Liposphere based lipoprotein-mimetic delivery system for 6-mercaptopurine.

ABSTRACT

Long-circulating lipospheres containing 6-mercaptopurine (6-MP) were prepared by solidification of warm microemulsion at low temperature. Palmitoyl PEG was incorporated in the system to confer stealth-type nature. The size of lipospheres was in the range of 60-70 nm and was inversely proportional to sonication time. The size range was attained after 8 h. of sonication. The entrapped 6-MP contained 0.12 mmol/mole of lipid. The coating efficiency of 63-71% was attained. The zeta potential substantially decreased after PEG coating, however, the lipospheres were stable due to steric repulsion and exhibited no aggregation. The release of 6-MP was found to be 18-25% of administered dose in 24 h. and followed a mixed profile for stealth lipospheres. The percent dose remaining in plasma was found to be high even after 24 h as compared to control, indicating an increase in circulation time of lipospheres. Tissue accumulation of drug correlated with the pharmacokinetic behavior of lipospheres. The system seems to be an ideal carrier for anticancer drug delivery.