Preparation and evaluation of thiomer nanoparticles via high pressure homogenization

• Published in: Journal of microencapsulation 2010-09, Vol.27 (6), p.487-495
• Main Authors: Hoyer, Herbert, Schlocker, Wolfgang, Greindl, Melanie, Ostermann, Thomas, Bernkop-Schnürch, Andreas
• Format: Article
• Language: English
• Subjects: Acrylic Resins - chemistry; Armoracia - enzymology; Biological and medical sciences; chitosan; Chitosan - chemistry; Drug Carriers - chemistry; Drug Compounding - methods; General pharmacology; Glutathione - chemistry; High pressure homogenizer; Horseradish Peroxidase - administration & dosage; Horseradish Peroxidase - metabolism; Medical sciences; nanoparticles; Nanoparticles - chemistry; Nanoparticles - ultrastructure; Nanotechnology - methods; Particle Size; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; poly(acrylic acid); Pressure; Sulfhydryl Compounds - chemistry; thiomer
• ISSN: 0265-2048; 1464-5246
• DOI: 10.3109/02652040903518460

The aim of this study was to establish and evaluate a high pressure homogenization method for the preparation of thiomer nanoparticles. Particles were formulated by incorporation of the model protein horseradish peroxidase in chitosan-glutathione (Ch-GSH) and poly(acrylic acid)-glutathione (PAA-GSH) via co-precipitation followed by air jet milling. The resulting microparticles were suspended in distilled water using an Ultraturax and subsequently micronized by high pressure homogenization. Finally, resulting particles were evaluated regarding size distribution, shape, zeta potential, drug load, protein activity and release behaviour. The mean particle size after 30 cycles with a pressure of 1500 bar was 538 ± 94 nm for particles consisting of Ch-GSH and 638 ± 94 nm for particles consisting of PAA-GSH. Nanoparticles of Ch-GSH had a positive zeta-potential of +1.03 mv, whereas nanoparticles from PAA-GSH had a negative zeta potential of −6.21 mv. The maximum protein load for nanoparticles based on Ch-GSH and based on PAA-GSH was 45 ± 2% and 37 ± %, respectively. The release profile of nanoparticles followed a first order release kinetic. Thiolated nanoparticles prepared by a high pressure homogenization technique were shown to be stable and provide controlled drug release characteristics. The preparation method described here might be a useful tool for a more upscaled production of nanoparticulate drug delivery systems.