Production and in vitro characterization of lisinopril-loaded nanoparticles for the treatment of restenosis in stented coronary arteries

Abstract

Lisinopril, an angiotensin converting enzyme (ACE) inhibitor drug, was encapsulated in poly(lactide-co-glicolide) (PLGA) nanoparticles (NP) for site-specific delivery by catheters in prevention of restenosis. NP were prepared by emulsification–diffusion method. The PLGA type, stabilizing agent type and its concentration were studied as process variables. The z-average particle size varied between 265–412 nm. The highest zeta potential was seen in NP prepared with Pluronic F-68. None of the studied variables or their interactions had a significant effect on the particle size while all had main effect on the zeta potential. The highest entrapment efficiency was 93% and all studied variables and their interactions except PLGA type and its interaction with the stabilizer type had significant effects on the loading. Baker-Lonsdale model was the most appropriate model for release of lisinopril from NP. Five per cent PLGA 75 : 25 and 5% Pluronic F-68 showed promising results for 21 days release of lisinopril as an anti-restenotic agent.

Keywords::

• Restenosis
• ACE inhibitor
• lisinopril
• polymeric nanoparticles
• PLGA

Acknowledgements

The authors wish to thank the Nanotechnology Committee of Isfahan Pharmaceutical Sciences Research Center and Research vice Chancellery of Isfahan University of Medical Sciences of Iran that supported this work by project No. 185235. The authors also appreciate Miss Ladan Zoheidi for her technical assistances.