The pioglitazone loaded poly(lactide-co-glycolide)(PLGA) nanospheres were prepared by emulsion-evaporation method and optimized for particle size and entrapment efficiency. The optimized particles were 125∼170 nm in size with narrow size distribution and showed above 85% entrapment efficiency at 30% of pioglitazone loading when prepared with 3% w/v of poly(vinyl alcohol) (PVA) as a surfactant. These particulate carriers exhibited a controlled in vitro release of pioglitazone for 40 days at a nearly constant rate. The pioglitazone loaded PLGA nanospheres were not only effective to reduce the blood sugar level of diabetic rats but also non-toxic for the animal body, in particular for sensitive organs like kidney, liver, heart, lung and spleen. These results indicate that PLGA nanospheres have a great potential for oral delivery of pioglitazone.

Pioglitazone을 봉입한 poly(lactide-co-glycolide)(PLGA) 나노입자를 emulsion-evaporation 방법을 이용하여 제조하여 최적의 나노입자와 봉입률을 조절하였다. 제조된 나노입자의 크기는 125∼170 nm이었으며 30% pioglitazone이 봉입된 나노입자(3% PVA)의 봉입률은 85% 이상이었다. 이러한 나노입자들은 40일 동안 일정하게 용출이 되었다. 당뇨병 모델을 이용한 동물실험에서 글루코오스 농도를 저하시켰을 뿐만 아니라, 조직검사에서는 낮은 독성을 가지고 있는 것을 확인하였다. 이러한 결과는 pioglitazone 경구투여를 위한 약물전달을 위한 운반체로 사용될 수 있음을 확인하였다.

Keywords: pioglitazone; PLGA nanospheres; type 2 diabetes; drug delivery; controlled release