호흡기 전달용 부데소나이트 함유 다공성 PLGA 미립구

Abstract

Asthma is a chronic pulmonary disease that inflames and narrows the airways. Most common treatment method for asthma is a use of an inhaled corticosteroid such as budesonide. But, frequent uses of steroid may cause many side effects to patients. We hypothesized that porous microparticles could be effective for treatment of asthma, as the sustained delivery of corticosteroid and reduced number of dosage can be achieved by using porous polymeric microaprticles. Porous microparticles were prepared from poly(lactic-co-glycolic acid) (PLGA) by the w/o/w double emulsion method. Ammonium bicarbonate was a as porogen, and budesonide was chosen as a model drug. The morphology, size and porosity of porous PLGA microparticles were controlled by varying porogen concentrations. The size of porous microparticles was not significantly changed, but the porosity of increased as the concentration of porogen increased from 0% to 3%. The loading efficiency of budesonide in nonporous PLGA microparticles was higher than that of porous PLGA microparticles, and budesonide from porous PLGA microparticles was continually released in vitro during 72h. The lung uptake efficiency of porous PLGA microparticles with 3% porogen was enhanced, compared with both nonoporous PLGA microparticles and porous microparticles prepared with 1.5% porogen. When observed budesonide-loaded porous PLGA microparticles were delivered into asthma model mice, the number of inflammatory cells in BAL fluid and tissue sections was significantly reduced. This approaching to using porous PLGA microparticles can find useful applications for pulmonary delivery of many therapeutic drugs.