Interfacial Polymerization, A Useful Method for the Preparation of Polymethylcyanoacrylate Nanoparticles

Abstract

An interfacial polymerization procedure was developed for the preparation of polymethylcyanoacrylate (PMCA) nanoparticles loaded with triamcinolone acetonide. The nanoparticles were characterized concerning their interior structure, size distribution, drug content, drug release and in vivo distribution. These results (except those for the in vivo distribution) were compared with those obtained with nanoparticles prepared by micell polymerization [5]. Both preparation procedures yielded particles with a mean diameter below 500 nm. The drug content of the nanoparticles prepared by interfacial polymerization ranged from 6,5% w/w to 1,9% w/w depending on the employed monomer concentration in contrast to 0,045% w/w for nanoparticles prepared by micell polymerization [5]. In comparison to microcrystalline substance the drug release from the nanoparticles could be sustained in all cases, but there was no difference in drug release between the nanoparticles prepared by both methods.

After removal of surface adherent drug from nanoparticles prepared by both methods those prepared by interfacial polymerization had an about 12 times higher drug content and the remaining drug amount was released more slowly by these particles. Furthermore, using increasing monomer concentrations during interfacial polymerization (125 - 500 mg/100 ml emulsion) drug release was slowed down, but no further improvement could be achieved for monomer concentrations exceeding 250 mg/100 ml emulsion.

After intravenous injection of ^99mTc labeled PMCA nanoparticles into rats they accumulated predominantly in liver, spleen and kidney, a distribution pattern usually found for colloidal particles.