Preparation, characterization and in vitro release properties of morphine-loaded PLLA-PEG-PLLA microparticles via solution enhanced dispersion by supercritical fluids

摘要

Morphine-loaded poly(L-lactide)-poly(ethylene glycol)-poly(L-lactide) (PLLA-PEG-PLLA) microparticles were prepared using solution enhanced dispersion by supercritical CO_2 (SEDS). The effects of process variables on the morphology, particles size, drug loading (DL), encapsulation efficiency and release properties of the microparticles were investigated. All particles showed spherical or ellipsoidal shape with the mean diameter of 2.04-5.73 urn. The highest DL of 17.92 % was obtained when the dosage ratio of morphine to PLLA-PEG-PLLA reached 1:5, and the encapsulation efficiency can be as high as 87.31 % under appropriate conditions. Morphine-loaded PLLA-PEG-PLLA microparticles displayed short-term release with burst release followed by sustained release within days or long-term release lasted for weeks. The degradation test of the particles showed that the degradation rate of PLLA-PEG-PLLA microparticles was faster than that of PLLA microparticles. The results collectively suggest that PLLA-PEG-PLLA can be a promising candidate polymer for the controlled release system.