheres in non-target organs.