[Uptake of drug-containing nanoparticles in dog catotid and femoral arteries].

OBJECTIVE

To study the uptake of drug-containing nanoparticles in artery for local therapy of restenosis.

METHODS

Polylactic polyglycolic acid copolymer (PLGA) nanoparticles containing an antiproliferative agent 2-amino-chromone were formulated with an oil-in-water sonication emulsion/solvent evaporation technique. Arterial uptake of nanoparticles was assessed both in vitro and in vivo models of dog and rat carotid and femoral arteries. Epoxide, cyanoacrylate, fibrinogen, fibronectin, didodecyldimethylammonium bromide (DMAB), L-alpha-phosphatidylethanolaine, and lipofectin were selected to modify the surface of nanoparticles to enhance arterial uptake of nanoparticles.

RESULTS

The nanoparticle size ranged from 100 nm to 200 nm, the drug loading in nanoparticles was about 15%, the nanoparticle morphology was observed by scanning electron microscopy and showed spherical shape with smooth surface. Arterial uptake of nanoparticles was enhanced greatly by surface modified nanoparticle with positively charged active agent DMAB. Once nanoparticles located in artery, a high drug level could be maintained at local site for 2 days in vivo model.

CONCLUSION

The primary results of animal experiments suggested that nanoparticle could be used as drug carrier of local drug delivery for treating cardiovascular diseases.