(97a) Preparation of Glucan Microparticles with Curcumin for Treatment of Idiopatic Inflammation Diseases

One of the novel methods of pharmaceutical formulation is the loading of the drug into biocompatible microparticles, preferably extracted from natural sources. This approach offers several potential advantages, e.g. increased bioavailability (the ratio of the administered drug, which actually enters the bloodstream) compared to conventional drug delivery methods, enabling the option of oral administration even for parenteral drugs. Multiple principles of the loading process are possible – drug encapsulation, adsorption onto the particle surface or precipitation inside the pores a hollow particle. The presented work focuses on precipitation of a drug from an organic solvent inside glucan particles. Glucan microparticles are ellipsoid porous shells, which are obtained from cell walls of Saccharomyces cerevisiae (baker´s yeast). The particle size is 2-5 micrometers. Cell walls of glucan particles are mainly composed of β-1,3-glucans. In order to prevent inflammatory reaction in organism, the yeast organelles are removed by a series of alkaline and acidic extraction steps. Subsequently, present lipopolysacharides are extracted using different organic solvents.
Lymphatic cells are mainly present in inflammation area in organism where they are responsible for progress of inflammation. Glucan particles (GPs) interact with lymphatic cell´s receptors on their surface and after that β-1,3-glucans are phagocytosed by the lymphatic cells. Therefore, GPs represent an effective oral delivery system for transporting of biological active substances. Curcumin is an anti-inflammatory flavonoid, which occurs in plants of family Zingiberacaea. In our project, curcumin was delivered to an inflammation in organism using GPs. Loading of curcumin into GPs was enabled via precipitation of curcumin from organic solvents. Curcumin dissolved in organic solvents was added to the GPs and through pores penetrated into cavity of glucan shell. Next, the solvent was removed and the curcumin was precipitated in glucan microparticles. GPs with the flavonoid inside were observed using confocal microscopy and SEM (scanning electron microscopy). The achieved content of curcumin was successfully analyzed by other methods, which can not be mentioned directly due to article in preparation. Furthermore, the curcumin-loaded GPs were tested in vitro on macrophage‑like cells and in vivo on laboratory mice in order to evaluate their effectivity. The obtained results show that these composites are promising materials for biomedical applications such as efficient treatment of inflammatory diseases (e.g. idiopatic inflammatory bowel disease, rheumatoic arthritis).