Development of nanoparticulate drug delivery systems based on thiolated poly(acrylic acid)

Abstract

In this study the preparation and stabilization of poly(acrylic acid)-cysteine nanoparticles and incorporation of a fluorescence marked model-compound was investigated. Nanoparticles were prepared by ionic gelation of a poly(acrylic acid)-cysteine conjugate with calcium chloride. Poly(acrylic acid)-cysteine nanoparticles display high cohesive properties due to a cross-linking process via calcium bridges in the core and the pervasive formation of disulphide bonds and were 139 ± 34 nm in size. Nanoparticles were loaded with FITC-dextrans (flourescein isothiocyanate-dextrans) of 4, 20 and 40 kDa molecular mass as model-compound via sonication method or via vibration method for 3 and 24 h. In vitro release studies showed an initial burst release followed by an extended release of model-compounds. The lower the molecular mass of the FITC-dextrans, the higher was the amount of incorporated and released model compounds. Vibration seems to be a proper method for the incorporation of hydrophilic and macromolecular drugs in poly(acrylic acid)-cysteine nanoparticles.

• Nanoparticles
• ionic gelation
• thiomers
• mucoadhesion
• poly(acrylic acid)
• cross-linking