Drug delivery in poly(lactide-co-glycolide) nanoparticles surface modified with poloxamer 407 and poloxamine 908: in vitro characterisation and in vivo evaluation

Poly(D,L-lactide-co-glycolide) (PLGA) nanoparticles of 150-nm mean size were produced by an interfacial deposition method. The polar model drug Rose Bengal was successfully loaded into the nanoparticles during production and the surface of these particles was subsequently modified with poloxamer 407 and poloxamine 908 in order to create a steric stabilising layer of PEG on the surface. Drug loading was low (<1%) which can be attributed to the polar nature of the drug and the small size of the nanoparticles. Drug release was biphasic with 50% release measured within 30 min in serum. After intravenous injection in rats, the drug loaded nanoparticles substantially avoided capture by the Kupffer cells of the liver as compared to free drug. The half-life of Rose Bengal in the blood stream when administered in the nanoparticles was greatly extended with <similar to>30% remaining after 1 h as compared to only 8% of Rose Bengal left 5 min after administration in solution. These surface modified nanoparticles would have potential as carriers for drugs td specific sites within the body or for slow release of drug within the circulation. (C) 2001 Elsevier Science B.V. All rights reserved.