抄録
A biodegradable polymer, poly(L-lactide) (L-PLA), was used to prepare nano- and microparticles loaded with an anticancer drug. We used a supercritical antisolvent (SAS) process modified with polar antisolvents such as alcohols to prepared drug loaded nano- and microparticles. Various short-chain alcohols such as methanol, ethanol, 1-propanol, 2-propanol, 1-butanol and 2-methyl-1-propanol were employed as polar antisolvents to investigate the effect of molecular structures of antisolvents on the formation of nano- and microparticles and their drug encapsulation. It was revealed that the addition of polar antisolvents to supercritical CO2 results in a significant improvement in the recovery of L-PLA particles and a large reduction in the particle size. An anticancer drug, 5-fluorouracil (5-FU), was entrapped to L-PLA and the effects of various factors such as the formulation ratio, temperature and pressure on the formation of drug loaded nano- and microparticles were investigated in detail. The recovery of 5-FU loaded nanoparticles was found to be higher than that of L-PLA nano- and microparticles prepared in the absence of 5-FU. The highest encapsulation efficiency was obtained when the ratio of 5-FU to L-PLA was 20 %, yielding about 95% in vitro release from L-PLA nanoparticles for one month.
