Abstract The poly(lactic-co-glycolic acid) (PLGA) nano-microspheres containing hydroxycamptothecin (HCPT) was prepared using solvent and anti-solvent precipitation method with HCPT as the model drug, degradable PLGA as the carrier. The effects of different solvents and anti-solvents system on the drug loading capacity and entrapment efficiency were investigated. The results showed that the microspheres prepared with acetone-water as solvent system had better performance, spherical appearance, round and smooth surface, uniform particle size (the average particle size of 160 nm) and good dispersion. The entrapment efficiency of drug-loaded microspheres decreased with the increase of drug loading. It was found that the entrapment efficiency was 87.68% in the HCPT/PLGA microspheres when drug loading was 7.83%. The cumulative release amount was 50% after 28 days. This HCPT/PLGA drug delivery system clearly demonstrated its good sustained-release effect.
